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Sample records for captopril

  1. Captopril in the hepatorenal syndrome

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    Cobden, I.; Shore, A.; Wilkinson, R.; Record, C.O.

    1985-08-01

    Five patients with hepatorenal syndrome were treated with the orally active angiotensin-converting enzyme inhibitor captopril (25 or 50 mg 6 hourly) for up to 48 hours. Only one patient showed a significant increase in urinary sodium concentration (from less than 10 to 70 mmol/liter), but without associated diuresis; renal function continued to deteriorate in all patients with persistent oliguria and rising serum creatinine. The outcome was uniformly fatal. These results suggest that in the hepatorenal syndrome, captopril in standard dosage is without benefit, and provide further evidence that the changes in the renin-angiotensin system are probably secondary to reduced renal perfusion from some other cause.

  2. Compound list: captopril [Open TG-GATEs

    Lifescience Database Archive (English)

    Full Text Available captopril CAP 00094 ftp://ftp.biosciencedbc.jp/archive/open-tggates/LATEST/Human/in_vitro/captop...ril.Human.in_vitro.Liver.zip ftp://ftp.biosciencedbc.jp/archive/open-tggates/LATEST/Rat/in_vitro/captop...ril.Rat.in_vitro.Liver.zip ftp://ftp.biosciencedbc.jp/archive/open-tggates/LATEST/Rat/in_vivo/Liver/Single/captop...open-tggates/LATEST/Rat/in_vivo/Liver/Repeat/captopril.Rat.in_vivo.Liver.Repeat.zip ftp://ftp.biosciencedbc....jp/archive/open-tggates/LATEST/Rat/in_vivo/Kidney/Single/captopril.Rat.in_vivo.Kidney.Single.zip ftp://ftp.b

  3. Development studies of captopril certified reference material

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    Raquel Nogueira

    2011-06-01

    Full Text Available This paper describes the studies performed with the candidate Certified Reference Material (CRM of captopril, the first CRM of an active pharmaceutical ingredient (API in Brazil, including determination of impurities (organic, inorganic and volatiles, homogeneity testing, short- and long-term stability studies, calculation of captopril content using the mass balance approach, and estimation of the associated measurement uncertainty.Este artigo descreve os estudos realizados com o candidato a Material de Referência Certificado (MRC de captopril, primeiro MRC de fármacos no Brasil, incluindo a determinação de impurezas (orgânicas, inorgânicas e voláteis, testes de homogeneidade, testes de estabilidade de curta e longa duração, cálculo do teor de captopril por balanço de massa e estimativa da incerteza de medição associada ao valor certificado.

  4. CHARACTERIZATION OF CAPTOPRIL-ETHYL CELLULOSE MICROSPHERES BY THERMAL ANALYSIS

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    RakeshGupta

    2010-06-01

    Full Text Available The objective of the present study was to study the physical characterization of Captopril-ethyl cellulose microspheres by thermal analysis such as Differential Scanning Calorimetry (DSC, Differential thermal analysis (DTA and Thermo gravimetry (TG. Drug polymer interaction can directly affect the dosage form stability, drug encapsulation into polymers and dissolution patterns. In this study thermal analysis has been carried out for the physical mixtures and microspheres of captopril and ethyl cellulose prepared by solvent evaporation method.

  5. Permeation Studies of Captopril Transdermal Films Through Human Cadaver Skin.

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    Nair, Rajesh Sreedharan; Nair, Sujith

    2015-01-01

    Mortality rate due to heart diseases increases dramatically with age. Captopril is an angiotensin converting enzyme inhibitor (ACE) used effectively for the management of hypertension. Due to short elimination half-life of captopril the oral dose is very high. Captopril is prone to oxidation and it has been reported that the oxidation rate of captopril in skin tissues is considerably low when compared to intestinal tissues. All these factors make captopril an ideal drug candidate for transdermal delivery. In this research work an effort was made to formulate transdermal films of captopril by utilizing polyvinylpyrrolidone (PVP) and polyvinyl alcohol (PVA) as film formers and polyethylene glycol 400 (PEG400) as a plasticizer. Dimethyl sulfoxide (DMSO) and dimethylformamide (DMF) were used as permeation enhancers. Physicochemical parameters of the films such as appearance, thickness, weight variation and drug content were evaluated. The invitro permeation studies were carried out through excised human cadaver skin using Franz diffusion cells. The in-vitro permeation studies demonstrated that the film (P4) having the polymer ratio (PVP:PVA = 80:20) with DMSO (10%) resulted a promising drug release of 79.58% at 24 hours with a flux of 70.0 µg/cm(2)/hr. No signs of erythema or oedema were observed on the rabbit skin as a result of skin irritation study by Draize test. Based on the stability report it was confirmed that the films were physically and chemically stable, hence the prepared films are very well suited for transdermal application.

  6. Voltammetric Determination of Captopril Using Chlorpromazine as a Homogeneous Mediator

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    Hossein Bahramipur

    2011-01-01

    Full Text Available Chlorpromazine was used as a homogeneous electrocatalyst in the oxidation of captopril. The anodic peak current of chlorpromazine was increased substantially in the presence of low concentrations of captopril (pH 4. Cyclic voltammetry and chronoamperometry were used to study the kinetics of the catalytic electron transfer reaction. The values of electron transfer coefficient ( and catalytic rate constant (cat were estimated to be 0.34 and 8.48×102M−1sec−1, respectively. Linear sweep voltammetry was used for the determination of captopril in the presence of chlorpromazine. A linear calibration curve was obtained in the concentration range of captopril of 10.0–300.0 μM, with a limit of detection of 3.65 μM. The relative standard deviation (RSD% for 5 replicate measurements of captopril (100 μM was 1.96%. The method was applied to the determination of captopril in pharmaceutical formulations and blood serum samples with satisfactory results.

  7. Interação medicamentosa de venlafaxina com captopril Drug interaction of velanfaxine with captopril

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    Douglas D Sucar

    2000-09-01

    Full Text Available O autor descreve um caso de interação medicamentosa, em uma senhora de 53 anos de idade, com diagnóstico de depressão e de hipertensão arterial. Com níveis pressóricos estáveis, em conseqüência de um regime dietético e de uso do captopril -anti-hipertensivo inibidor da enzima de conversão da angiotensina -, passou a apresentar constantes descompensações do seu quadro clínico, com elevações da tensão arterial (TA, logo após a introdução da venlafaxina no seu esquema terapêutico. Esse medicamento é um potente antidepressivo de última geração, que atua no sistema nervoso central (SNC, inibindo a recaptação de serotonina e noradrenalina. Demonstra a interação pelo monitoramento da TA e aplicação do instrumento de Naranjo. Descreve as condições clínicas gerais da paciente e sua evolução, e discute os mecanismos prováveis que conduziram a interação pela hipótese que envolve o aumento de noradrenalina nos terminais sinápticos, o sistema renina-angiotensina e a bradicinina, concluindo que a venlafaxina agiu como antagonista, de modo indireto, sobre os efeitos hipotensores do captopril.This is a case report of drug interaction in a 53 year-old woman diagnosed with depression and arterial hypertension. As a result of a low-salt diet and the use of the captopril (an antihypertensive that inhibites the angiotensine conversion enzyme, her pressoric levels had been stable till venlafaxine was introduced in her therapeutic regime. By then she started to show an unstableclinical condition, with elevations of her arterial blood pressure (ABP. Venlafaxine is a potent last generation antidepressant drug, acting in the central nervous system (CNS by inhibiting the reuptake of serotonine and noradrenaline. The drug interaction is demonstrated by monitoring the ABP and using the Naranjo's tool.The patient's general clinical conditions and herprogress are presented, and the hypothetical mechanisms to the interaction, such as

  8. Captopril nephrography and diagnosis of hypertension; Captopril-Nephrographie und Diagnostik der Hypertonie

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    Scheubeck, M. [Wuerzburg Univ. (Germany). Klinik und Poliklinik fuer Nuklearmedizin; Rendl, J. [Wuerzburg Univ. (Germany). Klinik und Poliklinik fuer Nuklearmedizin; Seybold, S. [Wuerzburg Univ. (Germany). Klinik und Poliklinik fuer Nuklearmedizin; Reiners, C. [Wuerzburg Univ. (Germany). Klinik und Poliklinik fuer Nuklearmedizin

    1996-12-01

    Renovascular hypertension (RVH) is caused by renal artery stenosis (NAST) and is potentially curable by surgical treatment or percutaneous transluminal renal angioplasty (PTRA). For the evaluation of these hypertensive patients many tests with different advantages and disadvantages are available. Currently most patients are screened with angiography, which is regarded as gold standard in diagnosis of renal artery stenosis. But angiography only describes morphologic alterations without knowledge of the hemodynamic significance of the stenosis and is both invasive and expensive. In times of decreasing budgets in health systems all over the world non-invasive, cost-effective screening test for identifying patients with potentially correctable hypertension or renal impairment due to renovascular disease are desirable. In case of appropriate clinical preselection of high-risk patients captopril renal scintigraphy (CNG) with a sensitivity and specifity of each about 90% is a sufficient accurate technique in diagnosing renal artery stenosis. In addition, CNG permits accurate selection of patients with renal artery stenosis who will benefit from renal artery repair. However, captopril renal scintigraphy may have limitations in certain clinical situations such as poorly preserved function of the affected kidney. (orig.) [Deutsch] Die renovaskulaere Hypertonie (RVH) ist durch eine Nierenarterienstenose (NAST) verursacht und ist potentiell durch Operation oder perkutane transluminale renale Angioplastie (PTRA) heilbar. Fuer die Diagnostik dieser Erkrankung steht eine Reihe von bildgebenden Verfahren mit unterschiedlichen Vor- und Nachteilen zur Verfuegung. Gegenwaertig wird die Indikation zur Revaskularisation zumeist angiographisch gestellt, was nach wie vor als Goldstandard angesehen wird. Allerdings kann die Angiographie lediglich morphologische Veraenderungen erkennen, ohne dass sie deren haemodynamische Auswirkungen erfasst; sie ist zudem teuer und invasiv. In Zeiten

  9. Application of potassium ferricyanide in the spectrophotometric determination of captopril

    Institute of Scientific and Technical Information of China (English)

    Shi Lei Wang; Min Wang; Quan Min Li

    2009-01-01

    A novel method for the determination of captopril by speetrophotometer is described in this paper. The experiment is based on the fact that Fe(Ⅲ) is reduced to Fe(Ⅱ) by captopril, then the in situ formed Fe(Ⅱ) reacts with potassium ferricyanide to give the soluble prussian blue at pH 4.00, and its maximal adsorption wavelength (λmax) is 735 nm. Good linear relationship is obtained between the absorbance and the concentration of captopril in the wide range of 0.05-20 μg/mL. The linear regression equation is A = -0.04314 + 0.11423C (μg/mL) with a correlation coefficient R = 0.9998. The detection limit (3a/k) is 0.04 μg/mL, the molar absorption coefficient is 2.5×104 L/mol cm. By mensurating the absorbance of soluble prussian blue, the indirect determination of eaptopril can be obtained. This method has been successfully applied to determination of captopril in pharmaceutical samples.Analytical results obtained are satisfactory.

  10. Effects of Sublingual Captopril in Immediate Treatment of Hypertensive Crisis

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    H. Kazerani

    2007-04-01

    Full Text Available Introduction & Objective: Sublingual captopril was shown to be a safe and effective drug to control hypertensive urgencies. However the exact time and efficacy of lowering blood pressure (BP is a matter of interest and importance. In this study we evaluated the time and efficacy of 25 mg sublingual captopril in lowering blood pressure. Materials & Methods: In a randomized clinical trial 101 patients (34 men, 67 women with blood pressure of 180/110 mmHg (or more who had no finding of major organ damage (heart – brain -eyes –renal were studied by prescription of 25 mg sublingual captopril. Then systolic and diastolic blood pressure was measured at 5, 10, 15, 20, 25, 30, 40, 50, 60, 75, 90, 105, 120 minutes following drug administration. Data analysis was performed using paired t-test and SPSS software. Results: The results showed that almost all the patients had some decrease in BP. After 120 minutes blood pressure dropped about 5% in 30%, and 5-30% in 70% of patients, compared to first measured BP. Maximal effect was observed in 25-30 minutes after drug administration: after 30 minutes systolic pressure dropped in 68.4% and diastolic pressure in 65.3% of patients about 5-25%. 47 patients had low response to therapy after 60 minutes, so they received another 25 mg captopril sublingual, which BP dropped in 45% of them. 19 patients were prescribed IV furosemide after 120 minutes. This group had resistant HTN and 25 cases of them were treated with ACEI previously. BP decreased gradually and not more than 30% of first BP. None of the patients encountered side effects. Conclusion: Sublingual captopril is a good, safe, effective, available and cost effective drug, with very low side effects in treating patients with hypertensive crisis. It is recommended to use this drug instead of Nifedipine in all hypertensive patients.

  11. Captopril augments acetylcholine-induced bronchial smooth muscle contractions in vitro via kinin-dependent mechanisms.

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    Agrawal, Naman; Akella, Aparna; Deshpande, Shripad B

    2016-06-01

    Angiotensin converting enzyme (ACE) inhibitors therapy is aassociated with bothersome dry cough as an adverse effect. The mechanisms underlying this adverse effect are not clear. Therefore, influence of captopril (an ACE inhibitor) on acetylcholine (ACh)-induced bronchial smooth muscle contractions was investigated. Further, the mechanisms underlying the captopril-induced changes were also explored. In vitro contractions of rat bronchial smooth muscle to cumulative concentrations of ACh were recorded before and after exposure to captopril. Further, the involvement of kinin and inositol triphosphate (IP₃) pathways for captopril-induced alterations were explored. ACh produced concentration-dependent (5-500 µM) increase in bronchial smooth muscle contractions. Pre-treatment with captopril augmented the ACh-induced contractions at each concentration significantly. Pre-treatment with aprotinin (kinin synthesis inhibitor) or heparin (inositol triphosphate, IP₃-inhibitor), blocked the captopril-induced augmentation of bronchial smooth muscle contractions evoked by ACh. Further, captopril-induced augmentation was absent in calcium-free medium. These results suggest that captopril sensitizes bronchial smooth muscles to ACh-induced contractions. This sensitization may be responsible for dry cough associated with captopril therapy.

  12. Enthalpy of captopril-angiotensin I-converting enzyme binding.

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    Ortiz-Salmerón, E; Barón, C; García-Fuentes, L

    1998-09-18

    High-sensitivity titration calorimetry is used to measure changes in enthalpy, heat capacity and protonation for the binding of captopril to the angiotensin I-converting enzyme (ACE; EC 3.4.15.1). The affinity of ACE to captopril is high and changes slightly with the pH, because the number of protons linked to binding is low. The determination of the enthalpy change at different pH values suggests that the protonated group in the captopril-ACE complex exhibits a heat protonation of approximately -30 kJ/mol. This value agrees with the protonation of an imidazole group. The residues which may become protonated in the complex could be two histidines existing in two active sites, which are joined to the amino acids coordinated to Zn2+. Calorimetric measurements indicate that captopril binds to two sites in the monomer of ACE, this binding being enthalpically unfavorable and being dominated by a large positive entropy change. Thus, binding is favored by both electrostatic and hydrophobic interactions. The temperature dependence of the free energy of binding deltaG degrees is weak because of the enthalpy-entropy compensation caused by a large heat capacity change, deltaCp =-4.3+/-0.1 kJ/K/mol of monomeric ACE. The strong favorable binding entropy and the negative deltaCp indicate both a large contribution to binding due to hydrophobic effects, which seem to originate from dehydration of the ligand-protein interface, and slight conformational changes in the vicinity of the active sites.

  13. Treatment effects of captopril on non-proliferative diabetic retinopathy

    Institute of Scientific and Technical Information of China (English)

    WANG Ning; ZHENG Zhi; JIN Hui-yi; XU Xun

    2012-01-01

    Background Diabetic retinopathy (DR) is one of the most common complications of diabetes.Angiotensin-converting enzyme inhibitor is thought to play an important role in preventing and treating retinal diseases in animal models of DR.The aim of the present study was to investigate the role of angiotensin-converting enzyme inhibitor (ACEI,captopril) in the treatment of patients with non-proliferative DR.Methods Three hundred and seventeen type 2 diabetic patients (88.05% of participants) without or with mild to moderate non-proliferative retinopathy were randomly divided into captopril group (n=202) and placebo group (n=115).All subjects received 24-month follow-up.General clinical examinations,including blood pressure and glycated hemoglobin,as well as comprehensive standardized ophthalmic examinations were performed.Color fundus photography and optical coherence tomography (OCT) were used to grade diabetic retinopathy and detect macular edema respectively.Results The levels of blood pressure and glycated hemoglobin in the two groups of patients remained within the normal range during the entire follow-up and no significant difference was found between the initial and last visits,suggesting that ACEI drugs play a protective role on the DR patients independent of its anti-blood pressure role.DR classification showed that 169 eyes (83.66%) remained unchanged and the DR grade of 33 eyes (16.34%) increased in captopril group,while 84 eyes (73.04%) remained unchanged and the grade of 31 eyes (26.96%) increased in placebo group (P=0.024).Captopril treatment improved macular edema in 55.45% eyes,which was significantly higher than the 37.39% improvement in placebo group (P=0.002).No significant difference was found in the visual acuity between the two groups (P=0.271).Conclusion Captopril can improve or delay the development of DR and macular edema,which can be used in the early treatment of DR patients with type 2 diabetic mellitus.

  14. Nifedipine and captopril in hypertensive crisis in children.

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    Fernando Zapata

    2009-11-01

    Full Text Available Introducción: La crisis hipertensiva es una urgencia pediátrica que se debe manejar con medicamentos de rápida acción, de fácil administración y sin mayores efectos secundarios. El medicamento usado tradicionalmente ha sido el nitroprusiato de sodio endovenoso en infusión continua lo que implica hospitalización en cuidados intensivos con mayores costos y riesgos. Objetivos: Comparar la eficacia y seguridad de la nifedipina y el captopril sublingual en crisis hipertensivas. Material y métodos: Se llevó a cabo un estudio prospectivo en niños entre 1 y 12 años de edad que ingresaron al servicio de pediatría urgencias del Hospital Universitario del Valle en Cali, Colombia, con diagnóstico de crisis hipertensiva. Se realizó monitoreo de la presión arterial sistólica, diastólica y media y de la frecuencia cardíaca antes de administrar los medicamentos y a los 5, 15, 30, 60, 120, 180, 240, 300 y 360 minutos después de administrados. Los dos medicamentos se dieron por vía sublingual a dosis de 0.2 mg/kg. Se vigilaron efectos secundarios después de su administración. Resultados: Durante 16 meses ingresaron 21 pacientes, 10 asignados a nifedipina y 11 a captopril, 13 niños y 8 niñas, con un promedio de edad de 7 años. La reducción de la presión arterial por debajo del percentil 95 inducida por la nifedipina sublingual fue más rápida, en promedio a los 20 minutos, que con captopril (50 minutos. Hasta los 30 minutos las cifras de presión arterial sistólica, diastólica y media fueron estadísticamente inferiores con nifedipina que con captopril, para luego tener una actividad muy similar. Se necesitó una segunda dosis en tres pacientes con nifedipina y uno con captopril. No hubo respuesta en dos pacientes con captopril. No se presentaron efectos secundarios mayores. Con la nifedipina se observó aumento promedio de 10% en la frecuencia cardíaca a los 5 minutos después de ser administrada. Conclusiones: Ambas drogas son

  15. Histomorphologic change of radiation pneumonitis in rat lungs: captopril reduces rat lung injury induced by irradiation

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    Kim, Jin Hee [College of Medicine, Keimhyung Univ., Taegu (Korea, Republic of)

    1999-09-01

    To assess the histomorphologic changes in the rat lung injury induced by radiation, to determine whether captopril reduces the rat lung injury and to evaluate change in TNF-{alpha} and TGF {beta} and rat lung damage by radiation and captopril. Right lungs in male Sprague-Dawley rats were divided irradiation alone (10, 20, 30 Gy) or radiation (same dose with radiation alone group) with captopril (500 mg/L). Radiation alone group were sacrificed at twelve hours and eleven weeks after radiation and radiation with captopril group (captopril group) were sacrificed at eleven weeks after radiation with captopril. We examined the light microscope and electron microscopic features in the groups. In radiation alone group, there were patch parenchymal collapse and consolidation at twelve hours after radiation. The increase of radiation dose shows more prominent the severity and broader the affected areas. Eleven weeks after radiation, the severity and areas of fibrosis had increased in proportion to radiation dose given in the radiation alone group. There was notable decrease of lung fibrosis in captopril group than in radiation alone group. The number of mast cells rapidly increased with increase of radiation dose in radiation alone group and the degree of increase of mast cell number and severity of collagen accumulation more decreased in captopril group than in radiation alone group. In radiation alone group expression of TNF-{alpha} and TGF-{beta}] increased according to increase of radiation dose at twelve hours after radiation in both group. At eleven weeks after radiation, expression of TGF- P increased according to increase of radiation dose in radiation group but somewhat decreased in captopril group. In the captopril group the collagen deposition increased but less dense than those of radiation alone group. The severity of perivascular thickening, capillary change, the number and degranulation of mast cells more decreased in the captopril group than in the radiation

  16. Therapeutic effect of Captopril on rheumatoid arthritis in rats

    Institute of Scientific and Technical Information of China (English)

    Hong-Mei Liu; Kai-Jie Wang

    2014-01-01

    Objective:To investigate the therapeutic effect of the intervention treatment with different doses ofCaptopril onTNF-αcontents in serum of rheumatoid arthritis(RA) rats, and to provide the theoretical proofs for clinical application ofCaptopril in treatments of rheumatoid diseases. Methods:FiftyWistar rats were randomly divided into5 groups, namely,GroupA,GroupB, GroupC,GroupD,GroupE with10 ratsin each group.Injection ofFreund’s complete adjuvant was employed to establish adjuvant-induced arthritis model in rats.GroupA was model group; after model establishment, rats were treated with20 mL normal saline as placebo(ip.).Rats inGroupB were treated with8 mg/kg cyclophosphamide(ip.).Rats inGroupC,D andE were intraperitoneally injected with30 mg/kg,100 mg/kg and300 mg/kgCaptopril respectively.Rats in each group were subjected to continuous treatment for3 weeks, and then sacrificed.Eyeballs of rats were excised and blood was collected.TNF-αcontent in serum were detected usingELISA; each group rats were compared for the hind legs arthrocele.Right ankle tissues of rats were collected to prepare section, and microscopic observation of pathological changes was performed. Results:TNF-αcontent in serum ofGroupA rats was significantly higher than that of rats in other4 groups(P0.05).FromDay8, ankle arthrocele of rats inGroupsB,C,D andE was obviously relieved compared with that ofGroupA rats; the anti-inflammatory effects were gradually enhanced with the extension of medication time.Treatments ofGroupsC,D andE showed significant activities against tardive arthrocele; the degree of ankle arthrocele in rats of these three groups was lower than that ofGroupA rats(P<0.01).Histological observation showed that large amount of inflammatory cells and plasmocyte infiltration was found in ankle synovial tissues ofGroupA rats.Relief of hyperaemia and edema of right ankle synovial tissues as well as significant decrease in synoviocyte layer hyperplasia, intra-articular inflammatory

  17. The effect of captopril on thallium 201 myocardial perfusion in systemic sclerosis

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    Kahan, A.; Devaux, J.Y.; Amor, B.; Menkes, C.J.; Weber, S.; Venot, A.; Strauch, G. (Rene Descartes Univ., Paris (France))

    1990-04-01

    In systemic sclerosis, abnormalities of myocardial perfusion are common and may be caused by a disturbance of the coronary microcirculation. We evaluated the long-term effect of captopril (75 to 150 mg per day) on thallium 201 myocardial perfusion in 12 normotensive patients with systemic sclerosis. Captopril significantly decreased the mean (+/- SD) number of segments with thallium 201 myocardial perfusion defects (6.5 +/- 1.9 at baseline and 4.4 +/- 2.7 after 1 year of treatment with captopril; p less than 0.02) and increased the mean global thallium score (9.6 +/- 1.7 at baseline and 11.4 +/- 2.1 after captopril; p less than 0.05). In a control group of eight normotensive patients with systemic sclerosis who did not receive captopril, no significant modification in thallium results occurred. Side effects with captopril included hypotension (six patients), taste disturbances (one patient), and skin rash (one patient). These side effects subsided when the dosage was reduced. These findings demonstrate that captopril improves thallium 201 myocardial perfusion in patients with systemic sclerosis and may therefore have a beneficial effect on scleroderma myocardial disease.

  18. Mucosal-dominant pemphigus vulgaris in a captopril-taking woman with angioedema.

    Science.gov (United States)

    Gornowicz-Porowska, Justyna; Dmochowski, Marian; Pietkiewicz, Pawel; Bowszyc-Dmochowska, Monika

    2015-01-01

    We describe a 39-year-old woman with an apparent captopril-induced, contact mucosal-dominant pemphigus vulgaris and angioedema, who took captopril during a bout of arterial hypertension. This exposure suggests that captopril and pathophysiology of angioedema stimulated the development of pemphigus vulgaris, which was diagnosed using the novel, indirect immunofluorescence BIOCHIP mosaic, with the modification to detect serum IgG4 autoantibodies. We discuss the patient, who experienced a chain of events leading to the active stage of pemphigus vulgaris, and review concepts of pemphigus vulgaris inducible by drugs and pathological immunity.

  19. NIR hyperspectral imaging to evaluate degradation in captopril commercial tablets.

    Science.gov (United States)

    França, Leandro de Moura; Pimentel, Maria Fernanda; Simões, Simone da Silva; Grangeiro, Severino; Prats-Montalbán, José M; Ferrer, Alberto

    2016-07-01

    Pharmaceutical quality control is important for improving the effectiveness, purity and safety of drugs, as well as for the prevention or control of drug degradation. In the present work, near infrared hyperspectral images (HSI-NIR) of tablets with different expiration dates were employed to evaluate the degradation of captopril into captopril disulfide in different layers, on the top and on the bottom surfaces of the tablets. Multivariate curve resolution (MCR) models were used to extract the concentration distribution maps from the hyperspectral images. Afterward, multivariate image techniques were applied to the concentration distribution maps (CDMs), to extract features and build models relating the main characteristics of the images to their corresponding manufacturing dates. Resolution methods followed by extracting features were able to estimate the tablet manufacture date with a prediction error of 120days. The model developed could be useful to evaluate whether a sample shows a degradation pattern consistent with the date of manufacturing or to detect abnormal behaviors in the natural degradation process of the sample. The information provided by the HIS-NIR is important for the development of the process (QbD), looking inside the formulation, revealing the behavior of the active pharmaceutical ingredient (API) during the product's shelf life.

  20. Renal scintigraphy by captopril in hypertension with hypokalemia; Scintigraphie renal au captopril dans l`hypertension avec hypokaliemie

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    Grandet, P.J. [CH PAU, BP 1156, 64046 PAU Universite Cedex (France)

    1997-12-31

    A study on 30 files of hypertensive patients with an associated hypokalemia was achieved from January 1996 to May 1997. The technique was that of a basic examination effected by MAG 3 (80 MBq), followed by oral intake of 25 to 50 mg of Captopril; one hour after, a new examination was done by MAG 3, with 130 MBq. The classical aspect of isotopic nephro-gram (IN) was not constantly found in case of renal artery stenosis. The reduction of the peak of the level approached might be the only sign, even without any delay of this summit; the lowering of the peak after Captopril of at least 50% should be taken into account. Thus, on the basis of these arguments, we have found 5 stenoses of renal artery. Twenty patients considered as normal have had not arteriography and are relatively well-equilibrated by medical treatment. Among the false negatives, one is explained by a renal insufficiency given an IE of bad quality, while the other is a dysplasia of renal arteries. The 3 false positives presented a discrete difference between the two examinations by MAG 3. Consequently, we considered that the discrete signs should not be retained. The slowing down of transit time, the net lowering of the peak or its delay (classically, 11 min) are good arguments

  1. Captopril-induced sialadenitis in a patient with end-stage renal disease

    Science.gov (United States)

    Mahdiabadi, Fatemeh Musavi; Nikvarz, Naemeh

    2016-01-01

    Sialadenitis is a rare adverse effect of captopril. We report a case of captopril-induced sialadenitis in a patient with end-stage renal disease (ESRD). A 20-year-old man with ESRD encountered parotid and submandibular swelling after receiving two doses of captopril, administered sublingually. Despite of prescribing dexamethasone, resuming hemodialysis, and discontinuing other drugs that also can cause parotitis, he improved later than what was reported in patients with normal renal function. In conclusion recovery from captopril-induced sialadenitis in patients with ESRD may be more prolonged than that of patients with normal renal function; moreover, early hemodialysis which helps in drug removal may be the most effective treatment. PMID:27162811

  2. Immunomodulatory effect of captopril and local irradiation on myeloid-derived suppressor cells

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    Cho, Won Kyung; Shin, Sung Won; Kim, Shin Yeong; Choi, Chang Hoon; Park, Won; Noh, Jae Myoung [Dept. of Radiation Oncology, Samsung Medical Center, Sungkyunkwan University School of Medicine, Seoul (Korea, Republic of); Hong, Chang Won [Dept. of Physiology, Kyungpook National University School of Medicine, Daegu (Korea, Republic of)

    2016-09-15

    This study is to investigate the effect of captopril when combined with irradiation. 4T1 (mouse mammary carcinoma) cells were injected in the right hind leg of Balb/c mice. Mice were randomized to four groups; control (group 1), captopril-treated (group 2), irradiated (group 3), irradiated and captopril-treated concurrently (group 4). Captopril was administered by intraperitoneal injection (10 mg/kg) daily and irradiation was delivered on the tumor-bearing leg for 15 Gy in 3 fractions. Surface markers of splenic neutrophils (G-MDSCs) and intratumoral neutrophils (tumor-associated neutrophils [TANs]) were assessed using flow cytometry and expression of vascular endothelial growth factor (VEGF) and hypoxia-inducible factor 1 alpha (HIF-1α) of tumor was evaluated by immunohistochemical (IHC) staining. The mean tumor volumes (±standard error) at the 15th day after randomization were 1,382.0 (±201.2) mm{sup 3} (group 1), 559.9 (±67.8) mm{sup 3} (group 3), and 370.5 (± 48.1) mm{sup 3} (group 4), respectively. For G-MDSCs, irradiation reversed decreased expression of CD{sub 101} from tumor-bearing mice, and additional increase of CD{sub 101} expression was induced by captopril administration. Similar tendency was observed in TANs. The expression of tumor-necrosis factor-associated molecules, CD{sub 120} and CD{sub 137}, are increased by irradiation in both G-MDSCs and TANs. Further increment was observed by captopril except CD{sub 120} in TANs. For IHC staining, VEGF and HIF-1α positivity in tumor cells were decreased when treated with captopril. Captopril is suggested to have additional effect when combined to irradiation in a murine tumor model by modulation of MDSCs and angiogenesis.

  3. Captopril and lisinopril only inhibit matrix metalloproteinase-2 (MMP-2) activity at millimolar concentrations.

    Science.gov (United States)

    Kuntze, Luciana B; Antonio, Raquel C; Izidoro-Toledo, Tatiane C; Meschiari, Cesar A; Tanus-Santos, Jose E; Gerlach, Raquel F

    2014-03-01

    Matrix metalloproteinase-2 (MMP-2) shares structural similarities with the angiotensin-converting enzyme (ACE). ACE inhibitors have been described to inhibit MMP-2, but this inhibitory potential was not shown using a highly purified MMP-2. This study aimed to investigate the inhibitory potential of captopril and lisinopril regarding MMP-2 activity. The first objective was to test the potential of captopril to change the pH of the buffer solution. The second objective was to test the direct inhibitory effect of captopril and lisinopril on plasma MMP-2 and on recombinant human MMP-2 (rhMMP-2). The in vitro activity assays included gelatin zymography and a fluorimetric assay. Captopril solubilization significantly decreased the pH of the 50 mM Tris buffer solution at the following concentrations: 2 mM (p MMP-2 and rhMMP-2 showed that inhibition only happened at captopril concentrations ≥ 4 and 1 mM, respectively (p MMP-2 (p MMP-2 are 3 orders of magnitude higher than those present in vivo after drug administration. We also discuss possible pitfalls for gelatinase inhibitory assays (besides the obvious pH problem already cited). In conclusion, this study's data show that captopril and lisinopril did not inhibit MMP-2 directly at the concentrations reached in vivo.

  4. Detection of captopril based on its enhanced resonance light scattering signals of fluorosurfactant-capped gold nanoparticles

    Institute of Scientific and Technical Information of China (English)

    2010-01-01

    In this study,based on its enhancement effect on resonance light scattering (RLS) of fluorosurfactant (FSN)-capped gold nanoparticles (GNPs),we reported a simple approach for the rapid sensing of captopril. Under optimum conditions,the lowest detectable concentration of captopril through this approach (S/N=3) was 0.01μg/mL. The calibration curve was linear over the range of 0.08-4.0μg/mL for the detection of captopril. The recoveries of captopril were found to fall in the range between 99% and 100%. We have...

  5. Clonidine versus Captopril for Severe Postpartum Hypertension: A Randomized Controlled Trial

    Science.gov (United States)

    Noronha Neto C, Carlos; Katz, Leila; Coutinho, Isabela C.; Souza, Alex R.; Amorim, Melania M.

    2017-01-01

    Background Changes during the puerperium are still unclear, particularly in women with hypertension. The choice of antihypertensives, both to control very high blood pressure episodes and to keep blood pressure stable, also requires further elucidation. Currently, there are no clear data to guide the decision for the choice of postpartum antihypertensives. Captopril plays an important role in the treatment of very high blood pressure episodes and may be used postpartum. Clonidine has been used as an alternative in pregnant or postpartum women with contraindications to captopril, with satisfactory effect. The objective of the present study was to evaluate the effectiveness and safety of clonidine compared to captopril for treating severe postpartum hypertension. Methods and findings A randomized, drug-controlled, triple-blind clinical trial evaluating postpartum women receiving captopril or clonidine. Inclusion criteria consisted of: women with hypertensive disorders of pregnancy systolic blood pressure (SBP) ≥180 mmHg and/or diastolic blood pressure (DBP) ≥110 mmHg], requiring magnesium sulfate. Exclusion criteria were: heart disease, smoking, illicit drug use, contraindications to captopril, clonidine or oral medication, and having used captopril/clonidine previously. The primary outcome was the frequency of very high blood pressure episodes while in the obstetric intensive care unit. A total of 90 postpartum women met the study inclusion criteria, with 45 randomized to each group. There were fewer very high blood pressure episodes during hospitalization (2.1 ± 2.1 vs. 3.5 ± 4.7, p = 0.08), greater percentage reduction in SBP (14.0% ± 8.6% vs. 10.8% ± 8.8%, p = 0.08) and fewer women requiring sodium nitroprusside (2.3% vs. 13.3%; RR: 0.17; 95%CI: 0.02–1.39; p = 0.06) in the clonidine group compared to the captopril group; however, these differences were not significant. The groups were similar regarding daily mean SBP or DBP; however, on the third

  6. Determination of captopril by hplctandem mass spectrometry: application in a bioequivalence study

    Directory of Open Access Journals (Sweden)

    Aline Kércia Alves Soares

    2012-03-01

    Full Text Available Objective: To assess three different captopril tablet formulations of 25mg for their bioavailability (Capoten® as the reference formulation and Captopril from FURP and Farmanguinhos as the test formulations in 24 healthy volunteers of both sexes. Methods: The volunteers were free from serious disease, as assessed by physical and psychiatricexamination, EKG, and laboratory tests. The study was open, with a three-period crossover design and a five-day washout period. Plasma samples were obtained over a 24-hour interval.Captopril concentrations were determined by reversed phase liquid chromatography tandem mass spectrometry (LC-MS-MS. Results: The geometric mean for Capoten® /Captopril- FURP 25 mg was 96.9 % for AUC0-24, 95.58 % for AUC0-∞, and 98.17% for Cmax. The 90% confidence intervals (CI were 84.8-100.65%, 88.5-109.42% and 82.52-116.8%, respectively. The geometric mean for Capoten®/Captopril-Farmanguinhos 25 mg was 99.63 % for AUClast, 98.52% for AUC0-∞, and 95.52 for Cmax. The 90% CI were 87.23-113.8%, 86.06-112.79% and 80.29-113.64%, respectively. Therefore, the 90% CI for Cmax, AUClast, AUC0-∞ were within the 80-125% interval proposed by the Food and Drug Administration. Conclusion: Captopril- FURP and Captopril-Farmanguinhos 25 mg tablets were bioequivalent to Capoten® 25 mg,according to both the rate and extent of absorption.

  7. Alteration of split renal function during Captopril treatment. Diagnostic significance in renovascular hypertension

    Energy Technology Data Exchange (ETDEWEB)

    Aburano, Tamio; Takayama, Teruhiko; Nakajima, Kenichi; Tonami, Norihisa; Hisada, Kinichi; Yasuhara, Shuichirou; Miyamori, Isamu; Takeda, Ryoyu

    1987-07-01

    Two different methods to evaluate the alteration of split renal function following continued Captopril treatment were studied in a total of 21 patients with hypertension. Eight patients with renovascular hypertension (five with unilateral renal artery stenosis and three with bilateral renal artery stenoses), three patients with diabetic nephropathy, one patient with primary aldosteronism, and nine patients with essential hypertension were included. The studies were performed the day prior to receiving Captopril (baseline), and 6th or 7th day following continued Captopril treatment (37.5 mg or 75 mg/day). Split effective renal plasma flow (ERPF) and glomerular filtration rate (GFR) after injections of I-131 hippuran and Tc-99m DTPA were measured using kidney counting corrected for depth and dose, described by Schlegel and Gates. In the patients with renovascular hypertension, split GFR in the stenotic kidney was significantly decreased 6th or 7th day following continued Captopril treatment compared to a baseline value. And split ERPF in the stenotic kidney was slightly increased although significant increase of split ERPF was not shown. In the patients with diabetic nephropathy, primary aldosteronism or essential hypertension, on the other hand, split GFR was not changed and split ERPF was slightly increased. These findings suggest that the Captopril induced alterations of split renal function may be of importance for the diagnosis of renovascular hypertension. For this purpose, split GFR determination is more useful than split ERPF determination.

  8. A Prospective Comparison of Duplex Ultrasonography, Captopril Renography, MRA, and CTA in Assessing Renal Artery Stenosis

    Energy Technology Data Exchange (ETDEWEB)

    Ekloef, H.; Ahlstroem, H.; Magnusson, A.; Andersson, L.G.; Andren, B.; Haegg, A.; Bergqvist, D.; Nyman, R. [Uppsala Univ. Hospital (Sweden). Depts. of Radiology, Clinical Physiology, Medicine, and Surgery

    2006-10-15

    Purpose: To prospectively compare the diagnostic accuracy of duplex ultrasonography, captopril renography, computed tomography angiography (CTA), and 3D Gd magnetic resonance angiography (MRA) in diagnosing hemodynamically significant renal artery stenosis (RAS). Material and Methods: The standard of reference was measurement of transstenotic pressure gradient. Fifty-eight hypertensive patients with suspicion of RAS were evaluated, when possible, by all five techniques. Sensitivity and specificity to detect RAS were compared for each technique on both a patient and kidney basis. Discrepancies were evaluated separately and classified as borderline, method dependent, or operator dependent. Results: The prevalence of RAS was 77%. The sensitivity/specificity of ultrasonography, captopril renography, CTA, and MRA in detecting kidneys with RAS was 73/71%, 52/63%, 94/62%, and 93/91%, respectively. Ultrasonography had a significantly lower sensitivity than CTA and MRA (P <0.001) but higher than captopril renography (P = 0.013). Borderline RAS was the main cause for discrepancies. Conclusion: MRA and CTA were significantly better than duplex ultrasonography and captopril renography in detecting hemodynamically significant RAS. The ultrasonography criteria for RAS based on the evaluation of renal peak systolic velocity and renal/aortic ratio are questionable. Captopril renography cannot be recommended for assessing RAS.

  9. Central injection of captopril inhibits the blood pressure response to intracerebroventricular choline

    Directory of Open Access Journals (Sweden)

    N. Isbil-Buyukcoskun

    2001-06-01

    Full Text Available In the present study, we investigated the involvement of the brain renin-angiotensin system in the effects of central cholinergic stimulation on blood pressure in conscious, freely moving normotensive rats. In the first step, we determined the effects of intracerebroventricular (icv choline (50, 100 and 150 µg on blood pressure. Choline increased blood pressure in a dose-dependent manner. In order to investigate the effects of brain renin-angiotensin system blockade on blood pressure increase induced by choline (150 µg, icv, an angiotensin-converting enzyme inhibitor, captopril (25 and 50 µg, icv, was administered 3 min before choline. Twenty-five µg captopril did not block the pressor effect of choline, while 50 µg captopril blocked it significantly. Our results suggest that the central renin-angiotensin system may participate in the increase in blood pressure induced by icv choline in normotensive rats.

  10. Determination of captopril by high-performance liquid chromatography with direct electrogenerated chemiluminescence

    Science.gov (United States)

    Sun, Yonghua; Zhang, Zhujun; Zhang, Xinfeng

    2013-03-01

    Captopril exhibit electrogenerated chemiluminescence (ECL) in NaNO3 solution when constant current is exerted. Based on this observation, a direct ECL method coupled with high-performance liquid chromatography (HPLC) separation is developed for determination of captopril in human serum. Factors affected the ECL emission are investigated. Under the optimal conditions, the ECL intensity has a linear relationship with the concentration of captopril in the range of 4.0 × 10-6-2.0 × 10-3 g mL-1 and the detection limit is 2 × 10-6 g mL-1 (S/N = 3). Compared with the common electrogenerated chemiluminescence experiments, the developed method need no any other fluorescence additives.

  11. Captopril-induced reduction of regurgitation fraction in aortic insufficiency

    Energy Technology Data Exchange (ETDEWEB)

    Kropp, J.; Reske, S.N.; Biersack, H.J.; Heck, I.; Mattern, H.; Winkler, C.

    1984-01-01

    Stimulated Renin-Angiotensin System (RAS) in aortic insufficiency (AI) leads to increased afterload and consequently to augmented aortic regurgitation (R). Therefore Captopril (C) mediated RAS-inhibition should diminish systemic vascular resistance and thus reduce R. In 9 patients (pts) with pure severe AI regurgitation fraction (RF) and left ventricular ejection fraction (LVEF) were determined before and 1 hr after i.v. injection of 25 mg C by gated radionuclide ventriculographie (RNV), using red blood cells labeled in vivo with 15 mCi Tc-99m. Enddiastolic and endsystolid frames were derived from the left ventricular volume curve. ROI's were selected over both ventricles. Ventricular boundaries were defined by a fourier phase image overlay. RF was calculated by the background corrected count rate ratio of left and right ventricular ROI. Arterial blood pressure (BP), heart rate (HR), plasma levels of angiotensin I, II (A1,A2), and the activity of angiotensin converting enzyme (ACE) were determined before and 1 hr after C-injection. Before C-medication mean RF was 54% (range 34% - 67%), after C mean RF decreased to 37% (17% - 59% range, rho<.05). Mean LVEF increased not significantly from 60% (range 51%-70%) to 66% (range 56% - 77%, rho>0.55). C did not significantly change HR or BP (HR: rho>0.9, BP: rho>0.6). A2 and ACE activity decreased to 40% and 50% of control values (rho<.01), respectively. A1 increased excessively. The authors conclude that the inhibition of ACE reduces significantly aortic regurgitation in patients with A1 and has thus a beneficial effect on left ventricular performance.

  12. Valsartan, captopril, or both in myocardial infarction complicated by heart failure, left ventricular dysfunction, or both

    DEFF Research Database (Denmark)

    Pfeffer, Marc A; McMurray, John J V; Velazquez, Eric J;

    2003-01-01

    BACKGROUND: Angiotensin-converting-enzyme (ACE) inhibitors such as captopril reduce mortality and cardiovascular morbidity among patients with myocardial infarction complicated by left ventricular systolic dysfunction, heart failure, or both. In a double-blind trial, we compared the effect of the...

  13. Targeting of captopril to the kidney : towards selective renal ACE inhibition

    NARCIS (Netherlands)

    Kok, Robbert Jan

    1998-01-01

    The present thesis deals with the targeting of the angiotensin converting enzyme (ACE) inhibiting drug captopril to the kidney. Drug targeting is a technique that aims at a more specific action of drugs by restricting their distribution to a specific part of the body. In other words, the targeting o

  14. Application and evaluation of postural stimulation test and captopril challenge test in diagnosis of primary aldosteronism

    Institute of Scientific and Technical Information of China (English)

    郝岩

    2014-01-01

    Methods One hundred and twenty-eight patients with essential hypertension and 71 patients with primary aldosteronism were included in this study.The efficacy of different diagnostic indices of postural stimulation test(PST)with captopril challenge test(CCT)were compared by constructing receiver operating characteristic curve.The

  15. Captopril and telmisartan treatments attenuate cadmium-induced testicular toxicity in rats.

    Science.gov (United States)

    Fouad, Amr A; Jresat, Iyad

    2013-04-01

    The possible protective effect of captopril, an angiotensin-converting enzyme inhibitor, vs. telmisartan, an angiotensin II-receptor antagonist, was investigated in rats with testicular injury induced by a single i.p. injection of cadmium chloride (2 mg/kg). Captopril (60 mg/kg/day, p.o.) and telmisartan (10 mg/kg/day, p.o.) were given for five consecutive days, starting 3 days before cadmium administration. Both agents significantly increased serum testosterone level, which was reduced by cadmium, suppressed lipid peroxidation, restored the depleted reduced glutathione, decreased the elevations of nitric oxide, tumor necrosis factor-α, and cadmium ion levels, and attenuated the reductions of selenium and zinc ions in testicular tissue resulted from cadmium administration. Immunohistochemical analysis revealed that both captopril and telmisartan significantly reduced the cadmium-induced expression of inducible nitric oxide synthase, nuclear factor-κB, Fas ligand, and caspase-3 in testicular tissue. The differences between the results obtained with captopril and telmisartan were insignificant, suggesting that both drugs equally protected the testicular tissue from the detrimental effects of cadmium.

  16. Influence of tiopronin, captopril and levamisole therapeutics on the oxidative degradation of hyaluronan.

    Science.gov (United States)

    Valachová, Katarína; Baňasová, Mária; Topoľská, Dominika; Sasinková, Vlasta; Juránek, Ivo; Collins, Maurice N; Šoltés, Ladislav

    2015-12-10

    The ability to protect hyaluronic acid (HA) from oxidative degradation by cupric ions and ascorbate (production of (•)OH and peroxy-type radicals) during acute phase joint inflammation has been investigated using the following drugs: tiopronin, captopril, and levamisole. Radical scavenging activity, i.e. the propensity for donation of electrons was assessed for the drugs by ABTS and DPPH assays. The kinetics of HA degradation have been measured in the presence of each drug using rotational viscometry. The results of ABTS and DPPH assays show the highest radical scavenging activity for captopril, followed by tiopronin. For levamisole, no effect was observed. Captopril and tiopronin prevented HA degradation induced by (•)OH radicals in a similar manner, while tiopronin was more effective in scavenging peroxy-type radicals. On the other hand, levamisole was shown to be a pro-oxidant. Recovered HA fragments were characterized using FT-IR analysis, the incorporation of a sulphur atom from captopril and tiopronin but not from levamisole into the HA molecule was demonstrated.

  17. Renovascular hypertension identified by captopril-induced changes in the renogram

    Energy Technology Data Exchange (ETDEWEB)

    Geyskes, G.G.; Oei, H.Y.; Puylaert, C.B.; Mees, E.J.

    1987-05-01

    Radioisotope renography was performed in 21 patients with hypertension and unilateral renal artery stenosis with and without premedication with 25 mg of captopril, and the results were compared with the effect of percutaneous transluminal angioplasty on the blood pressure, assessed 6 weeks after angioplasty. Angioplasty caused a considerable decrease in blood pressure in 15 of the 21 patients. In 12 of these 15 patients, captopril induced changes in the time-activity curves of the affected kidney only, suggesting deterioration of the excretory function of that kidney, while the function of the contralateral kidney remained normal. After angioplasty the asymmetry in the time-activity curves diminished despite identical pretreatment with captopril. Such captopril-induced unilateral impairment of the renal function was not seen in the six patients with unilateral renal artery stenosis whose blood pressure did not change after percutaneous transluminal angioplasty or in 13 patients with hypertension and normal renal arteries. The functional impairment of the affected kidneys was characterized by a decrease of /sup 99m/Tc-diethylenetriamine pentaacetic acid uptake and a delay of /sup 131/I-hippurate excretion, while the /sup 131/I-hippurate uptake remained unaffected. These data are in agreement with a reduced glomerular filtration rate and diuresis during preservation of the renal blood flow, changes that can be expected after converting enzyme inhibition in a kidney with low perfusion and an active, renin-mediated autoregulation of the glomerular filtration rate. These data suggest that functional captopril-induced unilateral changes, shown by split renal function studies with noninvasive gamma camera scintigraphy, can be used as a diagnostic test for renovascular hypertension caused by unilateral renal artery stenosis.

  18. Reusable fluorescent sensor for captopril based on energy transfer from photoluminescent graphene oxide self-assembly multilayers to silver nanoparticles

    Science.gov (United States)

    Sun, Xiangying; Liu, Bin; Li, Shuchun; Li, Fang

    2016-05-01

    In this work we designed a self-assembly multilayers, in which photoluminescent graphene oxide was employed as a fluorescence probe. This multilayers film can effectively recognize captopril by resonance energy transfer from graphite oxide to silver nanoparticles. A new interfacial sensing method for captopril with high signal to noise ratio was established, by means of that multilayers was quenched by silver nanoparticles and subsequently recovered by adding captopril. The linear relation between intensity and captopril concentration was good, and the detection limit was found to be 0.1578 μM. Also, this novel detection platform demonstrated intriguing reusable properties, and the sensor could be repeated more than ten times without obviously losing its sensing performance.

  19. [The effects of captopril and metoprolol on blood pressure and side effects in patients with mild to moderate hypertension].

    Science.gov (United States)

    Kornerup, H J; Korsager, S

    1989-04-03

    A material of 76 patients from general practice treated with diuretics for mild to moderate hypertension were randomized to supplementary treatment with captopril (39 patients) and metoprolol (37 patients), respectively, on account of diastolic blood pressure greater than or equal to 95 mmHg. Satisfactory regulation of the blood pressure (diastolic blood pressure less than or equal to 90 mmHg) and acceptable wellbeing was obtained in 29 patients in the captopril group and in 23 patients in the metoprolol group. Six patients in the captopril group were excluded on account of absence of effect on the blood pressure and four dropped out on account of side effects. In the metoprolol group, nine patients were excluded on account of absence of effect on the blood pressure and five on account of side effects. This difference was not significant. In the captopril group, 14 side effects were registered in eight patients while 23 side effects were observed in 15 patients in the metoprolol group. This difference was not statistically significant, p greater than 0.05 (risk for type 2 error = 60%). It is concluded that captopril + a diuretic is just as effective a form of treatment of slight to moderate hypertension as metoprolol + a diuretic and that treatment with captopril + a diuretic is associated with so few side effects that it may be considered as an alternative first choice of treatment in cases of slight to moderate hypertension.

  20. Effect of enhancers on permeation kinetics of captopril for transdermal system

    Directory of Open Access Journals (Sweden)

    Desai B

    2008-01-01

    Full Text Available Transdermal drug delivery system has seen a veritable explosion in the past decades. In the present scenario, very few transdermal patches are commercially available. The captopril being an antihypertensive drug requires chronic administration. Since the drug has an extensive first-pass metabolism, an attempt was made to develop transdermal drug delivery system for better patient compliance. In this study, flux and permeation enhancement trials of captopril were carried out using modified Franz diffusion cells through siloxane membrane for 8 h. Citral and dimethyl formamide as permeation enhancers showed the best permeability as compared to sodium tauroglycholate, sodium lauryl sulfate, etc. One longstanding approach for improving transdermal drug delivery uses penetration enhancers (also called sorption promoters or accelerants, which penetrate into skin to reversibly decrease the barrier resistance.

  1. Therapeutic Effect of Captopril, Pentoxifylline, and Cordyceps Sinensis in Pre-Hepatic Portal Hypertensive Rats

    Science.gov (United States)

    Ahmed, Ahmed F.; El-Maraghy, Nabila N.; Ghaney, Rasha H. Abdel; Elshazly, Shimaa M.

    2012-01-01

    Background/Aim: Portal hypertension is an important and potentially fatal complication of liver disease whereby cellular and fibrotic alterations manifest to increase portal venous pressure. The aim of this study is to investigate the effect of captopril, pentoxifylline (PTX), and cordyceps sinensis in pre-hepatic portal hypertensive rats. Settings and Design: Wister male rats were divided at random into 3 main groups: the first group: control rats. The second group: sham-operated rats and the third group: prehepatic portal hypertensive rats (PHPHT) induced by regulated pre-hepatic portal vein ligation. After 14 days, Group 3 was subdivided into 5 subgroups. Subgroup (1): portal vein-ligated (PVL) was killed at once; Subgroup (2): received distilled water for 30 days (untreated PVL group); subgroups 3-5 were treated with captopril (60 mg/kg, orally); PTX (100 mg/kg, orally); and C. sinensis (200 mg/kg, orally), respectively, as a single daily dose for 30 days. Patients and Methods: Portal pressure, nitric oxide (NO), antioxidant enzymes, Liver enzymes, and creatinine levels were measured to evaluate the status of the liver state. Results: Portal vein ligation produced significant increments in liver enzymes, NO, creatinine and portal pressure concomitant with significant decrements in glutathione content and superoxide dismutase activity. Treatment with captopril, PTX, and C. sinensis resulted in a significant reduction in liver enzymes, NO, creatinine and portal pressure and observable increase in antioxidant enzymes. Conclusions: captopril, PTX, and C. sinensis have promising effect in controlling PHPHT and reducing hyperdynamic circulatory state through reduction of portal pressure and NO level. PMID:22626797

  2. Therapeutic effect of captopril, pentoxifylline, and cordyceps sinensis in pre-hepatic portal hypertensive rats

    Directory of Open Access Journals (Sweden)

    Ahmed F Ahmed

    2012-01-01

    Full Text Available Background/Aim: Portal hypertension is an important and potentially fatal complication of liver disease whereby cellular and fibrotic alterations manifest to increase portal venous pressure. The aim of this study is to investigate the effect of captopril, pentoxifylline (PTX, and cordyceps sinensis in pre-hepatic portal hypertensive rats. Settings and Design: Wister male rats were divided at random into 3 main groups: the first group: control rats. The second group: sham-operated rats and the third group: prehepatic portal hypertensive rats (PHPHT induced by regulated pre-hepatic portal vein ligation. After 14 days, Group 3 was subdivided into 5 subgroups. Subgroup (1: portal vein-ligated (PVL was killed at once; Subgroup (2: received distilled water for 30 days (untreated PVL group; subgroups 3-5 were treated with captopril (60 mg/kg, orally; PTX (100 mg/kg, orally; and C. sinensis (200 mg/kg, orally, respectively, as a single daily dose for 30 days. Patients a nd M ethods: Portal pressure, nitric oxide (NO, antioxidant enzymes, Liver enzymes, and creatinine levels were measured to evaluate the status of the liver state. Results: Portal vein ligation produced significant increments in liver enzymes, NO, creatinine and portal pressure concomitant with significant decrements in glutathione content and superoxide dismutase activity. Treatment with captopril, PTX, and C. sinensis resulted in a significant reduction in liver enzymes, NO, creatinine and portal pressure and observable increase in antioxidant enzymes. Conclusions: captopril, PTX, and C. sinensis have promising effect in controlling PHPHT and reducing hyperdynamic circulatory state through reduction of portal pressure and NO level.

  3. Consequences of reversal of hypertensive cardiac hypertrophy by captopril on left ventricular pumping ability and performance.

    Science.gov (United States)

    Saragoça, M A; Cezaretti, M L; Bessa, A M; Casarini, D; Almeida, J B; Amorim, M P; Ramos, O L

    1987-12-01

    Left ventricular hypertrophy can be reversed by treatment of hypertension with captopril but the consequences of this regression are not yet fully described. We studied the maximal capacity of the hypertrophied and hypertrophy-reversed ventricle to generate pressure during transient total occlusion of the aorta, and also the left ventricular end-diastolic pressure required to meet this maximal effort. Two-kidney, one clip Goldblatt (renal hypertensive rats; RHR) hypertension was induced in 17 Wistar rats, eight of which were treated with captopril (RHR-C: 50 mg/kg given orally) from the fourth to the eighth week. Sham-operated controls (SC) remained untreated, or were treated with similar doses of captopril (SC-C). Significantly lower heart weights were found in RHR-C than in RHR (2.88 +/- 0.15 versus 2.38 +/- 0.04; P less than 0.001). During transient total occlusion of the aorta, the maximal intraventricular pressure developed in RHR-C was not significantly different from that in RHR, but left ventricular end-diastolic pressure was significantly less in RHR-C than in RHR (21.4 +/- 2.2 versus 34.3 +/- 3.8; P less than 0.01). The analysis of pressure-volume characteristics of the hypertrophied left ventricles and those in which hypertrophy was reversed revealed similar compliances between these two groups. Our data suggest that there was a mechanical improvement in the heart function after reversal of left ventricular hypertrophy.

  4. EFFECTS OF CAPTOPRIL, DILTIAZEM AND DOBUTAMINE ON PERMEABILITY OF RAT AORTIC ENDOTHELIAL CELL MONOLAYERS

    Institute of Scientific and Technical Information of China (English)

    王晓峰; 由广旭; 皮绍文; 秦永文

    2001-01-01

    To investigate the effects of angiotensin converting enzyme inhibitor captopril, calcium channel blocker diltiazem and β-adrenoceptor antagonist dobutamine on the permeability of rat aortic endothelial monolayers.Methods Trauma-free isolation by Chen et al was adopted in the culture of rat aortic endothelial cells. Rat aortic endothelial cells were seeded on the nitrocellulose microporous filters. Eight days after seeding, the monolayers could be used for measuring the permeability. Before being perfused, monolayers were treated with captopril, diltiazem and dobutamine for 4 hours successively. The prepared filters were mounted on the Boydon chambers and perfused with hyperlipemia containing FITC-labeled albumin. The fluid filtering through the monolayers and the filter was collected and the albumin concentration was measured. At the same time, cholesterol, triglyceride, lipoprotein A and lipoprotein B concentrations of the collected fluid were also measured by ELISA.Results The above three drugs decreased the permeability of aortic endothelial cell monolayers to water, cholesterol, triglyceride lipoprotein A and lipoprotein B significantly. Dobutamine had more significant effects than the other two drugs. But diltiazem worked well in the clearance of albumin, while the other two drugs had no obvious effect.Conclusion Captopril, diltiazem and dobutamine may decrease the infiltration of lipids and lipoproteins into the subendothelial space, thus they can be used to prevent and ameliorate atherosclerosis.

  5. Preparation and Characterization of Cerium (III Doped Captopril Nanoparticles and Study of their Photoluminescence Properties

    Directory of Open Access Journals (Sweden)

    Ghamami Shahriar

    2016-01-01

    Full Text Available In this research Ce3+ doped Captopril nanoparticles (Ce3+ doped CAP-NP were prepared by a cold welding process and have been studied. Captopril may be applied in the treatment of hypertension and some types of congestive heart failure and for preventing kidney failure due to high blood pressure and diabetes. CAP-NP was synthesized by a cold welding process. The cerium nitrate was added at a ratio of 10% and the optical properties have been studied by photoluminescence (PL. The synthesized compounds were characterized by Fourier transform infrared spectroscopy. The size of CAP-NP was calculated by X-ray diffraction (XRD. The size of CAP-NP was in the range of 50 nm. Morphology of surface of synthesized nanoparticles was studied by scanning electron microscopy (SEM. Finally the luminescence properties of undoped and doped CAP-NP were compared. PL spectra from undoped CAP-NP show a strong pack in the range of 546 nm after doped cerium ion into the captopril appeared two bands at 680 and 357 nm, which is ascribed to the well-known 5d–4f emission band of the cerium.

  6. Comparative study between the use of isosorbide dinitrate and captopril in hypertensive emergency treatment.

    Directory of Open Access Journals (Sweden)

    Brandy Viera Valdés

    2005-04-01

    Full Text Available Fundament: Oral antihypertensive drugs are lacking in our environment at present in tog hypertensive urgencies, that is why new therapeutic alternatives are necessary to treat this medical problem. Objective: To assess the effect of Isosorbide Dinitrate in the treatment of hypertensive urgencies the system of urgencies. Method: a cuasi experimental study was designed with 60 patients with this diagnosis. The patients were divided into two groups. The patients of one group received treatment for the hypertensive crisis with Isosorbide Dinitrate 10 mg sub lingually and the others had their treatment with Captopril 25 mg p.o. Results: The response of the treatment with Isosorbide Dinitrate with similar to the treatment with Captopril. High Blood Pressure was controlled in 66,6 % with Isosorbide Dinitrate and in 73,3 % with Captopril, with few effects for both medications. Conclusions: Results were similar in this search with the use of Isosorbide Dinitrate and other antihypertensive drugs in the treatment of hypertensive urgencies . In the future, with the appearance of new evidencies Isosorbide Dinitrate could be used as an alternative in the treatment of hypertension at the urgency department when there is no possibility for applying any other medication.

  7. Combined effects of low-dose spironolactone and captopril therapy in a rat model of genetic hypertrophic cardiomyopathy.

    Science.gov (United States)

    de Resende, Micheline Monteiro; Kriegel, Alison Jessica; Greene, Andrew Seth

    2006-12-01

    For several years, the severe side effects associated with the use of high doses of the aldosterone antagonist, spironolactone, limited its clinical use. Studies have recently shown efficacy and minimal side effects of low-dose spironolactone combined with standard therapy in the treatment of heart failure and hypertensive patients. The authors evaluated the effects of low-dose spironolactone alone or in combination with angiotensin-converting enzyme (ACE) inhibitors on the progression of left ventricular dysfunction and remodeling in a congenic rat model of hypertrophic cardiomyopathy. The congenic SS-16/Mcwi rats developed severe cardiac hypertrophy despite being normotensive even on high-salt diet. SS-16/Mcwi and SS/Mcwi rats were fed a low-salt (0.4% NaCl) diet and were treated with vehicle (CON), spironolactone (20 mg/kg/d subcutaneously), captopril (100 mg/kg/d drinking water), or both spironolactone and captopril for 4 weeks. Blood pressure, plasma peptides, cardiac fibrosis, and echocardiography measurements were evaluated. Spironolactone at a low dose had no effect on blood pressure, cardiac hypertrophy, and fibrosis in either strain. However, in combination with captopril, spironolactone decreased the cardiac hypertrophy more than captopril treatment alone. In the SS-16/Mcwi rats, the combined therapy significantly preserved the cardiac index when compared with control. These data indicate that the addition of low-dose spironolactone to captopril treatment was more effective in preventing the progression of heart hypertrophy and ventricular dysfunction in the SS-16/Mcwi than captopril alone. This study suggests that combined spironolactone and captopril therapy may be useful in the treatment of hypertrophic cardiomyopathy.

  8. Weak interactions in clobazam-lactose mixtures examined by differential scanning calorimetry: Comparison with the captopril-lactose system

    Energy Technology Data Exchange (ETDEWEB)

    Toscani, S. [Departement de Chimie - UMR 6226, Faculte des Sciences, Universite de Rennes 1, Batiment 10B, 263 avenue du General Leclerc, F-35042 Rennes Cedex (France); Cornevin, L. [Universite de Rennes 1, Faculte de Pharmacie, 2 Avenue Leon Bernard, F-35043 Rennes Cedex (France); Burgot, G., E-mail: Gwenola.burgot@univ-rennes1.fr [Universite de Rennes 1, Faculte de Pharmacie, Laboratoire de Chimie Analytique, EA 1274 ' Mouvement, sports, sante' , 2 Avenue Leon Bernard, F-35043 Rennes Cedex (France); CHGR Rennes, Pole Medico-Technique Pharmacie, F-35703 Rennes Cedex (France)

    2012-09-10

    Highlights: Black-Right-Pointing-Pointer Thermodynamic and kinetic parameters of weak interactions in binary systems by DSC. Black-Right-Pointing-Pointer Energy-barrier decrease for lactose dehydration induced by clobazam. Black-Right-Pointing-Pointer Recrystallisation of metastable liquid clobazam induced by anhydrous alpha lactose. Black-Right-Pointing-Pointer Decrease of lactose dehydration temperature in binary mixtures with captopril. Black-Right-Pointing-Pointer Increase of lactose dehydration enthalpy in binary mixtures with captopril. - Abstract: The thermal behaviour of binary mixtures of two drugs (clobazam and captopril, respectively) and a pharmaceutical excipient (lactose monohydrate) was measured with differential scanning calorimetry to determine thermodynamic and kinetic parameters (dehydration and melting enthalpies and dehydration and glass-transition activation energies) which might be affected by intermolecular interactions. A kinetic study showed that lactose dehydration is not a single-step conversion and that clobazam contributed to reduce the energy barrier for the bulk dehydration of the excipient. On the other hand, the physical interactions between metastable liquid clobazam and crystalline anhydrous {alpha}-lactose obtained from monohydrate dehydration gave rise to the recrystallisation of clobazam. In the captopril-lactose system, the liquid captopril influenced the lactose dehydration: a sharp increase of the dehydration enthalpy and a concurrent reduction of the dehydration temperature were observed. Finally, it turned out that solid-phase transitions were enhanced by the contact with a liquid phase.

  9. Prediction of response to revascularization in patients with renal artery stenosis by Tc-99m-ethylene dicysteine captopril scintigraphy

    Energy Technology Data Exchange (ETDEWEB)

    Ugur, O.; Ergun, E.L.; Peksoy, I.; Cekirge, S. [Hacettepe Univ., Ankara (Turkey). Medical School; Serdengecti, M.; Karacalioglu, O.

    1999-04-01

    The aim of the present study was to assess the predictive value of captopril scintigraphy with the new renal agent {sup 99m}Tc-ethylene dicysteine ({sup 99m}Tc-EC) for post-interventional improvement in blood pressure. Twelve patients who had persistently high blood pressure with previous demonstration of various degrees of renal artery lesion on angiography were included into the study. Baseline and captopril scintigraphies were performed on the same day at 4 hour intervals after the injection of 74 and 296 MBq of {sup 99m}Tc-EC, respectively. All patients had percutaneous transluminal angioplasty (PTA), and improvement in blood pressure was evaluated 3-6 months after the intervention. {sup 99m}Tc-EC captopril scintigraphy successfully predicted a positive or negative outcome in 11 of 12 patients. In one patient with captopril induced renal function deterioration, scintigraphy failed to predict post-interventional response. Our preliminary findings showed that {sup 99m}Tc-EC captopril scintigraphy can be used to determine patients who will benefit from revascularization. (author)

  10. Estudo termoanalítico de comprimidos revestidos contendo captopril através de termogravimetria (TG e calorimetria exploratória diferencial (DSC Thermal analysis study of captopril coated tablets by thermogravimetry (TG and differential scanning calorimetry (DSC

    Directory of Open Access Journals (Sweden)

    Giovana Carolina Bazzo

    2005-09-01

    Full Text Available No presente trabalho foram desenvolvidos comprimidos de captopril revestidos com hidroxipropilmetilcelulose (HPMC, Opadry®, polivinilpirrolidona (PVP, Eudragit® E e goma laca. Foi realizado estudo termoanalítico do fármaco e das formulações através de termogravimetria (TG e calorimetria exploratória diferencial (DSC. Através da análise das curvas DSC verificou-se que não houve a ocorrência de interação entre o fármaco e os excipientes lactose, celulose microcristalina, croscarmelose sódica, Aerosil® e talco, utilizados na formulação do comprimido. Através desta técnica detectou-se a possibilidade de interação entre captopril e estearato de magnésio. De acordo com os resultados obtidos através de DSC não foram observadas alterações na cristalinidade do fármaco decorrentes dos processos de compressão e revestimento. A termogravimetria foi utilizada para o estudo da cinética de degradação do captopril e dos comprimidos. Os parâmetros cinéticos foram determinados através do método de Ozawa. Os resultados demonstraram que não houve alteração da estabilidade térmica do captopril na forma de comprimido. A formulação revestida com HPMC foi a que apresentou maior estabilidade térmica, quando comparada às demais formulações de revestimento.In the present study, captopril coated tablets with hydroxypropylmethylcellulose (HPMC, Opadry®, polyvinylpirrolidone (PVP, Eudragit® and shellac were produced. Differential scanning calorimetry (DSC and thermogravimetry (TG were used to evaluate the thermal properties of the drug and the formulations. On the basis of DSC results, captopril was found to be compatible with lactose, microcrystalline cellulose, sodium croscarmellose, Aerosil® and talc. Some possibility of interaction between drug-excipient was observed with magnesium stearate. However, additional techniques to confirm the results obtained are needed. There was no influence of mechanical treatment (tableting

  11. Influence of formulation properties on chemical stability of captopril in aqueous preparations.

    Science.gov (United States)

    Kristensen, S; Lao, Y E; Brustugun, J; Braenden, J U

    2008-12-01

    The influence of various formulation properties on the chemical stability of captopril in aqueous media at pH 3 was investigated, in order to reformulate and increase the shelf-life of an oral mixture of the drug. At this pH, chemical stability is improved by an increase in drug concentration (1-5 mg/ml) and a decrease in temperature (5-36 degrees C), the latter demonstrated by a linear Arrhenius-plot. The activation energy is low (Ea = 10.2 kcal/mol), thus the Q10 value is only 1.8 in pure aqueous solutions. The degradation at the lowest concentration investigated in pure aqueous solution apparently follows zero order kinetics. The reaction order is changed at higher concentrations. We are presenting a hypothesis of intramolecular proton transfer from the thiol to the ionized carboxylic group as the initial step in the oxidative degradation pathways of captopril. Long-term stability of 1 mg/ml captopril in aqueous solutions at pH 3, stored at 36 degrees C for one year, shows that the sugar alcohol sorbitol accelerates degradation of the drug while Na-EDTA at a concentration as low as 0.01% is sufficient to stabilize these samples. Purging with N2-gas prior to storage is not essential for drug stability, as long as Na-EDTA is present. Only at a low level of Na-EDTA (0.01%) combined with a high level of sorbitol (35%), purging with N2-gas appears to have a small effect. The destabilizing effect of sugar alcohols is confirmed by accelerated degradation also in the presence of glycerol. The efficient stabilization in the presence of Na-EDTA at a low concentration indicates that the metal-ion-catalyzed oxidation pathway dominates the chemical degradation process at low pH, although several mechanisms seem to be involved depending on excipients present.

  12. BENEFICIAL EFFECTS OF CAPTOPRIL ON PROGNOSIS IN ELDERLY PATIENTSWITH ACUTE MYOCARDIAL INFARCTION

    Institute of Scientific and Technical Information of China (English)

    蔡煦; 沈卫峰; 李明洲; 龚兰生

    1998-01-01

    This study sought to investigate the effects of early and long-term intervention with angiotensin-converting enzyme(ACE) inhibitor captopril on the elderly patients with acute myocardial infarction(AMI), and observe its in-hospitsl and post-hospital outcomes during serial follow-up of 54 months. Methods. 631 elderly patients(60~75 years old) with AMI and without cardioganie shock were hospitalized within 72 hours of symptoms and were randondy allocated to captopril (n= 361; treatment group) and conventional treatment (n=270,contro1 group), The survival and cardiac events(congestive heart failure, reinfarction, severe arthythmias and cardiac death)of each group were determined during hospitalization and follow-up. Results. During hospitalization, the survival was higher in treatment group than in control group(P<0. 0001). On the other hand, in treatment group lower mortality was true for patients with anterior myocardial infarction(P= 0. 001 ) or with anterior+inferior myocardial infarction(P= 0. 026), but not statistically significant in ones with inferior myocardial infarction(P= 0. 061). During follow-up, the occurrence of cardiae death, heart failure, reinfaretion and severe arrhythmiss were lower in treatment group(P=0.0001, P=0.05, P=0. 0004 and P=0.027). So higher survival(P= 0.005) and lower total cardiac events(P=0. 0008) could be seen in treatment group over this period. Conclusions. Early and long-term treatment with captopril in the elderly patients with AMI has beneficial outcomes in both in-hospital and follow-up periods,

  13. Antithrombotic effect of captopril and losartan is mediated by angiotensin-(1-7).

    Science.gov (United States)

    Kucharewicz, Iwona; Pawlak, Robert; Matys, Tomasz; Pawlak, Dariusz; Buczko, Wlodzimierz

    2002-11-01

    It is well established that renin-angiotensin system blockers exert NO/prostacyclin-dependent antithrombotic effects. Because some beneficial effects of these drugs are mediated by angiotensin (Ang)-(1-7), in the present study we examined if their antithrombotic action could be mediated by Ang-(1-7). Intravenous infusion of Ang-(1-7) (1, 10, or 100 pmol/kg per minute for 2 hours) into rats developing venous thrombosis caused 50% to 70% reduction of the thrombus weight. This effect was dose-dependently reversed by cotreatment with A-779 (selective Ang-[1-7] receptor antagonist) or EXP 3174 (angiotensin type 1 receptor antagonist) but not by PD 123,319 (angiotensin type 2 receptor antagonist). Similarly, the antithrombotic effects of captopril (ACE inhibitor) and losartan (angiotensin type 1 receptor blocker) were attenuated by A-779 in a dose-dependent manner. The effect of Ang-(1-7) was completely abolished by concomitant administration of NO synthase inhibitor (N(G)-nitro-L-arginine methyl ester) and prostacyclin synthesis inhibitor (indomethacin), as has been shown previously for captopril and losartan. Thus, the antithrombotic effect of renin-angiotensin system blockers involves Ang-(1-7)-evoked release of NO and prostacyclin.

  14. Alginate beads of Captopril using galactomannan containing Senna tora gum, guar gum and locust bean gum.

    Science.gov (United States)

    Pawar, Harshal A; Lalitha, K G; Ruckmani, K

    2015-05-01

    Gastro-retentive Captopril loaded alginate beads were prepared by an ionotropic gelation method using sodium alginate in combination with natural gums containing galactomannans (Senna tora seed gum, guar gum and locust bean gum) in the presence of calcium chloride. The process variables such as concentration of sodium alginate/natural polymer, concentration of calcium chloride, curing time, stirring speed and drying condition were optimized. Prepared beads were evaluated for various parameters such as flow property, drug content and entrapment efficiency, size and shape, and swelling index. Surface morphology of the beads was studied using scanning electron microscopy. In vitro mucoadhesion and in vitro drug release studies were carried out on the prepared beads. From the entrapment efficiency and dissolution study, it was concluded that galactomannans in combination with sodium alginate show sustained release property. The bead formulation F4 prepared using combination of sodium alginate and guar gums in the ratio 2:1 showed satisfactory sustained release for 12h. The release of Captopril from the prepared beads was found to be controlled by the swelling of the polymer followed by drug diffusion through the swelled polymer and slow erosion of the beads.

  15. Captopril Modulates Hypoxia-Inducible Factors and Erythropoietin Responses in a Murine Model of Total Body Irradiation

    Science.gov (United States)

    2011-01-01

    high-dose irradiation may aid in DNA repair, cell survival, and hematopoietic cell recovery [54]. We previously observed that captopril treatment...expression in tumor cells and other tissues. Oncologist. 2004;9(suppl 5):18–30. 28. Lam SY, Tipoe GL, Fung ML. Upregulation of erythropoietin and its

  16. Synergistic Antihypertensive Effect of Carthamus tinctorius L. Extract and Captopril in l-NAME-Induced Hypertensive Rats via Restoration of eNOS and AT1R Expression

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    Putcharawipa Maneesai

    2016-02-01

    Full Text Available This study examined the effect of Carthamus tinctorius (CT extract plus captopril treatment on blood pressure, vascular function, nitric oxide (NO bioavailability, oxidative stress and renin-angiotensin system (RAS in Nω-Nitro-l-arginine methyl ester (l-NAME-induced hypertension. Rats were treated with l-NAME (40 mg/kg/day for five weeks and given CT extract (75 or 150 or 300 or 500 mg/kg/day: captopril (5 mg/kg/day or CT extract (300 mg/kg/day plus captopril (5 mg/kg/day for two consecutive weeks. CT extract reduced blood pressure dose-dependently, and the most effective dose was 300 mg/kg/day. l-NAME-induced hypertensive rats showed abnormalities including high blood pressure, high vascular resistance, impairment of acetylcholine-induced vasorelaxation in isolated aortic rings and mesenteric vascular beds, increased vascular superoxide production and plasma malondialdehyde levels, downregulation of eNOS, low level of plasma nitric oxide metabolites, upregulation of angiotensin II type 1 receptor and increased plasma angiotensin II. These abnormalities were alleviated by treatment with either CT extract or captopril. Combination treatment of CT extract and captopril normalized all the abnormalities found in hypertensive rats except endothelial dysfunction. These data indicate that there are synergistic antihypertensive effects of CT extract and captopril. These effects are likely mediated by their anti-oxidative properties and their inhibition of RAS.

  17. Chelation Study of Captopril with Cd2+ and Pb2+

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    Mohammad Joshaghani

    2008-01-01

    Full Text Available The protonation constants of Captopril, (1-(3-mercapto-2-(S-methyl-1-oxopropyl-S(L proline, (CPL and stabilities of its two divalent metal ions Cd(II and Pb(II were determined potentiometrically in two different metal to ligand ratio 1:1 and 1:2 systems and in water and methanol-water binary mixtures using the computer Best program. Two protonation constants were obtained which were assigned to the carboxylic and thiol groups. All protonation and stability constants increased with decreasing the dielectric constant on going from the pure water to the binary mixtures. An excellent similarity in stabilities of studied metal ions strongly suggests that both metal ions are coordinated by CPL in a same manner through the thiol group.

  18. Ionic gelation controlled drug delivery systems for gastric-mucoadhesive microcapsules of captopril

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    Altaf M

    2008-01-01

    Full Text Available A new oral drug delivery system was developed utilizing both the concepts of controlled release and mucoadhesiveness, in order to obtain a unique drug delivery system which could remain in stomach and control the drug release for longer period of time. Captopril microcapsules were prepared with a coat consisting of alginate and a mucoadhesive polymer such as hydroxy propyl methyl cellulose, carbopol 934p, chitosan and cellulose acetate phthalate using emulsification ionic gelation process. The resulting microcapsules were discrete, large, spherical and free flowing. Microencapsulation efficiency was 41.7-89.7% and high percentage efficiency was observed with (9:1 alginate-chitosan microcapsules. All alginate-carbopol 934p microcapsules exhibited good mucoadhesive property in the in vitro wash off test. Drug release pattern for all formulation in 0.1 N HCl (pH 1.2 was diffusion controlled, gradually over 8 h and followed zero order kinetics.

  19. [The interaction of the converting-enzyme inhibitor captopril with cardiac glycosides in the rat kidney].

    Science.gov (United States)

    Kuz'min, O B; Tarasov, S V

    1995-01-01

    Strophanthin (0.1 mg.kg, i.v.) and digoxin (0.1 mg/kg, i.v.) moderately increase blood supply of the renal cortical and medullary layers in unconscious rats and enhance renal excretion of sodium and water. Preadministration of the converting enzyme inhibitor captopril (10 mg/kg/day, per os, for 6 days) promoted vascular dilatation in the inner and outer areas of the medulla, which occurred under the action of these agents and substantially increased their natriuretic and diuretic effects. It is concluded that the renin-angiotension system is directly involved into the mechanism of action of cardiac glycosides in the kidneys, acting as a modulator that prevents their vasodilating and tubular effects.

  20. Análise da prescrição de captopril em pacientes hospitalizados Analysis of the prescription of captopril to hospitalized patients

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    Márcio Galvão Oliveira

    2008-12-01

    Full Text Available Uma das complicações mais comuns da hipertensão arterial sistêmica é a crise hipertensiva¹ que se caracteriza por uma elevação sintomática da pressão arterial (PA, com ou sem envolvimento de órgãos-alvo, que pode conduzir a um risco imediato ou potencial de vida2-4. A crise hipertensiva pode se manifestar como emergência ou urgência hipertensiva. Na emergência, há a rápida deterioração de órgãos-alvo e risco imediato de vida, situação que não ocorre na urgência hipertensiva2-4. Além disso, as situações em que o paciente apresenta PA elevada diante de algum evento emocional, doloroso ou desconfortável, sem evidências de lesões de órgãos-alvo ou risco imediato de vida, caracterizam a pseudocrise hipertensiva, condição em que não é necessário o uso da terapia anti-hipertensiva de emergência1-3,5. Apesar disso, tem se tornado comum a prática de prescrever anti-hipertensivos precedendo situações em que se identifica algum risco de elevação abrupta da PA, independentemente de sintomas. O presente estudo tem como objetivo avaliar a freqüência de prescrição do captopril precedendo elevação da PA em pacientes internados em um hospital universitário. Pretende também mapear os locais (enfermarias clínicas ou cirúrgicas onde essa conduta foi mais freqüente.One of the most common complications of Systemic Arterial Hypertension is the hypertensive crisis¹ characterized by a symptomatic elevation of blood pressure (BP with or without involvement of target organs, which may lead to immediate or potential risk to life2-4. The hypertensive crisis may manifest itself as hypertensive emergency or urgency. In the emergency there is fast deterioration of target organs and immediate risk to life, a situation that does not occur in hypertensive urgency2-4. On the other hand, situations in which the patient presents elevated BP due to an emotionally charged, painful or uncomfortable event, with no evidence of

  1. Losartan renography for the detection of renal artery stenosis: comparison with captopril renography and evaluation of dose and timing

    Energy Technology Data Exchange (ETDEWEB)

    Guenay, Emel Ceylan; Erguen, Eser Lay; Salanci, Bilge Volkan; Ugur, Oemer; Caner, Biray [Hacettepe University Faculty of Medicine, Department of Nuclear Medicine, Ankara (Turkey); Oeztuerk, M. Halil; Hekimoglu, Baki [Social Security Hospital Clinic of Radiology, Ankara (Turkey); Altun, Buelent [Hacettepe University Faculty of Medicine, Department of Nephrology, Ankara (Turkey); Cil, Barbaros [Hacettepe University Faculty of Medicine, Department of Radiology, Ankara (Turkey)

    2005-09-01

    Radionuclide renography with angiotensin converting enzyme (ACE) inhibition plays an important role in the diagnosis of haemodynamically significant renal artery stenosis. Angiotensin receptor antagonists inhibit the renin angiotensin system at different levels from ACE inhibitors by selectively blocking the binding of angiotensin II to AT1 receptors. The AT1 angiotensin receptor antagonist losartan has recently been used clinically in the treatment of hypertension. However, the available data on the use of losartan with renography for the detection of renovascular hypertension are limited and contradictory. The purpose of this prospective study was to compare the effectiveness of losartan renography and captopril scintigraphy in revealing renal artery stenosis. A total of 61 renal units in 32 patients with hypertension were studied in two groups based on the losartan dosage (50 mg in group A and 100 mg in group B). Group A consisted of 17 patients, in whom 19 renal units had angiographically proven renal artery stenosis ({>=}50%). In group B, there were 15 patients, in whom 20 renal arteries were stenotic. All of the patients underwent three renographies (baseline, captopril renography and early losartan renography). Early losartan renography was performed at 1 h after oral losartan administration in both groups. In group B, seven patients underwent additional losartan renography (late losartan) performed 3 h after oral losartan administration; these patients composed group B1. The sensitivities of captopril and losartan studies were 63.2% and 42% in group A, 65% and 65% in group B and 55.6% and 66.6% in group B1, respectively. From our preliminary results, we conclude that losartan is not superior to captopril renography for the detection of haemodynamically significant renal artery stenosis. However, a high dose (100 mg) of losartan provided higher sensitivity than the lower dose (50 mg). Late losartan scintigraphy provided similar diagnostic efficacy to early

  2. The effects of captopril vs atenolol on memory, information processing and mood: a double-blind crossover study.

    OpenAIRE

    Deary, I J; Capewell, S; Hajducka, C; Muir, A.L

    1991-01-01

    1. Measures of memory, information processing ability, mood states and trait anxiety were estimated in a double-blind, double-dummy, randomised cross-over trial which compared the effects of atenolol (50 or 100 mg once daily) and captopril (25 or 50 mg twice daily), each taken for 6 weeks. Eighteen patients with mild to moderately severe hypertension were included. 2. There were no significant differences in systolic or diastolic blood pressure reduction between the two drugs. Pulse rate was ...

  3. Sensitive Voltammetric Determination of Captopril Using a Carbon Paste Electrode Modified with Nano-TiO2/Ferrocene Carboxylic Acid

    Institute of Scientific and Technical Information of China (English)

    Jahan Bakhsh RAOOF; Reza OJANI; Mehdi BAGHAYERI

    2011-01-01

    A carbon paste electrode (CPE) modified with ferrocene carboxylic acid (FcCA) and TiO2 nanoparticles was constructed by incorporating TiO2 nanoparticles and ferrocene carboxylic acid into the carbon paste matrix.The electrochemical behavior of captopril (CAP) at the surface of the modified electrode was investigated using electroanalytical methods.The modified electrode showed excellent electrocatalytic activity for the oxidation of CAP in aqueous solutions at physiological pH values.Cyclic voltammetric curves showed that the oxidation of CAP at the surface of the modified electrode reduced its overpotential by more than 290 mV.The modified electrode was used for detecting captopril using cyclic voltammetry and square wave voltammetry techniques.A calibration curve in the range of 0.03 to 2400μmol/L was obtained that had a detection limit of 0.0096 μmol/L (3σ) under the optimized conditions.The modified electrode was successfully used for the determination of captopril in pharmaceutical and biological samples.

  4. Effect of captopril and telmisartan on methotrexate-induced hepatotoxicity in rats: impact of oxidative stress, inflammation and apoptosis.

    Science.gov (United States)

    Kelleni, Mina T; Ibrahim, Salwa A; Abdelrahman, Aly M

    2016-06-01

    Methotrexate (MTX) is a commonly used antineoplastic and anti-rheumatoid drug whose efficacy is limited by its hepatotoxicity. The aim of this study was to investigate the possible protective role of captopril (100 mg/kg/day, p.o. for seven days), an angiotensin converting enzyme inhibitor, and telmisartan (10 mg/kg/day p.o. for seven days), an angiotensin II receptor blocker with peroxisome proliferative receptor gamma (PPARγ) agonism, in a model of MTX (single dose 20 mg/kg i.p. at the fifth day) induced hepatotoxicity in rats. Results of the present study revealed MTX-induced hepatotoxicity as demonstrated by increased level of liver enzymes and confirmed by histopathology. Pretreatment with captopril or telmisartan produced a significant hepatic protection manifested as a significant (p < 0.05) decrease in serum levels of alanine transferase (ALT) and aspartate transferase (AST) and alkaline phosphatase (ALP) enzymes; hepatic malondialdehyde (MDA) and total nitrites and nitrates (NOx) levels; as well as a significant increase in hepatic superoxide dismutase (SOD) activity. In addition, there was a remarkable improvement in the histopathological features and a significant reduction in the expression of COX-2, iNOS and caspase-3 enzymes as compared with the MTX group. We recommend considering captopril/Telmisartan, if tolerated and not contraindicated, as preferable antihypertensive agents in patients receiving MTX in their chemotherapy protocols.

  5. Utilization of oxidation reactions for the spectrophotometric determination of captopril using brominating agents

    Science.gov (United States)

    El-Didamony, Akram M.; Erfan, Eman A. H.

    2010-03-01

    Three simple, accurate and sensitive methods (A-C) for the spectrophotometric assay of captopril (CPL) in bulk drug, in dosage forms and in the presence of its oxidative degradates have been described. The methods are based on the bromination of captopril with a solution of excess brominating mixture in hydrochloric acid medium. After bromination, the excess brominating mixture is followed by the estimation of surplus bromine by three different reaction schemes. In the first method (A), the determination of the residual bromine is based on its ability to bleach the indigo carmine dye and measuring the absorbance at 610 nm. Method B, involves treating the unreacted bromine with a measured excess of iron(II) and the remaining iron(II) is complexed with 1,10-phenanthroline and the increase in absorbance is measured at 510 nm. In method (C), the surplus bromine is treated with excess of iron(II) and the resulting iron(III) is complexed with thiocyanate and the absorbance is measured at 478 nm. In all the methods, the amount of bromine reacted corresponds to the drug content. The different experimental parameters affecting the development and stability of the color are carefully studied and optimized. Beer's law is valid within a concentration range of 0.4-6.0, 0.4-2.8 and 1.2-4.8 μg mL -1 for methods A, B and C, respectively. The calculated apparent molar absorptivity was found to be 5.16 × 10 4, 9.95 × 10 4 and 1.74 × 10 5 L mol -1 cm -1, for methods A, B and C, respectively. Sandell's sensitivity, correlation coefficients, detection and quantification limits are also reported. No interference was observed from common additives found in pharmaceutical preparations. The proposed methods are successfully applied to the determination of CPL in the tablet formulations with mean recoveries of 99.94-100.11% and the results were statistically compared with those of a reference method by applying Student's t- and F-test.

  6. Diagnostic potential of renal scintigraphy following ACE-inhibition ('captopril scintigraphy') for the detection of renovascular hypertension. Wertigkeit der Nierenszintigraphie unter ACE-Blockade ('Captoprilszintigraphie') in der Diagnostik der renovaskulaeren Hypertonie

    Energy Technology Data Exchange (ETDEWEB)

    Baum, R.P.; Maul, F.D.; Hoer, G. (Frankfurt Univ. (Germany). Abt. fuer Nuklearmedizin)

    1991-12-01

    The purpose of this paper is to: (a) briefly review the pathophysiological basis of renovascular hypertension and the renin-angiotensin-system; (b) to outline the potential of captopril scintigraphy especially using Tc-99m MAG{sub 3}; and (c) to propose a practical protocol for captopril scintigraphy and its role in screening for renovascular hypertension. (orig./MG).

  7. The Brain-Heart Connection: Frontal Cortex and Left Ventricle Angiotensinase Activities in Control and Captopril-Treated Hypertensive Rats—A Bilateral Study

    Directory of Open Access Journals (Sweden)

    Ana B. Segarra

    2013-01-01

    Full Text Available The model of neurovisceral integration suggests that the frontal cortex (FC and the cardiovascular function are reciprocally and asymmetrically connected. We analyzed several angiotensinase activities in the heart left ventricle (VT of control and captopril-treated SHR, and we search for a relationship between these activities and those determined in the left and right FC. Captopril was administered in drinking water for 4 weeks. Samples from the left VT and from the left and right FC were obtained. Soluble and membrane-bound enzymatic activities were measured fluorometrically using arylamides as substrates. The weight of heart significantly decreased after treatment with captopril, mainly, due to the reduction of the left VT weight. In the VT, no differences for soluble activities were observed between control and treated SHR. In contrast, a generalized significant reduction was observed for membrane-bound activities. The most significant correlations between FC and VT were observed in the right FC of the captopril-treated group. The other correlations, right FC versus VT and left FC versus VT in controls and left FC versus VT in the captopril group, were few and low. These results confirm that the connection between FC and cardiovascular system is asymmetrically organized.

  8. CLINICAL OUTCOMES OF FIVE-YEAR FOLLOW-UP OF EARLY AND LONG-TERM TREATMENT WITH CAPTOPRIL ON THE PATIENTS WITH ACUTE MYOCARDIAL INFARCTION

    Institute of Scientific and Technical Information of China (English)

    蔡煦; 苏静英; 沈卫峰; 龚兰生

    2002-01-01

    Objective To investigate clinical outcomes of early and long-term treatment with captopril on patients with acute myocardial infarction (AMI) during a five-year follow-up. Methods In a randomi-zed trial, 822 patients (623 males, 199 females) with a first AMI with less 72h of symptoms were treated with captopril (treatment group, n=478, dosage from a first 6.25mg to 25mg t.i.d) and conventional treatment (control group, n=344). Multivariable Cox regression were used to analyze relative risk of independent variables. Cumulative survival of both groups were calculated with Kaplan-Meier analysis and analyzed by using log-rank comparison. Results During the five-year follow-up, the age, Killip class (≥Ⅱ), anterior infarction, diabetes mellitus, and peak CPK increased relative risk of death after AML, but the effects of captopril, beta-blocker, antiplatelet drug, and thrombolytic therapy on the relative risk of death were contrary. The cumulative survival in different time during follow-up was higher in patients with captopril than controls (P<0.001). Conclusion Early and long-term treatment with captopril was related to a beneficial outcome during the five-year follow-up after AMI.

  9. A simple spectrophotometric method for the determination of captopril in pharmaceutical preparations using ammonium molybdate

    Energy Technology Data Exchange (ETDEWEB)

    Ribeiro, P.R.S., E-mail: pauloufma@ufma.b [Universidade Federal do Maranhao (CCSST/UFMA), Imperatriz, MA (Brazil). Centro de Ciencias Sociais, Saude e Tecnologia; Pezza, L.; Pezza, H.R. [UNESP, Araraquara, SP (Brazil). Inst. de Quimica

    2010-09-15

    A simple, rapid and sensitive spectrophotometric method for the determination of captopril (CPT) in pharmaceutical formulations is proposed. This method is based on the reduction reaction of ammonium molybdate, in the presence of sulphuric acid, for the group thiol of CPT, producing a green compound ({lambda}{sub max} 407 nm). Beer's law is obeyed in a concentration range of 4.60 x 10{sup -4} - 1.84 x 10{sup -3} mol l{sup -1} of CPT with an excellent correlation coefficient (r = 0.9995). The limit of detection and limit of quantification were 7.31 x 10{sup -6} and 2.43 x 10{sup -5} mol l{sup -1} of CPT, respectively. The proposed method was successfully applied to the determination of CPT in commercial brands of pharmaceuticals. No interferences were observed from the common excipients in the formulations. The results obtained by the proposed method were favorably compared with those given by the official reported method at 95 % confidence level. (author)

  10. Binding Interaction of Captopril with Metal Ions: A Fluorescence Quenching Study

    Institute of Scientific and Technical Information of China (English)

    SIDDIQI K.S.; BANO Shaista; MOHD Ayaz; KHAN Aslam Aftab Parwaz

    2009-01-01

    The binding interaction of captopril(CPL)with biologically active metal ions Mg2+,Ca2+,Mn2+,Co2+,Ni2+,Cu2+ and Zn2+ was investigated in an aqueous acidic medium by fluorescence spectroscopy.The experimental results showed that the metal ions quenched the intrinsic fluorescence of CPL by forming CPL-metal complexes.It was found that static quenching was the main reason for the fluorescence quenching.The quenching constant in the case of Cu2+ was highest among all quenchers,perhaps due to its high nuclear charge and small size.Quenching of CPL by metal ions follows the order Cu2+> Ni2+> Co2+> Ca2+>Zn2+ > Mn2+ > Mg2+.The quenching constant Ksv,bimolecular quenching constant Kq,binding constant K and the binding sites "n" were determined together with their thermodynamic parameters at 27 and 37℃.The positive entropy change indicated the gain in configurational entropy as a result of chelation.The process of interaction was spontaneous and mainly △S-driven.

  11. Captopril-induced reduction of regurgitation fraction in aortic insufficiency: Acute and long-term effects

    Energy Technology Data Exchange (ETDEWEB)

    Kropp, J.; Heck, I.; Reske, S.N.; Biersack, H.J.; Mattern, H.; Winkler, C.; Polikl, M.

    1985-05-01

    In aortic insufficiency (AI) the inhibition of the stimulated Renin-Angiotensin-System (RAS) by Captopril (C) reduced afterload and leads consequently to a diminished regurgitation fraction (RF). In 17 patients (pts) with pure severe AI RF, left ventricular ejection fraction (LVEFE) and heart rate were determined before (1) and 1 hr after (2) administration of 25 mg of C.Long term dosis was 3 x 25 mg of C and follow up time was 3-11 months (medium:6). The values were determined by gated radionuclide ventriculography using red blood cells labeled in vivo with 15 mCi Tc-99mROI's were selected over both ventricles in enddiastolic and endsystolic frames. Ventricular boundaries were defined by a fourier phase image overlay. RF was calculated by the background corrected count rate ratio of left and right ventricular ROI. Systolic and diastolic blood pressure (BPs,BPd), plasma levels of angiotensin I,II(A1,A2) and the activity of angiotensin converting enzyme (ACE) were determined before and 1 hr after C administration. After C there is a decrease in RF which persists in the long term follow period in up to to now 8 pts. The authors conclude: inhibition of ACE reduces significantly aortic regurgitation in patients with AI and has thus a beneficial effect on left ventricular performance. This effect persists in long term treatment and therefore seems beneficial to delay the point of operation.

  12. Determination of Captopril Based on the Photoluminescence Quenching of the pH Sensitive Mercaptopropanoic Acid Capped CdTe Quantum Dots

    Science.gov (United States)

    Khan, S.; Lima, A. A.; Aucelio, R. Q.

    2017-01-01

    The determination of captopril was performed by measuring the photoluminescence quenching of pH sensitive mercaptopropanoic acid capped CdTe quantum dots. Under optimum conditions, the calibration model (log F0/F as a function of the concentration of captopril) was linear up to 8 × 10-6 mol/L (1.7 μg/mL) and the limit of detection (xb - 3sb) was 2.7 × 10-7 mol/L (18 ng/mL). A possible mechanism for quenching is proposed. The method was applied in the determination of captopril in two commercial pharmaceutical formulations, indicating that it can be used for simple and fast quantitative control of commercial medicines or pharmaceutical preparations.

  13. Comparative study between the use of isosorbide dinitrate and captopril in hypertensive emergency treatment. Estudio comparativo entre el uso del dinitrato de isosorbide y el captopril en el traramiento de la urgencia hipertensiva.

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    Brandy Viera Valdés

    2005-05-01

    Full Text Available Fundament: Oral antihypertensive drugs are lacking in our environment at present in tog hypertensive urgencies, that is why new therapeutic alternatives are necessary to treat this medical problem. Objective: To assess the effect of Isosorbide Dinitrate in the treatment of hypertensive urgencies the system of urgencies. Method: a cuasi experimental study was designed with 60 patients with this diagnosis. The patients were divided into two groups. The patients of one group received treatment for the hypertensive crisis with Isosorbide Dinitrate 10 mg sub lingually and the others had their treatment with Captopril 25 mg p.o. Results: The response of the treatment with Isosorbide Dinitrate with similar to the treatment with Captopril. High Blood Pressure was controlled in 66,6 % with Isosorbide Dinitrate and in 73,3 % with Captopril, with few effects for both medications. Conclusions: Results were similar in this search with the use of Isosorbide Dinitrate and other antihypertensive drugs in the treatment of hypertensive urgencies . In the future, with the appearance of new evidencies Isosorbide Dinitrate could be used as an alternative in the treatment of hypertension at the urgency department when there is no possibility for applying any other medication.

    Fundamentación: En nuestro medio existen grandes dificultades con la disponibilidad de antihipertensivos orales para el tratamiento de la urgencia hipertensiva, por lo que es necesario la búsqueda de nuevas alternativas terapéuticas para este fin. Objetivo: Evaluar el efecto del dinitrato de isosorbide en el tratamiento de la urgencia hipertensiva en los sistema de urgencia. Métodos: Se diseñó un estudio cuasi experimental, donde fueron incluidos 60 pacientes con este diagnóstico, los cuales se

  14. Desenvolvimento e validação do ensaio de dissolução para captopril em cápsulas magistrais por CLAE Development and validation of dissolution test for captopril in capsules by HPLC

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    Roberta de Cássia Pimentel Azevedo

    2008-06-01

    Full Text Available O captopril é um fármaco anti-hipertensivo e vasodilatador utilizado na insuficiência cardíaca congestiva e encontra-se disponível, no mercado brasileiro, sob as formas de comprimidos e cápsulas, sendo estas manipuladas em farmácias. O objetivo deste estudo foi validar o procedimento de dissolução e o método de análise. A avaliação do perfil de dissolução do captopril na forma farmacêutica cápsulas magistrais quando submetidas a diferentes condições de pH, aparatos, velocidades de agitação do meio de dissolução e métodos para quantificação foram alvo deste estudo. As concentrações do fármaco no meio foram determinadas por cromatografia líquida e espectrofotometria. Os resultados mostraram que o método cromatográfico foi o mais adequado para avaliação de captopril na forma farmacêutica cápsulas, enquanto o método espectrofotométrico (recomendado pelas Farmacopéias Brasileira e Americana apresentou baixa especificidade. O procedimento de dissolução nas condições estabelecidas foi preciso, exato e seletivo. O método foi linear. Com base nos resultados obtidos as condições do teste de dissolução para cápsulas foram o uso de HCl 0,01 M (900 mL, 37 ºC ± 0,5 ºC, aparato cesta, 50 rpm, tempo de coleta (20 minutos e quantificação pelo método cromatográfico. Todas as cápsulas apresentaram resultados satisfatórios nos testes de qualidade a que foram submetidas.Captopril is an anti-hypertensive and vasodilator agent utilized in the congestive cardiac insufficiency and it can be commercially found in Brazil in the form of tablets and compounded capsules. The aim of this study was to evaluate the dissolution profile of captopril in capsules dosage obtained from compounded pharmacies, when submitted to different conditions of pH, apparatus, stirring speed of dissolution medium and analytical method, as well the validation of the dissolution procedure and of the method of analysis. The drug

  15. Autoradiographic visualization of angiotensin-converting enzyme in rat brain with (/sup 3/H)captopril: localization to a striatonigral pathway

    Energy Technology Data Exchange (ETDEWEB)

    Strittmatter, S.M.; Lo, M.M.S.; Javitch, J.A.; Snyder, S.H.

    1984-03-01

    The authors have visualized angiotensin-converting enzyme (ACE; dipeptidyl carboxypeptidase, peptidylpeptide hydrolase, EC 3.4.15.1) in rat brain by in vitro (/sup 3/H)captopril autoradiography. (/sup 3/H)Captopril binding to brain slices displays a high affinity (K/sub d/ = 1.8 x 10/sup -9/ M) and a pharmacological profile similar to that of ACE activity. Very high densities of (/sup 3/H)captopril binding were found in the choroid plexus and the subfornical organ. High densities were present in the caudate putamen and substantia nigra, zona reticulata. Moderate levels were found in the entopeduncular nucleus, globus pallidus, and median eminence of the hypothalamus. Lower levels were detectable in the supraoptic and paraventricular nuclei of the hypothalamus, the media habenula, the median preoptic area, and the locus coeruleus. Injection of ibotenic acid or colchicine into the caudate putamen decreased (/sup 3/H)captopril-associated autoradiographic grains by 85% in the ipsilateral caudate putamen and by > 50% in the ipsilateral substantia nigra. Thus, ACE in the substantia nigra is located on presynaptic terminals of axons originating from the caudate putamen, and ACE in the caudate putamen is situated in neuronal perikarya or at the terminals of striatal interneurons. The lack of effect of similar injections into the substantia nigra confirmed that the caudate putamen injections did not cause trans-synaptic changes. The presence of (/sup 3/H)captopril binding is consistent with an ACE-mediated production of angiotensin II in some brain regions. Although (/sup 3/H)captopril autoradiography reveals ACE in a striatonigral pathway, there is no evidence for angiotensin II involvement in such a neuronal pathway. 26 references, 4 figures, 2 tables.

  16. The use of the SeDeM diagram expert system for the formulation of Captopril SR matrix tablets by direct compression.

    Science.gov (United States)

    Saurí, J; Millán, D; Suñé-Negre, J M; Pérez-Lozano, P; Sarrate, R; Fàbregas, A; Carrillo, C; Miñarro, M; Ticó, J R; García-Montoya, E

    2014-01-30

    The SeDeM diagram expert system has been used to study excipients, Captopril and designed formulations for their galenic characterization and to ascertain the critical points of the formula affecting product quality to obtain suitable formulations of Captopril direct compression SR matrix tablets. The application of the SeDeM diagram expert system enables selecting excipients with in order to optimize the formula in the preformulation and formulation studies. The methodology is based on the implementation of ICH Q8, establishing the design space of the formula with the use of experiment design, using the parameters of the SeDeM diagram expert system as system responses.

  17. Effects of Angiotensin Ⅱ and ACE Inhibitor, Captopril on L-type Calcium Current and Sodium Current of Single Guinea Myocytes

    Institute of Scientific and Technical Information of China (English)

    徐延敏; 黄体钢; 陈元禄

    2002-01-01

    Objectives To investigateeffect of AngⅡ, captopril on single guinea myocytes onL - type calcium current and sodium current. MethodsMembrane patch clamp whole cell recording tech-nique was used to investigate effect of angⅡ, captoprilon L- Ca maximum current density and sodium maxi-mum current density. Resutls AngⅡ increased themaximum current density compared with control afterpeffused 5 min, 357.7±219.7 Vs 279.5±240.5PA/PF, increase rate is 27.9 %, the shape of current- voltage relationship curve was unchanged, peaked at+ 10 my, indicated that angⅡ increased L- Ca cur-rent density in voltage -dependent. After perfusedwith captopril, captopril ± angⅡ 3, 5 rmin, L-Cacurrent was recorded, results suggest L - Ca maximumcurrent density decreased significantly compared withcontrol, in captopril group, 128.4 ± 92.6Vs286.2 ±89.7, 66.7 ±68.3Vs 286.2 ± 89.7, respectively, rateof inhibition is 55.1%, 76.6 %, respectively. L - Cacurrent further decreased in captopril perfused 5 mincompared with 3 rmin, 66.7 ± 68.3 Vs 128.4 ± 92.6,in captopril + angⅡ group, L- Ca current decreasedgreatly in 3, 5 min than control, 143.4 ± 117.6Vs267.7±141.4, 96.4±82.5 Vs 267.7+141.4, re-spectively, rate of inhibition is 46.4 %, 63.9 % re-spectively. We also investigated effect of captopril onNa current, which decreased significantly in 1 rmin and3 rmin compared with control, 939.1 ±319. 1 Vs1398.0 ± 144.6 PA/PF, 469.95±314.9 Vs 1398.0±144.6 PA/PF, respectively, rate of inhibition is32.8 %, 66. 3 %, respectively. Na current density de-creased significantly in 3 min compared with 1 min,469.9 ± 314.9 Vs 939. 1 ± 319. 1PA/PF, rate of in-hibition is 49.9 % . Conclusions Angiotensin Ⅱexerts increased maximum current density of L - Ca involtage dependent, captopril decreased maximum cur-rent density of L - Ca in voltage dependent, decreasedsodium maximum current density, which is the promi-nently antiarrhythmia mechanisms through inhibition ofangiotensin Ⅱ evoked

  18. Efectos terapéuticos de la microdosis de captopril en la hipertensión arterial esencial

    OpenAIRE

    Santana Téllez, Tomás Noel

    2012-01-01

    Fundamento: Prescribir una terapéutica adecuada para un diagnóstico específico siempre es complejo, más cuando los índices de control clínico y la seguridad de los medicamentos que se utilizan en la actualidad no satisfacen tales objetivos. Objetivo: Demostrar los efectos de la microdosis de captopril administrada por vía bucal en el tratamiento de la hipertensión arterial esencial. Método: Se realizaron dos ensayos clínicos aleatorizados, unicéntricos, de grupos paralelos y contr...

  19. Diagnostic Role of Captopril Challenge Test in Korean Subjects with High Aldosterone-to-Renin Ratios

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    Jung Hee Kim

    2016-06-01

    Full Text Available BackgroundDiagnosis of primary aldosteronism (PA begins with aldosterone-to-renin ratio (ARR measurement followed by confirmative tests. However, the ARR has high false positive rates which led to unnecessary confirmatory tests. Captopril challenge test (CCT has been used as one of confirmatory tests, but the accuracy of it in the diagnosis of PA is still controversial. We aimed to examine the clinical efficacy of CCT as a post-screening test in PA.MethodsIn a prospective study, we enrolled subjects with suspected PA who had hypertension and ARR >20 (ng/dL/(ng/mL/hr. Sixty-four patients who underwent both the saline infusion test and the CCT were included.ResultsThe diagnostic performance of plasma aldosterone concentration (PAC post-CCT was greater than that of ARR post-CCT and ARR pre-CCT in PA (area under the curve=0.956, 0.797, and 0.748, respectively; P=0.001. A cut-off value of 13 ng/dL showed the highest diagnostic odds ratio considering PAC post-CCT at 60 and 90 minutes. A PAC post-CCT of 19 ng/dL had a specificity of 100%, which can be used as a cut-off value for the confirmative test. Determining the diagnostic performance of PAC post-CCT at 90 minutes was sufficient for PA diagnosis. Subjects with PAC post-CCT at 90 minutes <13 ng/dL are less likely to have PA, and those with PAC post-CCT at 90 minutes ≥13 but <19 ng/dL should undergo secondary confirmatory tests.ConclusionThe CCT test may be a reliable post-screening test to avoid the hospitalization in the setting of falsely elevated ARR screening tests.

  20. The Interaction Between Angiotensin Converting Enzyme Inhibitor (Captopril and Heat Stress in The Male Albino rats. 2-Tissue Analysis

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    Talaat E.I. Abd-Rabo

    2000-12-01

    Full Text Available Daily exposure to heat stress causes sustained elevation of blood pressure in rats. It is known that the renin-angiotensin system is activated during episodes of behavioral stress, and the purpose of this work was to assess the action of captopril in the development of stress induced hypertension in rats. Animals were divided into four groups. The first group served as a control, while the other groups were subjected to heat stress of 40C and high hamidity of 80% for 10 successive days. The second group was served as heat stress, while the third and the fourth groups were received low and high doses of captopril (0.7 & 1.4 mg/kg. b.wt., respectively. After 10 days of treatment, half of animals from each group were decapitated and brain, liver, muscle, heart and kidney were separated and analysed. The other half of animals were left for another 10 days without any additional treatment for recovery.The results revealed a significant decrease in total protein of liver, heart, kidney, total lipids of heart, muscle and brain and total cholesterol of liver. On the other hand, insignificant change was noticed in muscle and brain total protein. Similarly, AST and ALT activities were also within the normal values for all the organs examined.Results exhibited that renin-angiotensin system may be important in the development of stress-induced hypertension in rats.

  1. Preparation and Characterization in vitro of Sustained-release Captopril/Chitosan-gelatin Net-polymer Microspheres(Cap/CGNPMs)

    Institute of Scientific and Technical Information of China (English)

    SONG Yimin; CHEN Xiguang; TANG Xuexi; LIU Chengshen; MENG Xianghong; YU Luojun

    2006-01-01

    The captopril/Chitosan-gelatin net-polymer microspheres (Cap/CGNPMs) were prepared using Chitosan(CS) and gelatin(Gel) by the methods of emulsification. A cross linked reagent alone or in combination with microcrystalline cellulose(MCC) was added in the process of preparation of microspheres to eliminate dose dumping and burst phenomenon of microspheres for the improvement of the therapeutic efficiency and the decrease of the side effects of captopril(Cap). The results indicate that Cap/CGNPMs have a spherical shape , smooth surface morphology and integral inside structure and no adhesive phenomena and good mobility,and the size distribution is mainly from 220 to 280 μm. Researches on the Cap release test in vitro demonstrate that Cap/CGNPMs are of the role of retarding release of Cap compared with Cap ordinary tablets (COT), embedding ratio (ER) ,drug loading (DL), and swelling ratio (SR), and release behaviors of CGNPMS are influenced by process conditions of preparation such as experimental material ratio (EMR) , composition of cross linking reagents. Among these factors , the EMR(1/4),CLR (FOR+TPP) and 0.75% microcrystalline cellulose (MCC) added to the microspheres are the optimal scheme to the preparation of Cap/CGNPMs. The Cap/CGNPMs have a good characteristic of sustained release of drug, and the process of emulsification and cross-linking process is simple and stable. The CGNPMs is probable to be one of an ideal sustained release system for water-soluble drugs.

  2. Combining use of captopril and losartan attenuates the progress of Streptococcus pneumoniae-induced tympanosclerosis through the suppression of TGF-β1 expression.

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    Wenqing Yan

    Full Text Available In this study, using an Streptococcus pneumoniae-induced tympanosclerosis (TS model, we explored the effects of captopril and losartan in the treatment of TS and the possible mechanisms.A prospective experimental animal study.We set up the TS models in both guinea pig and wistar rat by inoculation of type-3 Streptococcus pneumoniae microorganisms and then treated the animals with the combining use of captopril and losartan. Otomicroscopy was employed to observe the development of TS. Auditory brainstem response was used to test the hearing function of animals. Hematoxylin-eosin and von Kossa staining were performed to determine the morphological changes and calcium depositions. The protein expressions of transforming growth factor β1 (TGF-β1 were assessed by western blot and immunohistochemistry staining, and the mRNA level of TGF-β1 was measured by quantitative reverse transcription- polymerase chain reaction.The combining use of captopril and losartan attenuated TS responses in terms of a decrease in the TS incidence and the ABR threshold, a reduction of hyalinization and calcification in the middle ear mucosa and the thickness of the mucosa. In addition, the TGF-β1 expression was decreased at both protein and mRNA levels.Our data indicate, for the first time, that the combining use of captopril and losartan obviously attenuates TS progress through inhibiting the overexpressing of TGF-β1.

  3. Renal dynamic scintigraphy with captropil in systemic arterial hypertension diagnosis; Cintilografia renal dinamica com captopril no diagnostico da hipertensao arterial renovascular

    Energy Technology Data Exchange (ETDEWEB)

    Cervo, Marco Antonio Cadorna; Amarante Junior, Jose Luiz de Medeiros; Souza, Ricardo Alberto Manhaes; Evangelista, Maria Gardenia [Hospital Naval Marcilio Dias, Rio de Janeiro, RJ (Brazil). Servico de Medicina Nuclear

    1995-12-31

    Forty one patients, 15 male and 16 female presenting systemic arterial hypertension were submitted to Basal RDC and after being simulated by Captopril; the radiotracer used was 99 mTc-DTPA (dietileno triamino pentacetic acid-99 Tc-technetium). From the 41 patients studied, 13 had the GFR (Glomerular filtration rate) Captopril when compared to Basal RDC radioactive, 11 of them were confirmed as having vascular renal disease by Renal Artiography and two of them were false (one case renal litiase and the other chronic pyelonephritis). Two more false negative cases have occurred in the RDC and three patients refused to be submitted to a Renal Arteriography. In the cases which the Total Glomerular Filtration Rate was reduced, there was an agreement of 89,5% between the RDC and the Renal Arteriography. No alterations have been observed in the Renal Arteriography on the remaining 23 patients and in the RDC after Captopril there was normal increase in the Glomerular Filtration Rate when compared to the Basal RDC. The method has showed sensitivity of 84% and specificity of 92%. We can conclude that the RDC with Captopril test is not an invasive method, it has good sensitivity and specificity and it can be indicated as a beginning test to select patients when you intend to detect vascular renal disease; nevertheless the RDC will never be used as a final test of vascular lesion. (author) 22 refs., 7 figs., 2 tabs.

  4. Glomerular filtration rate measured by {sup 51}Cr-EDTA clearance: evaluation of captopril-induced changes in hypertensive patients with and without renal artery stenosis

    Energy Technology Data Exchange (ETDEWEB)

    Chaves, Anna Alice Rolim; Buchpiguel, Carlos Alberto; Praxedes, Jose Nery; Bortolotto, Luiz Aparecido; Sapienza, Marcelo Tatit, E-mail: annaalice100@yahoo.com.b [Universidade de Sao Paulo (USP), SP (Brazil). Faculdade de Medicina. Dept. de Neurologia

    2010-07-01

    Introduction: renal artery stenosis can lead to renovascular hypertension; however, the detection of stenosis alone does not guarantee the presence of renovascular hypertension. Renovascular hypertension depends on activation of the renin-angiotensin system, which can be detected by functional tests such as captopril renal scintigraphy. A method that allows direct measurement of the baseline and post-captopril glomerular filtration rate using chromium-51 labeled ethylenediamine tetraacetic acid ({sup 51}Cr-EDTA) could add valuable information to the investigation of hypertensive patients with renal artery stenosis. The purposes of this study were to create a protocol to measure the baseline and post-captopril glomerular filtration rate using {sup 51}Cr-EDTA, and to verify whether changes in the glomerular filtration rate permit differentiation between hypertensive patients with and without renal artery stenosis. Methods: this prospective study included 41 consecutive patients with poorly controlled severe hypertension. All patients had undergone a radiological investigation of renal artery stenosis within the month prior to their inclusion. The patients were divided into two groups: patients with (n=21) and without renal artery stenosis, (n=20). In vitro glomerular filtration rate analysis ({sup 51}Cr-EDTA) and {sup 99m}Tc-DMSA scintigraphy were performed before and after captopril administration in all patients. Results: the mean baseline glomerular filtration rate was 48.6+-21.8 ml/kg/1.73 m{sup 2} in the group with renal artery stenosis, which was significantly lower than the GFR of 65.1+-28.7 ml/kg/1.73m{sup 2} in the group without renal artery stenosis (p=0.04). Captopril induced a significant reduction of the glomerular filtration rate in the group with renal artery stenosis (to 32.6+-14.8 ml/kg/1.73m{sup 2}, p=0.001) and an insignificant change in the group without RAS (to 62.2+-23.6 ml/kg/1.73m{sup 2}, p=0.68). Scintigraphy with technetium-99m dimercapto

  5. Glomerular filtration rate measured by 51Cr-EDTA clearance: evaluation of captopril-induced changes in hypertensive patients with and without renal artery stenosis

    Directory of Open Access Journals (Sweden)

    Anna Alice Rolim Chaves

    2010-01-01

    Full Text Available INTRODUCTION: Renal artery stenosis can lead to renovascular hypertension; however, the detection of stenosis alone does not guarantee the presence of renovascular hypertension. Renovascular hypertension depends on activation of the renin-angiotensin system, which can be detected by functional tests such as captopril renal scintigraphy. A method that allows direct measurement of the baseline and post-captopril glomerular filtration rate using chromium-51 labeled ethylenediamine tetraacetic acid (51Cr-EDTA could add valuable information to the investigation of hypertensive patients with renal artery stenosis. The purposes of this study were to create a protocol to measure the baseline and post-captopril glomerular filtration rate using 51Cr-EDTA, and to verify whether changes in the glomerular filtration rate permit differentiation between hypertensive patients with and without renal artery stenosis. METHODS: This prospective study included 41 consecutive patients with poorly controlled severe hypertension. All patients had undergone a radiological investigation of renal artery stenosis within the month prior to their inclusion. The patients were divided into two groups: patients with (n=21 and without renal artery stenosis, (n=20. In vitro glomerular filtration rate analysis (51Cr-EDTA and 99mTc-DMSA scintigraphy were performed before and after captopril administration in all patients. RESULTS: The mean baseline glomerular filtration rate was 48.6±21.8 ml/kg/1.73 m² in the group wuth renal artery stenosis, which was significantly lower than the GFR of 65.1±28.7 ml/kg/1.73m² in the group without renal artery stenosis (p=0.04. Captopril induced a significant reduction of the glomerular filtration rate in the group with renal artery stenosis (to 32.6±14.8 ml/kg/1.73m², p=0.001 and an insignificant change in the group without RAS (to 62.2±23.6 ml/kg/1.73m², p=0.68. Scintigraphy with technetium-99m dimercapto-succinic acid (DMSA did not show

  6. Flow-injection spectrophotometric determination of captopril in pharmaceutical formulations using a new solid-phase reactor containing AgSCN immobilized in a polyurethane resin

    Directory of Open Access Journals (Sweden)

    Fernando Campanhã Vicentini

    2012-06-01

    Full Text Available A simple flow-injection analysis procedure was developed for determining captopril in pharmaceutical formulations employing a novel solid-phase reactor containing silver thiocyanate immobilized in a castor oil derivative polyurethane resin. The method was based on silver mercaptide formation between the captopril and Ag(I in the solid-phase reactor. During such a reaction, the SCN- anion was released and reacted with Fe3+, which generated the FeSCN2+ complex that was continuously monitored at 480 nm. The analytical curve was linear in the captopril concentration range from 3.0 × 10-4 mol L-1 to 1.1 × 10-3 mol L-1 with a detection limit of 8.0 × 10-5 mol L-1. Recoveries between 97.5% and 103% and a relative standard deviation of 2% for a solution containing 6.0 × 10-4 mol L-1 captopril (n = 12 were obtained. The sample throughput was 40 h-1 and the results obtained for captopril in pharmaceutical formulations using this procedure and those obtained using a pharmacopoeia procedure were in agreement at a 95% confidence level.Um procedimento simples de análise por injeção em fluxo foi desenvolvido para a determinação de captopril em formulações farmacêuticas empregando um novo reator em fase sólida contendo tiocianato de prata imobilizado em resina poliuretana obtida a partir de óleo de mamona. O método foi baseado na formação de um mercapto composto de prata, no reator em fase sólida, obtido entre o captopril e Ag (I imobilizada. Durante a reação, íons SCN- eram liberados e reagiam com Fe3+, gerando o complexo FeSCN2+, que foi continuamente monitorado em 480 nm. A curva analítica foi linear no intervalo de concentração de captopril entre 3,0 × 10-4 a 1,1 × 10-3 mol L-1 com um limite de detecção de 8,0 × 10-5 mol L-1. Recuperações entre 97,5-103% e desvio padrão relativo de 2% para uma solução contendo 6,0 × 10-4 mol L-1 de captopril (n = 12 foram obtidos. A frequência de amostragem foi de 40 h-1 e os resultados

  7. The role of captopril and losartan in prevention and regression of tamoxifen-induced resistance of breast cancer cell line MCF-7: an in vitro study.

    Science.gov (United States)

    Namazi, Soha; Rostami-Yalmeh, Javad; Sahebi, Ebrahim; Jaberipour, Mansooreh; Razmkhah, Mahboobeh; Hosseini, Ahmad

    2014-06-01

    Innate and acquired tamoxifen (TAM) resistance in estrogen receptor positive (ER+) breast cancer is an important problem in adjuvant endocrine therapy. The underlying mechanisms of TAM resistance is yet unknown. In the present study, we evaluated the role of renin-angiotensin system (RAS) in the acquisition of TAM resistance in human breast cancer cell line MCF-7, and the potential role of captopril and captopril+losartan combination in the prevention and reversion of the TAM resistant phenotype. MCF-7 cells were continuously exposed to 1 μmol/L TAM to develop TAM resistant cells (TAM-R). MTT cell viability assay was used to determine the growth response of MCF-7 and TAM-R cells, and quantitative real-time polymerase chain reaction (qRT-PCR) was used to assess angiotensin I converting enzyme (ACE), angiotensin II receptor type-1 and type-2 (AGTR1 and AGTR2) mRNA expressions. Preventive and therapeutic effects of RAS blockers - captopril and losartan - were examined on MCF-7 and TAM-R cells. Based on qRT-PCR, TAM-R cells compared to MCF-7 cells, had a mean ± SD fold increase of 319.1 ± 204.1 (P = 0.002) in production of ACE mRNA level, 2211.8 ± 777.9 (P = 0.002) in AGTR1 mRNA level, and 265.9 ± 143.9 (P = 0.037) in production of AGTR2 mRNA level. The combination of either captopril or captopril+losartan with TAM led to the prevention and even reversion of TAM resistant phenotype.

  8. Following specific podocyte injury captopril protects against progressive long term renal damage [version 1; referees: 1 approved, 2 approved with reservations

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    Yu S Zhou

    2015-06-01

    Full Text Available Background: Angiotensin converting enzyme inhibitors (ACEi reduce proteinuria and preserve kidney function in proteinuric renal diseases. Their nephroprotective effect exceeds that attributable to lowering of blood pressure alone. This study examines the potential of ACEi to protect from progression of injury after a highly specific injury to podocytes in a mouse model. Methods: We created transgenic (Podo-DTR mice in which graded specific podocyte injury could be induced by a single injection of diphtheria toxin. Transgenic and wild-type mice were given the ACEi captopril in drinking water, or water alone, commencing 24h after toxin injection. Kidneys were examined histologically at 8 weeks and injury assessed by observers blinded to experimental group. Results: After toxin injection, Podo-DTR mice developed acute proteinuria, and at higher doses transient renal impairment, which subsided within 3 weeks to be followed by a slow glomerular scarring process. Captopril treatment in Podo-DTR line 57 after toxin injection at 5ng/g body weight reduced proteinuria and ameliorated glomerular scarring, matrix accumulation and glomerulosclerosis almost to baseline (toxin: 17%; toxin + ACEi 10%, p<0.04; control 7% glomerular scarring. Podocyte counts were reduced after toxin treatment and showed no recovery irrespective of captopril treatment (7.1 and 7.3 podocytes per glomerular cross section in water and captopril-treated animals compared with 8.2 of wild-type controls, p<0.05. Conclusions: Observations in Podo-DTR mice support the hypothesis that continuing podocyte dysfunction is a key abnormality in proteinuric disease. Our model is ideal for studying strategies to protect the kidney from progressive injury following podocyte depletion. Demonstrable protective effects from captopril occur, despite indiscernible preservation or restoration of podocyte counts, at least after this degree of relatively mild injury.

  9. Gene expression profiles of vascular smooth muscle show differential expression of mitogen-activated protein kinase pathways during captopril therapy of heart failure.

    Science.gov (United States)

    Chen, Frank C; Brozovich, Frank V

    2008-01-01

    Congestive heart failure (CHF) is characterized by increased vascular tone and an impairment in nitric-oxide-mediated vasodilatation. We have demonstrated that the blunted response to nitric oxide is due, in part, to a reduction in the leucine-zipper-positive isoform of the myosin-targeting subunit (MYPT1) of myosin light-chain phosphatase. Additionally, we have shown that angiotensin-converting enzyme inhibition, but not afterload reduction with prazosin, preserves leucine-zipper-positive MYPT1 isoform expression in vascular smooth muscle cells and normalizes the sensitivity to cGMP-mediated vasodilatation. We therefore hypothesized that in CHF, growth regulators and cytokines downstream of the angiotensin II receptor are involved in modulating gene expression in vascular tissue. Rats were divided into control and captopril-treated groups following left coronary artery ligation. Gene expression profiles in the aorta and portal vein at baseline and 2 and 4 weeks after myocardial infarction (MI) were analyzed using microarray technology and quantitative real-time PCR. After MI, microarray analysis revealed differential mRNA expression of 21 genes in the aorta of captopril-treated rats 2 and 4 weeks after surgery when compared to gene expression profiles at baseline and without captopril therapy. Real-time PCR demonstrated that captopril suppressed the expression of protein kinases in the angiotensin-II-mediated mitogen-activated protein kinase signaling pathway, including Taok1 and Raf1. These data suggest that in CHF, captopril therapy modulates gene expression in vascular smooth muscle, and some of the beneficial effects of ACE inhibition may be due to differential gene expression in the vasculature.

  10. Effect of ivabradine, captopril and melatonin on the behaviour of rats in L-nitro-arginine methyl ester-induced hypertension.

    Science.gov (United States)

    Aziriova, S; Repova, K; Krajcirovicova, K; Baka, T; Zorad, S; Mojto, V; Slavkovsky, P; Hodosy, J; Adamcova, M; Paulis, L; Simko, F

    2016-12-01

    Cardiovascular diseases including hypertension are often associated with behavioural alterations. The aim of this study was to show, whether ivabradine, the blocker of If-channel in sinoatrial node, is able to modify the behaviour of rats in L-nitro-arginine methyl ester (L-NAME)-induced hypertension and to compare the effect of ivabradine with captopril and melatonin. 12-week-old male Wistar rats were divided into the following groups: controls, ivabradine (10 mg/kg/24 h), L-NAME (40 mg/kg/24 h), L-NAME + ivabradine, L-NAME + captopril (100 mg/kg/24 h), L-NAME + melatonin (10 mg/kg/24 h). Systolic blood pressure (SBP) and heart rate (HR) were measured by tail-cuff method once a week. The behaviour of rats was investigated during 23-hours in the phenotyper after four weeks of the treatment. Chronic administration of L-NAME induced hypertension without a change in HR. All tested substances partly prevented the increase of SBP, while ivabradine and melatonin also reduced HR. Ivabradine, captopril and melatonin reduced daily food intake, slightly decreased daily water intake and attenuated body weight gain. In L-NAME group, locomotor activity was enhanced by ivabradine, whereas exploratory behaviour was increased by melatonin and captopril. In conclusion, ivabradine, besides its potentially protective hemodynamic actions, does not seem to exert any disturbing effects on behaviour in L-NAME-induced hypertension in rats, while some of its effects were similar to captopril or melatonin. It is suggested that ivabradine used in cardiovascular indications is harmless regarding the effect on behaviour.

  11. Determinação da constante de dissociação (Ka do captopril e da nimesulida: experimentos de química analítica para o curso de farmácia

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    Airton Vicente Pereira

    2011-09-01

    Full Text Available This paper presents the determination of the dissociation constant (Ka of captopril and nimesulide as contextualized experiments to teach chemical concepts to students of Pharmacy. Captopril is an antihypertensive drug, which presents high water-solubility and weak acid properties. The pKa of carboxylic acid group of captopril is 3.7. Nimesulide is a non-steroidal anti-inflammatory drug sparingly soluble in water. It is weakly acidic (pKa ≈ 6.5 because of its methanesulfonamide functional group. The pKa of captopril was determined by potentiometric titration with NaOH 2.0 x 10-2 moL L ¹. The pKa of nimesulide was determined by using spectrophotometry and photometric titration. The experimental values of pKa of both drugs are in very good agreement with those from literature

  12. Effect of captopril on serum TNF-α level in acute lung injury rats induced by HCL

    Institute of Scientific and Technical Information of China (English)

    Hong-Mei Liu; Yu-Na Guo

    2014-01-01

    Objective:To observe the effect of captopril on the tumor necrosis factor-α (TNF-α) level and arterial blood gases in acute lung injury (ALI) induced by HCL in rats, and to analyze its protective mechanism. Methods:Fifty Wistar rats were selected and randomly divided into three groups, with 20 rats in GroupⅠandⅡ, respectively and 10 animals in GroupⅢ. ALI model was constructed by intratracheal injection of diluted hydrochloric acid (pH=1.25, 1.2 mL/kg). Group I rats received not any treatment after construction of ALI model. GroupⅡrats were treated with captopril (5 mg/kg, i.p.) 5 min after induction of ALI. GroupⅢserved as normal control without any treatment. Ninety minutes after construction of ALI model, all the rats were sacrificed. Blood was withdrawn for detection of TNF-αlevel and arterial blood gases index. And lung tissue slices of the three groups were prepared for observation of pathologic histology changes. Results:TNF-αlevel in serum of GroupⅠand Ⅱrats was significantly higher than that in GroupⅢ(P<0.05), while TNF-αlevel in serum of GroupⅡwas significantly lower in Group I (P<0.05). PaCO2 level was significantly higher (P<0.05), while PaO2 was significantly lower (P<0.05) in Group I andⅡrats than those in GroupⅢ. PaCO2 was significantly lower (P<0.05) and PaO2 was significantly higher (P<0.05) in GroupⅡthan those in Group I. Histological observation showed diffuse congestion and severe edema of lung tissue, obvious thickening and structure damage of alveolar walls and a large amount of neutrophil infiltration in Group I rats. GroupⅡrats showed mild edema of lung tissue;only a small portion of alveolar walls showed thickening and only a few of neutrophil infiltration could be observed. The degree of injury was remarkably slighter than that of Group I rats. GroupⅢrats showed clear lung tissue structure and normal morphology;alveolar walls were uniform and the margin was smooth and few neutrophil could be observed

  13. Direct electrochemical oxidation of S-captopril using gold electrodes modified with graphene-AuAg nanocomposites

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    Pogacean F

    2014-02-01

    Full Text Available Florina Pogacean,1 Alexandru R Biris,2 Maria Coros,1 Mihaela Diana Lazar,1 Fumiya Watanabe,3 Ganesh K Kannarpady,3 Said A Farha Al Said,4 Alexandru S Biris,3 Stela Pruneanu1 1Department of Isotopic Physics and Technology, 2Department of Mass Spectrometry, Chromatography, and Applied Physics, National Institute for Research and Development of Isotopic and Molecular Technologies, Cluj-Napoca, Romania; 3Center for Integrative Nanotechnology Sciences, University of Arkansas at Little Rock, Little Rock, Arkansas, USA; 4Department of Physics, College of Science, King Abdulaziz University, Jeddah, Saudi Arabia Abstract: In this paper, we present a novel approach for the electrochemical detection of S-captopril based on graphene AuAg nanostructures used to modify an Au electrode. Multi-layer graphene (Gr sheets decorated with embedded bimetallic AuAg nanoparticles were successfully synthesized catalytically with methane as the carbon source. The two catalytic systems contained 1.0 wt% Ag and 1.0 wt% Au, while the second had a larger concentration of metals (1.5 wt% Ag and 1.5 wt% Au and was used for the synthesis of the Gr-AuAg-1 and Gr-AuAg-1.5 multicomponent samples. High-resolution transmission electron microscopy analysis indicated the presence of graphene flakes that had regular shapes (square or rectangular and dimensions in the tens to hundreds of nanometers. We found that the size of the embedded AuAg nanoparticles varied between 5 and 100 nm, with the majority being smaller than 20 nm. Advanced scanning transmission electron microscopy studies indicated a bimetallic characteristic of the metallic clusters. The resulting Gr-AuAg-1 and Gr-AuAg-1.5 samples were used to modify the surface of commonly used Au substrates and subsequently employed for the direct electrochemical oxidation of S-captopril. By comparing the differential pulse voltammograms recorded with the two modified electrodes at various concentrations of captopril, the peak current

  14. Molecular Structural Studies of Captopril Drug, Using Thermal Analysis, mass Spectral Fragmentation and Semi- empirical MO- Calculations

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    H. M. Arafa

    2014-12-01

    Full Text Available In this work captopril an antihypertensive (KPL drug, was investigated using thermal analysis (TA measurements (TG-DTA in comparison with electron impact (EI mass spectral (MS fragmentation at 70 eV. Semi-empirical molecular (MO calculations, using PM3 method in the neutral and positively charged forms of the drug. These include molecular geometry, bond order, charge distribution, heats of formation and ionization energy. The behavior of the drug under drug TA decomposition, reveal a moderate stability up to 160Co before a completely decomposition in the range 160-240 Co. The initial decomposition is due to COOH + CH3 loss, followed by SH loss. On the other hand, the molecular ion can easily fragmented by CO2 loss followed by SH loss. This is the best-selected pathway comparable with decomposition using TA. MO-Calculation is used to declare these observations.

  15. Compensatory function of bradykinin B1 receptor in the inhibitory effect of captopril on cardiomyocyte hypertrophy and cardiac fibroblast proliferation in neonatal rats

    Institute of Scientific and Technical Information of China (English)

    ZOU Jun; REN Jiang-hua; FENG Dan; WANG Hong; XU Jiang

    2008-01-01

    Background Bradykinin(BK)acts mainly on two receptor subtypes:B1 and B2,and activation of B2 receptor mediates the most well-known cardioprotective effects of angiotensin converting enzyme inhibitors(ACEi),however,the role that B1 receptor plays in ACEi has not been fully defined.We examined the role of B1 receptor in the inhibitory effect of ACE inhibitor captopril on rat cardiomyocyte hypertrophy and cardiac fibroblast proliferation induced by angiotensin Ⅱ(Ang Ⅱ) and explored its possible mechanism.Methods Neonatal cardiomyocytes and cardiac fibroblasts(CFs)were randomly treated with Ang Ⅱ,captopril,B2 receptor antagonist(HOE-140)and B1 receptor antagonist(des-Arg10,Leu9-kallidin)alone or in combination.Flow cytometry was used to evaluate cell cycle,size and protein content.Nitric oxide(NO)and intracellular cyclic guanosine monophosphate(cGMP)level were measured by colorimetry and radioimmunoassay.Results After the CFs and cardiomyocytes were incubated with 0.1 μmol/L Ang Ⅱ for 48 hours.the percentage of CFs in the S stage,cardiomyocytes size and protein content significantly increased(both P<0.01 vs control),and these increases were inhibited by 10 μmol/L captopril.However,NO and cGMP levels were significantly higher than that with Ang Ⅱ alone(both P<0.01).1 μmol/L HOE-140 or 0.1 μmol/L des-Arg10,Leu9-kallidin attenuated the effects of captopril,which was blunted further by blockade of both B1 and B2 receptors.Conclusions Acting via B2 receptor,BK contributes to the antihypertrophic and antiproliferative effects of captopril on cardiomyocytes and CFs.In the absence of B2 receptor,B1 receptor may act a compensatory mechanism for the B2 receptor and contribute to the inhibition of cardiomyocyte hypertrophy and CFs proliferation by captopril.NO and cGMP play an important role in the effect of B1 receptor.

  16. Preparation and in vitro release performance of sustained-release captopril/Chitosan-gelatin net-polymer microspheres

    Science.gov (United States)

    Zhou, Li; Xu, Junming; Song, Yimin; Gao, Yuanyuan; Chen, Xiguang

    2007-07-01

    The captopril/Chitosan-gelatin net-polymer microspheres (CTP/CGNPMs) were prepared using Chitosan (CTS) and gelatin (GT) by the methods of emulsification, cross-linked reagent alone or in combination and microcrystalline cellulose (MCC) added in the process of preparation of microspheres, which aimed to eliminate dose dumping and burst phenomenon of microspheres for the improvement of the therapeutic efficiency and the decrease of the side effects of captopril (CTP). The results indicated that CTP/CGNPMs had a spherical shape, smooth surface and integral structure inside but no adhesive phenomena in the preparation. The size distribution ranged from 220 μm to 280 μm. The CTP release test in vitro demonstrated that CTP/CGNPMs played the role of retarding the release of CTP compared with ordinary CTP tablets. The release behaviors of CGNPMS were influenced by preparation conditions such as experimental material ratio (EMR) and composition of cross linking reagents. Among these factors, the EMR (1/4), CLR (FA+SPP) and 0.75% microcrystalline cellulose (MCC) added to the microspheres constituted the optimal scheme for the preparation of CTP/CGNPMs. The ER, DL and SR of CTP/CGNPMs prepared according to the optimal scheme were 46.23±4.51%, 9.95±0.77% and 261±42%, respectively. The CTP/CGNPMs had the good characteristics of sustained release of drug and the process of emulsification and cross-linking were simple and stable. The CGNPMs are likely to be an ideal sustained release formulation for water-soluble drugs.

  17. Preparation and in vitro Release Performance of Sustained-release Captopril/Chitosan-gelatin Net-polymer Microspheres

    Institute of Scientific and Technical Information of China (English)

    2007-01-01

    The captopril/Chitosan-gelatin net-polymer microspheres (CTP/CGNPMs) were prepared using Chitosan (CTS) and gelatin (GT) by the methods of emulsification, cross-linked reagent alone or in combination and microcrystalline cellulose (MCC) added in the process of preparation of microspheres, which aimed to eliminate dose dumping and burst phenomenon of microspheres for the improvement of the therapeutic efficiency and the decrease of the side effects of captopril (CTP). The results indicated that CTP/CGNPMs had a spherical shape, smooth surface and integral structure inside but no adhesive phenomena in the preparation. The size distribution ranged from 220 μm to 280 μm. The CTP release test in vitro demonstrated that CTP/CGNPMs played the role of retarding the release of CTP compared with ordinary CTP tablets. The release behaviors of CGNPMS were influenced by preparation conditions such as experimental material ratio (EMR) and composition of cross linking reagents. Among these factors, the EMR (1/4), CLR (FA+SPP) and 0.75% microcrystalline cellulose (MCC) added to the microspheres constituted the optimal scheme for the preparation of CTP/CGNPMs. The ER, DL and SR of CTP/CGNPMs prepared according to the optimal scheme were 46.23±4.51%, 9.95±0.77% and 261±42%, respectively. The CTP/CGNPMs had the good characteristics of sustained release of drug and the process of emulsification and cross-linking were simple and stable. The CGNPMs are likely to be an ideal sustained release formulation for water-soluble drugs.

  18. Arterial morphology responds differently to Captopril then N-acetylcysteine in a monocrotaline rat model of pulmonary hypertension

    Science.gov (United States)

    Molthen, Robert; Wu, Qingping; Baumgardt, Shelley; Kohlhepp, Laura; Shingrani, Rahul; Krenz, Gary

    2010-03-01

    Pulmonary hypertension (PH) is an incurable condition inevitably resulting in death because of increased right heart workload and eventual failure. PH causes pulmonary vascular remodeling, including muscularization of the arteries, and a reduction in the typically large vascular compliance of the pulmonary circulation. We used a rat model of monocrotaline (MCT) induced PH to evaluated and compared Captopril (an angiotensin converting enzyme inhibitor with antioxidant capacity) and N-acetylcysteine (NAC, a mucolytic with a large antioxidant capacity) as possible treatments. Twenty-eight days after MCT injection, the rats were sacrificed and heart, blood, and lungs were studied to measure indices such as right ventricular hypertrophy (RVH), hematocrit, pulmonary vascular resistance (PVR), vessel morphology and biomechanics. We implemented microfocal X-ray computed tomography to image the pulmonary arterial tree at intravascular pressures of 30, 21, 12, and 6 mmHg and then used automated vessel detection and measurement algorithms to perform morphological analysis and estimate the distensibility of the arterial tree. The vessel detection and measurement algorithms quickly and effectively mapped and measured the vascular trees at each intravascular pressure. Monocrotaline treatment, and the ensuing PH, resulted in a significantly decreased arterial distensibility, increased PVR, and tended to decrease the length of the main pulmonary trunk. In rats with PH induced by monocrotaline, Captopril treatment significantly increased arterial distensibility and decrease PVR. NAC treatment did not result in an improvement, it did not significantly increase distensibility and resulted in further increase in PVR. Interestingly, NAC tended to increase peripheral vascular density. The results suggest that arterial distensibility may be more important than distal collateral pathways in maintaining PVR at normally low values.

  19. Captopril associado à hidroclorotiazida no tratamento da hipertensão leve e moderada. Estudo multicêntrico brasileiro

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    Santello José Luiz

    1998-01-01

    Full Text Available OBJETIVO: Avaliar a eficácia e tolerabilidade da associação de captopril 50mg com hidroclorotiazida 25mg em hipertensos com pressão arterial diastólica (PAD entre 95 e 115mmHg. MÉTODOS: Estudo aberto, multicêntrico, não comparativo. Na fase inicial, durante 2 semanas, os pacientes receberam placebo, seguida de ½ comprimido da associação. Os pacientes foram avaliados após 4, 8 e 12 semanas. Após 8 semanas de tratamento, naqueles em que a PAD foi >90mmHg, foi prescrito um comprimido/dia. RESULTADOS: Foram analisados 433 pacientes, com idades de 47±10 anos, sendo 30% mulheres e 76% brancos. As pressões sistólica/diastólica iniciais foram de 156±16/103±11mmHg, após 14 dias de placebo, 156±15/103±9mmHg (p>0,05 e, após 4, 8 e 12 semanas, mostraram progressiva redução (p<0,05 para 143±14/95±11, 140±13/91±9 e 134±11/86±8mmHg. O controle pressórico foi observado em 45, 67 e 88% (p<0,05, após 4, 8 e 12 semanas. Tosse foi o sintoma mais importante registrado em 7% dos pacientes em placebo e 12% nos que usavam a associação. A tolerabilidade foi considerada boa por 98% dos pacientes. CONCLUSÃO: A associação de captopril com hidroclorotiazida é eficaz e tem boa tolerabilidade, sendo prescrita em dose única diária em monoterapia, para hipertensos leves e moderados.

  20. SYNTHESIS AND IN VITRO CHARACTERIZATION OF HYDROXYPROPYL METHYLCELLULOSE-GRAFT-POLY (ACRYLIC ACID/2-ACRYLAMIDO-2-METHYL-1-PROPANESULFONIC ACID) POLYMERIC NETWORK FOR CONTROLLED RELEASE OF CAPTOPRIL.

    Science.gov (United States)

    Furqan Muhammad, Iqbal; Mahmood, Ahmad; Aysha, Rashid

    2016-01-01

    A super-absorbent hydrogel was developed by crosslinking of 2-acrylamido-2-methyl-1-propanesulfonic acid (AMPS) and acrylic acid with hydroxypropyl methylcellulose (HPMC) for controlled release drug delivery of captopril, a well known antihypertensive drug. Acrylic acid and AMPS were polymerized and crosslinked with HPMC by free radical polymerization, a widely used chemical crosslinking method. N,N'-methylenebisacrylamide (MBA) and potassium persulfate (KPS) were added as cross-linker and initiator, respectively. The hydrogel formulation was loaded with captopril (as model drug). The concentration of captopril was monitored at 205 nm using UV spectrophotometer. Equilibrium swelling ratio was determined at pH 2, 4.5 and 7.4 to evaluate the pH responsiveness of the formed hydrogel. The super-absorbent hydrogels were evaluated by FTIR, SEM, XRD, and thermal analysis (DSC and TGA). The formation of new copolymeric network was determined by FTIR, XRD, TGA and DSC analysis. The hydrogel formulations with acrylic acid and AMPS ratio of 4: 1 and lower amounts of crosslinker had shown maximum swelling. Moreover, higher release rate of captopril was observed at pH 7.4 than at pH 2, because of more swelling capacity of copolymer with increasing pH of the aqueous medium. The present research work confirms the development of a stable hydrogel comprising of HPMC with acrylic acid and AMPS. The prepared hydrogels exhibited pH sensitive behav-ior. This superabsorbent composite prepared could be a successful drug carrier for treating hypertension.

  1. Captopril pretreatment protects the lung against severe acute pancreatitis induced injury via inhibiting angiotensin II production and suppressing Rho/ROCK pathway.

    Science.gov (United States)

    Yu, Qi-Hong; Guo, Jie-Fang; Chen, Yan; Guo, Xiao-Rong; Du, Yi-Qi; Li, Zhao-Shen

    2016-09-01

    Acute pancreatitis (AP) usually causes acute lung injury, which is also known as acute pancreatitis associated lung injury (APALI). This study aimed to investigate whether captopril pretreatment was able to protect lung against APALI via inhibiting angiotensin II (Ang II) production and suppressing Rho/ROCK (Rho kinase) pathway in rats. Severe AP (SAP) was introduced to rats by bile-pancreatic duct retrograde injection of 5% sodium taurocholate. Rats were randomly divided into three groups. In the sham group, sham operation was performed; in the SAP group, SAP was introduced; in the pre-cpl + SAP group, rats were intragastrically injected with 5 mg/kg captopril 1 hour prior to SAP induction. Pathological examination of the lung and pancreas, evaluation of pulmonary vascular permeability by wet/dry ratio and Evans Blue staining, detection of serum amylase, Western blot assay for Ang II receptor type 1 (AT1), RhoA, ROCK (Rho kinase), and MLCK (myosin light chain kinase) were performed after the animals were sacrificed at 24 hours. After the surgery, characteristic findings of pancreatitis were observed, accompanied by lung injury. The serum amylase, Ang II, and lung expression of AT1, RhoA, ROCK, and MLCK increased dramatically in SAP rats. However, captopril pretreatment improved the histological changes, reduced the pathological score of the pancreas and lung, inhibited serum amylase and Ang II production, and decreased expression of AT1, RhoA, ROCK, and MLCK in the lung. These findings suggest that captopril pretreatment is able to protect the lung against APALI, which is, at least partially, related to the inhibition of Ang II production and the suppression of the Rho/ROCK pathway.

  2. Long-term follow-up of Captopril-mediated decrease of regurgitation in aortic and mitral insufficiency. Pt. 2. Hemodynamic changes

    Energy Technology Data Exchange (ETDEWEB)

    Kropp, J.; Biersack, H.J. (Bonn Univ. (Germany). Dept. of Nuclear Medicine); Heck, I. (Lukas Hospital, Altenkirchen (Germany). Dept. of Internal Medicine); Nitsch, J. (St.-Agnes Hospital, Bocholt (Germany). Dept. of Internal Medicine); Reske, S.N. (City Hospital, Wuppertal (Germany). Dept. of Nuclear Medicine)

    Nineteen patients with aortic- and 10 patients with mitral insufficiency were investigated by gated-radionuclide-ventriculography (RNVG). RNVG was performed before and 1 h after administration of 25 mg of Captopril (C) as well as during longterm treatment. From the RNVG studies ejection fraction (EF), left ventricular end-diastolic volume index and regurgitation volume index were derived. EF remained unchanged after C as heart rate. All hemodynamic benefits could be maintained during long-term treatment. (orig./MG).

  3. Determination of Captopril in Human Plasma by High—Performance Liquid Chromatography and Study on the Pharmacokinetics after a Single Oral Dose

    Institute of Scientific and Technical Information of China (English)

    YANGLi; XUAi-xia; ZHAORong-sheng; YANBao-xia

    2003-01-01

    Aim:To establish a simple high-performance liquid chromatography method for the determination of captopril in human plasma and study the phamacokinetics of captopril in healthy volunteers.Methods:Captopril was stabilized by forming an adduct with p-bromophenacyl bromide and this adduct in plasma was measured by high-performance liquid chromatography with UV detection following a single oral dose 50mg of captopril test and reference preparations respectively given to 18 healthy volunteers.Results:The standard curve was liner over a range of 25-1200ng·mL-1.The quantitative limit of detection was 25ng·mL-1.The RSD of inter-and intra-assay were below 8%.On the basis of elaborated method,single-dose pharmacokinetics in 18 healthy volunteers have been investigated.The comparison of the pharmacokinetic parameters was performed.The pharmacokinetic parameters of test and reference tablets were calculated as follows:tmax were (0.64±0.18)h and (0.82±0.41)h;Cmax were (600.2±194.3)ng·mL-1 and (582.7±175.3)ng·mL-1.AUC0→gh were (1448.5±483.7)ng·h·mL-1 and (1389.9±392.5)ng·h·mL-1;AUC0→∞ were (1869.4±701.6)ng·h·mL-1 and (1781±615.5)ng·h·mL-1and (1389.9±392.5)ng·h·mL-1;AUC0→∞were (1869.4±701.6)ng·h·mL-1 and (1781.8±615.5)ng·h·mL-1,respectively.Conclusion:The improved analytical method for captopril was found to be sensitive,simple and rapid,suitable for application in pharmacokinetic studies and routine determination of numerous samples.

  4. New formulation of an old drug in hypertension treatment: the sustained release of captopril from cyclodextrin nanoparticles

    Directory of Open Access Journals (Sweden)

    de Azevedo MB

    2011-05-01

    Full Text Available Mariangela de Burgos M de Azevedo1, Ljubica Tasic2, Juliana Fattori2, Fábio HS Rodrigues2, Fabiana C Cantos1, Leandro P Ribeiro1, Vanice de Paula3, Danielle Ianzer3, Robson AS Santos31Biopharmaceuticals and Hormones, Center of Biotechnology, Instituto de Pesquisas Energéticas e Nucleares (IPEN, Sao Paulo, Brazil; 2Chemical Biology Laboratory, Department of Organic Chemistry, Instituto de Química (UNICAMP, Sao Paulo, Brazil; 3Hypertension Laboratory, Department of Physiology and Biophysics, Instituto de Ciências Biológicas (ICB, Universidade Federal de Minas Gerais (ICB-UFMG, Minas Gerais, BrazilAbstract: Captopril (CAP was the first angiotensin I-converting enzyme (ACE inhibitor to be developed and is widely used in hypertension treatment. On the other hand, cyclodextrins (CDs are cyclic oligosaccharides whose cone-shaped cavity allows formation of noncovalent inclusion complexes with appropriately sized guest molecules, thus modifying guest physical, chemical, and biological properties. Herein, the physicochemical characterization and in vivo ACE inhibition evaluation of seven CAP/CD complexes are reported. The inclusion complexes were prepared by spray-drying, freeze-drying, kneading, or lyophilization methods and characterized by nuclear magnetic resonance, Fourier-transformed infrared spectroscopy, X-ray diffraction, differential scanning calorimetry, and scanning electron microscopy techniques. In vivo assays compared CAP and CAP/CD complex administration (0.5 mg kg-1 or 0.09 mg kg-1, n = 4–7 to evaluate the ACE inhibition by continuous infusion of angiotensin I (30 ng 50 µL-1 min-1 in conscious Wistar rats. The physicochemical analysis demonstrated complete amorphization and complexation between CAP and CDs, indicating the substitution of water molecules inside the CD cavity with CAP. During the infusion of angiotensin I, the administration of all CAP/CD complexes induced a reduction in mean arterial pressure similar to that

  5. EFFECT OF CAPTOPRIL ON RENAL HEMODYNAMICS AND RENAL PROSTAGLANDINS IN EARLY TYPE Ⅱ DIABETIC PATIENTS WITH NORMO-OR MICROALBUMINURIA

    Institute of Scientific and Technical Information of China (English)

    肖新华; 甘佩珍; 余明炎; 李竞; 韩其蔚

    1996-01-01

    In this study,we investigated the effect of captopril (CPT) on glomerular filtration rate (GFR),effective renal plasma flow(ERPF),filtration fraction(FF),urinary albumin excretion (UAE) and daily urinary exceretion of thromboxane B2(TXB2) and 6-keto-prostaglandin F1a(6-keto-PGF1a) in 29 normotensive non-insulin-dependent diabetes (NIDDM) patients withour clinically discernible nephropathy.Before treatment,urinsry excretion 6-keto-PGF]a was sienificantly increased (P<0.05) in 29 NIDDM patients compared with 25 health subjects matched for age and sex.The values of GFR and FF were significantly higher (P<0.01 and P<0.005,respectively) in NIDDm than in normal volunters,whereas ERPF was comparable in both groups.Meanwhile we observed that UAE of early NIDDM was increased before treatment.After CPT treatment,GFR,FF,UAE and urinary excretion of 6-keto-PGF1a were significantoly reduce (all P<0.005) compared with those of NIDDM before treatment.These date indicated that CPT is effective in lowering glomerular filtration pressure and ameliorating microalbuminria in the normotensive early NIDDM.

  6. Value of renal scintigraphy with captopril test in the exploration of renovascular hypertension: Case report; Apport de la scintigraphie renale avec test au captopril dans l'exploration de l'hypertension arterielle renovasculaire: a propos d'un cas

    Energy Technology Data Exchange (ETDEWEB)

    Ghfir, I.; Berehou, F.Z.; Ben Rais, N. [Centre Hospitalier Universitaire de Rabat, Hopital Ibn-Sina, Service de Medecine Nucleaire (Morocco)

    2007-08-15

    Introduction Dynamic renal scintigraphy with {sup 99m}Tc-DTPA and captopril test is a non-invasive functional method for the diagnosis of renovascular hypertension. It allows differentiating between hypertension induced by renal arterial stenosis from primary arterial hypertension with an incidental stenosis. Case report A 14-year-old girl, without previous medical history, developed a severe arterial hypertension with cephalalgia and ears buzzing. Auscultation revealed a murmur in the left lumbar pit. Renal angiography objectified a stenosis of the infra renal aorta due to a circumferential parietal thickening associated to renal arteries stenosis more marked in the left side. Dynamic renal scintigraphy after administration of captopril highlighted a marked collapse of the rate of tracer uptake exceeding 40% on the left side with an increase in the time of collecting on the right side testifying a frankly positive test prevailing on the left. A transluminal angioplasty of the left renal artery and a revascularization surgery on the right side were carried out. The evolution was marked by an improvement of blood pressure figures. Discussion Dynamic renal scintigraphy using {sup 99m}Tc-DTPA with captopril test constitutes a non-invasive process with a low dosimetry for the patients. Its principal goal is to affirm the role of renovascular stenosis in the origin of arterial hypertension and to determine which hypertensive patients with renal arterial stenosis can be treated successfully by surgical or endoscopic revascularization of the kidney. (authors)

  7. The critical role of NIR spectroscopy and statistical process control (SPC) strategy towards captopril tablets (25 mg) manufacturing process understanding: a case study.

    Science.gov (United States)

    Curtivo, Cátia Panizzon Dal; Funghi, Nathália Bitencourt; Tavares, Guilherme Diniz; Barbosa, Sávio Fujita; Löbenberg, Raimar; Bou-Chacra, Nádia Araci

    2015-05-01

    In this work, near-infrared spectroscopy (NIRS) method was used to evaluate the uniformity of dosage units of three captopril 25 mg tablets commercial batches. The performance of the calibration method was assessed by determination of Q value (0.9986), standard error of estimation (C-set SEE = 1.956), standard error of prediction (V-set SEP = 2.076) as well as the consistency (106.1%). These results indicated the adequacy of the selected model. The method validation revealed the agreement of the reference high pressure liquid chromatography (HPLC) and NIRS methods. The process evaluation using the NIRS method showed that the variability was due to common causes and delivered predictable results consistently. Cp and Cpk values were, respectively, 2.05 and 1.80. These results revealed a non-centered process in relation to the average target (100% w/w), in the specified range (85-115%). The probability of failure was 21:100 million tablets of captopril. The NIRS in combination with the method of multivariate calibration, partial least squares (PLS) regression, allowed the development of methodology for the uniformity of dosage units evaluation of captopril tablets 25 mg. The statistical process control strategy associated with NIRS method as PAT played a critical role in understanding of the sources and degree of variation and its impact on the process. This approach led towards a better process understanding and provided the sound scientific basis for its continuous improvement.

  8. The Profile of the Serum Levels of Inflammatory Cytokines TNF-a,IL-6, IL-10 and Captopril Intervention in Reno-hypertensive Rats

    Institute of Scientific and Technical Information of China (English)

    Li Zhongchen; Liu Fengying

    2005-01-01

    Objectives To observe the profile of the serum levels of inflammatory cytokines interleukin-6 (IL-6), tumor necrosis factor (TNF-o) and interleukin-10 (IL-10) and evaluate the effects of angiotensin- converting enzyme inhibitor-Captopril on them in renohypertensive rats. Methods Using reformed two-kidney-one-clip (2K 1C ) method, renal hypertensive rats (RHR) were obtained by ligating abdominal aorta.30 Wistar rats were randomized into three groups:sham-operation group (A)、 model control group ( B ) and captopril group (C). All rats were killed after being given the trial drugs 5 weeks, ELISA assays were used to detect the levels of IL-6 and IL-10, the levels of TNF-alpha were measured with radioimmtmoassays.hypertrophy was aggravated in group B significantly,the ratio of left ventricle and body weight(LV/BW) was 0.00318 ±0.00030 (B)and 0.00256 ±0.00040 (A)respectively(P < 0.001 ), the levels of IL-6 and TNF-o increased significantly (P < 0.001 and P < 0.002respectively), whereas the levels of IL-10 were not compared with group B, the LV/BW was 0.00266 ±0.00018 (C) and 0.00318±0.00030 (B) respectively(P < 0.001), the levels of IL-6 and TNF-α decreased significantly ( P < 0.01), whereas the levels of IL-10were not changed between the two groups (P > 0.05);Conclusions Angiotensin converting enzyme inhibitor-captopril can lower the serum levels of proinflammatory cytokines IL-6 and TNF-α effectively,but can not increase the levels of anti-inflammatory cytokine IL-10, it suggests that captopril may have a feature to prevent or slow the development of hypertensive complications by means of lowering the levels of pro-inflammatory cytokines but not by increasing anti-inflammatory cytokine IL-10.

  9. Pretreatment with aldosterone or corticosterone blocks the memory-enhancing effects of nimodipine, captopril, CGP 37,849, and strychnine in mice.

    Science.gov (United States)

    Mondadori, C; Gentsch, C; Hengerer, B; Ducret, T; Borkowski, J; Racine, A; Lederer, R; Haeusler, A

    1992-01-01

    Oral pretreatment with aldosterone or corticosterone blocked the memory-enhancing effects of the calcium antagonist nimodipine, the ACE inhibitor captopril, the NMDA blocker CGP 37,849, and the glycine antagonist strychnine in a passive-avoidance test in mice. The memory-disturbing effects of phenobarbitone, diazepam, CGP 37,849 and scopolamine were not influenced by the hormonal pretreatment. These findings could indicate the involvement of a steroid-sensitive mechanism in drug-induced improvement of memory. In the light of clinical observations showing elevated cortisol levels in Alzheimer patients, the results might also explain why only a limited number of these patients respond to therapy with memory enhancers.

  10. 卡托普利改善老年充血性心力衰竭伴低血压患者平板运动试验%Observation of captopril in improving the effect of plate exercises in old patients with congestive heart failure associated with hypotension

    Institute of Scientific and Technical Information of China (English)

    杨喜山; 关继红; 曾莉; 董平栓

    2002-01-01

    Objective To observe captopril in improving the effect of plate exercises in old patients with congestive heart failure(CHF) associated with hypotension.Methods 40 old patients of CHF were divided into 2 groups:Group A(routine treatment group) and group B(routine treatment plus captopril group) after basic treatment of anti heart failure adjustment.Result After 12 weeks of treatment,cardiac function,ejection fraction of left ventricle,exercise time,and metabolic equilent were significantiy improved in group B but not in group A.Conclusion Captopril can improve exercise time and metabolic equilent in old patients with CHF associated hypotension.

  11. Radionuclide venticulography in the evaluation of Captopril-mediated decrease of regurgitation in aortic and mitral insufficiency. Pt. 1. Methods and hormonal response

    Energy Technology Data Exchange (ETDEWEB)

    Kropp, J.; Schmidt, H.; Knopp, R.; Biersack, H.J. (Bonn Univ. (Germany). Dept. of Nuclear Medicine); Heck, I. (Lukas Hospital, Altenkirchen (Germany). Dept. of Internal Medicine); Nitsch, J. (St.-Agnes Hospital, Bocholt (Germany). Dept. of Internal Medicine)

    Nineteen patients with valve insufficency (VI) were investigated by gated-radionuclide-ventriculography (RNVG) to evaluate regurgitation fraction (RF). Ten of these patients were evaluated with right- and left heart catheterization (LRHC). 16 patients without valvular disease were investigated by left ventricular cineventriculography (LVCV) and RNVG. RNVG-left ventricular enddiastolic volume (LVEDV) was determined by a count-based method (LVED{sub cb}) as well as by a geometrical method (LVEDV{sub g}). After administration of Captopril (C), levels of angiotensin I increased in patients with VI (from 233 to 864 pg/ml, p<0.001) while angiotensin II decreased (from 43 to 30 pg/ml, p<0.001). Correlation of LRHC-RF and RNVG-RF, LVCV-LVEDV and LVEDV{sub cb}, LVCV-LVEDV and LVEDV{sub g} was characterized by the following equations: y=0.78x+6.9r=0.89; y=1.0x+5.7,r=0.93; and y=0.5x+92,r=0.45, respectively. Indexterms: Valve insufficency - radionuclide ventriculography - Captopril - Afterload reduction - regurgitation volume. (orig.).

  12. Captopril and Valsartan May Improve Cogniti ve Function Through Potentiation of the Brain Antioxidant Defense System and Attenuation of Oxidative/Nitrosative Damage in STZ - Induced Dementia in Rat

    Directory of Open Access Journals (Sweden)

    Yasaman Arjmand Abbassi

    2016-12-01

    Full Text Available Purpose: Previous findings have shown the crucial roles of brain renin-angiotensin system (RAS in pathogenesis of Alzheimer’s disease (AD. Since RAS inhibitors may have beneficial effects on dementia and cognitive function in elderly people, the aim of present study was to examine the neuroprotective actions of captopril and valsartan on memory function and neuronal damage in experimental model of AD. Methods: Adult forty male Wistar rats (220-280g were randomly divided into 5 groups; Control, Vehicle, Alzheimer and treatment groups. AD was induced by the injections of streptozotocin (3mg/kg, bilateral intracerebroventricular at days 1&3. Treated rats received orally captopril (50mg/kg/day and valsartan (30mg/kg/day. Memory function and histological assessments were done at termination of experiment. Finally, superoxide dismutase (SOD and catalase (CAT activities as well as malondialdehyde (MDA and NOx contents were determined. Results: There was a significant increase in the mean value of latency in Alzheimer group (66%. Captopril and valsartan considerably decreased this value in both treatment groups (45% and 72%, respectively. In Alzheimer group the activities of brain’s SOD and CAT reduced (40% and 47%, respectively in accompany with an increase in MDA and NOx contents (49% and 50%, respectively. Captopril and valsartan significantly increased the activities of brain’s SOD and CAT concomitant reduction in MDA and NOx contents. Also, histopathological damages noticeably decreased in both treatment groups. Conclusion: Our findings indicate that RAS inhibition by using captopril and valsartan potentiates the antioxidant defense system of brain and reduces oxidative/nitrosative stress in accompany with neuronal damage during AD.

  13. 缬沙坦或卡托普利或二者联合治疗心肌梗塞伴心力衰竭和(或)左心室功能障碍的评价%Evaluation of Valsartan, Captopril or Both in Myocardial Infarction Complicated by Heart Failure, Left Ventricular Dysfunction, or Both

    Institute of Scientific and Technical Information of China (English)

    钱卫民

    2005-01-01

    Pfeffer MA, McMurray JV, Velazquez E J, et al. Valsartan, Captopril, or both in myocardial infarction complicated by heart failure, left ventricular dysfunction, or both [J]. N Engl J Med, 2003, 349 (20) : 1893-1905.

  14. Cyclodextrin- and solvent-modified micellar electrokinetic chromatography for the determination of captopril, hydrochlorothiazide and their impurities: A Quality by Design approach.

    Science.gov (United States)

    Pasquini, Benedetta; Orlandini, Serena; Caprini, Claudia; Del Bubba, Massimo; Innocenti, Massimo; Brusotti, Gloria; Furlanetto, Sandra

    2016-11-01

    A fast and selective capillary electrophoresis method has been developed for the simultaneous determination of the antihypertensive drugs captopril and hydrochlorothiazide and their related impurities in a combined dosage form. Method development was carried out implementing each step of Quality by Design workflow, the new paradigm of quality outlined in International Conference on Harmonisation Guidelines. Captopril is characterized by the lack of a strong chromophore and contains a proline-similar moiety, which gives rise to the presence of interconverting cis-trans isomers and leads to the possible interference between electrophoretic migration and reaction of isomerization. The scouting phase was dedicated to the investigation of several operative modes in order to overcome detection and isomerization issues. The best performances were obtained with sodium cholate-based micellar electrokinetic chromatography with the addition of n-butanol and γ-cyclodextrin. Critical quality attributes were represented by the critical resolution values and by analysis time. Critical process parameters were defined as temperature, voltage, concentration and pH of borate buffer, concentration of sodium cholate, n-butanol and γ-cyclodextrin. Screening experimental design was applied for investigating knowledge space. Response surface methodology pointed out several significant interaction effects, and with Monte-Carlo simulations led to map out the design space at a selected probability level. Robustness testing was carried out and a control strategy based on system suitability tests was defined. The selected working conditions gave a complete separation of the analytes in less than three minutes. The method was validated and applied to the analysis of a real sample of coformulation tablets.

  15. The angiotensin converting enzyme inhibitor, captopril, prevents the hyperactivity and impulsivity of neurokinin-1 receptor gene 'knockout' mice: sex differences and implications for the treatment of attention deficit hyperactivity disorder.

    Science.gov (United States)

    Porter, Ashley J; Pillidge, Katharine; Grabowska, Ewelina M; Stanford, S Clare

    2015-04-01

    Mice lacking functional neurokinin-1 receptors (NK1R-/-) display behavioural abnormalities resembling attention deficit hyperactivity disorder (ADHD): locomotor hyperactivity, impulsivity and inattentiveness. The preferred ligand for NK1R, substance P, is metabolised by angiotensin converting enzyme (ACE), which forms part of the brain renin angiotensin system (BRAS). In view of evidence that the BRAS modulates locomotor activity and cognitive performance, we tested the effects of drugs that target the BRAS on these behaviours in NK1R-/- and wildtype mice. We first tested the effects of the ACE inhibitor, captopril, on locomotor activity. Because there are well-established sex differences in both ADHD and ACE activity, we compared the effects of captopril in both male and female mice. Locomotor hyperactivity was evident in male NK1R-/- mice, only, and this was abolished by treatment with captopril. By contrast, male wildtypes and females of both genotypes were unaffected by ACE inhibition. We then investigated the effects of angiotensin AT1 (losartan) and AT2 (PD 123319) receptor antagonists on the locomotor activity of male NK1R-/- and wildtype mice. Both antagonists increased the locomotor activity of NK1R-/- mice, but neither affected the wildtypes. Finally, we tested the effects of captopril on the performance of male NK1R-/- and wildtype mice in the 5-choice serial reaction-time task (5-CSRTT) and found that ACE inhibition prevented the impulsivity of NK1R-/- mice. These results indicate that certain behaviours, disrupted in ADHD, are influenced by an interaction between the BRAS and NK1R, and suggest that ACE inhibitors could provide a novel treatment for this disorder.

  16. The ACE inhibitors enalapril and captopril modulate cytokine responses in Balb/c and C57Bl/6 normal mice and increase CD4(+)CD103(+)CD25(negative) splenic T cell numbers.

    Science.gov (United States)

    Albuquerque, Deijanira; Nihei, Jorge; Cardillo, Fabíola; Singh, Ram

    2010-01-01

    Increasing evidence implies beneficial effects of angiotensin-converting enzyme (ACE) inhibitors beyond those of their original indications to control hypertension. One of the most attractive non-hemodynamic properties of ACE inhibitors is their ability to regulate cytokine production. The mechanism(s) underlying the role of ACE inhibitors on cytokine synthesis are not well understood but they have traditionally been attributed to the inhibition of angiotensin (Ang) II formation. In fact, it has been extensively demonstrated that ACE inhibitors decrease Ang II-induced production of proinflammatory cytokines and chemokines. However, it is not well described if inhibition of endogenous Ang II generation by ACE inhibitors modulates systemic cytokine production in mice. To verify that, in this work, we investigated the effects of treatment with the ACE inhibitors enalapril and captopril on cytokine synthesis in C57Bl/6 and Balb/c mice. Our results show that enalapril up regulates IL-10 produced by splenocytes from Balb/c and C57Bl/6 mice and captopril increased it only in Balb/c mice. Furthermore, CD4(+)CD103(+) presented increased IL-10 production after enalapril treatment. Enalapril as well as captopril short-term treatment enhanced IL-2 synthesis in Balb/c mice. Besides, enhanced IL-2 and IL-10 levels correlates with increased CD4(+)CD103(+)CD25(negative) T cells numbers in spleens from enalapril-treated mice.

  17. CUSP9* treatment protocol for recurrent glioblastoma: aprepitant, artesunate, auranofin, captopril, celecoxib, disulfiram, itraconazole, ritonavir, sertraline augmenting continuous low dose temozolomide.

    Science.gov (United States)

    Kast, Richard E; Karpel-Massler, Georg; Halatsch, Marc-Eric

    2014-09-30

    CUSP9 treatment protocol for recurrent glioblastoma was published one year ago. We now present a slight modification, designated CUSP9*. CUSP9* drugs--aprepitant, artesunate, auranofin, captopril, celecoxib, disulfiram, itraconazole, sertraline, ritonavir, are all widely approved by regulatory authorities, marketed for non-cancer indications. Each drug inhibits one or more important growth-enhancing pathways used by glioblastoma. By blocking survival paths, the aim is to render temozolomide, the current standard cytotoxic drug used in primary glioblastoma treatment, more effective. Although esthetically unpleasing to use so many drugs at once, the closely similar drugs of the original CUSP9 used together have been well-tolerated when given on a compassionate-use basis in the cases that have come to our attention so far. We expect similarly good tolerability for CUSP9*. The combined action of this suite of drugs blocks signaling at, or the activity of, AKT phosphorylation, aldehyde dehydrogenase, angiotensin converting enzyme, carbonic anhydrase -2,- 9, -12, cyclooxygenase-1 and -2, cathepsin B, Hedgehog, interleukin-6, 5-lipoxygenase, matrix metalloproteinase -2 and -9, mammalian target of rapamycin, neurokinin-1, p-gp efflux pump, thioredoxin reductase, tissue factor, 20 kDa translationally controlled tumor protein, and vascular endothelial growth factor. We believe that given the current prognosis after a glioblastoma has recurred, a trial of CUSP9* is warranted.

  18. Dual influence of spontaneous hypertension on membrane properties and ATP production in heart and kidney mitochondria in rat: effect of captopril and nifedipine, adaptation and dysadaptation.

    Science.gov (United States)

    Ziegelhöffer, A; Mujkošová, J; Ferko, M; Vrbjar, N; Ravingerová, T; Uličná, O; Waczulíková, I; Ziegelhöffer, B

    2012-09-01

    This study deals with changes, induced by hypertension and its treatment, in the function and properties of mitochondria in the heart and kidneys. Male, 16-week-old hypertensive rats were allocated to 3 groups: (i) animals treated daily for 4 weeks with captopril (CAP, 80 mg·(kg body mass)(-1), n = 45), (ii) animals treated with CAP + nifedipine (NIF, 10 mg·kg(-1), n = 45), or (iii) untreated hypertensive controls (n = 96). Wistar rats (n = 96) were used as normotensive controls. Systolic blood pressure (SBP), heart rate (HR), and heart mass / body mass (HW/BW) ratio were measured at the beginning and end of the experiments; measurements for mitochondrial Mg(2+)-ATPase activity, O(2)-consumption (QO(2)), respiratory control index (RCI), ADP/O, oxidative phosphorylation rate (OPR), conjugated diene content (CD), and membrane fluidity (MF) were also taken at different time intervals. In the heart, elevated SBP, HR, and HW/BW accompanied increased QO(2), OPR, and Mg(2+)-ATPase activity, indicating an adaptive response to hypertension-induced increase in the energy demands of the myocardium. Treatments with CAP or with CAP + NIF were very similar in their prevention of increase in SBP, HR, HW/BW, and the rise in OPR (all p NIF was more detrimental than treatment with CAP alone. Heart and kidney mitochondria exhibited negligible changes in CD and moderately increased MF, which was more potentiated by treatment with CAP alone than with CAP + NIF.

  19. 评价卡托普利试验诊断原发性醛固酮增多症的价值%Clinical Value of Captopril Test for Primary Aldosteronism Diagnosis

    Institute of Scientific and Technical Information of China (English)

    王立雪; 母义明; 巴建明; 窦京涛; 吕朝晖; 王先令; 杜锦; 杨国庆; 陆菊明

    2016-01-01

    Objective: To evaluate the clinical value of Captopril test for diagnosing primary aldosteronism (PA) and to calculate the best cut-off point for PA diagnosis. Methods: We retrospectively analyzed 96 PA patients with conifrmed diagnosis by clinical situation, laboratory test and auxiliary examination in our hospital from 1994-06 to 2012-05, and meanwhile, studied 45 highly suspicious PA patients with final exclusion by confirmed diagnosis of primary hypertension (PH). All patients received the in-hospital Captopril test, the area under the curve of receiver operating characteristic (AUCROC) was applied to evaluate plasma aldosterone level and the ratio of aldosterone/renin after Captopril test and to obtain the best cut-off point with the corresponding sensitivity and speciifcity for PA diagnosis. Results: At 1h and 2h after Captopril test, AUCROC for plasma levels of aldosterone were 0.831 and 0.818, the ratios of aldosterone/rennin were 0.909 and 0.922 respectively. At 1h after Captopril test, the cut-off point of aldosterone level was 544.95 pmol/L and the diagnostic sensitivity was 70%, speciifcity was 90.7%; at 2h after Captopril test, the cut-off point of aldosterone level was 466.8 pmol/L and the diagnostic sensitivity was 69.8%, speciifcity was 70.5%. At 1h after Captopril test, the ratio of aldosterone/rennin was 34.6 [ng/dl: μg/(ml·h)] with the sensitivity at 78.3% and speciifcity at 88.4%. At 2h after Captopril test, the maximum AUCROC for the ratio of aldosterone/rennin was obtained, when cut-off point of aldosterone level was 42.2[ng/dl: μg/(ml·h)] , the diagnostic sensitivity was 76.7%, speciifcity was 95.3%. Conclusion: At 1h and 2h after Captopril test, plasma aldosterone level and the ratio of aldosterone/rennin had been valuable for PA diagnosis, the maximum diagnostic value could be obtained at 2h after Captopril test.%目的:评价卡托普利试验对于原发性醛固酮增多症的诊断意义,并计算

  20. Validação de métodos analíticos na quantificação de comprimidos de Captopril - comparação de metodologias para um programa de garantia de qualidade - DOI: 10.4025/actascihealthsci.v26i2.1590 Validation of analytical methods for quantifying captopril in tablets – a comparison of methodologies for a quality control program - DOI: 10.4025/actascihealthsci.v26i2.1590

    Directory of Open Access Journals (Sweden)

    Graciette Matioli

    2004-04-01

    Full Text Available Atualmente, quando todos os caminhos levam à busca da qualidade total, torna-se indispensável conhecer perfeitamente cada fase de um processo produtivo. Neste caso, a validação é a ferramenta adequada para garantir a confiabilidade de instalação de um processo produtivo, de equipamento e, inclusive, da metodologia analítica. Dessa forma, o presente trabalho teve por objetivo analisar os principais aspectos da validação de métodos analíticos na quantificação do captopril. Foi realizada a validação e a comparação dos seguintes métodos: titulométrico por óxido-redução, espectrofotométrico por Folin-Ciocalteau e cromatográfico por cromatografia líquida de alta eficiência - CLAE. Os atributos de exatidão, precisão, linearidade, especificidade e robustez foram estudados para cada metodologia. Os resultados obtidos demonstraram que o método cromatográfico foi o mais adequado para as análises dos comprimidos de Captopril 25 mg, enquanto que os métodos espectrofotométrico e titulométrico demonstraram valores que satisfazem os critérios de aceitação, porém, com maior variabilidade e menor sensibilidade.Nowadays, when all approaches lead to the search for total quality, a thorough knowledge of every stage of a production process is vital. Validation is an appropriate tool to guarantee the reliabilities of: productive process installation, equipment and also analytical methodology. The aim of the present study was to analyze the main aspects of analytical methods validation for quantifying captopril. Validation and comparison of the following methods were carried out: titrimetric for oxide-reduction, spectrophotometry for Folin-Ciocalteau and high-efficiency liquid chromatography - HPLC. The attributes of accuracy, precision, linearity, specificity and robustness were studied for each methodology. The results show that the chromatographic method was the most suitable for Captopril 25 mg tablets evaluation, while the

  1. An improved synthesis of captopril intermediate%卡托普利中间体的制备工艺改进

    Institute of Scientific and Technical Information of China (English)

    周群; 樊学忠; 张倩; 柳恒; 宋新潮

    2009-01-01

    An improved synthetic process of captopril intermediate,D-3-acetylthio-2-methylpropanoyl-L-proline,was carried out using potassium hydroxide and potassium dihydrogen phosphate buffer as a condensating agent.Add potassium dihydrogen phosphate into a raw material of the L-proline,then,drop potassium hydroxide to form potassium hydroxide and potassium dihydrogen phosphate buffer as a condensating agent,the title compound was synthesized by dropping another raw material of 3-acetylthio-2-methyl-propanoyl chloride into above prepared solution.The pH of reaction system keeps in from 7.5 to 8.5,the reaction process is simple and efficient, and the average yield of product was improved from 33% to 39.5%.%使用磷酸氢二钾-氢氧化钾缓冲溶液作为缩合剂,对卡托普利关键中间体D-3-乙酰硫基-2-甲基丙酰-L-脯氨酸的制备工艺进行了改进.反应过程中,加入磷酸氢二钾至L-脯氨酸中,滴加氢氧化钾溶液作缩合剂,形成磷酸氢二钾-氢氧化钾缓冲溶液,然后与3-乙酰硫基-2-甲基丙酰氯缩合,制得标题产物.反应溶液的pH值很容易保持在7.5~8.5,反应平稳,操作简便,产品平均收率由33%提高到39.5%.

  2. 差分脉冲伏安法测定卡托普利%Determination of Captopril by Using Differential Pulse Voltammetry

    Institute of Scientific and Technical Information of China (English)

    杜虹; 刘会; 赵常志

    2011-01-01

    A simple and sensitive electrochemical method was described by using differential pulse voltammetry for the determination of captopril (CPT). The method was based on the adsorption and oxidation of CPT at a gold electrode. The electrochemical behavior of CPT on the electrode was investigated with cyclic voltammetry and differential pulse voltammetry. Under the optimized experimental conditions, the voltammetric response was proportional to the concentration of CPT over the range from 0.217 to 3.04 mg/L with a correlation coefficient of 0. 9991, and the detection limit was estimated to be 0. 152 mg/L at a signal/noise ratio of 3. The relative standard deviation was less than 2.41% (n=5) and the recovery was in the range of 96.5%~101% for the determination of CPT in pharmaceutical samples.%本文基于金电极表面对巯基化合物的吸附作用,提出了一种简便灵敏的测定抗高血压药物卡托普利的新方法.研究了卡托普利在金电极上的伏安响应,优化了差分脉冲伏安法测定卡托普利的实验条件.研究结果表明:在0.217~3.04 mg/L的范围内,卡托普利的氧化峰电流与其浓度呈良好的线性关系,检出限为0.152 mg/L.测定药物中卡托普利的相对标准偏差小于2.41%,加标回收率为96.5%~101%.

  3. Liquid chromatographic method for the simultaneous determination of captopril, piroxicam, and amlodipine in bulk drug, pharmaceutical formulation, and human serum by programming the detector.

    Science.gov (United States)

    Sultana, Najma; Arayne, M Saeed; Ali, Saeeda Nadir

    2013-10-01

    A highly sensitive LC method with UV detection has been developed for the simultaneous determination of coadministered drugs captopril, piroxicam, and amlodipine in bulk drug, pharmaceutical formulations, and human serum at the isosbestic point (235 nm) and at individual λmax (220, 255, and 238 nm, respectively) by programming the detector with time to match the individual analyte's chromophore, which enhanced the sensitivity with linear range. The assay involved an isocratic elution of analytes on a Bondapak C18 (10 μm, 25 × 0.46 cm) column at ambient temperature using a mobile phase of methanol/water 80:20 at pH 2.9 and a flow rate of 1.0 mL/min. Linearity was found to be 0.25-25, 0.10-6.0, and 0.20-13.0 μg/mL with correlation coefficient >0.998 and detection limits of 7.39, 3.90, and 9.38 ng/mL, respectively, whereas calibration curves for wavelength-programmed analysis were 0.10-6.0, 0.04-2.56, and 0.10-10.0 μg/mL with correlation coefficient >0.998 and detection limits of 5.79, 2.68, and 3.87 ng/mL, respectively. All the validated parameters were in the acceptable range. The recovery of drugs was 99.32-100.39 and 98.65-101.96% in pharmaceutical formulation and human serum, respectively, at the isosbestic point and at individual λmax . This method is applicable for the analysis of drugs in bulk drug, tablets, serum, and in clinical samples without interference of excipients or endogenous serum components.

  4. Angiotensin-converting enzyme inhibitors in preventing remodeling and development of heart failure after acute myocardial infarction: results of the German multicenter study of the effects of captopril on cardiopulmonary exercise parameters (ECCE).

    Science.gov (United States)

    Kleber, F X; Sabin, G V; Winter, U J; Reindl, I; Beil, S; Wenzel, M; Fischer, M; Doering, W

    1997-08-04

    Early action of angiotensin-converting enzyme (ACE) inhibitors after myocardial infarction (MI) has been shown in large scale clinical trials to reduce mortality over the first weeks. However, the mechanisms involved are yet unclear and several trials showed a tendency toward a small, albeit unexpected, rise in cardiogenic shock or mortality. Since cardiopulmonary exercise testing (CPX) has become a "gold standard" in assessing the severity of heart failure, we studied--after finishing a pilot trial--the effect of captopril versus placebo in 208 patients who were individually titrated (titrated dose, mean 46/69 mg/day after 7 days/4 weeks, respectively) in order to preserve their blood pressure in the acute phase of myocardial infarction; we followed the development of congestive heart failure (CHF) over 4 weeks by measuring oxygen consumption. After 4 weeks, overall oxygen consumption at the anaerobic threshold (VO2-AT; 13.7 vs 13.1), maximal oxygen consumption (VO2max 19.3 vs 18.9 mL/kg per min) and exercise duration (896 vs 839 sec) showed a nonsignificant difference in favor of the captopril group. The predefined, categorized, combined endpoint of severe heart failure or death (heart failure necessitating ACE inhibition, VO2max 10 patients per 100 treated gained major benefits from this therapy.

  5. 卡托普利治疗急性心肌梗塞早期和长期作用与年龄关系%Relationship between age and effect of early and long-term captopril treatment in patients with acute myocardial infarction

    Institute of Scientific and Technical Information of China (English)

    蔡煦; 沈卫峰; 龚兰生

    2001-01-01

    Abstract:Objective To analyse the relationship between age and treatment with captopril after acute myocardial infarction (AMI).Methods In a randomized trial, 822 patients with a first AMI received conventional medical treatment, including intravenous thrombolytic therapy and oral aspirin or metoprolol, and then were randomly allocated to captopril [dosage from the first 6.25?mg to 25?mg/t.i.d, 209 younger patients (≤64 years), 269 elderly patients (65-75 years)] or conventional treatment only (131 younger patients, 213 elderly). Survival in the four groups was calculated with the Kaplan-Meier method. Multivariate analysis was performed to understand the degree that multi-variables (including age) affect survival in patients taking captopril in the hospital or during long term follow-up.Results The survival of patients who took captopril correlated significantly with age (P0.05) during hospitalization. During follow-up, the survival of patients who took captopril correlated insignificantly with age (P>0.05), but both the elderly and the younger patients have good survival rates (all P0.05);老年治疗组25例,老年对照组52例(9.29% vs. 24.41%,RR=0.37,95%CI: 0.29~0.48;P0.05);老年和年轻治疗组死亡和心性事件均低于相应对照组(P<0.01).结论卡托普利治疗对急性心梗早期作用有年龄差异,对老年患者有明显的有益作用;而长期应用改善预后作用无年龄差异.

  6. 美托洛尔联合卡托普利治疗肺源性心脏病的临床分析%Curative Effect of Metoprolol and Captopril in Cor Pulmonale

    Institute of Scientific and Technical Information of China (English)

    程凡花

    2015-01-01

    Objective To analyze the effect of combined captopril with metoprolol in cor pulmonale.Methods From March 2014 to March 2015,we chose 68 patients with cor pulmonale in our hospital,according to the order of admission parity law,which was divided into a control group(n=34) and observation group(n=34). The control group used metoprolol alone,the observation group used metoprolol combination with captopril. the clinical efficacy and side effects with two groups were compared.Results Observation group the total effective rate was 97.06%,significantly higher than 82.35% in the control group(P 0.05,there was no statisticaly significant difference. Conclusion Using captopril combine with metoprolol treat the cor pulmonale has two advantages that is good clinical curative effect and high safety.%目的:分析联合应用美托洛尔及卡托普利对肺源性心脏病的疗效情况。方法2014年3月~2015年3月选择我院68例肺源性心脏病患者,按照入院顺序奇偶法,将其分为对照组(n=34例)及观察组(n=34例)。对照组单纯应用美托洛尔,观察组联合应用美托洛尔及卡托普利,比较两组临床疗效及副反应发生情况。结果观察组总有效率为88.24%,高于对照组67.65%(P0.05,差异无统计学意义。结论联合应用美托洛尔及卡托普利治疗肺源性心脏病,不仅临床疗效好,而且安全性高。

  7. Effect of captopril on vWF in radiation renal injury%卡托普利对放射性肾损伤中血管性血友病因子的影响

    Institute of Scientific and Technical Information of China (English)

    张银铃; 曹永珍; 张文学; 耿凯; 王克强; 周琰; 毛羽; 魏健; 李素芬

    2013-01-01

    .05).且卡托普利+照射组的大鼠肾脏未出现明显的病理变化.结论 卡托普利能够降低放射性肾损伤大鼠血浆和肾小球中的vWF,并有效地保护了肾脏.%Objective To explore the effect of captopril on plasma and glomerular vWF in radiation renal injury.Methods A total of 96 male SD rats weighing 280-300 g were randomly divided into three groups:control group (n =20),radiation alone group (n =38),captopril + radiation group (n =38).The latter two groups were subjected to a single-dose of 12 Gy 5 MeV electron rays to the kidneys.The captopril + radiation group began to receive captopril at the concentration of 0.38-0.50 mg/ml at 24 h before irradiation.The blood and urine samples were collected in the radiation alone and captopril +radiation groups at 48 h,1,2,4,8,16,24 weeks after irradiation (six rats per time in each group).Except for the 2 weeks after irradiation,kidneys were removed in the two groups at other point in time(six rats per time in each group).The kidneys,blood and urine samples were collected in the control group at 48 h,4,24 weeks after irradiation (six rats per time in each group).The glomerular vWF was detected by immunohistochemistry,collagen deposition in glomeruli by Sirius Red F3B in saturated carbazotic acid stain and plasma vWF and cystatin C levels by ELISA.Roche biochemical automatic analyzer and roche specific reagent were used to examine urine protein and urine creatinine,and urine protein clearance by urine protein and urine creatinine were calculated.The renal morphological feature was observed under light microscope after HE staining.Results In radiation alone group,glomerulus vWF increased gradually at 16 and 24 weeks after irradiation (t =3.53-6.95,5.71-12.66,P < 0.05),collagen deposition in glomerular also gradually increased at 8,16 and 24 weeks after irradiation(t =3.03-5.13,3.48-4.68,4.68-9.03,P < 0.05),and there was an obvious positive correlation between collagen and vWF (r =0.819,P <0

  8. Avaliação do perfil lipídico de pacientes diabéticos e hipertensos tratados com captopril Evaluation of lipid profile in diabetic and hypertensive patients treated with captopryl

    Directory of Open Access Journals (Sweden)

    Fernanda Bernardes Fernandes Santos

    2009-06-01

    Full Text Available INTRODUÇÃO E JUSTIFICATIVA: Doença arterial coronariana (DAC é a principal causa mundial de morte em indivíduos adultos, e como importantes fatores de risco tratáveis envolvidos estão o diabetes mellitus (DM, as dislipidemias e a hipertensão arterial sistêmica (HAS. O tratamento com anti-hipertensivos pode provocar alterações indesejáveis no perfil lipídico, atenuando seus efeitos benéficos antiaterogênicos na redução da pressão arterial (PA. OBJETIVO: Avaliar o perfil lipídico de indivíduos diabéticos tipo 2 com hipertensão essencial tratados somente com captopril ou em combinação com outros anti-hipertensivos, procurando evidenciar a melhora no padrão lipídico destes pacientes, levando a efeito protetor. MATERIAL E MÉTODOS: Foram avaliados níveis de colesterol total (CT, colesterol da lipoproteína de alta densidade (HDL-C, colesterol da lipoproteína de baixa densidade (LDL-C e triglicérides (TG de 140 pacientes encaminhados ao laboratório de análises clínicas da Universidade do Oeste Paulista (UNOESTE, com idade média de 59,7 ± 10,9 anos, de ambos os sexos, portadores de diabetes tipo 2 e hipertensão. O controle glicêmico foi determinado pela dosagem de hemoglobina glicada (HG. Estes pacientes foram subdivididos de acordo com controle metabólico glicêmico (satisfatório ou comprometido em dois grupos: tratados somente com captopril (DC e tratados com combinação captopril e hidroclorotiazida (HCTZ. Dos pacientes com HG 11,2% (não-controlado, DC e HCTZ obtiveram respectivamente níveis de CT (214,3 ± 45,9 e 197 ± 49,5, HDL (35,3 ± 20,5 e 41,5 ± 0,7, LDL (121 ± 43,3 e 116,5 ± 38,9, TG (271,5 ± 175,2 e 194 ± 49,5 e G (232,3 ± 102,9 e 272 ± 53,7, também não havendo diferenças significativas. No entanto, observa-se que, nestes últimos, a combinação do captopril com hidroclorotiazida levou a menores níveis de TG e níveis de HDL ligeiramente elevados, indicando que a associação tem efeito

  9. 阿司匹林对卡托普利引起的咳嗽的逆转作用%Effects of aspirin on captopril-related cough

    Institute of Scientific and Technical Information of China (English)

    余静; 赵锋; 郭雪娅; 阎炜; 李秀丽; 常鹏; 张缤

    2007-01-01

    目的 观察卡托普利相关的咳嗽特点及应用卡托普利、氯沙坦血栓素B2(TXB2)和6-酮前列环素F1α(6-Keto-PGF1α)的变化,并对卡托普利咳嗽者换用氯沙坦或加用阿斯匹林后咳嗽特点进行分析.方法 心血管病患者598例,分为卡托普利组300例和氯沙坦组298例,观察两组咳嗽发生率及咳嗽特点,对56例卡托普利咳嗽者28例改服氯沙坦,另28例加用阿斯匹林.应用放射免疫分析法检测用药前后血、尿TXB2和6-Keto-PGF1α含量.结果 (1)咳嗽发生率在卡托普利组为18.67%,氯沙坦组为1.68%.卡托普利组咳嗽者28例换用氯沙坦后,27例咳嗽停止;另28例加用阿斯匹林300 mg/d后,21.43%咳嗽消失,25%咳嗽减轻;(2)卡托普利咳嗽者血TXB2升高,血、尿中6-Keto-PGF1α下降,TXB2/6-Keto-PGF1α比值增加(均P<0.05);(3)卡托普利咳嗽者,TXB2/6-Keto-PGF1α比值在改服氯沙坦或加阿斯匹林后下降(P<0.05或P<0.01).结论 血栓素和前列环素变化失衡是卡托普利咳嗽的原因之一.卡托普利咳嗽患者可换用氯沙坦,加服阿斯匹林可增加卡托普利在心血管病患者中应用的比例,降低治疗费用.%Objective To investigate the relationships between captopril CT-related cough and thromboxane B2 (TXB2) as well as F1α(6-Keto-PGF1α) and to confirm whether adding aspirin or substituting losartan (LS) to CT can alleviate CT-related cough or not. Methods Five hundred and ninety-eight cases suffered from cardiovascular diseases were divided into CT group and LS group. The symptoms and incidence of the cough were evaluated. LS was used to replace CT in 28 patients with CT-induced cough and aspirin was given to other 28 patients with cough. Contents of TXB2 and 6-Keto-PGF1α in plasma and urine were detected by radioimmunoassay. Results (1) The incidence of the cough was 18.67% in CT group while 1.68% in LS group (P <0.01). Twenty-seven out of 28 patients with CT-induced cough stopped coughing as CT was

  10. 卡托普利联合低分子肝素治疗肾病综合征的临床疗效分析%Analysis of nephrotic syndrome treatment by captopril combined with low molecular heparin

    Institute of Scientific and Technical Information of China (English)

    黄恬

    2014-01-01

    Objective To observe the treatment effect of captopril combined low molecular heparin in nephrot-ic syndrome .Methods Sixty and eight patients with nephrotic syndrome were collected from Chongqing cancer hos-pital ,which were randomly divided into control group and observation group .Conventional treatment were used in the control group ,captopril combined with low molecular heparin were added in the observation group .cholesterol , triglyceride ,urine protein ,whole blood viscosity ,hematocrit ,fibrinogen ,hematocrit of pigeon before and after treat-ment were compared .Results Total effective rate of observation group was 92 .1% ,which was significantly higher than the control group′s 83 .3% ,the difference was statistically significant (P<0 .05) .The observation group′s cho-lesterol ,triglyceride ,urine protein ,whole blood viscosity ,hematocrit ,fibrinogen ,hematocrit of pigeon were significant lower than those of the control group (P<0 .05) .Conclusion On the basis of conventional treatment ,captopril and low molecular heparin could significantly improve curative effect ,renal function and high coagulation state on pa-tients with nephrotic syndrome .%目的:观察卡托普利联合低分子肝素治疗肾病综合征的临床效果。方法选择本院收治的68例肾病综合征患者为研究对象。对照组30例患者,给予常规治疗28 d;观察组38例患者,在常规治疗的基础上给予卡托普利联合低分子肝素治疗28 d。观察并比较两组患者治疗前后胆固醇、三酰甘油、肌酐、清蛋白、尿蛋白、全血高切黏度、全血低切黏度、血浆黏度、血浆纤维蛋白原、血细胞比容等指标变化情况。结果观察组治疗总有效率达92.1%,明显高于对照组的83.3%,比较差异有统计学意义( P<0.05)。治疗28 d后,观察组胆固醇、三酰甘油、尿蛋白、全血黏度、血浆黏度、血浆纤维蛋白原、血细胞比容等指标明显低于对照

  11. 载卡托普利聚(乳酸-羟基乙酸)纳米纤维毡及其释药研究%PLGA Captopril-loaded nanofibers and their in vitro release profiles

    Institute of Scientific and Technical Information of China (English)

    张婳; 娄少峰; 金成成; 聂华丽; 权静; 朱利民

    2012-01-01

    应用静电纺丝技术,以Captopril(CPL)为模型药物,以聚(乳酸-羟基乙酸)(PLGA)为载体高分子材料制备CPL/PLGA载药纳米纤维。探讨了静电纺丝工艺参数,得出最佳较优纺丝条件为原液浓度20%(质量分数),载药量:m(CPL):m/(PLGA)=2:10,电压12.5kV,流速1mL/h,溶剂为V(二氯甲烷):V(丙酮)=2:1。应用扫描电子显微镜(SEM)、傅立叶红外光谱仪(FT-IR)、差示扫描量热仪(DSC)和采用多晶衍射仪(XRD)对所制备的载药纤维进行了表征。体外(Invitro)释药性研究实验结果表明,PLGA载药纳米纤维具有明显的初期突释,随着缓冲溶液pH值增加,初期突释减弱,药物释放度也会随之减弱。%Ultrafine captopril(CPL)-loaded poly(lactic-co-glycolic acid) (PLGA) fibers were successfully pre-pared by electrospinning method from co-dissolving solutions of PLGA and Captopril in dichloromethane (DMC) .acetone(ACT)(2 : 1) that was made as the spinning solutions. The optimal spinning parameters wereobtained that was PLGA 20wt%, m (CPL) : m (PLGA) = 2:10, voltage : 12.5kV, the rate : lmL/h, the ratio of solvent : V(DCM) : V(ACT)=2 : 1. The samples thereby obtained were characterized by scanning electronmicroscopy (SEM), Fourier transform infrared spectroscopy (FT-IR), differential scanning caborimetry) (DSC) and X-ray diffraction (XRD) measurements. In vitro release study showed that a sustained release wasachieved after a burst release at the early stage. The burst release and overall drug was reduced as the pH ofbuffer solution increased.

  12. To Observe the Curative Effect of the Combination of Captopril Tablets and Alprostadil Injection in Treating Diabetic Nephropathy%卡托普利片、前列地尔注射液联合应用治疗糖尿病肾病的疗效观察

    Institute of Scientific and Technical Information of China (English)

    袁峰

    2015-01-01

    目的:探讨卡托普利片联合前列地尔注射液治疗糖尿病肾病临床应用效果。方法对照组在常规治疗基础上加用卡托普利片,研究组在常规治疗基础上加用卡托普利片、前列地尔注射液联合治疗,两组糖尿病肾病患者均持续治疗2周后,记录其临床疗效及不良反应发生情况,将所得资料经专业统计学分析后获得结论。结果两组糖尿病肾病患者治疗前各项肾功能指标对比,P>0.05;两组BUN、UAER、24 h尿蛋白定量、Scr均较之前降低,但研究组改善效果优于对照组, P<0.05;研究组不良反应发生率为17.07%略高于对照组12.20%,P>0.05。结论对糖尿病肾病患者给予卡托普利、前列地尔注射液可提高其疗效,有利于保障患者生活质量及生命安全。%Objective To investigate the captopril tablets combined alprostadil injection clinical effect in treating diabetic nephropathy. Methods Control group in the on the basis of routine treatment with captopril tablets, study group on base of routine treatment plus captopril tablet, alprostadil injection combined with treatment, two groups of patients with diabetic nephropathy (DN) continued to two weeks of treatment, the recorded incidence of the clinical efifcacy and adverse reactions, the income data after statistical analysis professional conclusion. Results Before the renal function indexes were compared with the treatment of two groups of patients with diabetic nephropathy (DN), P>0.05, bun, UAER, 24 h urine protein, SCR were compared to the previous decreased signiifcantly, but the study group was signiifcantly better than that of the control group (P0.05. Conclusion In patients with diabetic nephropathy given captopril, alprostadil injection can signiifcantly improve the therapeutic effects, is conducive to protect the quality of life of patients and life safety.

  13. 氨氯地平联合卡托普利治疗高血压合并冠心病40例%Amlodipine Combination With Captopril Treatment Hypertension With 40 Cases of Coronary Heart Disease

    Institute of Scientific and Technical Information of China (English)

    王谦

    2015-01-01

    Objective To explore the amlodipine in combination withcaptopril combined application effect in patients with coronary heart disease in hypertension. Methods Selected 80 cases of hypertension with coronary heart disease patients of our hospital, according to the different method of treatment were divided into two groups, 40 cases in each group, control group given hydrochlorothiazide tablets, different isosorbide dinitrate and the group of ground treatment, observation group to amlodipine with enalapril therapy, observe the therapeutic effect of two groups. Results The observation group effective rate was 97.5%, the control group was 87.5%, total effective rate of observation group was higher than that of control group, and two groups of systolic pressure, diastolic blood pressure after treatment than before treatment, P<0.05,. had difference statistically signiifcance. Conclusion Amlodipine in combination with captopril in the treatment of hypertension with coronary heart disease can increase the total effective rate, improve the patients' blood pressure.%目的:探究氨氯地平联合卡托普利在高血压合并冠心病患者中的应用效果。方法选取我院收治的高血压合并冠心病患者80例,按照治疗方法的不同分成两组,每组40例,对照组给以氢氯噻嗪片、硝酸异山梨酯片以及尼群地平治疗,观察组给以氨氯地平联合卡托普利治疗,观察两组的治疗效果。结果观察组有效率为97.5%,对照组为87.5%,观察组的治疗总有效率高于对照组,且对比治疗前后两组收缩压、舒张压,P<0.05,差异具有统计学意义。结论氨氯地平联合卡托普利在高血压合并冠心病治疗中能够提高治疗总有效率,改善患者血压。

  14. Captopril Combined urban Tampa Bay Sand Treatment of High Blood Pressure and Improve Left Ventricular Myocardial Hypertrophy Curative Effect Observation%卡托普利联合厄贝沙坦治疗高血压及改善左室心肌肥厚疗效观察

    Institute of Scientific and Technical Information of China (English)

    王泽; 杜莉

    2012-01-01

      目的:观察卡托普利联合厄贝沙坦治疗高血压及改善左室心肌肥厚疗效.方法:选择高血压患者并行心脏彩超(提示左室心肌肥厚)患者118例,给予卡托普利联合厄贝沙坦口服治疗半年,检查血压及心脏彩超,了解左室舒张末期内径(LVDd)、舒张末期室间隔厚度(IVSd)、左室后壁厚度(LVPWd)、及计算左室重量指数(LVMI)评价疗效.结果:高血压患者治疗后收缩压及舒张压明显降低,左室舒张末期内径、舒张末期室间隔厚度、左室后壁厚度、及计算左室重量指数明显改善.治疗前后对比存在统计学意义(P<0.05).结论:卡托普利联合厄贝沙坦治疗高血压有效并明显改善左室心肌肥厚.%  Objective:To observe the captopril combined urban Tampa bay sand treatment of high blood pressure and improve left ventricular myocardial hypertrophy curative effect.Methods: choose hypertension and heart do colour to exceed (hint left ventricular myocardial hypertrophy) patient 118 examples, give captopril combined e bay sand jotham oral treatment half a year, check blood pressure and heart to exceed, understand left ventricular end-diastolic diameter (LVDd), end-diastolic interventricular septum thickness (IVSd), left ventricular posterior wall thickness (LVPWd), and calculation left ventricular mass index (LVMI) assessment of curative effect. Results:After treatment in patients with high blood pressure and diastolic pressure systolic blood pressure significantly, left ventricular end-diastolic diameter, end-diastolic interventricular septum thickness, left ventricular posterior wall thickness, and calculation left ventricular weight index obviously improved. Existing contrast before and after treatment (P < 0.05). Conclusions:captopril combined e bay sand jotham could treat high blood pressure effectively and significantly improve left ventricular myocardial hypertrophy.

  15. 卡托普利早期和长期治疗对老年急性心肌梗死患者生存率的影响%Comparison of the effects of early and long-term captopril treatment on the elderly and younger patients after acute myocardial infarction

    Institute of Scientific and Technical Information of China (English)

    蔡煦; 沈卫峰; 龚兰生

    2001-01-01

    Objective To compare the effects of early and long-term treatment with captopril on clinical outcome between elder patients (65-75 years old) and younger patients (< 64 years old) suffering from acute myocardial infarction (AMI).  Methods In a randomized trial, 822 patients with a first AMI were treated with captopril at initial dosage of 6.25 mg and adjusted to 25 mg t.i.d according to blood pressure (209 younger patients, 269 elder patients) and conventional treatment (131 younger patients, 213 elder patients). Survival rate of the four groups was calculated with Kaplan-Meier method.  Results The survival of treatment group was correlated significantly with age during hospitalization (P=0.0002). Eight patients in younger treatment group and 10 patients in younger control group (3.83% vs 7.63%, P>0.05), 25 patients in elder treatment group and 52 patients in elder control group (9.29% vs 24.41%, relative risk = 0.37, 95% CI 0.29-0.48, P<0.0001) were died. During follow-up period, the survival was however not related to the age (P>0.05), and both the elder and younger patients had better survival (all P<0.01 ) and lower cardiac events (all P<0.01) during captopril treatment.  Conclusions  Captopril exerts less effect on the younger patients but more effect on the elder patients during hospitalization after AMI. Long-term captopril had no difference between the youngers and the elders in prognosis.%目的 比较早期和长期卡托普利治疗对≥65岁和<65岁急性心肌梗死(心梗)患者生存率的影响。 方法 根据是否早期及长期卡托普利治疗,将822例首次心梗72 h内入院患者分为<65岁卡托普利组209例、≥65岁卡托普利组269例,<65岁对照组131例、≥65岁对照组213例。  结果 住院期(1~42 d)<65岁卡托普利组死亡8例(3.83%),<65岁对照组死亡10例(7.63%),差异无显著性(P>0.05);≥65岁卡托普利组死亡25例(9.29%),≥65

  16. Protective effect and mechanism of captopril against endothelial dysfunction of thoracic aortas from atherosclerotic rabbits%卡托普利对动脉粥样硬化家兔血管内皮功能的保护作用及其机制

    Institute of Scientific and Technical Information of China (English)

    徐文娟; 冯梅; 刘丽华; 鲁长武; 熊燕

    2012-01-01

    目的 探讨卡托普利对动脉粥样硬化(AS)家兔血管内皮功能和形态的保护作用及其机制.方法 采用高脂、高胆固醇饲料饲养家兔制备AS模型的同时口服给予卡托普利8 mg·kg-1,每天1次,连续12周;HE染色观察血管组织形态,检测血清总胆固醇(TC)、甘油三酯(TG)、低密度脂蛋白(LDL)和高密度脂蛋白(HDL);高效液相色谱测定血清非对称性二甲基精氨酸(ADMA)浓度;用重组编码人类二甲基精氨酸-二甲胺水解酶2(hDDAH2)基因的腺病毒感染AS家兔离体胸主动脉环2h,检测对乙酰胆碱累积浓度诱导的最大舒张反应(Emax)、半数有效量(EC50)及DDAH活性.结果 与正常组比较,高脂模型家兔胸主动脉内膜和中膜增厚,血清TC,TG和LDL水平升高;血清ADMA浓度升高至(2.24±0.28) μmol·L-1(P<0.01);血管壁DDAH活性降至(0.048±0.007) U· g-1蛋白(P<0.01); Emax降低至(56±8)%(P<0.01),EC50升高至(158±52) nmol·L-1 (P <0.01).与AS模型组比较,卡托普利治疗组血管内膜增厚减轻,血脂无明显降低,血清ADMA浓度显著降低至(1.37 ±0.23) μmol· L-1 (P <0.01),血管DDAH活性增加至(0.084±0.013)U·g-1蛋白(P<0.01),内皮依赖性血管舒张功能改善,Emax增加至(88±4)%(P<0.01),EC50降低至(90±35) nmol·L-1(P<0.01).AS模型血管转染DDAH2基因后,血管Emax回升至(88±4)%,EC50降低至(98±42) nmol·L-1,DDAH活性升高至(0.112 ±0.017)U·g-1蛋白,与卡托普利治疗组相似.结论 卡托普利对AS家兔血管形态和内皮功能具有明显保护作用,其机制可能与增加血管DDAH活性,降低内源性ADMA浓度有关.%OBJECTIVE To investigate the protective effects and mechanisms of captopril against vascular endothelial dysfunction and morphologic damage in atherosclerotic ( AS) rabbits. METHODS The rabbits were fed a high-cholesterol and high-fat diets to induce AS, and at the same time treated with captopril (po 8 mg·kg-1) once daily for 12 week. The

  17. MMP-2和 TIMP-2在多柔比星肾病大鼠中的表达及卡托普利对其影响的研究%MMP-2 and TIMP-2 expression in doxorubicin nephropathy in rats and studied the impact of captopril

    Institute of Scientific and Technical Information of China (English)

    安辉军

    2014-01-01

    Objective To explore the MMP - 2 and TIMP - 2 expression in doxorubicin nephropathy in rats and captopril on the im-pact of nephropathy rats. Method Male SD rats as the research object,through the tail vein injection doxorubicin method nephrotic syn-drome model was established,the control injection of saline solution. In experiment 7,14,28,and 42 days testing rats,24 hours urinary protein level and MMP - 2 and TIMP - 2 levels in serum and kidney tissue were determined by ELISA. And put to death in the rat,kid-ney tissues did light microscope examination,to observe changes in renal morphology of rates. 42 days with the conventional method to de-tect the serum triglyceride(TG),total cholesterol(TC),albumin(propagated),total protein(TP),creatinine(Scr),urea nitrogen ( BUN). Results ①at different times for 24 h urine protein quantitative treatment group was obviously lower,and compared with normal group and model group had significant difference( P﹤ 0. 01). ②total cholesterol,triglycerides,treatment group was obviously lower in different periods at the same time the normal group,model group( P﹤ 0. 01);Albumin,total protein was significantly higher than the lat-ter two( P﹤ 0. 01);Similar creatinine and urea nitrogen content between the 3 groups( P﹥ 0. 05). ③the application in different peri-ods after captopril treatment group serum and kidney tissue concentrations of MMP - 2 and at the same time model group than lower( P﹤0. 01),and 24 h urine protein between quantitative and were positively correlated(r = 0. 859,P﹤ 0. 01 and r = 0. 902,)and TIMP -2 with the model group than higher( P﹤ 0. 01). Conclusion MMP - 2 and TIMP - 2 with nephrotic syndrome( PNS)is closely related to the occurrence and development. Captopril has the effect of degradation of MMP - 2.%目的:探讨MMP-2和TIMP-2在多柔比星肾病大鼠中的表达及卡托普利对其影响。方法:以雄性SD大鼠为研究对象,通过尾静脉注射多柔比星的方法建立肾病

  18. Effects of angiotensin Ⅱ and captopril on outward potassium channel currents in canine atrial myocytes%血管紧张素Ⅱ及卡托普利对犬心房肌细胞外向钾通道电流的作用

    Institute of Scientific and Technical Information of China (English)

    代建军; 李广平; 李健; 许纲; 杨万松

    2009-01-01

    Objective To observe effects of angieminⅡ(AngⅡ)and captopril on outward potassium channel currents in canine atrial myoeytes,and to study mechanisnof Ang II and capupril on atrial arrhythmia.Method Ten healthy adult mongrel dogs(general class),weighing 15 to 20 kg,male and female informality,were provided bythe service centre of Tianjin Li-qun experimental animals.Single canine atrial myotcyte was acutely isolated and whole-cell configtmtion of the patch-clamp tchnique was used to detec trapidly activating delayed reefifier outward K+ current(Ikr),slowly activating delayed recti fier outward K+ current(Iks),ultra-rapidly aetivatin delayed rectifier outward K+ current(Ikur)and transient outward potassium current(Ito)before and after An II and captopril peffion.Software of pClamp 7.0 for windows and pClampfit 7.0 Was used to measure current and data were expressed as mean±standard deviation(x±s).SPSS 10.0 statistical was used for statistical analysis.The paired t test was useel for comparison betwn before and after treatment.P<0.05 was comidered as statistical significance.Results AngII(0.5/mol/L)increased Ikr and Iks,ilfibited Ito[(19.54±2.41)pA/pF vs.(24.83±2.52)pA/pF,P=0.001;(20.69±2.29)pA/pF Vfl.(25.59±3.42)pA/pF,P:0.0003;(6.34±1.93)pA/pF vs.(3.71±1.50)pA/pF,P=0.001)],and had no effect on k[(19.78±1.22 pA/pr Vs.(20.39±1.50)pA/pF,P=0.258)].Captopril(5tot/L)had no significant effect on Ikr.,b.k and[(19.11 4-4.91)pA/pF vs.(18.99 4-4.04)-∥pF,P=0.808;(20.76 4-2.89)pA/pF vs.(20.27 a-3.46)pA/pF,P=0.305;(18.50 4-3.78)pA/pF vs.(18.25 4-4.02)pA/pF,P=0.704;(7.31±1.99)pA/pF vs.(6.89±2.12)pA/pF,P=0.136)].Conclusioas AngⅡmay promote atrial electrical remocof atrial fibrillation through outward potassium currents.As angiotemin-eonverting enzy/ne inhibitor.captioruk can prevent atrial electrical rodding of atrial fibrillation by inhibiting renin-angiotensin-system.%目的 观察血管紧张素Ⅱ(AngⅡ)及卡托普利对犬心房肌细胞外向钾通道电

  19. Effect of captopril on the expression of angiotensin-converting enzyme (ACE)/ ACE2 induced by albumin in human proximal tubular cells%卡托普利对白蛋白引起HK-2细胞ACE/ACE2表达的影响

    Institute of Scientific and Technical Information of China (English)

    高珺; 刘必成; 王艳丽; 李青; 张晓良

    2008-01-01

    目的 观察血管紧张素转换酶抑制剂(ACEI)卡托普利 (captopril, CAP)对白蛋白引起的肾小管上皮细胞表达ACE、 ACE2及其作用产物Ang Ⅱ的影响. 方法实验分组:对照组(未干预的人近端肾小管上皮细胞株,HK-2);牛血清白蛋白(BSA)组(10 mg·ml-1); CAP组(10 μmol·L-1);BSA加CAP组.分别采用实时定量RT-PCR和Western Blot检测ACE、ACE2 mRNA和蛋白的表达水平;采用放射免疫法(RIA)检测细胞上清液中Ang Ⅱ的浓度. 结果实时定量RT-PCR显示,与对照组比较(相对表达量为0), CAP组ACE mRNA表达差异无统计学意义(0.27±0.09 vs 0,P>0.05);CAP能显著抑制BSA引起的ACE mRNA表达上调[(BSA+CAP)组∶BSA组为(0.80±0.05) vs (1.58±0.20),P<0.05].同时,由BSA引起的ACE2 mRNA表达下调作用也被显著抑制[(BSA+CAP)组∶BSA组为(-0.59±0.08) vs (0.24±0.11),P<0.05].Western Blot显示BSA引起的ACE蛋白表达增加被显著抑制[(BSA+CAP)组∶BSA组为(0.85±0.09) vs (1.2±0.10),P< 0.05],而ACE2蛋白表达的减少也明显减轻[(BSA+CAP)组∶BSA组为(0.49±0.09) vs (0.35±0.09),P<0.05].RIA结果显示CAP可显著抑制BSA引起的细胞上清液中Ang Ⅱ浓度增加 [(BSA+CAP)组∶BSA组为(55.25±4.8) vs (97.25±10.4)pg·ml-1,P<0.05]. 结论 CAP可通过抑制ACE和增加ACE2表达而抑制白蛋白所引起的HK-2细胞肾素-血管紧张素系统激活.

  20. 舌下含服硝苯地平缓释片联合卡托普利治疗高血压急症的疗效评价%Efficacy of Sublingual Extended Release Nifedipine Tablets and Captopril Tablets for Treatment of Hypertensive Crisis

    Institute of Scientific and Technical Information of China (English)

    王载芳; 谢跃伟

    2016-01-01

    Objective:To assess the antihypertensive effects of single use of extended release nifedipine(NFP) tablets or Captopril(CTP) tablets and combination of these two drugs .Methods:135 cases of patients with hypertensive Crisis were randomly divided into three group ,each comprised 45 of them .The groups of patients received sublingual NFP or CTP alone served as control group ,with the groups of patients received both NFP and CTP as observation groups .Ob‐serve the changes of blood pressure (systolic blood pressure and diastolic blood pressure) and heart rate at the time be‐fore injection and 5 minutes ,10 minutes ,30 minutes ,1 hour ,2 hours ,4 hours ,6 hours ,8 hours after administration .Re‐sults:In NFP group ,the blood pressure significantly dropped 5minutes after oral ,and reached and maintained the maxi‐mal peak 1 hour after oral ,the total efficacy was 77 .8% ;in CTP group ,the blood pressure significantly dropped 4minutes after oral ,and reached and maintained the maximal peak 1~2 hours after oral ,the total efficacy was 84 .4% ;in the combined use of NFP and CTP group ,the blood pressure significantly dropped 5 minutes after oral ,and reached and maintained the maximal peak 30 minutes~2 hours after oral ,the total efficacy was 93 .3% .Three groups of heart rate has no obvious change(P>0 .05) .The combined use of NFP and CTP produced better effect in decreasing blood pressure than the sole use of NFP or CTP(P<0 .05) .Conclusion:Sublingual extended release NFP tablets and CTP tablets can get ideal antihypertensive effects in time for patients with hypertensive crisis .%目的:评价舌下含服硝苯地平缓释片联合卡托普利治疗高血压急症的降压疗效。方法:将我院收治的高血压急症患者135例随机分成3组,其中舌下含服硝苯地平缓释片组45例,舌下含服卡托普利片45例,同时含服硝苯地平缓释片、卡托普利片45例,观察三组用药前后血压、心率的变化。结果:硝

  1. Análise da prescrição de captopril em pacientes hospitalizados Analysis of the prescription of captopril to hospitalized patients

    OpenAIRE

    Márcio Galvão Oliveira; Antônio Carlos Beisl Noblat; Lúcia Noblat; Luiz Carlos Passos

    2008-01-01

    Uma das complicações mais comuns da hipertensão arterial sistêmica é a crise hipertensiva¹ que se caracteriza por uma elevação sintomática da pressão arterial (PA), com ou sem envolvimento de órgãos-alvo, que pode conduzir a um risco imediato ou potencial de vida2-4. A crise hipertensiva pode se manifestar como emergência ou urgência hipertensiva. Na emergência, há a rápida deterioração de órgãos-alvo e risco imediato de vida, situação que não ocorre na urgência hipertensiva2-4. Além disso, a...

  2. Drug: D10276 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D10276 Mixture, Drug Captopril - hydrochlorothiazide mixt; Capozide (TN) Captopril [DR:D00251], Hydrochlorot...Captopril and diuretics D10276 Captopril - hydrochlorothiazide mixt PubChem: 163312307 ...

  3. Temporary losartan or captopril in young SHR induces malignant hypertension despite initial normotension

    NARCIS (Netherlands)

    Racasan, S; Hahnel, B; van der Giezen, DM; Blezer, EL; Goldschmeding, R; Braam, B; Kriz, W; Koomans, HA; Joles, JA

    2004-01-01

    Background. Exposure of normotensive rats to angiotensin-converting enzyme (ACE) inhibitors in early life causes hypertrophy of intrarenal arteries. Similar defects have been found in knockout mice lacking angiotensinogen, ACE, or angiotensin II type 1 (AT(1)) receptors. On the other hand, transient

  4. Effects of losartan and captopril on left ventricular systolic and diastolic function after acute myocardial infarction

    DEFF Research Database (Denmark)

    Møller, Jacob E; Dahlström, Ulf; Gøtzsche, Ole

    2004-01-01

    BACKGROUND: Angiotensin-converting enzyme inhibitors have been shown to attenuate adverse remodeling after acute myocardial infarction (AMI), and the same has been suggested for angiotensin II type 1 receptor antagonists in animal models. Therefore the aim of the study was to compare the effects...

  5. Edema of epiglottis due to captopril%卡托普利致会厌水肿

    Institute of Scientific and Technical Information of China (English)

    向攀; 王芳; 王宇; 李坪

    2009-01-01

    1例73岁男性患者,高血压病史20余年,服用硝苯地平缓释片、呋噻米、安体舒通及阿司匹林等治疗.后因血压升高,在原治疗药物基础上加用卡托普利12.5 mg,3次/d治疗.服药3 d后,患者出现饮水呛咳、进食困难,伴咳嗽、恶心.胃镜提示会厌水肿明显.停服卡托普利,其他药物继续服用,2 d后患者饮水进食恢复,咳嗽减轻.

  6. Análise da prescrição de captopril em pacientes hospitalizados

    OpenAIRE

    Oliveira,Márcio Galvão; Noblat,Antônio Carlos Beisl; Noblat,Lúcia; Passos,Luiz Carlos

    2008-01-01

    Uma das complicações mais comuns da hipertensão arterial sistêmica é a crise hipertensiva¹ que se caracteriza por uma elevação sintomática da pressão arterial (PA), com ou sem envolvimento de órgãos-alvo, que pode conduzir a um risco imediato ou potencial de vida2-4. A crise hipertensiva pode se manifestar como emergência ou urgência hipertensiva. Na emergência, há a rápida deterioração de órgãos-alvo e risco imediato de vida, situação que não ocorre na urgência hipertensiva2-4. Além disso, a...

  7. 旋光法测定卡托普利片的含量%Determination of captopril tablets by polarimetry

    Institute of Scientific and Technical Information of China (English)

    汪杰

    2001-01-01

    目的:建立一种测定卡托普利片含量的方法.方法:运用旋光法测定.结果:浓度在5~30 mg.ml-1范围内与旋光度呈线性关系,平均回收率99.9%,RSD为0.4%.结论:本法简便、快捷、准确,适用于该制剂的含量测定.

  8. COMPARATIVE EFFECTS OF LOSARTAN AND CAPTOPRIL ON VENTRICULAR REMODELING AND FUNCTION AFTER MYOCARDIAL INFARCTION IN THE RAT

    Institute of Scientific and Technical Information of China (English)

    张高星; 沈学东; 浦寿月; 杨英珍; 潘文明; 陈灏珠

    1998-01-01

    Objective. To determine the effecm of losarcan and captoptil treatment on ventricular remodeling and function after myocardial infarction in rats. Methods. Thirty-two rats with MI induced by coxortary llgation after seven days were divided into four groups randomly and treated with eaptopri1(2 g. liter-1 , group A), loaartan(10mg. kg-1. d-1 , group B),losartsn(30 rag. kg-l.d-l,group C) and placebo (no drug,group D) for six weeks, respectively. Shamoperated rats(group E)served as ccmtrols. Echccardiography was performed at 1 and 7 weeks after MI, respectively. Results. Compared with the results before treazment,both LV end-diastollc inzemal diameter and volume decreased significantly and the thickened posterior wall was reversed in group A, B and C; the peak early filling velocity decreased whereas the peak velocity was increased in these three groulm. There are no significant difference among the three treated groups. However ,LV end-diastolic interned diameter and the E/A were still increasnd,whereas the thickness of anterior wall and the peak velocity of LV outflow were decreased in group A,B,and C after treatment comparing with group E. Conclusion. Both angiotensin converting enzyme inhibitor and angiotensin I receptor antagonist can prevent the ventricular remodeling and improve the ventricular function.

  9. Clonidine versus captopril for treatment of postpartum very high blood pressure: study protocol for a randomized controlled trial (CLONCAP)

    OpenAIRE

    2013-01-01

    Background The behavior of arterial blood pressure in postpartum of women with hypertension and pregnancy and the best treatment for very high blood pressure in this period still need evidence. The Cochrane systematic review assessing prevention and treatment of postpartum hypertension found only two trials (120 patients) comparing hydralazine with nifedipine and labetalol for the treatment of severe hypertension and did not find enough evidence to know how best to treat women with hypertensi...

  10. The effect of valsartan, captopril, or both on atherosclerotic events after acute myocardial infarction: an analysis of the Valsartan in Acute Myocardial Infarction Trial (VALIANT)

    DEFF Research Database (Denmark)

    McMurray, John; Solomon, Scott; Pieper, Karen;

    2006-01-01

    OBJECTIVES: We attempted to compare the effect of an angiotensin-converting enzyme (ACE) inhibitor and angiotensin receptor blocker (ARB) on atherosclerotic events. BACKGROUND: Angiotensin-converting enzyme inhibitors and ARBs interrupt the renin-angiotensin system by distinct mechanisms. It is n...

  11. HOW ADVERSE DRUG-REACTIONS CAN PLAY A ROLE IN INNOVATIVE DRUG RESEARCH - SIMILARITIES IN ADVERSE DRUG REACTION PROFILES OF CAPTOPRIL AND PENICILLAMINE

    NARCIS (Netherlands)

    RIKKEN, F; VOS, R

    1995-01-01

    We describe how adverse drug reactions (ADRs) can play an important role in pharmaceutical research and drug development. Not only do ADRs represent the risks and drawbacks associated with drugs but they can also be related to other knowledge available in pharmaceutical and medical research. We offe

  12. Effect of left ventricular remodeling after acute myocardial infarction in early stage using captopril in combination with metoprolol and single captopril%卡托普利联合美托洛尔对急性心肌梗死早期左室重构的影响

    Institute of Scientific and Technical Information of China (English)

    谢晓春; 邢淑慧; 王莹威

    2002-01-01

    目的:探讨急性心肌梗死(AMI)后早期应用卡托普利联合美托洛尔与单用卡托普利对左室重构的不同影响.方法:62例AMI患者随机分成治疗组(卡托普利联合美托洛尔)30例和对照组(单用卡托普利)32例,采用彩色多普勒心动超声仪,分别于发病后1,2,3 wk连续测量并计算左室形态、构型等多项指标.结果:2组AMI患者中,对照组左室形态和构型变化比治疗组显著加重(P<0.05),且从1 wk到3 wk呈进行性加重,wk 3最明显.结论:在AMI早期,卡托普利联合美托洛尔对左室重构的抑制作用明显优于单用卡托普利.

  13. Perindopril

    Science.gov (United States)

    Prestalia® (as a combination product containing Amlodipine, Perindopril) ... perindopril, angiotensin-converting enzyme (ACE) inhibitors such as benazepril (Lotensin, in Lotrel), captopril (Capoten), enalapril (Vasotec, in ...

  14. Estudo de equivalÃncia farmacÃutica dos fÃrmacos captopril e cloridrato de propranolol comercializados no programa farmÃcia popular do brasil.

    OpenAIRE

    AndrÃa Vieira Pontes Rohleder

    2009-01-01

    A equivalÃncia farmacÃutica entre dois medicamentos relaciona-se à comprovaÃÃo de que ambos contÃm o mesmo fÃrmaco na mesma dosagem e forma farmacÃutica, o que pode ser avaliado por meio de testes in vitro. No Brasil, os medicamentos alopÃticos sÃo divididos em trÃs categorias quanto ao registro junto à AgÃncia Nacional de VigilÃncia SanitÃria: medicamentos novos, medicamentos similares e medicamentos genÃricos. A legislaÃÃo atual dispÃe que para o registro de novos medicamentos genÃricos e s...

  15. 基于含氟表面活性剂修饰的金纳米粒子测定卡托普利%Detection of captopril via fluorosurfactant-capped gold nanoparticles

    Institute of Scientific and Technical Information of China (English)

    张楠; 张丽娟; 吕超

    2010-01-01

    在较高离子强度和一定温度下,卡托普利能引起非离子表面活性剂FSN-lOC修饰的14nm金纳米粒子胶体溶液快速聚集,引起金纳米粒子在519nm处的吸光度降低,而在640nm处的相对吸光度成线性增加.据此,建立了一种光度测定卡托普利的新方法.卡托普利药片制剂中常见赋形剂,如淀粉、糊精、葡萄糖、果糖、麦芽糖、蔗糖、明胶、山梨醇、乳糖等对本实验没有干扰.本方法具有快速、简便、选择性高等优点,线性范围为2.012.5μg/mL,卡托普利检出限((S/N=3)为1.25μg/mL.该方法成功用于药片制剂中卡托普利的测定,回收率在99%到103%之间.

  16. 卡托普利和依那普利对血管平滑肌细胞内钙的影响%Effects of captopril and enalapril on intracellular Ca2 + in vascular smooth muscle cell

    Institute of Scientific and Technical Information of China (English)

    齐建华; 章鲁; 王军; 魏丕敬; 顾培坤; 金正均; 黄明智; 王弘远

    1996-01-01

    To determine whether angiotensin-converting enzyme inhibitors can affect Ca2+ handling in cultured aortic smooth muscle cells (ASMC) directly.METHODS: Cultured ASMC derived from rat aorta were loaded with the intracellular Ca2+ ([Ca]i2+)fluorescent indicator Fura 2-AM and digital image processing technique was used. RESULTS: Resting [ Ca2 + ]i was greater in ASMC from SHR vs WKY(P < 0.01 ). KCl-, norepinephrine (NE)-,and angiotensin Ⅱ (Ang)- induced [ Ca2 + ] i increases were enhanced in ASMC of SHR vs WKY (220± 6, 212 ± 8, and 215 ± 14 vs 199 ± 6, 202 ± 7,(Cap) and enalapril (Ena) had no inhibitory effect on KCl-, NE-, and Ang-induced [Ca2+ ]i increases in ASMC of WKY. Cap and Ena inhibited KCl-,NE-, and Ang-increased [Ca2+ ]i in ASMC of SHR tively). Ena and nifedipine similarly decreased KCl-, NE-, and Ang-increased [Ca2+ ]i. CONCLUSION: Cap blocked KCl-, NE-, and Angincreased ([ Ca2+ ]i) via a voltage-dependent Ca2+channel of which function and specificity was altered in ASMC of SHR.%检测ACE抑制剂对主动脉平滑肌细胞内Ca2+的影响.方法:用荧光标计和图象处理技术结果:SHR细胞内Ca2+以及KCl,NE和Ang在SHR细胞引起的Ca2+增加多于WKY细胞.Cap和Ena不影响KCl和Ang在WKY细胞的作用,但Cap,Ena和Nif抑制KCl,NE和Ang在SHR细胞的作用.结论:Cap和Ena阻断功能和特异性已改变的电压依赖性钙通道.

  17. Comparison between Effects of Captopril and Terazosin on Patients with Hypertensive Left Ventricular Hypertrophy%卡托普利与特拉唑嗪对高血压病左室肥厚逆转作用的比较

    Institute of Scientific and Technical Information of China (English)

    李青; 齐连荣; 王茹; 郑燕; 王树亮

    2002-01-01

    目的了解卡托普利与特拉唑嗪对高血压病伴左室肥厚(LVH)的疗效.方法 将来院就诊符合原发性高血压并经超声心动图检测符合LVH的病人,随机分为卡托普利组(C组,n=32,服卡托普利25~100 mg/d)及特拉唑嗪组(T组,n=27,服特拉唑嗪3~10 mg/d),单服上述药物之一维持血压<140/90 mmHg,1年后复检超声心动图 ,计算左室重量指数(LVMI).结果 经分别比较两组治疗前后的LVMI[C组:(148.99±31.66)g与(132.47±26.15)g;T组:(146.41±28.94)g与(141.58±28.81)g]均有显著性差异(P<0.001),另比较两组治疗后LVMI[(132.47±26.15)g与(141.58±28.81)g]也有显著性差异(P<0.005).结论 用卡托普利或特拉唑嗪在达到有效降压的同时,可以显示出逆转LVH的作用,而前者此作用更强.

  18. 不同厂家复方卡托普利片分剂量的评价%Evaluation on Splitting Captopril/Hydrochlorothiazide Tablets Produced by Different Manufacturers

    Institute of Scientific and Technical Information of China (English)

    刘元江; 缪经纬; 邓欣

    2012-01-01

    目的 评价不同厂家复方卡托普利片分剂量的合理性,为临床用药提供参考.方法 将整个药片掰成两个半片,比较A、B厂复方卡托普利片分剂量准确性、重量损失百分比、半片脆碎度、半片含量均匀度及半片与整片的溶出行为.结果 A厂复方卡托普利片除含量均匀度外,其余评价指标均符合有关规定,B厂除重量损失百分比外,其余均不符合规定.结论 A厂、B厂复方卡托普利片均不适合分剂量.

  19. ACE inhibition is superior to angiotensin receptor blockade for renography in renal artery stenosis

    Energy Technology Data Exchange (ETDEWEB)

    Karanikas, Georgios; Becherer, Alexander; Wiesner, Karoline; Dudczak, Robert; Kletter, Kurt [Department of Nuclear Medicine, University of Vienna (Austria)

    2002-03-01

    Angiotensin converting enzyme (ACE) inhibitors as well as angiotensin II receptor antagonists are able to prevent the vasoconstrictive effect of angiotensin II on the efferent renal vessels, which is believed to play an important role in renovascular hypertension. This effect is assumed to be essential for the demonstration of renovascular hypertension by captopril renography. In this study, renographic changes induced by captopril and the AT1 receptor antagonist valsartan were compared in patients with a high probability for renovascular hypertension. Twenty-five patients with 33 stenosed renal arteries (grade of stenosis >50%) and hypertension were studied. Captopril, valsartan and baseline renography were performed within 48 h using technetium-99m mercaptoacetyltriglycine. Blood pressure was monitored, plasma renin concentration before and after intervention was determined and urinary flow was estimated from the urinary output of the hydrated patients. Alterations in renographic curves after intervention were evaluated according to the Santa Fe consensus on ACE inhibitor renography. Captopril renography was positive, indicating renovascular hypertension, in 25 of the 33 stenosed vessels, whereas valsartan renography was positive in only ten. Blood pressure during captopril and valsartan renography was not different; reduction in blood pressure was the same after valsartan and captopril. Plasma renin concentration was comparable for valsartan and captopril studies, showing suppressed values after intervention in as many as 12 of the 25 patients. Urinary flow after valsartan was higher than after captopril (P<0.05). However, this difference could not explain the markedly higher sensitivity of captopril compared with valsartan in demonstrating renal artery stenosis. In 14 of the 25 patients, blood pressure response to revascularisation was monitored, showing a much better predictive value for captopril renography. It is concluded that captopril renography is much

  20. Heart failure

    Institute of Scientific and Technical Information of China (English)

    1992-01-01

    920647 Comparative effects of commonvasodilators on experimental cardiac fai-lure. LI Zhijian (李志坚), et al. Dept Cardiol,2nd Hosp, Tianjin Med Coll. Tianjin Med J1992; 20(8): 456-458. A 9×9 latin square design was employed forcomparing the effects of (1) placebo, (2) nitr-oprusside, (3) phentolamine, (4) isosorbide dini-trate. (5) captopril, (6) captopril-isosorbide

  1. Hypertension and Cardiovascular Remodelling in Rats Exposed to Continuous Light: Protection by ACE-Inhibition and Melatonin

    Directory of Open Access Journals (Sweden)

    Fedor Simko

    2014-01-01

    Full Text Available Exposure of rats to continuous light attenuates melatonin production and results in hypertension development. This study investigated whether hypertension induced by continuous light (24 hours/day exposure induces heart and aorta remodelling and if these alterations are prevented by melatonin or angiotensin converting enzyme inhibitor captopril. Four groups of 3-month-old male Wistar rats (10 per group were treated as follows for six weeks: untreated controls, exposed to continuous light, light-exposed, and treated with either captopril (100 mg/kg/day or melatonin (10 mg/kg/day. Exposure to continuous light led to hypertension, left ventricular (LV hypertrophy and fibrosis, and enhancement of the oxidative load in the LV and aorta. Increase in systolic blood pressure by continuous light exposure was prevented completely by captopril and partially by melatonin. Both captopril and melatonin reduced the wall thickness and cross-sectional area of the aorta and reduced the level of oxidative stress. However, only captopril reduced LV hypertrophy development and only melatonin reduced LV hydroxyproline concentration in insoluble and total collagen in rats exposed to continuous light. In conclusion, captopril prevented LV hypertrophy development in the continuous light-induced hypertension model, while only melatonin significantly reduced fibrosis. This antifibrotic action of melatonin may be protective in hypertensive heart disease.

  2. 卡托普利联合美托洛尔对急性心肌梗死晚期左心室重构的影响%Effect of captopril combined with metoprolol on left ventricular remodeling after acute myocardial infarction

    Institute of Scientific and Technical Information of China (English)

    谢晓春; 杨军珂; 丁力平; 梁明; 白玉蓉; 刘胜林; 赵贵峰

    2006-01-01

    目的 探讨急性心肌梗死(AMI)后应用卡托普利联合美托洛尔治疗与单用卡托普利治疗对晚期左心室重构的影响.方法 将121例AMI患者随机分成治疗组(卡托普利联合美托洛尔)63例和对照组(卡托普利)58例,采用彩色多普勒心动超声仪分别于发病后早期(<24h)、3、6个月末连续随访并测量、计算左心室形态、构型等多项指标.结果 进行治疗组早期到6个月末前后比较,左心室形态均呈逐渐扩大,6个月末最大,对照组扩大程度更明显.对照组与治疗组同期对应比较,左心室形态逐渐扩大,6个月末最明显,且差异有显著性意义.同时左心室射血分数同组和两组间对应比较,均有明显改善(P<0.05,P<0.01).结论 AMI后应用卡托普利联合美托洛尔对晚期左心室重构的抑制作用明显优于单用卡托普利.

  3. 急性前壁心肌梗死早期使用倍他乐克或卡托普利61例分析%Analysis of 61 Cases with acute anterior myocardial infarction treated early by metoprolol or captopril

    Institute of Scientific and Technical Information of China (English)

    郝世同

    2009-01-01

    目的 观察倍他受体阻滞剂和ACE抑制剂对急性心肌梗死患者心肌的保护作用.方法 采用随机、双盲对照的方法.对61例急性前壁心肌梗死患者早期应用倍他乐克或卡托普利治疗进行观察.结果 这两种药物显示.平均血压降低相似.但是,只有倍他乐克治疗的患者.在早期心率显著降低.参照基线,分别在1周后和4周后,通过超声心动图观察心室舒张量,评估结果如下:卡托普利组58±14与64士19(P<0.05)和65±21ml/m2(P<0.05),倍他乐克组58±18与64士18(P

  4. Effects of Terazosin and Captopril on The Left Ventricular Remodeling of SCHF%特拉唑嗪和卡托普利对慢性充血性心力衰竭病人左室重塑的影响对比

    Institute of Scientific and Technical Information of China (English)

    周应红; 金兰惠; 韩小容

    2003-01-01

    目的对比α受体拮抗剂和血管紧张素转换酶抑制剂(ACEI)对慢性充血性心力衰竭病人(SCHF)心室重塑的影响.方法将CHF165人随机分为对照组55例、特拉唑嗪组55例和依拉普利组55例,于治疗前后进行UCG检查,测定心率(P)、平均动脉压(MAP)、心排量(SV)、左室射血分数(LVEF)、心输出量(CO)、心脏指数(CI)、室间隔厚度(LVST)、左室后壁厚度(LVPWT)、左室舒张末内径(LVDd),计算左室心肌重量指数(LVMI),了解二者对心室重塑的阻抑作用.结果特拉唑嗪组、卡托普利组与对照组比较,除了心率、平均动脉压无显著性差异外,SV、LVEF、CO、CI均明显升高(P<0.05),LVPWT、IVST、LVDd、LVMI均明显降低(P<0.05),而特拉唑嗪组和卡托普利组的各参数,在治疗前后无显著性差异.结论α受体拮抗剂能抑制慢性充血性心力衰竭病人的左室重塑过程,改善左室功能,其效果与卡托普利相近.

  5. 卡托普利与氯沙坦合用对冠心病人血清细胞因子水平的影响%Effects of captopril and losartan on the level of plasma cytokines in coronary heart disease patients

    Institute of Scientific and Technical Information of China (English)

    梁绪国; 潘其兴

    2002-01-01

    目的: 探讨卡托普利和氯沙坦对冠心病人血清细胞因子含量的影响.方法: 用放免方法和酶联免疫吸附法测定了患者血清肿瘤坏死因子-α(TNF-α)、转化生长因子-β(TGF-β)、白细胞介素-6(IL-6)、白细胞介素-8(IL-8)及可溶性白介素2受体(sIL-2R)水平的变化.结果: 患者应用药物后,体内的TNF-α明显降低,TGF-β显著升高,IL-6、IL-8、sIL-2R亦降低,与对照组比较有显著差异. 结论: 卡托普利与氯沙坦对冠心病人细胞因子水平有一定的调节作用,其对动脉粥样硬化的防治可能与对细胞因子的调节作用有关.

  6. Exercise testing in hypertensive patients taking different angiotensin-converting enzyme inhibitors

    Directory of Open Access Journals (Sweden)

    Maria Angela M. Q. Carreira

    2003-02-01

    Full Text Available OBJECTIVE: To compare blood pressure response to dynamic exercise in hypertensive patients taking trandolapril or captopril. METHODS: We carried out a prospective, randomized, blinded study with 40 patients with primary hypertension and no other associated disease. The patients were divided into 2 groups (n=20, paired by age, sex, race, and body mass index, and underwent 2 symptom-limited exercise tests on a treadmill before and after 30 days of treatment with captopril (75 to 150 mg/day or trandolapril (2 to 4 mg/day. RESULTS: The groups were similar prior to treatment (p<0.05, and both drugs reduced blood pressure at rest (p<0.001. During treatment, trandolapril caused a greater increase in functional capacity (+31% than captopril (+17%; p=0.01 did, and provided better blood pressure control during exercise, observed as a reduction in the variation of systolic blood pressure/MET (trandolapril: 10.7±1.9 mmHg/U vs 7.4±1.2 mmHg/U, p=0.02; captopril: 9.1±1.4 mmHg/U vs 11.4±2.5 mmHg/U, p=0.35, a reduction in peak diastolic blood pressure (trandolapril: 116.8±3.1 mmHg vs 108.1±2.5 mmHg, p=0.003; captopril: 118.2±3.1 mmHg vs 115.8±3.3 mmHg, p=0.35, and a reduction in the interruption of the tests due to excessive elevation in blood pressure (trandolapril: 50% vs 15%, p=0.009; captopril: 50% vs 45%, p=0.32. CONCLUSION: Monotherapy with trandolapril is more effective than that with captopril to control blood pressure during exercise in hypertensive patients.

  7. Epoxyeicosatrienoic acid analogue mitigates kidney injury in a rat model of radiation nephropathy.

    Science.gov (United States)

    Hye Khan, Md Abdul; Fish, Brian; Wahl, Geneva; Sharma, Amit; Falck, John R; Paudyal, Mahesh P; Moulder, John E; Imig, John D; Cohen, Eric P

    2016-04-01

    Arachidonic acid is metabolized to epoxyeicosatrienoic acids (EETs) by CYP epoxygenases, and EETs are kidney protective in multiple pathologies. We determined the ability of an EET analogue, EET-A, to mitigate experimental radiation nephropathy. The kidney expression of the EET producing enzyme CYP2C11 was lower in rats that received total body irradiation (TBI rat) compared with non-irradiated control. At 12 weeks after TBI, the rats had higher systolic blood pressure and impaired renal afferent arteriolar function compared with control, and EET-A or captopril mitigated these abnormalities. The TBI rats had 3-fold higher blood urea nitrogen (BUN) compared with control, and EET-A or captopril decreased BUN by 40-60%. The urine albumin/creatinine ratio was increased 94-fold in TBI rats, and EET-A or captopril attenuated that increase by 60-90%. In TBI rats, nephrinuria was elevated 30-fold and EET-A or captopril decreased it by 50-90%. Renal interstitial fibrosis, tubular and glomerular injury were present in the TBI rats, and each was decreased by EET-A or captopril. We further demonstrated elevated renal parenchymal apoptosis in TBI rats, which was mitigated by EET-A or captopril. Additional studies revealed that captopril or EET-A mitigated renal apoptosis by acting on the p53/Fas/FasL (Fas ligand) apoptotic pathway. The present study demonstrates a novel EET analogue-based strategy for mitigation of experimental radiation nephropathy by improving renal afferent arteriolar function and by decreasing renal apoptosis.

  8. Angiotensin Converting Enzyme (ACE) Inhibitor Extends Caenorhabditis elegans Life Span.

    Science.gov (United States)

    Kumar, Sandeep; Dietrich, Nicholas; Kornfeld, Kerry

    2016-02-01

    Animal aging is characterized by progressive, degenerative changes in many organ systems. Because age-related degeneration is a major contributor to disability and death in humans, treatments that delay age-related degeneration are desirable. However, no drugs that delay normal human aging are currently available. To identify drugs that delay age-related degeneration, we used the powerful Caenorhabditis elegans model system to screen for FDA-approved drugs that can extend the adult lifespan of worms. Here we show that captopril extended mean lifespan. Captopril is an angiotensin-converting enzyme (ACE) inhibitor used to treat high blood pressure in humans. To explore the mechanism of captopril, we analyzed the acn-1 gene that encodes the C. elegans homolog of ACE. Reducing the activity of acn-1 extended the mean life span. Furthermore, reducing the activity of acn-1 delayed age-related degenerative changes and increased stress resistance, indicating that acn-1 influences aging. Captopril could not further extend the lifespan of animals with reduced acn-1, suggesting they function in the same pathway; we propose that captopril inhibits acn-1 to extend lifespan. To define the relationship with previously characterized longevity pathways, we analyzed mutant animals. The lifespan extension caused by reducing the activity of acn-1 was additive with caloric restriction and mitochondrial insufficiency, and did not require sir-2.1, hsf-1 or rict-1, suggesting that acn-1 functions by a distinct mechanism. The interactions with the insulin/IGF-1 pathway were complex, since the lifespan extensions caused by captopril and reducing acn-1 activity were additive with daf-2 and age-1 but required daf-16. Captopril treatment and reducing acn-1 activity caused similar effects in a wide range of genetic backgrounds, consistent with the model that they act by the same mechanism. These results identify a new drug and a new gene that can extend the lifespan of worms and suggest new

  9. Mitigation of Late Renal and Pulmonary Injury After Hematopoietic Stem Cell Transplantation

    Energy Technology Data Exchange (ETDEWEB)

    Cohen, Eric P., E-mail: Eric.Cohen2@va.gov [Department of Medicine, Medical College of Wisconsin, Milwaukee, Wisconsin (United States); Bedi, Manpreet; Irving, Amy A. [Department of Radiation Oncology, Medical College of Wisconsin, Milwaukee, Wisconsin (United States); Jacobs, Elizabeth; Tomic, Rade [Department of Medicine, Medical College of Wisconsin, Milwaukee, Wisconsin (United States); Klein, John [Department of Biostatistics, Medical College of Wisconsin, Milwaukee, Wisconsin (United States); Lawton, Colleen A.; Moulder, John E. [Department of Radiation Oncology, Medical College of Wisconsin, Milwaukee, Wisconsin (United States)

    2012-05-01

    Purpose: To update the results of a clinical trial that assessed whether the angiotensin-converting enzyme inhibitor captopril was effective in mitigating chronic renal failure and pulmonary-related mortality in subjects undergoing total body irradiation (TBI) in preparation for hematopoietic stem cell transplantation (HSCT). Methods and Materials: Updated records of the 55 subjects who were enrolled in this randomized controlled trial were analyzed. Twenty-eight patients received captopril, and 27 patients received placebo. Definitions of TBI-HSCT-related chronic renal failure (and relapse) were the same as those in the 2007 analysis. Pulmonary-related mortality was based on clinical or autopsy findings of pulmonary failure or infection as the primary cause of death. Follow-up data for overall and pulmonary-related mortality were supplemented by use of the National Death Index. Results: The risk of TBI-HSCT-related chronic renal failure was lower in the captopril group (11% at 4 years) than in the placebo group (17% at 4 years), but this was not statistically significant (p > 0.2). Analysis of mortality was greatly extended by use of the National Death Index, and no patients were lost to follow-up for reasons other than death prior to 67 months. Patient survival was higher in the captopril group than in the placebo group, but this was not statistically significant (p > 0.2). The improvement in survival was influenced more by a decrease in pulmonary mortality (11% risk at 4 years in the captopril group vs. 26% in the placebo group, p = 0.15) than by a decrease in chronic renal failure. There was no adverse effect on relapse risk (p = 0.4). Conclusions: Captopril therapy produces no detectable adverse effects when given after TBI. Captopril therapy reduces overall and pulmonary-related mortality after radiation-based HSCT, and there is a trend toward mitigation of chronic renal failure.

  10. Effects of a novel ACE inhibitor, 3-(3-thienyl)-l-alanyl-ornithyl-proline, on endothelial vasodilation and hepatotoxicity in l-NAME-induced hypertensive rats.

    Science.gov (United States)

    Seth, Mahesh Kumar; Hussain, M Ejaz; Pasha, Santosh; Fahim, Mohammad

    2016-01-01

    Nitric oxide (NO) is a widespread biological mediator involved in many physiological and pathological processes, eg, in the regulation of vascular tone and hypertension. Chronic inhibition of NO synthase by N(G)-nitro-l-arginine methyl ester (l-NAME) hydrochloride results in the development of hypertension accompanied by an increase in vascular responsiveness to adrenergic stimuli. Recently, we developed a novel sulfur-containing angiotensin-converting enzyme inhibitor: 3-(3-thienyl)-l-alanyl-ornithyl-proline (TOP). Our previous studies indicated a superior nature of the molecule as an antihypertensive agent in spontaneously hypertensive rats (showing the involvement of renin-angiotensin-aldosterone system) in comparison to captopril. The aim of the present study was to investigate the effect of TOP on NO pathway in l-NAME-induced hypertensive rats, and captopril was included as the standard treatment group. Treatment with both TOP (20 mg/kg) and captopril (40 mg/kg) prevented the development of hypertension in l-NAME model, but TOP showed better restoration of NO and normal levels of angiotensin-converting enzyme. In addition, in vitro vasorelaxation assay showed an improvement in endothelium-dependent vasodilation in both the cases. Further, the biochemical (malondialdehyde, alanine aminotransferase, and aspartate aminotransferase) and the histopathological effects of TOP on rat liver tissues revealed a protective nature of TOP in comparison to captopril in the l-NAME model. In conclusion, TOP at 50% lesser dose than captopril was found to be better in the l-NAME model.

  11. Renovascular hypertension due to insufficient collateral flow in segmental artery occulusion

    Energy Technology Data Exchange (ETDEWEB)

    Park, Y. H.; Lee, S. Y.; Kim, S. H.; Sohn, H. S.; Chung, S. K. [College of Medicine, The Catholic Univ. of Korea, Seoul (Korea, Republic of)

    2001-07-01

    We report a case in which a 33-year-old woman with renovascular hypertension due to insufficient collateral flow in segmental renal artery occlusion demonstrated abnormality on captopril renal scintigram. Baseline renal scintigram with DTPA showed normal perfusion and excretion in left kidney and captopril renal scintigram with DTPA showed a focal area of decreased perfusion and delayed clearance in lower half of left kidney, suggesting segmental renal artery stenosis. Selective left renal arteriography showed complete obstruction in proximal portion of anterior segmental artery with multiple small collateral vessels from posterior segmental artery and capsular artery and delayed opacification in lower half of left kidney. These findings are suggestive of segmental hypoperfusion due to insufficient collateral blood flow resulting to positive captopril response. Patient's blood pressure have been controlled well with ACE (angiotensin converting enzyme) inhibitor and calcium channel blocker for 2 year. Follow-up baseline renal scintigram with MAG3 showed normal perfusion and excretion in left kidney and captopril renal scintigram with MAG3 showed a focal area of decreased perfusion and delayed clearance in lower lateral portion of left kidney, which was smaller size than that of previous renal scintigram. And captopril renal scintigram with DMSA demonstrated a small area of decreased DMSA uptake on this lesion compared to baseline DMSA scintigram.

  12. Evaluation of Medical Cystine Stone Prevention in an Animal Model

    Science.gov (United States)

    Sagi, Sreedhar; Wendt-Nordahl, Gunnar; Alken, Peter; Knoll, Thomas

    2007-04-01

    Medical treatment for cystinuria aims to decrease the concentration of cystine in the urine, increase its solubility and therefore prevent stone formation. Ascorbic acid and captopril have been recommended as alternatives to thiol drugs, though conflicting data undermining their efficacy has been widely reported, too. The aim of this study was to verify the effects of ascorbic acid and captopril on cystine stone formation in the cystinuria mouse model. A total of 28 male homozygous pebbles mice were used for characterizing the mice on normal diet, ascorbic acid and captopril supplemented diets. The baseline physiological parameters of the mice were determined initially. The normal diet was then replaced with the supplemented diet (ascorbic acid/captopril) for the next 48 weeks and various biochemical parameters in urine and plasma were analyzed. All homozygous mice developed urinary cystine stones during the first year of life. No reduction in the urinary cystine concentration was seen with either of the supplemented diets. The stone mass varied widely in the study and a beneficial effect of ascorbic acid in some of the animals was possible though an overall statistical significance was not seen. Conclusions: The cystinuria mouse model provides an ideal tool for evaluation of stone preventive measures in a standardized environment. This study confirms that ascorbic acid and captopril are not effective in cystinuria.

  13. [Pharmaceutical technology of Tensiomin].

    Science.gov (United States)

    Fekete, P

    1997-07-01

    The physical chemical properties, stability and incompatibility of captopril (the active ingredient of Tensiomin tablets) have been discussed. Captopril has two polimorphic crystal modifications, the form I. of higher melting point is applied in the therapy. Captopril has a better stability in solutions below pH 4, the degradation is accelerated by metallic ions (Cu, Fe). In solid phase the degradation is accelerated by the humidity of the air. No incompatibility was found with the tabletting excipients but stearic acid and sodium-carboxymethyl-starch. Under compaction at higher pressure captopril itself shows tendency for lamination. The dissolution rate of the Tensiomin tablets can meet the requirement of USP if direct tabletting method was used. In this case the breaking strength of the tablets has no influence on the dissolution rate. The main properties (weight uniformity, content uniformity, tensile strength, friability, disintegration time, dissolution time) of the Tensiomin tablets of 12.5 mg, 25 mg, 50 mg and 100 mg of captopril meet the requirement of USP not only after manufacturing but after the accelerated stability test of three month as well.

  14. Reduction of regurgitation in aortic insufficiency by inhibition of the renin/angiotensin conversion enzyme

    Energy Technology Data Exchange (ETDEWEB)

    Reske, S.N.; Heck, I.; Mattern, H.

    1984-10-01

    The effect of captopril-mediated afterload reduction on regurgitation was investigated in 10 patients with aortic insufficiency. Regurgitation was quantitated by the regurgitation fraction and the relation of regurgitant volume to end-diastolic volume, which were derived from gated radionuclide ventriculography. 19 patients with coronary artery disease and no evidence of valvular heart disease served as controls. In patients with coronary artery disease no significant reguration was found. In patients with aortic regurgitation the blood concentration of angiotensin I increased whereas that of angiotensin II decreased significantly after captopril-medication; thus, the conversion of angiotensin I to II was reduced to about 50% of the control value. Whereas blood pressure and heart rate did not change significantly, the regurgitation fraction and the normalized regurgitant volume were significantly reduced. The ejection fraction remained essentially unchanged. These findings suggest a favorable influence of captopril-induced afterload reduction on hemodynamics in aortic regurgitation.

  15. Efeito de drogas utilizadas no tratamento de hipertensão arterial sistêmica sobre a pressão intra-ocular: estudo experimental no cão

    Directory of Open Access Journals (Sweden)

    Hashimoto Mitsuo

    2002-01-01

    Full Text Available Objetivo: Estudar os efeitos de duas drogas utilizadas no tratamento de hipertensão arterial sistêmica (captopril e propranolol sobre a pressão intra-ocular (PIO e pressão de perfusão (PP em cães anestesiados. Métodos: Foram estudados 24 cães, divididos em 3 grupos de 8. No primeiro grupo (GI, foi administrado captopril (um inibidor da enzima conversora de angiotensina na dose de 1,5 mg/kg por via endovenosa. No segundo grupo (GII, foi administrado propranolol (um beta-bloqueador na dose de 1,5 mg/kg por via endovenosa. O terceiro grupo (GIII foi o grupo controle. A PIO e a pressão arterial média (PAm foram medidas por manometria. A pressão de perfusão (PP foi calculada pela diferença entre a PAm e a PIO. A freqüência cardíaca (FC foi monitorada com oxímetro de pulso. Os parâmetros foram estudados em 6 momentos (0, 10, 30, 60, 90 e 120 minutos. Resultados: Houve redução estatisticamente significativa da PIO (p<0,05 nos grupos em que foram administrados captopril e propranolol, sem diferença entre as drogas. Com captopril, houve redução da PAm e da PP aos 10 e 30 minutos. Com propranolol, não houve redução da PAm ou da PP. Conclusão: Houve redução da PIO com uso do captopril e também do propranolol. Entretanto, a redução acentuada da PAm e da PP causadas pelo captopril, podem ser indesejáveis para a irrigação do nervo óptico.

  16. Antihypertensive effects of Ocimum basilicum L. (OBL) on blood pressure in renovascular hypertensive rats.

    Science.gov (United States)

    Umar, Anwar; Imam, Guzelnur; Yimin, Wuliya; Kerim, Parhat; Tohti, Ibadet; Berké, Bénédicte; Moore, Nicholas

    2010-07-01

    Ocimum basilicum L. (OBL), sweet basil, is a medicinal herb used in traditional Chinese medicine to treat cardiovascular diseases including hypertension. The objective of the study was to investigate the possible antihypertensive effects of OBL extract in renovascular hypertensive rats. The two-kidney one-clip (2K1C) Goldblatt model of renovascular hypertension was used in Wistar rats. Rats were randomized into sham, untreated 2K1C, captopril- (30 mg kg(-1) per day orally) and OBL- (100, 200, 400 mg kg(-1) per day orally) (low (L)-, medium (M)-, high (H)-OBL) treated 2K1C groups (n=10-12 per group), followed up for 4 weeks. Blood pressure, heart weight/body weight, plasma angiotensin-II and endothelin (ET)-1 were studied. OBL reduced systolic and diastolic blood pressure by about 20 and 15 mm Hg, respectively, compared with 35 and 22 mm Hg for captopril, from the lowest dose tested with no dose dependency. Cardiac hypertrophy was reduced from 3.6+/-0.7 mg g(-1) for untreated 2K1C to 3.0+/-0.6, 2.9+/-0.6 and 2.4+/-0.4 mg g(-1) for L-, M- and H-OBL, respectively, compared with 2.6+/-0.5 for sham and 3.1+/-0.4 mg g(-1) for captopril (P<0.05). Renal function was improved with captopril. Angiotensin was reduced to a lesser extent than with captopril. ET was reduced to lower concentrations (78+/-15, 80+/-22, 82+/-15 pg ml(-1) for L-, M-, H-OBL, respectively) than in sham (116+/-31 pg ml(-1)), untreated 2K1C (174+/-72 pg ml(-1)) or captopril (117+/-72 pg ml(-1)) groups. The effects of OBL on blood pressure, cardiac hypertrophy and ET, are consistent with an effect on ET-converting enzyme, and warrant further exploration.

  17. Antihypertensive nano-ceuticales based on chitosan biopolymer: Physico-chemical evaluation and release kinetics.

    Science.gov (United States)

    Niaz, Taskeen; Shabbir, Saima; Manzoor, Shahid; Rehman, Asma; Rahman, Abdur; Nasir, Habib; Imran, Muhammad

    2016-05-20

    Prime risk factor behind cardiovascular associated mortality and morbidity is hypertension. The main challenge with antihypertensive (AHT) drug therapy is their extreme hydrophobic nature and very low oral bio-availability; which result into higher dosage/frequency and associated side effects of drugs. The main objective of this study was to fabricate AHT nano-ceuticals in hydrophilic carriers of natural origin to improve drugs' solubility, protection and sustained release. AHT nano-carrier systems (NCS) encapsulating captopril, amlodipine and valsartan were fabricated using chitosan (CS) polymer by ionic gelation assisted ultra-sonication method. Drug encapsulation efficiencies of 92±1.6%, 91±0.9% and 87±0.5% were observed for captopril, valsartan and amlodipine respectively. Scanning electron microscopy (SEM) based analysis had revealed that captopril loaded polymeric NCS were regular, smooth and without any agglomeration. FTIR analyses of drug loaded and empty NCS demonstrated that drugs were molecularly dispersed inside the nanoparticles via week hydrogen bonding. Captopril and valsartan have demonstrated grafting reaction with N-H group of chitosan. Zeta sizer results had confirmed that average size of chitosan nanoparticles was below 100 nm. Encapsulation of captopril had reduced the surface charge value from +52.6±4.8 to +46.5±5.2 mV. Controlled release evaluation of highly encapsulated drug captopril had revealed a slow release in vitro from NCS in physiological buffer. Thus, here reported innovative AHT nano-ceuticals of polymeric origin can improve the oral administration of currently available hydrophobic drugs while providing the extended-release function.

  18. 中西医结合治疗轻、中度充血性心力衰竭的临床研究%A Clinical Study of Treatment of Light, Middle Degree Congestive Heart Failure with Integration of Traditional and Western Medicine

    Institute of Scientific and Technical Information of China (English)

    潘从军

    2003-01-01

    Objective To evaluate the effects of combination of traditional medicine,captopril and metoprolol on lightand middle degree heart failure. Methods 150 patients in group A were treated with traditional medicine only, in group B withcaptopril and metoprolol, in group C with a combination of traditional medicine captopril and metoprolol. The effects weredecrease of pvc in group C compared to group A and B (P < 0.05). Conxclusion A combination of traditional medicinecaptopril and methoprolol for the treatment of light, middle degree heart failure would be expected to have a good result.

  19. The clinical case of sildenafil administration in a very premature infant with pulmonary hypertension

    Directory of Open Access Journals (Sweden)

    Galina A. Alyamovskaya

    2015-02-01

    Full Text Available We report the use of oral sildenafil in a 7-month-old preterm newborn with severe bronchopulmonary dysplasia and pulmonary arterial hypertension refractory to captopril and inhaled budesonide, and need of consistent oxygenation. Sildenafil was prepared as a powder for oral administration. Oral sildenafil treatment was continued for 11 months. Oxygen supplement was suspended after 4 months and captopril administration was finished after 7 months of sildenafil treatment. There were no adverse effects during the treatment period. The respiratory failure decreased significantly and pulmonary arterial pressure became normal after 7 months of sildenafil treatment.

  20. Different reactivity to angiotensin II of peripheral and renal arteries in spontaneously hypertensive rats: effect of acute and chronic angiotensin converting enzyme inhibition

    Science.gov (United States)

    Guidi, E.; Hollenberg, N. K.

    1986-01-01

    We assessed renal blood flow and pressor responses to graded angiotensin II doses in spontaneously hypertensive (SHR) and Wistar-Kyoto (WKY) rats ingesting a diet containing 1.6% sodium basally and after acute and chronic angiotensin converting enzyme (ACE) inhibition with captopril. In the basal state the pressor response to angiotensin II was enhanced (Prenal vascular response was blunted (Pacute captopril administration the pressor response was enhanced in both strains, and the difference between them was maintained, while the renal vascular response was enhanced in both, but more in SHR, so that the renal vascular response in the SHR became larger than in WKY (Prenal responses in WKY rats, but only the pressor response in SHR. The renal vessels of SHR seem to be different from those of WKY rats in reaction to exogenous angiotensin II, and in response to both acute administration of captopril (probably acting through blockade of angiotensin II production) and chronic administration of captopril (probably acting mainly through accumulation of kinin or production of prostaglandins).

  1. Antinociceptive effect of [Met5]enkephalin semicarbazide is not affected by dipeptidyl carboxypeptidase-I.

    Science.gov (United States)

    Rezaee, Zahra; Arabanian, Seyed Abbas; Balalaie, Saeed; Ahmadiani, Abolhassan; Khalaj, Leila; Nasoohi, Sanaz

    2012-02-01

    Dipeptidyl carboxypeptidase-I is an enzyme involved in the biological degradation of enkephalins. It has been suggested that C-terminal amidation of enkephalins enhances their resistance to dipeptidyl carboxypeptidase-I-mediated biodegradation. In this study, a novel [Met5]enkephalin amide (MEA) analogue [Met5]enkephalin (ME)-semicarbazide synthesized by another laboratory in our group was assessed for its antinociceptive effects compared with ME-ethylamide, MEA and ME, using tail flick test. To protect the administered drugs from biodegradation, rats were pretreated with peptidase inhibitors including amastatin, phosphoramidon and captopril. Then captopril (dipeptidyl carboxypeptidase-I inhibitor) was deleted from the peptidase inhibitors' combination for evaluating in vivo resistance of the synthetic drugs to dipeptidyl carboxypeptidase-I. According to the results, ME-semicarbazide and MEA were resistant enough to dipeptidyl carboxypeptidase-I to exert their strong antinociception following intrathecal administration even in the absence of captopril, whereas the antinociceptive effects produced by ME-ethylamide (10 nmol) were abolished in rats not pretreated with captopril, indicating that significant amounts of the ME-ethylamide were degraded by dipeptidyl carboxypeptidase-I. Replacement of the amide moiety of MEA with semicarbazide provides a new ME derivative, with high analgesic effects as well as more resistance to dipeptidyl carboxypeptidase-I-mediated biodegradation.

  2. 28. Critical pulmonary valve stenosis: Medical management beyond balloon dilation

    Directory of Open Access Journals (Sweden)

    Muhammad Arif Khan

    2015-10-01

    Conclusion: Phentolamine and/or Captopril have a therapeutic role in neonates with critical PVS who remain oxygen dependent after balloon dilation. Both medicationslead to vasodilatation of pulmonary and systemic vascularity. They facilitate inflowto the right ventricle. Right to left shunt across a PFO or/ ASD minimizesand saturation improves leading to a significantreduction in length of hospitalization.

  3. Valsartan in Acute Myocardial Infartion%缬沙坦治疗急性心肌梗塞伴心力衰竭或左心室功能障碍

    Institute of Scientific and Technical Information of China (English)

    廖洪涛; 吴书林

    2005-01-01

    文献类型:治疗.证据水平;1b.:文献来源 Pfeffer MA, McMurray JJ, Velazquez E J, et al.Valsartan, Captopril, or both in myocardial infarction complicated by heart failure, left ventricular dysfunction, or both [J]. N Engl J Med, 2003,349:1893-1906.

  4. Geographic variation in the treatment of acute myocardial infarction in the VALsartan In Acute myocardial iNfarcTion (VALIANT) trial

    DEFF Research Database (Denmark)

    Reed, Shelby D; McMurray, John J V; Velazquez, Eric J

    2006-01-01

    BACKGROUND: The VALIANT trial compared the efficacy and safety of captopril, valsartan, and their combination in patients with left ventricular systolic dysfunction, heart failure, or both after acute myocardial infarction (MI). By examining this international trial population of high-risk patients...

  5. Suppression of TGF-β1/Smad signaling pathway by sesamin contributes to the attenuation of myocardial fibrosis in spontaneously hypertensive rats.

    Science.gov (United States)

    Zhao, Mengqiu; Zheng, Shuguo; Yang, Jieren; Wu, Yuanjie; Ren, Younan; Kong, Xiang; Li, Wei; Xuan, Jiali

    2015-01-01

    This study investigated the effect of sesamin on myocardial fibrosis in spontaneously hypertensive rats (SHRs) and the possible mechanisms involved. Twenty-eight male SHRs were randomly allocated to SHR group, Ses160 group (sesamin 160 mg/kg), Ses80 group (sesamin 80 mg/kg) and Cap30 group (captopril 30 mg/kg). Seven male WKY rats were used as control. Sesamin and captopril were administered intragastrically for 12 weeks. Captopril significantly reduced systolic blood pressure and angiotensin II (Ang II) levels in SHRs, accompanied by a marked attenuation of left ventricular hypertrophy (LVH) and collagen deposition (P sesamin had no significant influence on Ang II levels, and the hypotensive effect was also significantly inferior to that of captopril (P Sesamin markedly reduced transforming growth factor-β1 (TGF-β1) content in cardiac tissues, with Smad3 phosphorylation decreased and Smad7 protein expression increased notably (P sesamin (P sesamin significantly increased total antioxidant capacity and superoxide dismutase protein in cardiac tissues (P sesamin was able to suppress Ang II induced phosphorylation of Smad3 and secretion of TGF-β1 and type I and type III collagen in cultured rat cardiac fibroblasts. These data suggest that sesamin is capable of attenuating hypertensive myocardial fibrosis through, at least partly, suppression of TGF-β1/Smad signaling pathway.

  6. Polyionic hybrid nano-engineered systems comprising alginate and chitosan for antihypertensive therapeutics.

    Science.gov (United States)

    Niaz, Taskeen; Nasir, Habib; Shabbir, Saima; Rehman, Asma; Imran, Muhammad

    2016-10-01

    Hydrophobic nature of virtually all antihypertensive (AHT) drugs is the major hindrance towards their oral administration. Current study focuses on the development of polyionic hybrid nano drug delivery systems comprising sodium alginate and chitosan, loaded with distinct AHT drugs (captopril, amlodipine and valsartan). Encapsulation efficiency of hybrid NCS increased in the order of amlodipine>valsartan>captopril with average value of 42±0.9%, 91±1.5% and 96±1.9%, respectively. Scanning electron microscopy revealed hybrid NCS with smooth topography and round appearance in case of captopril. FTIR analysis confirmed the cross-linking between amino and carboxylate group of chitosan and alginate to form polyionic structures at nano-scale. Zeta-sizer experiments revealed that particle size distribution had increased from 197±12nm to 341±15nm for void and captopril loaded NCS. However, highly positive zeta potential of +32±1.6mV was not decreased significantly. In vitro sustained release assays reflected excellent retention of AHT drug in hybrid nanoparticles at 4°C and 37°C in physiological buffer, as less than 8% of the total drug was released in first 24h. Thus, carbohydrate-based hybrid NCS offering high loading capacity, stability and sustained release of hydrophobic drugs can be excellent alternative to current AHT therapeutics.

  7. Udvikling af sklerodermisk krise hos patient med uerkendt sklerodermi

    DEFF Research Database (Denmark)

    Madsen, Kristine Lindhard; Hansen, Alastair; Halberg, Poul;

    2014-01-01

    Less than 10% of the patients with systemic scleroderma develop renal crisis, i.e. acute renal failure and severe hypertension in most cases. Kidney biopsy shows hypertensive arteriolar changes. This complication was lethal until treatment with captopril was introduced in 1976. Since that time...

  8. Role of the renin-angiotensin system in regulation and autoregulation of renal blood flow

    DEFF Research Database (Denmark)

    Sørensen, Charlotte Mehlin; Leyssac, Paul Peter; Skøtt, Ole;

    2000-01-01

    The role for ANG II in renal blood flow (RBF) autoregulation is unsettled. The present study was designed to test the effect of clamping plasma ANG II concentrations ([ANG II]) by simultaneous infusion of the angiotensin-converting enzyme inhibitor captopril and ANG II on RBF autoregulation in ha...

  9. The exenatide analogue AC3174 attenuates hypertension, insulin resistance, and renal dysfunction in Dahl salt-sensitive rats

    Directory of Open Access Journals (Sweden)

    Fernandez Rayne

    2010-08-01

    Full Text Available Abstract Background Activation of glucagon-like peptide-1 (GLP-1 receptors improves insulin sensitivity and induces vasodilatation and diuresis. AC3174 is a peptide analogue with pharmacologic properties similar to the GLP-1 receptor agonist, exenatide. Hypothetically, chronic AC3174 treatment could attenuate salt-induced hypertension, cardiac morbidity, insulin resistance, and renal dysfunction in Dahl salt-sensitive (DSS rats. Methods DSS rats were fed low salt (LS, 0.3% NaCl or high salt (HS, 8% NaCl diets. HS rats were treated with vehicle, AC3174 (1.7 pmol/kg/min, or GLP-1 (25 pmol/kg/min for 4 weeks via subcutaneous infusion. Other HS rats received captopril (150 mg/kg/day or AC3174 plus captopril. Results HS rat survival was improved by all treatments except GLP-1. Systolic blood pressure (SBP was lower in LS rats and in GLP-1, AC3174, captopril, or AC3174 plus captopril HS rats than in vehicle HS rats (p Conclusions Thus, AC3174 had antihypertensive, cardioprotective, insulin-sensitizing, and renoprotective effects in the DSS hypertensive rat model. Furthermore, AC3174 improved animal survival, an effect not observed with GLP-1.

  10. Effects of aspirin on angiotensin-converting enzyme inhibition and left ventricular dilation one year after acute myocardial infarction

    NARCIS (Netherlands)

    Oosterga, M; Anthonio, RL; de Kam, PJ; Kingma, JH; Crijns, HJGM; van Gilst, WH

    1998-01-01

    There are conflicting reports on the interaction of aspirin with angiotensin-converting enzyme inhibitors in heart failure and systemic hypertension. A past hoc analysis of the Captopril and Thrombolysis Study (CATS) study was conducted. At randomization, 94 patients (31.5%) took aspirin. In patient

  11. Effect of L-5-Hydroxytryptophan on drinking behavior in Coturnix japonica (Temminck and Schlegel, 1849 (Galliformes: Aves: involvement of renin-angiotensin system

    Directory of Open Access Journals (Sweden)

    PL Cedraz-Mercez

    Full Text Available The purpose of this study was to explore the role of L-5-hydroxytryptophan (L-HTP and its relationship with the renin-angiotensin system (RAS on the drinking behavior in Japanese quails. Normally-hydrated quails that received injections of L-HTP (12.5; 25 and 50 mg.kg-1 by the intracoelomic route (ic expressed an increase in water intake, which was inhibited by captopril, an angiotensin converting enzyme (ACE inhibitor. In addition, captopril also induced such a response in birds under previous fluid deprivation. High doses of captopril (35-70 mg.kg-1, sc in normally-hydrated quails decreased the spontaneous water intake while low doses of captopril (2-5 mg.kg-1, sc did not prompt water intake after L-HTP administration. Losartan, an AT1 receptor antagonist in mammals, did not change the water intake levels in normally-hydrated or water-deprivated birds. Serotonin (5-HT injections did not provoke its known dipsogenic response.

  12. Modification of exercise performance by sharp reduction of blood pressure. A study in patients with uncomplicated hypertension.

    Science.gov (United States)

    Agostoni, P G; Doria, E; Alimento, M; Riva, S; Muratori, M; Tamborini, G

    1993-12-01

    We evaluated exercise performance in 14 patients with uncomplicated essential hypertension 1 h after the administration of a single dose of placebo, nifedipine (20 mg), captopril (50 mg), and propranolol (80 mg). Drugs were administered at the same time of day following a randomized, double-blind protocol. Mean resting blood pressure (+/- SE) was 135 +/- 3 mm Hg with placebo administration, 118 +/- 4 with captopril, 110 +/- 4 with nifedipine, and 115 +/- 5 with propranolol and increased with exercise to 163 +/- 4, 146 +/- 3, 136 +/- 4, 136 +/- 4, respectively. Oxygen consumption at peak exercise and at ventilatory anaerobic threshold (VAT) was 25.2 +/- 1.1 and 18.1 +/- 1.0 ml/min/kg with placebo. Only propranolol (-2.3 ml/min/kg) decreased peak exercise oxygen consumption. Oxygen consumption at VAT was reduced by nifedipine and propranolol but unaffected by captopril. The effects on exercise capacity of blood pressure reduction in hypertensive patients are dependent on the drug utilized and are not related to the amount of blood pressure reduction. The lowered oxygen consumption at VAT observed with nifedipine and propranolol, and not with captopril, might be due to an excessive downward shift of the muscle perfusion pressure--oxygen consumption relationship which might take place during exercise.

  13. Comparative effects of chelating agents on distribution, excretion, and renal toxicity of gold sodium thiomalate in rats.

    Science.gov (United States)

    Takahashi, Y; Funakoshi, T; Shimada, H; Kojima, S

    1994-05-31

    The effects of various chelating agents, such as (2S)-1-(3-mercaptopropionyl)-L-proline (captopril), N-(2-mercaptopropionyl)-glycine (tiopronin), L-cysteine (L-Cys), D-cysteine (D-Cys), N-acetyl-L-cysteine (L-NAC), N-benzyl-D-glucamine dithiocarbamate (BGD), and ethylenediaminetetraacetate (EDTA), on the distribution, excretion, and renal toxicity of gold sodium thiomalate (AuTM) in rats were investigated. Rats were intraperitoneally injected with the chelating agents (1.2 mmol/kg each) immediately after intravenous injection of AuTM (0.026 mmol/kg). Treatment with captopril or tiopronin significantly prevented increases in the urinary excretion of protein, aspartate aminotransferase (AST), and glucose and the blood urea nitrogen (BUN) level after AuTM injection. L-NAC and D-Cys significantly prevented increases in the urinary excretion of protein, AST, and glucose after AuTM injection, but did not reduce to control levels. Treatment with BGD, EDTA, or L-Cys did not prevent AuTM-induced increases in the urinary excretion of protein, AST, and glucose and BUN level. Tiopronin significantly increased the urinary excretion of gold. Captopril slightly promoted both the urinary and fecal excretion of gold, resulting in the significant increase in the total excretion of the metal. Tiopronin and captopril significantly decreased the gold concentration in the kidney and liver. L-Cys, D-Cys, L-NAC, BGD, and EDTA had no significant effect on the excretion or distribution of gold at 7 days after AuTM injection. These results indicate that tiopronin and captopril can ameliorate the renal toxicity induced by AuTM. In addition, the comparative effects of 2,3-dimercaptopropane sulfonate (DMPS), N-(2-mercapto-2-methylpropanoyl)-L-cysteine (bucillamine), captopril, and tiopronin at various dose levels (1.2, 0.4 or 0.2 mmol/kg) on the distribution and renal toxicity of gold were studied. DMPS was effective in removing gold from the kidney and in protecting against the renal toxicity

  14. The effect of ACE inhibition on the pulmonary vasculature in combined model of chronic hypoxia and pulmonary arterial banding in Sprague Dawley rats

    Science.gov (United States)

    Clarke, Shanelle; Baumgardt, Shelley; Molthen, Robert

    2010-03-01

    Microfocal CT was used to image the pulmonary arterial (PA) tree in rodent models of pulmonary hypertension (PH). CT images were used to measure the arterial tree diameter along the main arterial trunk at several hydrostatic intravascular pressures and calculate distensibility. High-resolution planar angiographic imaging was also used to examine distal PA microstructure. Data on pulmonary artery tree morphology improves our understanding of vascular remodeling and response to treatments. Angiotensin II (ATII) has been identified as a mediator of vasoconstriction and proliferative mitotic function. ATII has been shown to promote vascular smooth muscle cell hypertrophy and hyperplasia as well as stimulate synthesis of extracellular matrix proteins. Available ATII is targeted through angiotensin converting enzyme inhibitors (ACEIs), a method that has been used in animal models of PH to attenuate vascular remodeling and decrease pulmonary vascular resistance. In this study, we used rat models of chronic hypoxia to induce PH combined with partial left pulmonary artery occlusion (arterial banding, PLPAO) to evaluate effects of the ACEI, captopril, on pulmonary vascular hemodynamic and morphology. Male Sprague Dawley rats were placed in hypoxia (FiO2 0.1), with one group having underwent PLPAO three days prior to the chronic hypoxia. After the twenty-first day of hypoxia exposure, treatment was started with captopril (20 mg/kg/day) for an additional twenty-one days. At the endpoint, lungs were excised and isolated to examine: pulmonary vascular resistance, ACE activity, pulmonary vessel morphology and biomechanics. Hematocrit and RV/LV+septum ratio was also measured. CT planar images showed less vessel dropout in rats treated with captopril versus the non-treatment lungs. Distensibility data shows no change in rats treated with captopril in both chronic hypoxia (CH) and CH with PLPAO (CH+PLPAO) models. Hemodynamic measurements also show no change in the pulmonary vascular

  15. Effects of a novel ACE inhibitor, 3-(3-thienyl-L-alanyl-ornithyl-proline, on endothelial vasodilation and hepatotoxicity in L-NAME-induced hypertensive rats

    Directory of Open Access Journals (Sweden)

    Seth MK

    2016-04-01

    Full Text Available Mahesh Kumar Seth,1–3 M Ejaz Hussain,2 Santosh Pasha,1 Mohammad Fahim3 1Peptide Synthesis Laboratory, CSIR, Institute of Genomics and Integrative Biology, Delhi, India; 2Centre for Physiotherapy and Rehabilitation Sciences, Jamia Millia Islamia, New Delhi, India; 3Department of Physiology, Jamia Hamdard Deemed University, New Delhi, India Abstract: Nitric oxide (NO is a widespread biological mediator involved in many physiological and pathological processes, eg, in the regulation of vascular tone and hypertension. Chronic inhibition of NO synthase by NG-nitro-L-arginine methyl ester (ʟ-NAME hydrochloride results in the development of hypertension accompanied by an increase in vascular responsiveness to adrenergic stimuli. Recently, we developed a novel sulfur-containing angiotensin-converting enzyme inhibitor: 3-(3-thienyl-ʟ-alanyl-ornithyl-proline (TOP. Our previous studies indicated a superior nature of the molecule as an antihypertensive agent in spontaneously hypertensive rats (showing the involvement of renin–angiotensin–aldosterone system in comparison to captopril. The aim of the present study was to investigate the effect of TOP on NO pathway in ʟ-NAME-induced hypertensive rats, and captopril was included as the standard treatment group. Treatment with both TOP (20 mg/kg and captopril (40 mg/kg prevented the development of hypertension in ʟ-NAME model, but TOP showed better restoration of NO and normal levels of angiotensin-converting enzyme. In addition, in vitro vasorelaxation assay showed an improvement in endothelium-dependent vasodilation in both the cases. Further, the biochemical (malondialdehyde, alanine aminotransferase, and aspartate aminotransferase and the histopathological effects of TOP on rat liver tissues revealed a protective nature of TOP in comparison to captopril in the ʟ-NAME model. In conclusion, TOP at 50% lesser dose than captopril was found to be better in the ʟ-NAME model. Keywords: nitric oxide

  16. Targeting the Renin–Angiotensin System Combined With an Antioxidant Is Highly Effective in Mitigating Radiation-Induced Lung Damage

    Energy Technology Data Exchange (ETDEWEB)

    Mahmood, Javed [Ontario Cancer Institute and the Campbell Family Institute for Cancer Research, Princess Margaret Cancer Centre, University Health Network, Toronto, Ontario (Canada); Radiation Medicine Program, STTARR Innovation Centre, Princess Margaret Cancer Centre, Toronto, Ontario (Canada); Jelveh, Salomeh [Radiation Medicine Program, STTARR Innovation Centre, Princess Margaret Cancer Centre, Toronto, Ontario (Canada); Zaidi, Asif [Ontario Cancer Institute and the Campbell Family Institute for Cancer Research, Princess Margaret Cancer Centre, University Health Network, Toronto, Ontario (Canada); Doctrow, Susan R. [Pulmonary Center, Department of Medicine, Boston University, Boston, Massachusetts (United States); Medhora, Meetha [Department of Radiation Oncology, Medical College of Wisconsin, Milwaukee, Wisconsin (United States); Hill, Richard P., E-mail: hill@uhnres.utoronto.ca [Ontario Cancer Institute and the Campbell Family Institute for Cancer Research, Princess Margaret Cancer Centre, University Health Network, Toronto, Ontario (Canada); Departments of Medical Biophysics and Radiation Oncology, University of Toronto, Toronto, Ontario (Canada)

    2014-07-15

    Purpose: To investigate the outcome of suppression of the renin angiotensin system using captopril combined with an antioxidant (Eukarion [EUK]-207) for mitigation of radiation-induced lung damage in rats. Methods and Materials: The thoracic cavity of female Sprague-Dawley rats was irradiated with a single dose of 11 Gy. Treatment with captopril at a dose of 40 mg/kg/d in drinking water and EUK-207 given by subcutaneous injection (8 mg/kg daily) was started 1 week after irradiation (PI) and continuing until 14 weeks PI. Breathing rate was monitored until the rats were killed at 32 weeks PI, when lung fibrosis was assessed by lung hydroxyproline content. Lung levels of the cytokine transforming growth factor-β1 and macrophage activation were analyzed by immunohistochemistry. Oxidative DNA damage was assessed by 8-hydroxy-2-deoxyguanosine levels, and lipid peroxidation was measured by a T-BARS assay. Results: The increase in breathing rate in the irradiated rats was significantly reduced by the drug treatments. The drug treatment also significantly decreased the hydroxyproline content, 8-hydroxy-2-deoxyguanosine and malondialdehyde levels, and levels of activated macrophages and the cytokine transforming growth factor-β1 at 32 weeks. Almost complete mitigation of these radiation effects was observed by combining captopril and EUK-207. Conclusion: Captopril and EUK-207 can provide mitigation of radiation-induced lung damage out to at least 32 weeks PI after treatment given 1-14 weeks PI. Overall the combination of captopril and EUK-207 was more effective than the individual drugs used alone.

  17. Effect of Pinggan-Maitong tables on nitric oxide, endothelin of hypertensive rats of Yin deficiency and Yang excess

    Institute of Scientific and Technical Information of China (English)

    Simailahong Mayinuer; Jian-Ping Wang; Jing-Wen Sun; Jun Hong

    2016-01-01

    Objective:To explore the effect of Pinggan-Maitong tables on nitric oxide, endothelin of hypertensive rats of Yin deficiency and Yang excess.Methods:Hypertensive rats of Yin deficiency and Yang excess were established by adopting the method of two kidney one clip and irrigation clothing monkshood. A total of 75 rats models were established successfully. They were randomly divided into blank control group, captopril group, low dose hepatic vein group, middle dose hepatic vein group, high dose hepatic vein group, with 15 cases in each group. They were only given 2 mL/100 g physiological saline, 10 mg/mL concentration of captopril solution, 10 mg/mL, 20 mg/mL, 40 mg/mL concentration of hepatic vein through solution to fill the stomach respectively, for four weeks. Tail arterial blood pressure, serum NO, endothelin 1 (ET-1), angiotensinⅡ (AngⅡ), plasma aldosterone (ALDO) and cardiac function index of left ventricular ejection fraction (EF)%, short axial shortening rate (FS)% were compared between groups before and after treatment.Results:The tail artery blood pressure, ET-1, AngⅡ in blank control group after treatment were significant rise, ALDO, NO significantly reduced, EF%, FS% had no significant change, while the tail artery blood pressure, ET-1, AngⅡ, ALDO in other four groups were significantly reduced, NO, EF%, FS% were significant rise. The tail artery blood pressure, ALDO in middle or high dose hepatic vein group were significantly lower than the captopril control group, NO, EF%, FS% were significantly higher than the captopril control group, the AngⅡ in hepatic vein on high dose group was significantly lower than the captopril control group.Conclusions:Pinggan-Maitong tables can reduce the blood pressure of hypertensive rats of Yin deficiency and Yang excess. It can reverse left ventricular hypertrophy, which may related to adjusting the serum NO, ET-1, AngⅡ, ALDO.

  18. Protective effects of Ginseng mixture on myocardial fibrosis in rats

    Institute of Scientific and Technical Information of China (English)

    Chun-Lai Zhang; Yue-Hong Li; Hong-Xia Zhou; Yu-Xin Zhang; Yong-Sheng Wang; Zhi-Yong Zhang; Ling-Li Meng; Xiao-Ming Shang

    2014-01-01

    Objective:To explore the protective effects of ginseng mixture on myocardial fibrosis(MF) in rats.Methods:A total of60Wistar rats were randomly divided into control group without modeling operation, and another4 groups using subcutaneous injections of isopropyl adrenaline for10 d to set up theMF model: model group with saline lavage treatment after modeling, captopril group with captopril lavage, ginseng mixture groupA and groupB with low and high dose mixture treatment respectively.After treatment for14 d, abdominal aorta and myocardial tissue were extracted to observe the pathological morphological changes and heart weight index in each group.Results:The left ventricular weight and heart heavy index of captopril group and groupB were significantly lower than that of model group and groupA(P<0.05);Model group and groupA showed a higher hydroxyproline(Hyp) content in myocardial tissue than the control group and lower catalase(CAT) activity than control group(P<0.05); captopril group and groupB showed a lowerHyp content and higherCAT activity compared with groupA and model group (P<0.05), a significantly lower level of serum glutathione peroxidase(GSH-PX) andCAT and a higher level of serum creatine kinase, lactate dehydrogenase andH2O2 in model group and group A were observed compared with the control group(P<0.05).A higher level ofGSH-PX andCAT and a lower level of creatine kinase, lactate dehydrogenase andH2O2 in captopril group and groupB were observed compared with groupA and model group(P<0.05); and histopathological examination showed that in captopril group and groupB, secretion of collagen fiber was significantly inhibited and myocardial injury was significantly lighter than that of model group. Conclusions:Ginseng mixture plays a protective effect on myocardium by inhibiting antioxidant process ofMF.

  19. Effect of angiotensin converting enzyme inhibition on myocardial phosphoinositide metabolism visualised with 1-[1-{sup 11}C]-butyryl-2-palmitoyl-rac-glycerol in myocardial infarction in the rat

    Energy Technology Data Exchange (ETDEWEB)

    Kagaya, Yutaka; Chida, Masanobu; Namiuchi, Shigeto; Takeda, Morihiko; Yamane, Yuriko; Otani, Hiroki; Watanabe, Jun; Fukuchi, Mitsumasa; Shirato, Kunio [Department of Cardiovascular Medicine, Tohoku University Graduate School of Medicine, 1-1 Seiryo-machi, Aoba-ku, Sendai 980-8574 (Japan); Imahori, Yoshio [Department of Neurosurgery, Kyoto Prefectural University of Medicine, Kyoto (Japan); Fujii, Ryou [Cyclotron Unit, Nishijin Hospital, Kyoto (Japan); Tezuka, Fumiaki [Department of Pathology, National Sendai Hospital, Sendai (Japan); Ido, Tatsuo [Cyclotron and Radioisotope Center, Tohoku University, Sendai (Japan)

    2002-11-01

    We recently reported that myocardial phosphoinositide (PI) metabolism can be visualised by 1-[1-{sup 11}C]-butyryl-2-palmitoyl-rac-glycerol ({sup 11}C-DAG) in rats with myocardial infarction (MI). Angiotensin II, the receptors for which are expressed predominantly in infarcted areas with active fibrogenesis rather than in non-infarcted regions, is involved in the upstream signalling systems of PI metabolism and plays an important role in the process of left ventricular (LV) remodelling after MI. We therefore hypothesised that the distribution of {sup 11}C-DAG after MI may be affected by the inhibition of angiotensin converting enzyme, which is one of the most important factors in the development of LV remodelling after MI. Rats were injected with {sup 11}C-DAG after 3 or 10weeks of treatment with captopril or no treatment following coronary artery ligation, and quantitative autoradiography was performed. Cells occupying the infarcted region were identified by immunohistochemistry. Compared with untreated rats, treatment with captopril for 3 weeks after MI elicited a reduction in the {sup 11}C-DAG uptake in the infarcted region (P<0.05) but not in the non-infarcted region, and was associated with a 22% decrease in the heart weight/body weight ratio. The thallium-201 distribution in the infarcted area was similarly low in the rats with and rats without the 3-week captopril treatment after MI. Abundant macrophages and myofibroblasts occupied the infarcted area in both rats with and rats without the captopril treatment for 3 weeks after MI. The {sup 11}C-DAG radioactivity in the infarcted region in the untreated rats was lower 10 weeks after MI than 3 weeks after MI (P<0.01). This finding was in agreement with the results of immunohistochemistry demonstrating that the number and size of macrophages and myofibroblasts were remarkably reduced in rats 10 weeks after MI compared with 3 weeks after MI. Captopril treatment for 10 weeks after MI did not decrease the {sup 11}C

  20. 氯沙坦与卡托普利治疗肺心病心力衰竭的疗效分析

    Institute of Scientific and Technical Information of China (English)

    任维

    2014-01-01

    objective to study the chlorine sand and the curative effect of captopril treatment of cor pulmonale heart failure. Methods randomly selected from 60 patients with cor pulmonale heart failure, male 32 cases, 28 cases women, aged 40 to 72 years old, heart failure duration 0.5 to 6 years, random grouping method is divided into chlorine temple group, captopril group, 30 cases in each group, respectively with chlorine sand and captopril treatment 2 weeks, observe the cardiac function improvement and adverse drug reactions. Results treatment group total effective rate of chlorine sand jotham 28 cases (93.3%), captopril group of 26 cases (86.7%), chlorine sand mitotane group appeared adverse drug reactions in 2 cases, 5 cases captopril group. Conclusion captopril and chlorine sand for cor pulmonale heart failure therapy are effective, but chlorine sand jotham low incidence of adverse drug reactions, easy to use.%目的:探讨氯沙坦与卡托普利治疗肺心病心力衰竭的疗效。方法随机选取我院肺心病心力衰竭患者60例,男32例,女28例,年龄40~72岁,心衰持续时间0.5~6年,随机分组法分为氯沙坦组、卡托普利组,每组各30例,分别用氯沙坦与卡托普利治疗2周,观察心功能改善及药物不良反应。结果治疗总有效率氯沙坦组28例(93.3%),卡托普利组26例(86.7%),出现药物不良反应氯沙坦组2例,卡托普利组5例。结论卡托普利与氯沙坦对肺心病心力衰竭治疗均有效,但氯沙坦药物不良反应发生率低,使用方便。

  1. Ativação da enzima conversora de angiotensina no coração após infarto do miocárdio e suas repercussões no remodelamento ventricular

    Directory of Open Access Journals (Sweden)

    Mill José Geraldo

    1997-01-01

    Full Text Available OBJETIVO: Determinar as alterações de atividade da enzima conversora de angiotensina (ECA no coração com infarto do miocárdio (IM e comparar os efeitos do captopril e losartan em parâmetros morfológicos e funcionais de ratos com IM. MÉTODOS: O IM foi produzido em ratos Wistar por ligadura de ramos da artéria coronária esquerda. Os controles (Con foram submetidos a uma cirurgia fictícia. Animais com IM e Con foram tratados com captopril (30mg/kg/dia ou losartan (15mg/kg/dia e estudados 30 dias após, determinando-se a atividade da ECA nos ventrículos direito (VD e esquerdo (VE, as alterações hemodinâmicas e as concentrações de hidroxiprolina (OH-Pro e proteína total no VD e VE. RESULTADOS: A atividade da ECA aumentou no VD (+25% e VE (+70% após IM. A maior atividade foi observada na cicatriz fibrótica, onde atingiu cerca de 4,5 vezes a do músculo do VE que sobreviveu ao IM (420±68 vs 94±8nmoles/g/min; P<0,01. O IM determinou aumento da pressão diastólica final e hipertrofia do VD e VE. Captopril e losartan foram igualmente eficazes em atenuar a hipertrofia e o aumento da pré-carga. O captopril também atenuou o aumento de OH-Pro no VD e VE após IM. O IM reduziu a concentração de proteína principalmente no músculo de VE, efeito esse acentuado pelo captopril. CONCLUSÃO: A grande atividade da ECA na cicatriz deve produzir altas concentrações de angiotensina II (AII no sangue que drena da cicatriz. Os efeitos dos inibidores da ECA seriam decorrentes, principalmente, da redução de geração local de AII, e não de aumento de cininas, uma vez que captopril e losartan exerceram efeitos similares no remodelamento pós-infarto.

  2. NMR-based metabolomics of urine for the atherosclerotic mouse model using apolipoprotein-E deficient mice.

    Science.gov (United States)

    Leo, Gregory C; Darrow, Andrew L

    2009-12-01

    NMR-based metabolomics of mouse urine was used in conjunction with the traditional staining and imaging of aortas for the characterization of disease advancement, that is, plaque formation in untreated and drug-treated apolipoprotein-E (apoE) knockout mice. The metabolomics approach with multivariate analysis was able to differentiate the captopril-treated from the untreated mice in general agreement with the staining results. Principal component analysis showed a pattern shift in both the drug-treated and untreated samples as a function of time that could possibly be explained as the effect of aging. Allantoin, a marker attributed to captopril treatment was elevated in the drug-treated mice. From partial least squares-discriminant analysis, xanthine and ascorbate were elevated in the untreated mice and were possible markers of plaque formation in the apoE knockout mice. Several additional peaks in the spectra characterizing the study endpoint were found but their respective metabolite identities were unknown.

  3. Effect of Yiqi Huoxue Recipe(益气活血方)on Cardiac Function and Ultrastructure in Regression of Pressure Overload-induced Myocardial Hypertrophy in Rats

    Institute of Scientific and Technical Information of China (English)

    2007-01-01

    Objective:To investigate the effect of Yiqi Huoxue Recipe(YHR,益气活血方)on the cardiac function and ultrastructure during the regression of myocardial hypertrophy induced by pressure overload in rats.Methods:The model of myocardial hypertrophy was established by abdominal aortic banding.Eighty male Wistar rats were divided into six groups,the normal control group Ⅰ(n=20),the normal control group Ⅱ(n=12),the hypertension model group [(n=12),the hypertension model group Ⅱ(n=12),the YHR group(n=12)and the Captopril group(n=12).The observation was carried out in the normal control group Ⅰ and the hypertension model group Ⅰ after 4weeks of modeling,and the other four groups were observed after 16 weeks of modeling(12 weeks of administration).The cardiac function was measured with a multichannel biological signal analysis system,and the myocardium ultrastructure was observed by a transmission electron microscope.Results:(1)Compared with the normal control group Ⅰ,the systolic blood pressure and cardiac coefficient(left ventricular weight/body weight)in the model Ⅰ group was higher(P<0.05,P<0.01).(2)In the YHR group,cardiac coefficient and -dp/dtmax were lower,left ventricular systolic pressure and +dp/dtmin were higher when compared with the model group Ⅱ and the Captopril group(P<0.05or P<0.01).In the Captopril group,only cardiac coefficient was lower when compared with the mode group Ⅱ(P<0.05).(3)Compared with the normal control group Ⅱ,+dp/dtrmax was higher(P<0.01),-dp/dtnmax and isovolumetric contraction time(ICT)was lower(P<0.05,P<0.01)in both the YHR group and the Captopril group.(4)Results of the myocardium ultrastructure showed edema under myocardium plasmalemma,enlarged sarcoplasmic reticulum and T tube,and significantly enlarged intercalated disc of the cardiac muscle in the model groups.In the Captopril group,the extension of sarcoplasmic reticulum and T tube as well as the pathological changes of intercalated disc

  4. Congestive heart failure and converting enzyme inhibition: failure of current prognostic criteria for predicting subsequent renal insufficiency.

    OpenAIRE

    1991-01-01

    Angiotensin-1-converting enzyme inhibitors have an effective and established role in the treatment of patients with congestive heart failure. However, a small number of such patients will subsequently develop renal insufficiency. These patients may be identified prior to, or shortly after, commencement of therapy by recognized criteria. This report describes 4 patients with congestive heart failure who developed severe renal insufficiency secondary to either enalapril or captopril therapy in ...

  5. Peptidases prevent μ-opioid receptor internalization in dorsal horn neurons by endogenously released opioids

    OpenAIRE

    Song, Bingbing; Marvizón, Juan Carlos G.

    2003-01-01

    To evaluate the effect of peptidases on μ-opioid receptor (MOR) activation by endogenous opioids, we measured MOR-1 internalization in rat spinal cord slices. A mixture of inhibitors of aminopeptidases (amastatin), dipeptidyl carboxypeptidase (captopril), and neutral endopeptidase (phosphoramidon) dramatically increased the potencies of Leu-enkephalin and dynorphin A to produce MOR-1 internalization, and also enhanced the effects of Met-enkephalin and α-neoendorphin, but not endomorphins or β...

  6. Treatment of hypertension and renal injury induced by the angiogenesis inhibitor sunitinib: preclinical study.

    Science.gov (United States)

    Lankhorst, Stephanie; Kappers, Mariëtte H W; van Esch, Joep H M; Smedts, Frank M M; Sleijfer, Stefan; Mathijssen, Ron H J; Baelde, Hans J; Danser, A H Jan; van den Meiracker, Anton H

    2014-12-01

    Common adverse effects of angiogenesis inhibition are hypertension and renal injury. To determine the most optimal way to prevent these adverse effects and to explore their interdependency, the following drugs were investigated in unrestrained Wistar Kyoto rats exposed to the angiogenesis inhibitor sunitinib: the dual endothelin receptor antagonist macitentan; the calcium channel blocker amlodipine; the angiotensin-converting enzyme inhibitor captopril; and the phosphodiesterase type 5 inhibitor sildenafil. Mean arterial pressure was monitored telemetrically. After 8 days, rats were euthanized and blood samples and kidneys were collected. In addition, 24-hour urine samples were collected. After sunitinib start, mean arterial pressure increased rapidly by ≈30 mm Hg. Coadministration of macitentan or amlodipine largely prevented this rise, whereas captopril or sildenafil did not. Macitentan, captopril, and sildenafil diminished the sunitinib-induced proteinuria and endothelinuria and glomerular intraepithelial protein deposition, whereas amlodipine did not. Changes in proteinuria and endothelinuria were unrelated. We conclude that in our experimental model, dual endothelin receptor antagonism and calcium channel blockade are suitable to prevent angiogenesis inhibition-induced hypertension, whereas dual endothelin receptor antagonism, angiotensin-converting enzyme inhibitor, and phosphodiesterase type 5 inhibition can prevent angiogenesis inhibition-induced proteinuria. Moreover, the variable response of hypertension and renal injury to different antihypertensive agents suggests that these side effects are, at least in part, unrelated.

  7. The toxicity of angiotensin converting enzyme inhibitors to larvae of the disease vectors Aedes aegypti and Anopheles gambiae.

    Science.gov (United States)

    Abu Hasan, Zatul-'Iffah; Williams, Helen; Ismail, Nur M; Othman, Hidayatulfathi; Cozier, Gyles E; Acharya, K Ravi; Isaac, R Elwyn

    2017-03-27

    The control of mosquitoes is threatened by the appearance of insecticide resistance and therefore new control chemicals are urgently required. Here we show that inhibitors of mosquito peptidyl dipeptidase, a peptidase related to mammalian angiotensin-converting enzyme (ACE), are insecticidal to larvae of the mosquitoes, Aedes aegypti and Anopheles gambiae. ACE inhibitors (captopril, fosinopril and fosinoprilat) and two peptides (trypsin-modulating oostatic factor/TMOF and a bradykinin-potentiating peptide, BPP-12b) were all inhibitors of the larval ACE activity of both mosquitoes. Two inhibitors, captopril and fosinopril (a pro-drug ester of fosinoprilat), were tested for larvicidal activity. Within 24 h captopril had killed >90% of the early instars of both species with 3(rd) instars showing greater resistance. Mortality was also high within 24 h of exposure of 1(st), 2(nd) and 3(rd) instars of An. gambiae to fosinopril. Fosinopril was also toxic to Ae. aegypti larvae, although the 1(st) instars appeared to be less susceptible to this pro-drug even after 72 h exposure. Homology models of the larval An. gambiae ACE proteins (AnoACE2 and AnoACE3) reveal structural differences compared to human ACE, suggesting that structure-based drug design offers a fruitful approach to the development of selective inhibitors of mosquito ACE enzymes as novel larvicides.

  8. [Psychotropic effects of angiotensin-converting enzyme inhibitors: what are the arguments?].

    Science.gov (United States)

    Mesure, G; Fallet, A; Chevalier, J F

    1995-01-01

    The authors report a case of acute mania induced by perindopril (Coversyl) in a 57 year old man with no prior history of mental illness. This Angiotensin-Converting Enzyme Inhibitor (ACEI) had been introduced eight days prior to the first signs of excitation, in order to treat recently diagnosed arterial hypertension. Without proof of reintroduction, and on the basis of clinical observations, the attribution appears plausible. Similar observations have been made for other molecules in this class of medication, such as captopril (Lopril). A review of literature regroups recent data concerning psychotropic effects of ACEIs. Several reports claim that captopril clearly acts as an antidepressant. Studies on the mood or the quality of life of treated hypertensive patients show ACEIs to have an euphoric-type positive effect compared to other anti-hypertensive treatments. Captopril and perindopril also act like potential antidepressants in experimental models of antidepression. Furthermore, pharmacologic data confirm that the most lipophilic ACEIs penetrate the central nervous system and argue in favor of the role of these molecules in activating central opioides. As these data provide evidence of mood swing in some patients, but also of an overall benefit in hypertensive populations, the clinical importance of the antidepressant effect of ACEIs needs further investigations.

  9. Angiotensin-converting enzyme inhibitors in congestive heart failure.

    Science.gov (United States)

    Deedwania, P C

    1990-09-01

    Angiotensin-converting enzyme inhibitors have had a significant impact on the treatment of congestive heart failure (CHF). Hemodynamic and clinical improvements in patients with severe CHF fostered the use of angiotensin-converting enzyme inhibitors in mild to moderate CHF. Angiotensin-converting enzyme inhibitors produce acute and sustained improvements in ventricular hemodynamics and quality of life. Captopril plus diuretic therapy is an effective alternative to digoxin in patients with mild to moderate CHF. Enalapril maleate and lisinopril have been shown to be effective in moderate to severe CHF when combined with digoxin and diuretics. Captopril and enalapril also improve survival in selected patients; captopril attenuates left ventricular dilatation after myocardial infarction. Although all angiotensin-converting enzyme inhibitors are similar in mechanism of action, pharmacokinetic differences impact their clinical use. Prolonged symptomatic hypotension compromising systemic perfusion and organ function has been reported with longer-acting agents; hypotension is usually short-lived and rarely compromises organ function with shorter-acting agents.

  10. Renovascular Hypertension: Clinical Features, Differential Diagnoses and Basic Principles of Treatment

    Directory of Open Access Journals (Sweden)

    Petrovic Dejan

    2016-09-01

    Full Text Available Renovascular hypertension is caused by renal artery stenosis. Its prevalence in populations of hypertensive patients is 1-8%, and in populations of patients with resistant hypertension, it is up to 20%. The two main causes of stenosis are atherosclerosis and fibromuscular dysplasia of the renal artery. The main clinical consequences of renal artery stenosis include renovascular hypertension, ischemic nephropathy and “flash” acute pulmonary oedema. Unilateral stenosis of the renal artery causes angiotensin II-dependent hypertension, and bilateral stenosis of the renal arteries produces volume-dependent hypertension. Renovascular aetiology of hypertension should be questioned in patients with resistant hypertension, hypertension with a murmur identified upon auscultation of the renal arteries, and a noticeable side-to-side difference in kidney size. Non-invasive diagnostic tests include the determination of concentrations of peripheral vein plasma renin activity, the captopril test, captopril scintigraphy, colour Doppler ultrasonography, computed tomography angiography, and nuclear resonance angiography. Renovasography represents the gold standard for the diagnosis of renovascular hypertension. The indications for revascularization of the renal artery include haemodynamically significant renal artery stenosis (with a systolic pressure gradient at the site of stenosis of - ΔP ≥ 20 mmHg, along with the ratio of the pressure in the distal part of the renal artery (Pd and aortic pressure (Pa less than 0.9 (Pd/Pa 0.8, chronic kidney disease (GFR <30 ml/min/1.73 m2 and negative captopril scintigraphy (lack of lateralization.

  11. Smooth muscle LDL receptor-related protein-1 deletion induces aortic insufficiency and promotes vascular cardiomyopathy in mice.

    Directory of Open Access Journals (Sweden)

    Joshua E Basford

    Full Text Available Valvular disease is common in patients with Marfan syndrome and can lead to cardiomyopathy. However, some patients develop cardiomyopathy in the absence of hemodynamically significant valve dysfunction, suggesting alternative mechanisms of disease progression. Disruption of LDL receptor-related protein-1 (Lrp1 in smooth muscle cells has been shown to cause vascular pathologies similar to Marfan syndrome, with activation of smooth muscle cells, vascular dysfunction and aortic aneurysms. This study used echocardiography and blood pressure monitoring in mouse models to determine whether inactivation of Lrp1 in vascular smooth muscle leads to cardiomyopathy, and if so, whether the mechanism is a consequence of valvular disease. Hemodynamic changes during treatment with captopril were also assessed. Dilation of aortic roots was observed in young Lrp1-knockout mice and progressed as they aged, whereas no significant aortic dilation was detected in wild type littermates. Diastolic blood pressure was lower and pulse pressure higher in Lrp1-knockout mice, which was normalized by treatment with captopril. Aortic dilation was followed by development of aortic insufficiency and subsequent dilated cardiomyopathy due to valvular disease. Thus, smooth muscle cell Lrp1 deficiency results in aortic dilation and insufficiency that causes secondary cardiomyopathy that can be improved by captopril. These findings provide novel insights into mechanisms of cardiomyopathy associated with vascular activation and offer a new model of valvular cardiomyopathy.

  12. Suppression of TGF-β1/Smad signaling pathway by sesamin contributes to the attenuation of myocardial fibrosis in spontaneously hypertensive rats.

    Directory of Open Access Journals (Sweden)

    Mengqiu Zhao

    Full Text Available This study investigated the effect of sesamin on myocardial fibrosis in spontaneously hypertensive rats (SHRs and the possible mechanisms involved. Twenty-eight male SHRs were randomly allocated to SHR group, Ses160 group (sesamin 160 mg/kg, Ses80 group (sesamin 80 mg/kg and Cap30 group (captopril 30 mg/kg. Seven male WKY rats were used as control. Sesamin and captopril were administered intragastrically for 12 weeks. Captopril significantly reduced systolic blood pressure and angiotensin II (Ang II levels in SHRs, accompanied by a marked attenuation of left ventricular hypertrophy (LVH and collagen deposition (P <0.05 or P <0.01. Though sesamin had no significant influence on Ang II levels, and the hypotensive effect was also significantly inferior to that of captopril (P <0.05 or P <0.01, however, the improvement of LVH and collagen deposition was similar to that in captopril group. Sesamin markedly reduced transforming growth factor-β1 (TGF-β1 content in cardiac tissues, with Smad3 phosphorylation decreased and Smad7 protein expression increased notably (P <0.05 or P <0.01. Protein expression of type I collagen and type III collagen, target genes of Smad3, was down-regulated markedly by sesamin (P <0.05 or P <0.01. In addition, sesamin significantly increased total antioxidant capacity and superoxide dismutase protein in cardiac tissues (P <0.05 or P <0.01, while the expression of NADPH oxidase subunit p47phox and malondialdehyde content were reduced markedly (P <0.05 or P <0.01. In vitro studies also demonstrated that sesamin was able to suppress Ang II induced phosphorylation of Smad3 and secretion of TGF-β1 and type I and type III collagen in cultured rat cardiac fibroblasts. These data suggest that sesamin is capable of attenuating hypertensive myocardial fibrosis through, at least partly, suppression of TGF-β1/Smad signaling pathway.

  13. A RETROSPECTIVE STUDY ON THE POTENTIAL DRUG INTERACTION BETWEEN ANGIOTENSIN CONVERTING ENZYME INHIBITOR OR ANGIOTENSIN RECEPTOR ANTAGONIST AND OTHER DRUGS IN END-STAGE CHRONIC RENAL FAILURE PATIENTS

    Directory of Open Access Journals (Sweden)

    Honey Iskandar

    2012-10-01

    Full Text Available Increasing number of chronic renal failure (CRF patients had reflected an increase in the number of patients with diabetes and hypertension. Therefore, health practitioners would be faced with management of complicated medical problems for the patients of chronic renal disease. In this way, various complications of chronic renal failure would lead to polypharmacy, where the patients receive three to five drugs in a dose. Development of polypharmacy had made the potential of drug interaction greater. The objective was to determine whether CRF patients admitted to hospital with specific adverse drug reactions were likely to have been prescribed with interacting drugs. Retrospective study was designed. The study was conducted at the General Practice Rooms Floor 1 – Floor VI of Central Army Hospital Gatot Soebroto Jakarta. The study was conducted from December 2011 – February 2012. The data were collected in a retrospective way for a year (January – December 2011. End-stage CRF patients who were having hemodialysis therapy and receiving ACE Inhibitor drugs or Angiotensin II Receptor Antagonist (AIIRA and receiving treatment at the General Practice Rooms at Central Army Hospital Gatot Soebroto Jakarta. During the period of January – December 2011, 84 patients were treated with end-stage CRF at the Central Army Hospital and having routine hemodialysis and 44 patients were receiving therapy with ACE Inhibitor and AIIRA. Other drugs simultaneously given with ACE Inhibitor and AIIRA were captopril-spironolactone, captopril-aspirin, captopril-allopurinol, captopril-KSR, captopril-furosemide, lisinopril-furosemide and valsartan-mefenemic acid. An increase in adverse effects of the drugs was found based on the clinical evaluation and laboratory examination. The adverse effects included hyperkalemia (9,09%, decrease in anti-hypertension effect (6,8%, acute hypotension (40%, and declining renal function (11,36%. The study identifies drug interaction

  14. Effect of different treatment methods on left ventricular remodeling after acute myocardial infarction%卡托普利联合美托洛尔治疗对改善急性心肌梗死后左心室重构的作用

    Institute of Scientific and Technical Information of China (English)

    彭晓玲

    2009-01-01

    Objective To study the effect of captopril combined with metoprolol and captopril alone on improving left ventricular remodeling(LVR)in acute myocardial infarction(AMI).Methods 100 AMI patients were randomly divided into treatment group of 50 cases(captopril combined metoprolol treatment)and 50 cases in the control group(captopril treatment).Using color Doppler ultrasound to deteimine left ventricular shape,configuration and indicators to compare two groups left ventricular remodeling after early(<2gh);3;6 month end.Results The indices of RaPD;ASL in control group after 6 months end[(63.01±4.10)%and(10.69 ±1.8)cm]were higher than the treatment group[(60.91±3.21)and(10.69±1.8)cm](t=2.121;2.210,all P<0.05);The LVEF in treatment group after 6 months(51.10±4.60)%were higher than the treatment group(49.10±5,10)%(t=2.231,P<0.05).Conclusion The captopril combined metoprolol on left ventricular remodeling inhibition significantly better than captopril alone in AMI.%目的 探讨应用卡托普利联合美托洛尔治疗对改善急性心肌梗死(AMI)后左心室重构的作用.方法 100例AMI患者随机分成治疗组50例(卡托普利联合美托洛尔治疗)和对照组50例(卡托普利治疗),采用彩色多普勒心动超声仪分别于发病后早期(<24 h)、3、6个月末观察左心室形态、构型等多项指标,比较两组发生左心室重构情况.结果 对照组6个月末RaPD、ASL分别为[(63.0l±4.10)%、(10.69±1.8)cm]高于治疗组[(60.91±3.21)、(10.69±1.8)cm](t=2.121、2.210,均P<0.05);治疗组6个月末LVEF(51.10±4.60)%高于对照组(49.10±5.10)%(t=2.231,P<0.05).结论 AMI后应用卡托普利联合美托洛尔对晚期并发左心室重构的抑制作用明显.

  15. EVALUASI PENGGUNAAN OBAT ANTI HIPERTENSI PADA PASIEN GAGAL GINJAL KRONIK YANG MENJALANI HEMODIALISIS

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    Woro Supadmi

    2011-05-01

    Full Text Available The intervention led to various complications in dialysis patients include hypertension intradialitik as a result of hemodynamic changes.The phenomenon of the paradox of which caused activation of endogenous vasopresor due to changes in volume status and antihypertensive medication terdialisisnya factor. This study aims to determine patterns of use of antihypertensive drugs, evaluating the rationality and side effects of antihypertensive drugs based on literarur. This study was performed with the patient’s condition based on the observation of patients to see medical records drug data, laboratory data of patients and patient’s condition.Retrospective study of hemodialysis patients in the hospital PKU Muhammadiyah Yogyakarta year period from 2009 to 2010. Patients according to inclusion criteria, anti-hypertensive drug receipts and complete medical record data. Evaluation of rationality involves the use of antihypertensive drugs right dose, right patient and side effects based on the Drug Information Hand Book 2005, Handbook of Clinical Drug Data, 2002. The study found 60 patients who fit the inclusion criteria. Based on the research patterns of use of antihypertensive drugs in patients with hemodialysis is captoril, furosemide, nifedipine, lisinopril, amlodipine, valsatran and clonidin. Evaluation rationality inappropriate use of drugs dose use of captopril 11 patients of 34 patients and furosemide 18 patients from 52 patients, inappropriate use of captopril patients was 9 patients of 34 patients.Side effects that occur in patients with hypokalemia due to the use of furosemide is 40 patients, cough due to captopril was 13 patients, side effects of nifedipine gastrointestinal disorders cough and 11 patients, 5 patients cough lisinopril. Conclusion:he use of antihypertensive medications in hemodialysis patientsat RSU PKU Muhammadiyah Yogyakarta is rational.

  16. Fosinopril and zofenopril, two angiotensin-converting enzyme (ACE) inhibitors, potentiate the anticonvulsant activity of antiepileptic drugs against audiogenic seizures in DBA/2 mice.

    Science.gov (United States)

    Sarro, Giovambattista De; Paola, Eugenio Donato Di; Gratteri, Santo; Gareri, Pietro; Rispoli, Vincenzo; Siniscalchi, Antonio; Tripepi, Giovanni; Gallelli, Luca; Citraro, Rita; Russo, Emilio

    2012-03-01

    The renin-angiotensin system (RAS) exists in the brain and it may be involved in pathogenesis of neurological and psychiatric disorders including seizures. The aim of the present research was to evaluate the effects of some angiotensin-converting enzyme inhibitors (ACEi; captopril, enalapril, fosinopril and zofenopril), commonly used as antihypertensive agents, in the DBA/2 mice animal model of generalized tonic-clonic seizures. Furthermore, the co-administration of these compounds with some antiepileptic drugs (AEDs; carbamazepine, diazepam, felbamate, gabapentin, lamotrigine, phenobarbital, phenytoin, topiramate and valproate) was studied in order to identify possible positive interactions in the same model. All ACEi were able to decrease the severity of audiogenic seizures with the exception of enalapril up to the dose of 100mg/kg, the rank order of activity was as follows: fosinopril>zofenopril>captopril. The co-administration of ineffective doses of all ACE inhibitors with AEDs, generally increased the potency of the latter. Fosinopril was the most active in potentiating the activity of AEDs and the combination of ACEi with lamotrigine and valproate was the most favorable, whereas, the co-administrations with diazepam and phenobarbital seemed to be neutral. The increase in potency was generally associated with an enhancement of motor impairment, however, the therapeutic index of combined treatment of AEDs with ACEi was predominantly more favorable than control. ACEi administration did not influence plasma and brain concentrations of the AEDs studied excluding pharmacokinetic interactions and concluding that it is of pharmacodynamic nature. In conclusion, fosinopril, zofenopril, enalapril and captopril showed an additive anticonvulsant effect when co-administered with some AEDs, most notably carbamazepine, felbamate, lamotrigine, topiramate and valproate, implicating a possible therapeutic relevance of such drug combinations.

  17. Differential cognitive outcomes in the Hypertensive Old People in Edinburgh study.

    Science.gov (United States)

    Starr, John M; Whalley, Lawrence J

    2005-03-15

    Hypertension is associated with cognitive impairment in older adults. The Hypertensive Old People in Edinburgh (HOPE) study reported improved scores in two psychometric tests in those subjects with the greatest fall in diastolic blood pressure during a 24-week randomised, double-blind trial of captopril versus bendrofluazide in 81 elderly hypertensive people with mild cognitive impairment. Three hundred and eighty-seven of the original sample of 603 older people with and without hypertension and/or cognitive impairment from which the trial subsample was drawn were available for adequate psychometric testing 4 years later. Blood pressure was related prospectively to Raven's Progressive Matrices (RPM), a measure of fluid intelligence, but not memory differences. RPM scores were obtained at baseline, 6 weeks, 12 weeks and at the end of the randomised controlled trial. For subjects on captopril mean scores at each time point adjusted for blood pressure change were 27.6 (95% CI 25.5-29.6), 27.2 (95% CI 25.1-29.2), 28.4 (95% CI 26.6-30.3) and 28.9 (95% CI 26.9-30.9), and for bendrofluazide 27.1 (95% CI 25.1-29.0), 28.9 (95% CI 26.9-30.9), 28.9 (95% CI 27.2-30.7) and 28.7 (95% CI 26.8-30.6). There was a significant improvement in scores for those on bendrofluazide compared with captopril at week 6 (F=8.10, p=0.006, partial eta2=0.11). There were no significant effects for either drug or blood pressure at any time point for tests of memory. Future trials of the effects of antihypertensive therapy on cognition should focus more on outcomes other than memory. Early differential effects of therapeutic agents may not be maintained.

  18. Blockade of Rennin-Angiotensin system blunts the fibrotic response in experimental acute pyelonephritis

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    Singal A

    2005-01-01

    Full Text Available Aim: To study the impact of Renin-Angiotensin system blockade in experimental acute pyelonephritis, induced by a novel surgical approach via dorsal lumbotomy incision. Materials and Methods : 45 Adult female WISTAR rats aged 8-12 weeks, underwent direct inoculation of 0.1 ml of E.coli suspension into the parenchyma of the surgically exposed kidney. 3 groups of rats were studied: Group A - treated with antibiotics only; Group B- Captopril and antibiotics and Group C- Losartan and antibiotics. Changes of acute inflammation, parenchymal destruction and scarring were compared between the groups on histopathological sections. Kruskal-Wallis test was used for statistical analysis. Results : Changes consistent with acute pyelonephritis were seen in all the kidneys. Mean% scar area in Group A, Group B and Group C was 37.08±1.79, 24.40±1.88 and 24.68±1.32% respectively at end of six weeks. Mean tubular density in Group A, B and C was 17.26±1.92, 47.18±3.00 and 47.00±5.08-tubules/lac mm2 respectively. The differences between the control and the treated animals were significant, though the results did not differ between the losartan and captopril treated rats. Conclusions : Dorsal lumbotomy approach to the kidney provides a good exposure of the kidney. Induction of acute pyelonephritis by direct inoculation of bacteria into renal cortex produced a consistent scar at 6 weeks. Blockade of renin angiotensin system by either captopril or losartan decreased the renal scar area by almost 1/3 at 6 weeks.

  19. The anti-inflammatory peptide Ac-SDKP is released from thymosin-β4 by renal meprin-α and prolyl oligopeptidase.

    Science.gov (United States)

    Kumar, Nitin; Nakagawa, Pablo; Janic, Branislava; Romero, Cesar A; Worou, Morel E; Monu, Sumit R; Peterson, Edward L; Shaw, Jiajiu; Valeriote, Frederick; Ongeri, Elimelda M; Niyitegeka, Jean-Marie V; Rhaleb, Nour-Eddine; Carretero, Oscar A

    2016-05-15

    N-acetyl-seryl-aspartyl-lysyl-proline (Ac-SDKP) is a natural tetrapeptide with anti-inflammatory and antifibrotic properties. Previously, we have shown that prolyl oligopeptidase (POP) is involved in the Ac-SDKP release from thymosin-β4 (Tβ4). However, POP can only hydrolyze peptides shorter than 30 amino acids, and Tβ4 is 43 amino acids long. This indicates that before POP hydrolysis takes place, Tβ4 is hydrolyzed by another peptidase that releases NH2-terminal intermediate peptide(s) with fewer than 30 amino acids. Our peptidase database search pointed out meprin-α metalloprotease as a potential candidate. Therefore, we hypothesized that, prior to POP hydrolysis, Tβ4 is hydrolyzed by meprin-α. In vitro, we found that the incubation of Tβ4 with both meprin-α and POP released Ac-SDKP, whereas no Ac-SDKP was released when Tβ4 was incubated with either meprin-α or POP alone. Incubation of Tβ4 with rat kidney homogenates significantly released Ac-SDKP, which was blocked by the meprin-α inhibitor actinonin. In addition, kidneys from meprin-α knockout (KO) mice showed significantly lower basal Ac-SDKP amount, compared with wild-type mice. Kidney homogenates from meprin-α KO mice failed to release Ac-SDKP from Tβ4. In vivo, we observed that rats treated with the ACE inhibitor captopril increased plasma concentrations of Ac-SDKP, which was inhibited by the coadministration of actinonin (vehicle, 3.1 ± 0.2 nmol/l; captopril, 15.1 ± 0.7 nmol/l; captopril + actinonin, 6.1 ± 0.3 nmol/l; P Ac-SDKP after actinonin treatment. We conclude that release of Ac-SDKP from Tβ4 is mediated by successive hydrolysis involving meprin-α and POP.

  20. Flax lignan concentrate attenuate hypertension and abnormal left ventricular contractility via modulation of endogenous biomarkers in two-kidney-one-clip (2K1C hypertensive rats

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    Sameer Hanmantrao Sawant

    Full Text Available ABSTRACT The present investigation was designed to study the effect of flax lignan concentrate obtained from Linum usitatissimum L., Linaceae, in two-kidney, one clip (2K1C hypertension model in Wistar rats. 2K1C Goldblatt model rats were divided randomly into six groups: sham, 2K1C control, captopril (30 mg/kg, flax lignan concentrate (200, 400 and 800 mg/kg. Flax lignan concentrate and captopril were administered daily for eight consecutive weeks. Sham-operated, and 2K1C control rats received the vehicle. Treatment with flax lignan concentrate (400 and 800 mg/kg significantly and dose-dependently restored the hemodynamic parameters systolic blood pressure, diastolic blood pressure, mean arterial blood pressure and left ventricular functions. The flax lignan concentrate significantly restored the elevated hepatic, renal and cardiac marker enzymes in the serum. It also restored the organs weights (kidney and heart, serum electrolyte level and histological abnormalities. Furthermore, flax lignan concentrate significantly elevated the level of biochemical markers that is enzymatic antioxidants superoxide dismutase, glutathione and decreased malondialdehyde in the heart and kidney tissues. Meanwhile, we found that plasma nitric oxide and plasma nitric oxide synthase contents were significantly increased in the flax lignan concentrate-treated group, and plasma endothelin-1 and renal angiotensin-II levels were significantly lower than 2K1C hypertensive group. In conclusion, the antihypertensive and antioxidant effect of flax lignan concentrate were dose-dependent and at the highest dose (i.e. 800 mg/kg similar to those of captopril (30 mg/kg. It is suggested that flax lignan concentrate reduced blood pressure by reduction of renal angiotensin-II level, inhibition of plasma endothelin-1 production, induction of the nitric oxide, nitric oxide synthase and in vivo antioxidant defense system.

  1. High Dose Astaxanthin Lowers Blood Pressure and Increases Insulin Sensitivity in Rats: Are These Effects Interdependent?

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    Harry G. Preuss, Bobby Echard, Eiji Yamashita, Nicholas V. Perricone

    2011-01-01

    Full Text Available The present investigation in Sprague-Dawley rats (SD was designed to examine effects of astaxanthin (Asta at different doses on elevated blood pressure (BP and glucose-insulin perturbations produced by heavy sucrose ingestion. We also examined effects of Asta on BP during restraint stress. SD were divided into six groups each containing eight rats. All SD ate a basic diet of ground regular rat chow with sucrose added at 30% w/w. The Control group received only the basic diet containing added sucrose, while the other five groups each received the same diet with added test material: captopril, (30 mg/Kg, pioglitazone (15.0 mg/Kg, low Asta (25 mg/Kg, medium Asta (50 mg/kg or high Asta (100 mg/Kg. Many tests were carried out to examine the mechanisms behind the effects of Asta on BP (serum ACE activity, losartan challenge, and LNAME challenge and the glucose-insulin system (glucose tolerance, HOMA measurement, and insulin challenge. In SD, a relatively low dose of Asta decreased SBP, but produced no major changes in the glucose-insulin system simulating results from a previous study using Zucker Fatty Rats. Increasing the dose of Asta resulted in both a lowering of elevated systolic BP and enhanced insulin sensitivity determined by many different estimations. BP lowering was consistent with changes in the renin-angiotensin (RAS and nitric oxide (NO systems. At the examined doses of each, captopril lowered BP in SD without influencing glucose-insulin metabolism, whereas pioglitazone favorably affected glucose-insulin metabolism while showing essentially no effects on BP. Accordingly, Asta beneficially affects both sucrose-induced elevations of BP and insulin resistance at relatively high doses in SD. Also, Asta at higher doses lessens restraint stress, whereas, captopril and pioglitazone did not at the doses examined, even though they influenced the BP and glucose-insulin systems respectively.

  2. Efecto hipotensor del extracto de ajo (Allium sativum macerado por 18 semanas en un modelo experimental in vivo

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    David Chaupis-Meza

    Full Text Available Objetivos. Determinar si el extracto de ajo (Allium sativum macerado por 18 semanas tiene igual o mejor efecto hipotensor que el captopril en ratas. Materiales y métodos. Se realizó un estudio experimental in vivo con ratas machos Holtzman, clasificados en cinco grupos: 100, 500 y 1000 mg/kg de extracto de ajo, Captopril de 100 mg/kg y un grupo vehículo. El L-NAME (N- -nitro L-arginina-metil-éster administrado vía intraperitoneal 50 mg/kg desde el inicio del experimento, elevó la presión arterial desde el tercer día. El análisis estadístico consistió en las pruebas T de Student para medias pareadas, ANOVA y comparación múltiple de Scheffe. Resultados. El ajo macerado extraído por un proceso hidroalcohólico durante 18 semanas provocó una disminución de la presión arterial en animales de experimentación. El análisis de los tratamientos sobre la presión arterial media (PAM, obtuvieron diferencias significativas desde el tercer día. La comparación sobre la PAM final versus PAM basal (medias no diferentes y el efecto hipotensor (% fueron: ajo-100 (p=0,008, 59,8%; ajo-500 (p=0,021, 80,6%; ajo-1000 (p=0,034, 88,5%, Captopril (p=0,437, 99,9% y vehículo (p=0,001, 0%. Conclusiones. El ajo macerado a un periodo de 18 semanas resultó eficaz para producir un efecto hipotensor en ratas, inducidas a hipertensión arterial por L-NAME

  3. Efecto hipotensor del extracto de ajo (Allium sativum macerado por 18 semanas en un modelo experimental in vivo

    Directory of Open Access Journals (Sweden)

    David Chaupis-Meza

    2014-07-01

    Full Text Available Objetivos. Determinar si el extracto de ajo (Allium sativum macerado por 18 semanas tiene igual o mejor efecto hipotensor que el captopril en ratas. Materiales y métodos. Se realizó un estudio experimental in vivo con ratas machos Holtzman, clasificados en cinco grupos: 100, 500 y 1000 mg/kg de extracto de ajo, Captopril de 100 mg/kg y un grupo vehículo. El L-NAME (N- -nitro L-arginina-metil-éster administrado vía intraperitoneal 50 mg/kg desde el inicio del experimento, elevó la presión arterial desde el tercer día. El análisis estadístico consistió en las pruebas T de Student para medias pareadas, ANOVA y comparación múltiple de Scheffe. Resultados. El ajo macerado extraído por un proceso hidroalcohólico durante 18 semanas provocó una disminución de la presión arterial en animales de experimentación. El análisis de los tratamientos sobre la presión arterial media (PAM, obtuvieron diferencias significativas desde el tercer día. La comparación sobre la PAM final versus PAM basal (medias no diferentes y el efecto hipotensor (% fueron: ajo-100 (p=0,008, 59,8%; ajo-500 (p=0,021, 80,6%; ajo-1000 (p=0,034, 88,5%, Captopril (p=0,437, 99,9% y vehículo (p=0,001, 0%. Conclusiones. El ajo macerado a un periodo de 18 semanas resultó eficaz para producir un efecto hipotensor en ratas, inducidas a hipertensión arterial por L-NAME

  4. Effects of angiotensin-converting enzyme inhibition on altered renal hemodynamics induced by low protein diet in the rat.

    OpenAIRE

    Fernández-Repollet, E; Tapia, E; Martínez-Maldonado, M

    1987-01-01

    We assessed the role of angiotensin II in mediating the alterations in renal hemodynamics known to result from low protein feeding to normal rats by examining the effect of the angiotensin-converting enzyme (ACE) inhibitor captopril. 2 wk of low protein (6% casein) diet resulted in decreased glomerular filtration rate (normal protein [NP], 1.82 +/- 0.17 vs. low protein [LP], 0.76 +/- 0.01 ml/min; P less than 0.05) and renal plasma flow (NP, 6.7 +/- 0.2 vs. LP, 3.3 +/- 0.3 ml/min; P less than ...

  5. Synthesis and characterization of nanoscale magnetic drug-inorganic composites

    Institute of Scientific and Technical Information of China (English)

    SUN Hui; ZHANG Hui; David G. Evans; DUAN Xue

    2005-01-01

    The synthesis by direct coprecipitation and characterization of captopril (Cpl) and 5-aminosalicylic acid (5-ASA) intercalated ZnAl layered double hydroxides coated on MgFe2O4 magnetic core particles are reported. Powder XRD analysis shows the well-defined crystallite structure of the composites. TEM and XPS results reveal that a core-shell structure involving a drug-LDHs layer coated on MgFe2O4 particles is formed through Zn-O-Mg and/or Al-O-Mg linkages. VSM measurements demonstrate that the novel magnetic drug-inorganic composites possess considerable magnetization.

  6. Factores inmunereactivos "digoxin-like" en la natriuresis tras expansi??n de volumen central inducida por atiortostatismo : Interrelaciones con el SRA-aldosterona ADH y prostaglandinas

    OpenAIRE

    Rodr??guez L??pez, Ju??n

    1989-01-01

    el antiortostatismo se muestra como m??todo de expansi??n de volumen con natriuresis, diuresis, (-) adh, (-) s.r.a.-aldosterona, pero no como m??todo que produzca elevaci??n de los f.digoxin-like. el tratamiento previo con captopril incrementa la diuresis y natriuresis con respecto al grupo control, tambi??n incrementa la diuresis y natriuresis con respecto al grupo control, al igual que los niveles hormonales de adh, aldosterona y digoxin-like por una flujo dependencia de orina que se ve cor...

  7. VALsartan In Acute myocardial iNfarcTion (VALIANT) trial: baseline characteristics in context

    DEFF Research Database (Denmark)

    Velazquez, Eric J; Pfeffer, Marc A; McMurray, John V

    2003-01-01

    BACKGROUND: The VALsartan In Acute myocardial iNfarcTion (VALIANT) trial compared outcomes with: (1) angiotensin-converting enzyme inhibition (ACEI) with the reference agent captopril; (2) angiotensin-receptor blockade (ARB) with valsartan; or (3) both in patients with heart failure (HF) and....../or left ventricular systolic dysfunction (LVSD) after myocardial infarction (MI). AIMS: a goal of this active-control trial was to simulate conditions that would lead current practitioners to use ACEIs. Thus, we compared characteristics of VALIANT patients with those of patients in placebo...

  8. Hyponatremic Hypertensive Syndrome in an Obese Man with Renal Ischemia

    Directory of Open Access Journals (Sweden)

    Saeed Khawer

    2006-01-01

    Full Text Available Renovascular hypertension occasionally manifests as an electrolyte disorder. The combination of hyponatremia and renovascular hypertension is known as hyponatremic-hypertensive syndrome. This syndrome was initially reported in children. Here, we describe a 45 year-old Saudi man who was admitted to the hospital with generalized body weakness and inability to walk. He was confused and was noted to have severe hypertension and very low serum sodium and potassium. The patient was recently started on captopril for blood pressure control, which was discontinued because of deterioration of renal function. Color Doppler renal ultrasound, and magnetic resonance angiography confirmed the diagnosis of renal artery stenosis.

  9. CONTROLE DE QUALIDADE DE MEDICAMENTOS ANTI-HIPERTENSIVOS SIMILARES COMERCIALIZADOS EM FARMÁCIAS DE IMPERATRIZ, MA, BRASIL

    OpenAIRE

    Ribeiro, Paulo Roberto da Silva

    2012-01-01

    A Hipertensão Arterial (HA) é uma doença crônica e multifatorial. O captopril (CPT) é um inibidor da enzima conversora de angiotensina amplamente utilizado no tratamento da HA. Casos de falsificação de medicamentos contendo CPT foram relatados e representam um perigo para a saúde dos pacientes que deles necessitam. O objetivo deste estudo foi avaliar a qualidade dos medicamentos similares contendo CPT. Para tanto, foi realizado o controle de qualidade físico-químico de doze amostras de CPT em...

  10. Lichen planus pemphigoides induced by a weight reduction drug.

    Science.gov (United States)

    Rosmaninho, Aristoteles; Sanches, Madalena; Oliveira, Ana; Alves, Rosario; Selores, Manuela

    2011-12-01

    Lichen planus pemphigoides is a rare autoimmune dermatosis characterized by bullous lesions arising on lichen planus (LP) papules and on clinically uninvolved skin, coexistence of histological features of LP and bullous pemphigoid and linear deposits of IgG and/or C3 along the basal membrane zone on direct immunofluorescence of peribullous skin. LPP has been reported to be associated with several medications such as ramipril, cinnarizine, simvastatin, captopril, psoralen ultraviolet A therapy and antituberculous medications. We report a case of a 41-year-old woman with LPP associated with a weight reduction drug.

  11. Lichen Planus Pemphigoides Associated with Bisoprolol

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    Turna İlknur

    2012-06-01

    Full Text Available Lichen planus pemphigoides (LPP is a disease characterized by tense bullae arising on lichen planus papules and on clinically uninvolved skin, lichenoid infiltration and subepidermal bulla in histopathology, and linear deposits of IgG and C3 along basal membrane zone on direct immunofluorescence. This rare bullous dermatosis is usually idiopathic. However, in a few cases in the literature, it has been reported to be induced by hepatitis B, malignancies, phototherapy and some medications such as ramipril, captopril, cinnarizine and simvastatin. We reported a 35-year-old woman with LPP possibly induced by bisoprolol.

  12. Controlled release from thermo-sensitive PNVCL-co-MAA electrospun nanofibers: The effects of hydrophilicity/hydrophobicity of a drug.

    Science.gov (United States)

    Liu, Lin; Bai, Shaoqing; Yang, Huiqin; Li, Shubai; Quan, Jing; Zhu, Limin; Nie, Huali

    2016-10-01

    The thermo-sensitive copolymer poly(N-vinylcaprolactam-co-methacrylic acid) (PNVCL-co-MAA) was synthesized by free radical polymerization and the resulting nanofibers were fabricated using an electrospinning process. The molecular weight of the copolymer was adjusted by varying the content of methacrylic acid (MAA) while keeping that of N-vinylcaprolactam (NVCL) constant. Hydrophilic captopril and hydrophobic ketoprofen were used as model drugs, and PNVCL-co-MAA nanofibers were used as the drug carrier to investigate the effects of drug on its release properties from nanofibers at different temperatures. The results showed that slow release over several hours was observed at 40°C (above the lower critical solution temperature (LCST) of PNVCL-co-MAA), while the drugs exhibited a burst release of several seconds at 20°C (below the LCST). Drug release slowed with increasing content of the hydrophobic monomer NVCL. The hydrophilic captopril was released at a higher rate than the hydrophobic ketoprofen. The drug release characteristics were dependent on the temperature, the portion of hydrophilic groups and hydrophobic groups in the copolymer and hydrophilicity/hydrophobicity of drug. Study on the mechanism of release showed that Korsmeyer-Peppas model as a major drug release mechanism. Given these results, the PNVCL-co-MAA copolymers are proposed to have useful applications in intellectual drug delivery systems.

  13. Evaluation of the rat embryo culture system as a predictive test for human teratogens.

    Science.gov (United States)

    Guest, I; Buttar, H S; Smith, S; Varma, D R

    1994-01-01

    Ingestion of the anticonvulsant drug valproic acid and of the angiotensin converting enzyme inhibitor captopril during pregnancy has been associated with abnormal fetal outcome in humans. In contrast, the use of the antiinflammatory drug ibuprofen and the antihistamine diphenhydramine has not been documented to be embryotoxic in humans. We evaluated the rat embryo culture system as a predictive model of teratogenesis, using these four drugs as test agents. Valproic acid, ibuprofen, and diphenhydramine were embryotoxic, inducing concentration-dependent decreases in growth and a significant increase in anomalies. Valproic acid caused an increase in neural tube defects, ibuprofen increased the incidence of abnormal maxillary processes, and diphenhydramine increased the number of embryos with distorted body morphology. These abnormalities were induced at concentrations of valproic acid and diphenhydramine that are used clinically, but ibuprofen only induced toxicity at concentrations greatly exceeding the therapeutic range. Captopril was not embryotoxic up to 5 mM, the highest concentration tested. These results suggest that the rat embryo culture system produces both false positive and false negative data on the teratogenic potential of drugs. Although such an in vitro assay may be suitable to determine the mechanism of teratogenesis, it is not a sensitive indicator of potential human teratogens on its own. These data support the view that in vitro systems can only supplement clinical and epidemiological observations in humans, possibly as a method to determine mechanisms of actions of teratogens.

  14. A new biolistic intradermal injector

    Science.gov (United States)

    Brouillette, M.; Doré, M.; Hébert, C.; Spooner, M.-F.; Marchand, S.; Côté, J.; Gobeil, F.; Rivest, M.; Lafrance, M.; Talbot, B. G.; Moutquin, J.-M.

    2016-01-01

    We present a novel intradermal needle-free drug delivery device which exploits the unsteady high-speed flow produced by a miniature shock tube to entrain drug or vaccine particles onto a skin target. A first clinical study of pain and physiological response of human subjects study is presented, comparing the new injector to intramuscular needle injection. This clinical study, performed according to established pain assessment protocols, demonstrated that every single subject felt noticeably less pain with the needle-free injector than with the needle injection. Regarding local tolerance and skin reaction, bleeding was observed on all volunteers after needle injection, but on none of the subjects following powder injection. An assessment of the pharmacodynamics, via blood pressure, of pure captopril powder using the new device on spontaneously hypertensive rats was also performed. It was found that every animal tested with the needle-free injector exhibited the expected pharmacodynamic response following captopril injection. Finally, the new injector was used to study the delivery of an inactivated influenza vaccine in mice. The needle-free device induced serum antibody response to the influenza vaccine that was comparable to that of subcutaneous needle injection, but without requiring the use of an adjuvant. Although no effort was made to optimize the formulation or the injection parameters in the present study, the novel injector demonstrates great promise for the rapid, safe and painless intradermal delivery of systemic drugs and vaccines.

  15. SINERGISMO FARMACODINÁMICO. A PROPÓSITO DE UN CASO INTERVENIDO QUIRÚRGICAMENTE DE URGENCIA BAJO ANESTESIA GENERAL.

    Directory of Open Access Journals (Sweden)

    Yesid Pallares Villarreal

    2004-01-01

    Full Text Available Presentamos una paciente femenina geriatrica con antecedentes de hipertensiòn arterial y trastornos psiquiatricos intervenida quirurgicamente de urgencia por un cuadro doloroso abdominal, con una interaccion farmacodinamica por sinergismo del doxepin y captopril potenciada por los efectos de la anestesia general. La hipotensiòn arterial fue la forma clínica de presentación. La paciente se recibió hipotensa por la administración preoperatoria de doxepin tratamiento de base y de captopril tratamiento impuesto por crisis hipertensiva antes de su llegada al hospital. Después de la inducción de la anestesia general desarrolla hipotensión arterial que sólo responde a la administración de noradrenalina. En un inicio se interpreta como un shock séptico en fase hipodinámica por el cuadro doloroso abdominal y la vasoplejia pero descartadas otras causas se concluye como hipotensión arterial de origen farmacológico con relación a la ingestión de antidepresivos triciclicos e inhibidores de la enzima convertora de angiotensina I en angiotensina II por su acción sobre el sistema nervioso simpático por potenciada por los agentes anestésicos. La paciente fue dada de alta del hospital satisfactoriamente a los 7 dias de operada.

  16. Inhibitory effects of Veratrum nigrum L. Var. ussurience Nakai alkaloids on the hypertrophy of cardiomyocytes from neonatal rat

    Institute of Scientific and Technical Information of China (English)

    WANG Li; LI Shu-yuan; LI Hua; ZHOU Qin

    2008-01-01

    Objective To examine the effects of Veratrum nigrum L. Vat. ussurience Nakai alkaloids (VnA) on angiotensin Ⅱ (Ang Ⅱ)-induced cardiomyocyte hypertrophy and to explore its possible mechanism. Methods The cadiocytes were induced by Ang Ⅱ to set up myocardial hypertrophy model, the animals were divided into six groups according to the different treatments: control group, model group, positive control group, VnA group (low, middle and high dose). The cell protein content, the cell diameter and the expression of calcineurin (CAN) were measured respectively by BCA method, the micrometer and immunofluo-rescence analysis. Results VnA (middle and high dose) and Captopril inhibited significantly the increase in the protein content induced by Ang Ⅱ (P<0.01). VnA and Captopril inhibited significantly the increase in the diameters induced by Ang Ⅱ (P< 0.01). By immunofluorescence analysis, the expression of calcineurin (CAN) was obviously increased in the Ang Ⅱ-induced model group. VnA decreased the expression of CaN significantly. Conclusions VnA could inhibit the cardiomyocyte hypertrophy induced by Ang Ⅱ significantly in a dose-dependent manner. The possible mechanism may be related to the inhibition of CAN expression.

  17. Generation of a 90 000 molecular weight fragment from human plasma angiotensin-I-converting enzyme by enzymatic or alkaline hydrolysis.

    Science.gov (United States)

    Yotsumoto, H; Lanzillo, J J; Fanburg, B L

    1983-12-12

    A catalytically active Mr 90 000 fragment was generated from native Mr 140 000 human plasma angiotensin-I-converting enzyme after treatment with reagents that induced a perturbation of the native tertiary conformation. Treatment of converting enzyme with 6 M urea produced an aggregation of molecules that was susceptible to proteolysis by either trypsin, chymotrypsin or Staphylococcus aureus V8 proteinase to generate the Mr 90 000 converting enzyme. Also, 1 M ammonium hydroxide, pH 11.3, or 0.01 M sodium hydroxide, pH 11.3, cleaved converting enzyme to the Mr 90 000 fragment. Degradation was not an autocatalytic phenomenon, since it was not prevented by inhibition of converting enzyme with EDTA. The enzymatically mediated, but not the alkaline mediated, cleavage was inhibited by specific converting enzyme inhibitors captopril and Merck L-154,826. This suggests that captopril and Merck L-154,826 can prevent converting-enzyme degradation by preserving a conformation that does not have sites exposed to proteolytic enzymes. This conformation may mimic the native conformation which is quite resistant to serine proteinases.

  18. Data of the natural and pharmaceutical angiotensin-converting enzyme inhibitor isoleucine-tryptophan as a potent blocker of matrix metalloproteinase-2 expression in rat aorta

    Directory of Open Access Journals (Sweden)

    Irakli Kopaliani

    2016-09-01

    Full Text Available The present data are related to the research article entitled “Whey peptide isoleucine–tryptophan inhibits expression and activity of matrix metalloproteinase-2 in rat aorta” [1]. Here we present data on removal of endothelium from aorta, endothelium dependent aortic relaxation and inhibition of expression of pro-MMP2 by di-peptide isoleucine–tryptophan (IW. Experiments were performed in rat aortic endothelial cells (EC and smooth muscle cells (SMC in vitro, along with isolated rat aorta ex vivo. The cells and isolated aorta were stimulated with angiotensin II (ANGII or angiotensin I (ANGI. ACE activity was inhibited by treatment with either IW or captopril (CA. Losartan was used as a blocker of angiotensin type-1 receptor. IW inhibited MMP2 protein expression induced with ANGI in a dose-dependent manner. IW was effective both in ECs and SMCs, as well as in isolated aorta. Similarly, captopril (CA inhibited ANGI-induced MMP2 protein expression in both in vitro and ex vivo. Neither IW nor CA inhibited ANGII-induced MMP2 protein expression in contrast to losartan. The data also displays that removal of endothelium in isolated rat aorta abolished the endothelium-dependent relaxation induced with acetylcholine. However, SMC-dependent relaxation induced with sodium nitroprusside remained intact. Finally, the data provides histological evidence of selective removal of endothelial cells from aorta.

  19. 蛇毒舒缓激肽增强肽%Snake venom bradykinin potentiating peptide

    Institute of Scientific and Technical Information of China (English)

    李旭慧; 权燕敏; 吴晓莎; 杨章民

    2013-01-01

    舒缓激肽增强肽(bradykinin potentiating peptide,BPP)是广泛分布于蝰科(主要是蝮亚科)蛇毒中的一类小分子生物活性肽.BPP具有增强舒缓激肽以及抑制血管紧张素Ⅰ转化酶(angiotensin-Ⅰ converting enzyme,ACE)活性的双重毒理学作用,是造成被毒蛇咬伤时血压骤降的主要组分,也是降压药开博通(Captopril)的天然模式分子.本文简要综述了蛇毒BPP分布与种类、结构和生物学功能等方面的研究进展.%Bradykinin potentiating peptides (BPPs) represent a class of short chain peptides with multiple biological activities,which are distributed widely in the snake venoms of Viperidae (mainly Crotalinae).BPPs can potentiate the actions of bradykinin,and can inhibit the activity of angiotensin-Ⅰ converting enzyme (peptidyl-dipeptidase A) 1 (ACE).The cooperative effects lead to lower the blood pressure in snakebite envenomation,and make it possible to be a natural lead for the anti-hypertension drug (Captopril) design.Here,we briefly review the recent advances in snake venom BPPs,including their distribution,variety,structure and biological functions.

  20. INFLUENCE OF COMBINED ANTIHYPERTENSIVE AND ANTIDEPRESSANT THERAPY ON LEFT VENTRICULAR REMODELING IN PATIENTS WITH ARTERIAL HYPERTENSION, ANXIETY AND DEPRESSION

    Directory of Open Access Journals (Sweden)

    Y. A. Vasyuk

    2008-01-01

    Full Text Available Aim. To assess influence of combined antihypertensive (captopril or metoprolol and antidepressant (thianeptin or sertralin therapy on clinical status, blood pressure (BP and myocardial function in patients with arterial hypertension (HT and affective disorders (AD.Material and methods. 106 patients with HT were involved in the study. 64 patients (60,4% had concomitant AD. All patients were divided into 3 groups. 46 patients with HT and AD were included in the 1-st group. They received metoprolol or captopril in combination with tianeptine or sertaline. The 2-nd group included 18 patients with HT and AD who received only antihypertensive therapy. The 3-rd group consisted of 42 patients with HT without AD. They also received only antihypertensive therapy.Results. After 6 month therapy patients of the 1-st and the 3-rd groups had more significant clinical improvement and BP reduction (according to 24- hour BP monitoring as well as more farourable structural and functional changes of left ventricular in comparison with patients of the 2-nd group.Conclusion. In patients with HT and concomitant AD combined antihypertensive and antidepressant therapy result in favourable clinical changes, effectively reduce BP, improve left ventricular structure and function.

  1. EFFECT OF CHRONIC ACE INHIBITION ON GLUCOSE TOLERANCE AND INSULIN SENSITIVITY IN HYPERTENSIVE TYPE 2 DIABETIC PATIENTS

    Institute of Scientific and Technical Information of China (English)

    尹卫东; G.Seghieri; C.Boni,G,Sanna; R.Anichinl; G.Bartolomei; E.Ferrannini

    1994-01-01

    We studied 14 moderately overweight Type 2 diabetic patients with essential hypertension in stable metabolic control after a run-in period,and again after 3 months of antihypertensive treatment with the angiotensin-convert-ing enzyme(ACE)inhibitor captopril.Glucose tolerance was tested with a 75g oral glucose load (OGTT) and in-sulin sensitivity was measured by the insulin suppression test (IST)while dietary and drug treatment of the hyper-glycemia was maintained constant.In the whole group,mean blood pressure (MBP) fell progressively over 3 months from a baseline value of 123±3mmHg(1 mmHg=0.133kpa)to a final value of 115±2mmHg(P<0.005).After treatment,fasting plasma glucose,insulin,free fatty acid (FFA),potassium,and glycosylated hemoglobin concentrations were unchanged from baseling.There were no significant differences in glucose toler-ance and insulin sensitivity between pre-and post-trearment values.Neither endogenous (oral glucose)nor exoge-nous(IST)insulin caused any change in plasma potassium concentration. This resistance to the hypokalemic action of insulin was not affected by captopril.

  2. The unified equation for the evaluation of first order reactions in dynamic electrophoresis.

    Science.gov (United States)

    Trapp, Oliver

    2006-02-01

    The unified equation was validated for first order reactions in dynamic CE with a data set of 31 250 elution profiles. Comparison with the results from conventional iterative computer simulation revealed that the unified equation is superior in terms of success rate and precision. The unified equation was applied to determine the cis-trans isomerization rate constants of the angiotensin converting enzyme inhibitor captopril. The separation of the rotational cis-trans isomeric drug has been performed in an aqueous 66 mM citric acid/Tris buffer at pH 3.0 in a 50 cm polyacrylamide-coated fused-silica capillary. Interconversion profiles featuring pronounced plateau formation and peak broadening were observed. Activation parameters DeltaH not equal and DeltaS not equal were obtained from temperature-dependent measurements between 10 and 25 degrees C in 2.5 K steps. From the activation parameters the isomerization barriers of captopril at 37 degrees C under acidic conditions were calculated to be DeltaG not equal trans-->cis=90.6 kJ/mol and DeltaG not equal cis-->trans=84.6 kJ/mol. By comparison of the kinetic data with the results obtained under basic conditions (pH 9.3) a mechanism of isomerization could be proposed.

  3. Adaptation of pharmaceutical excipients to FDM 3D printing for the fabrication of patient-tailored immediate release tablets.

    Science.gov (United States)

    Sadia, Muzna; Sośnicka, Agata; Arafat, Basel; Isreb, Abdullah; Ahmed, Waqar; Kelarakis, Antonios; Alhnan, Mohamed A

    2016-11-20

    This work aims to employ fused deposition modelling 3D printing to fabricate immediate release pharmaceutical tablets with several model drugs. It investigates the addition of non-melting filler to methacrylic matrix to facilitate FDM 3D printing and explore the impact of (i) the nature of filler, (ii) compatibility with the gears of the 3D printer and iii) polymer: filler ratio on the 3D printing process. Amongst the investigated fillers in this work, directly compressible lactose, spray-dried lactose and microcrystalline cellulose showed a level of degradation at 135°C whilst talc and TCP allowed consistent flow of the filament and a successful 3D printing of the tablet. A specially developed universal filament based on pharmaceutically approved methacrylic polymer (Eudragit EPO) and thermally stable filler, TCP (tribasic calcium phosphate) was optimised. Four model drugs with different physicochemical properties were included into ready-to-use mechanically stable tablets with immediate release properties. Following the two thermal processes (hot melt extrusion (HME) and fused deposition modelling (FDM) 3D printing), drug contents were 94.22%, 88.53%, 96.51% and 93.04% for 5-ASA, captopril, theophylline and prednisolone respectively. XRPD indicated that a fraction of 5-ASA, theophylline and prednisolone remained crystalline whilst captopril was in amorphous form. By combining the advantages of thermally stable pharmaceutically approved polymers and fillers, this unique approach provides a low cost production method for on demand manufacturing of individualised dosage forms.

  4. 3D printing of tablets containing multiple drugs with defined release profiles.

    Science.gov (United States)

    Khaled, Shaban A; Burley, Jonathan C; Alexander, Morgan R; Yang, Jing; Roberts, Clive J

    2015-10-30

    We have employed three-dimensional (3D) extrusion-based printing as a medicine manufacturing technique for the production of multi-active tablets with well-defined and separate controlled release profiles for three different drugs. This 'polypill' made by a 3D additive manufacture technique demonstrates that complex medication regimes can be combined in a single tablet and that it is viable to formulate and 'dial up' this single tablet for the particular needs of an individual. The tablets used to illustrate this concept incorporate an osmotic pump with the drug captopril and sustained release compartments with the drugs nifedipine and glipizide. This combination of medicines could potentially be used to treat diabetics suffering from hypertension. The room temperature extrusion process used to print the formulations used excipients commonly employed in the pharmaceutical industry. Attenuated Total Reflectance Fourier Transform Infrared Spectroscopy (ATR-FTIR) and X-ray powder diffraction (XRPD) were used to assess drug-excipient interaction. The printed formulations were evaluated for drug release using USP dissolution testing. We found that the captopril portion showed the intended zero order drug release of an osmotic pump and noted that the nifedipine and glipizide portions showed either first order release or Korsmeyer-Peppas release kinetics dependent upon the active/excipient ratio used.

  5. 加味温胆汤治疗自发性高血压大鼠Ⅰ、Ⅲ型胶原及AngⅡ的影响%Effects of Use of Jiawei Wendan Tang on Collagen- Ⅰ Ⅲ Contents and Angiotensin Ⅱ (Ang Ⅱ ) of Spontaneously Hypertensive Rats(SHRs)

    Institute of Scientific and Technical Information of China (English)

    韦品清; 吴君; 黄萍; 王静; 邵兵

    2012-01-01

    目的:本课题旨在探讨加味温胆汤与开博通(卡托普利)联用对自发性高血压大鼠( SHR)血压Ⅰ、Ⅲ型胶原及AngⅡ的影响.方法:将48只10周龄雄性SHR随机分为6组,分别为SHR对照组(SHR-K)、加味温胆汤高剂量和开博通联合用药组( ZX-H)、加味温胆汤中剂量和开博通联合用药组(ZX-M)、加味温胆汤低剂量和开博通联合用药组(ZX-L)、加味温胆汤中剂量组(Z)及开博通组(X),每组8只,治疗8周后,测量大鼠尾动脉收缩压,观察Ⅰ、Ⅲ型胶原及AngⅡ的改变.结果:加味温胆汤和开博通联用药治疗后,各剂量组大鼠收缩压均有所下降.加味温胆汤和开博通联用药高、中剂量组大鼠下降最明显(P<0.01),且降压效果优于加味温胆汤中剂量及开通博;各治疗组均可显著降低SHR大鼠左心室心肌组织胶原Ⅰ、Ⅲ型蛋白的表述,温胆汤和开博通联合用药组作用显著,明显优于纯中药组和西药开博通组;局部心肌Ang Ⅱ与自然病程对照组相比,各药物治疗组均可明显降低局部心肌AngⅡ浓度(P<0.05),其中加味温胆汤大剂量与开博通联合用药组效果最佳,与自然病程对照组相比,各药物治疗组均可明显降低血浆AngⅡ浓度(P<0.01~0.05).其中加味温胆汤各剂量与开博通联合用药组作用相似,降低血AngⅡ最显著,均优于加味温胆汤与开博通单用组( P<0.01~0.05).结论:味温胆汤和开博通联合用药具有降压、降低左心室心肌组织胶原Ⅰ、Ⅲ型蛋白的表达及降低血浆和心肌肉组织中AngⅡ的浓度.%Objective : This study was to investigate the effects of combination use of Jiawei Wendan Tang and Capoten Tablets (Captopril) on Collagen- Ⅰ , Ⅲ contentsand Angiotensin Ⅱ (Ang Ⅱ ) of Spontaneously Hypertensive Rats(SHRs). Methods: 48 ten-week-old male Spontaneously Hypertensive Rats (SHR) were assigned randomly into six groups: group placebo with distilled water (SHR

  6. Estudo da atividade inibitória enzimática da quercetina sobre a resposta vasodepressora induzida pela bradicinina

    Directory of Open Access Journals (Sweden)

    Luciane Pereira Nascimento Häckl

    2002-01-01

    Full Text Available Em estudos recentes tem sido sugerido que os flavonóides, compostos de origem vegetal sendo encontrados em vários produtos alimentares, possuem uma ação inibitória de vários sistemas enzimáticos. A inibição da enzima conversora da angiotensina (ECA tem sido utilizada no tratamento da hipertensão. O mecanismo de ação dos inibidores da ECA implica na formação da Angiotensina II e na degradação da bradicinina. O propósito do presente estudo foi de analisar a ação da quercetina na atividade da ECA através da avaliação do efeito da angiotensina I (AI e da bradicinina (BK na pressão arterial de ratos anestesiados. Foram utilizados neste estudo ratos Wistar machos adultos. Estes animais foram anestesiados com uretana e foi introduzida na traquéia uma cânula de polietileno (PE 240 para facilitar a respiração. Também foi isolada e canulada (PE 50 a veia jugular para administração das substâncias em estudo. Para registro da pressão arterial foi introduzida na artéria carótida comum esquerda uma cânula de polietileno (PE 50 acoplada a um transdutor de pressão. A administração de BK (10 nmol/kg, i.v. induziu um efeito hipotensor, enquanto que a administração de AI (0,1 nmol/kg induziu uma resposta hipertensora. Pré-tratamento com captopril v.o. (100 nmol/kg 45 min antes e i.v. (10 nmol/kg 5 min antes aumentou significativamente a resposta à BK; embora captopril reduziu, também significativamente, o efeito da AI. O tratamento com quercetina via oral (30 mg/kg 45 min antes e via intravenosa (5 mg/kg 5 min antes aumentou significativamente o efeito da BK. O efeito da AI foi significativamente reduzido por ambos os tratamentos. Estes resultados sugerem que a quercetina potenciou o efeito hipotensor da bradicinina e reduziu o efeito hipertensor da angiotensina I através de ação inibitória sobre a enzima conversora da angiotensina, portanto apresentando um mecanismo de ação semelhante ao captopril.

  7. 血管紧张素转换酶抑制剂治疗阿尔茨海默病的效果%Effects of angiotensin converting enzyme inhibitors on Alzheimer' s disease

    Institute of Scientific and Technical Information of China (English)

    储佺兵; 苑瑞敏; 童玉翠; 陈广生; 许家佳; 张晗; 孙永安

    2012-01-01

    目的 观察血管紧张素转换酶抑制剂( ACEI)治疗阿尔茨海默病(AD)痴呆患者的精神行为症状、认知功能损害的效果.方法 52例AD痴呆患者口服盐酸卡托普利治疗12周,采用神经精神科问卷(NPI)评定患者的精神行为症状变化,采用简易智能状态检查量表评定患者的认知功能变化.结果 治疗12周后,除情感淡漠外,NPI各项因子得分显著下降(P<0.05),NPI总分下降81.47% (P<0.05);照顾者的苦恼程度也随着患者精神行为症状的改善而降低;治疗前后患者的认知功能无显著性差异(P>0.05).结论 盐酸卡托普利可以明显改善AD痴呆患者的精神行为症状,但对患者的认知功能损害无明显疗效.%Objective To observe the effects of hydrochloride captopril, one of angiotensin converting enzyme inhibitors (ACEIs), on behavioral and psychological symptoms and cognitive impairments of Alzheimer' s disease. Methods Fifty-two patients with Alzheimer' s disease were treated with captopril for 12 weeks. The neural psychiatric questionnaire (NPI) and the mini-mental state examination(MMSE) were used to evaluate the efficacy and cognitive changes. Results After treated for 12 weeks, the scores of each NPI factor were significantly decreased(P0.05). Conclusion Hydrochloride captopril could significantly reduce the psychological and behavioral symptoms without improvement in the cognitive impairments.

  8. Effect of intraperitoneally administered hydrolyzed whey protein on blood pressure and renal sodium handling in awake spontaneously hypertensive rats

    Directory of Open Access Journals (Sweden)

    Costa E.L.

    2005-01-01

    Full Text Available The present study evaluated the acute effect of the intraperitoneal (ip administration of a whey protein hydrolysate (WPH on systolic arterial blood pressure (SBP and renal sodium handling by conscious spontaneously hypertensive rats (SHR. The ip administration of WPH in a volume of 1 ml dose-dependently lowered the SBP in SHR 2 h after administration at doses of 0.5 g/kg (0.15 M NaCl: 188.5 ± 9.3 mmHg vs WPH: 176.6 ± 4.9 mmHg, N = 8, P = 0.001 and 1.0 g/kg (0.15 M NaCl: 188.5 ± 9.3 mmHg vs WPH: 163.8 ± 5.9 mmHg, N = 8, P = 0.0018. Creatinine clearance decreased significantly (P = 0.0084 in the WPH-treated group (326 ± 67 µL min-1 100 g body weight-1 compared to 0.15 M NaCl-treated (890 ± 26 µL min-1 100 g body weight-1 and captopril-treated (903 ± 72 µL min-1 100 g body weight-1 rats. The ip administration of 1.0 g WPH/kg also decreased fractional sodium excretion to 0.021 ± 0.019% compared to 0.126 ± 0.041 and 0.66 ± 0.015% in 0.15 M NaCl and captopril-treated rats, respectively (P = 0.033. Similarly, the fractional potassium excretion in WPH-treated rats (0.25 ± 0.05% was significantly lower (P = 0.0063 than in control (0.91 ± 0.15% and captopril-treated rats (1.24 ± 0.30%, respectively. The present study shows a decreased SBP in SHR after the administration of WPH associated with a rise in tubule sodium reabsorption despite an angiotensin I-converting enzyme (ACE-inhibiting in vitro activity (IC50 = 0.68 mg/mL. The present findings suggest a pathway involving ACE inhibition but measurements of plasma ACE activity and angiotensin II levels are needed to support this suggestion.

  9. Effect of intraperitoneally administered hydrolyzed whey protein on blood pressure and renal sodium handling in awake spontaneously hypertensive rats.

    Science.gov (United States)

    Costa, E L; Almeida, A R; Netto, F M; Gontijo, J A R

    2005-12-01

    The present study evaluated the acute effect of the intraperitoneal (ip) administration of a whey protein hydrolysate (WPH) on systolic arterial blood pressure (SBP) and renal sodium handling by conscious spontaneously hypertensive rats (SHR). The ip administration of WPH in a volume of 1 ml dose-dependently lowered the SBP in SHR 2 h after administration at doses of 0.5 g/kg (0.15 M NaCl: 188.5 +/- 9.3 mmHg vs WPH: 176.6 +/- 4.9 mmHg, N = 8, P = 0.001) and 1.0 g/kg (0.15 M NaCl: 188.5 +/- 9.3 mmHg vs WPH: 163.8 +/- 5.9 mmHg, N = 8, P = 0.0018). Creatinine clearance decreased significantly (P = 0.0084) in the WPH-treated group (326 +/- 67 microL min-1 100 g body weight-1) compared to 0.15 M NaCl-treated (890 +/- 26 microL min-1 100 g body weight-1) and captopril-treated (903 +/- 72 microL min-1 100 g body weight-1) rats. The ip administration of 1.0 g WPH/kg also decreased fractional sodium excretion to 0.021 +/- 0.019% compared to 0.126 +/- 0.041 and 0.66 +/- 0.015% in 0.15 M NaCl and captopril-treated rats, respectively (P = 0.033). Similarly, the fractional potassium excretion in WPH-treated rats (0.25 +/- 0.05%) was significantly lower (P = 0.0063) than in control (0.91 +/- 0.15%) and captopril-treated rats (1.24 +/- 0.30%), respectively. The present study shows a decreased SBP in SHR after the administration of WPH associated with a rise in tubule sodium reabsorption despite an angiotensin I-converting enzyme (ACE)-inhibiting in vitro activity (IC50 = 0.68 mg/mL). The present findings suggest a pathway involving ACE inhibition but measurements of plasma ACE activity and angiotensin II levels are needed to support this suggestion.

  10. Effects of Qindan Capsule(芩丹胶囊) on Blood Pressure,Endothelin, Calcitonin Gene-related Peptide and Angiotensin-Ⅱ in Spontaneous Hypertensive Rats

    Institute of Scientific and Technical Information of China (English)

    2006-01-01

    Objective: To observe the hypotensive effects of Qindan Capsule (芩丹胶囊, QC) on spontaneous hypertensive rats (SHR) and its effect on the contents of endothelin (ET), calcitonin gene-related peptide (CGRP) and angiotensin-Ⅱ (Ang-Ⅱ ) in plasma and vascular tissues, and to investigate the possible mechanism of QC in lowering blood pressure. Methods: Forty SHRs were divided into 5 groups: the high dosage QC group [QCHD, 750 mg/(kg·d)], the low dosage QC group [QCLD, 150 mg/(kg·d)], the Niuhuang Jiangya Pill group [牛黄降压丸, NJP, 200 mg/(kg·d)], the Captopril group [ 15 mg/(kg·d)]and the model group, 8 in each group. Meanwhile, a normal control group consisting of 8 Wistar-Kyoto (WKY) rats was set up also. All the rats were administered with medicine through gastrogavage. Systolic blood pressure (SBP),level of ET, CGRP and Ang-Ⅱ in plasma and Ang-Ⅱ in tissues of mesenteric artery were detected in all the rats after 12 weeks of treatment. Results: The level of SBP after treatment in the QCHD group was lower than that in the model group ( P<0.01 ), but with no significant difference as compared with that in the Captopril group and the NJP group (P>0.05). After treatment, the plasma level of ET was lower and CGRP higher than those in the model group (both P<0.05), and also higher than those in the NJP and Captopril group (both P<0.05). As for the content of Ang- Ⅱ, in mesenteric arterial tissues, it was lower in the QCHD group than that in the model group ( P<0.05), but in plasma, it showed no significant difference between the two groups (P>0.05). Conclusion: QC has a satisfactory hypotensive action on SHR rats, and its mechanism may be associated with the regulation on plasma vasoactive peptide and regional renin-angiotensin system.

  11. 52例复方肾炎片与贝那普利联合治疗慢性肾小球肾炎的临床观察%Clinical Observation on 52 Cases of Compound Nephritis Tablets Combined with Benner Pury in Treatment of Chronic Glomerulonephritis Glomerulonephritis

    Institute of Scientific and Technical Information of China (English)

    庞春兰

    2014-01-01

    目的探究复方肾炎片联合贝那普利治疗慢性肾小球肾炎的临床效果。方法选取52例慢性肾小球肾炎患者作为研究对象,并随机分为观察组和对照组。给予观察组复方肾炎片联合贝那普利治疗,对照组单纯使用贝那普利治疗,分析比较两组的临床疗效。结果观察组的治疗总有效率为88.4%,对照组为65.4%,观察组的临床疗效明显优于对照组,且P0.05;两组的不良反应情况无明显差异,P>0.05。结论复方肾炎片联合贝那普利治疗慢性肾小球肾炎疗效确切,且安全可靠,值得推广。%Objective To explore the compound nephritis piece of joint Mr The clinical ef ect of captopril in patients with chronic glomerulonephritis.Methods Selecting 52 patients with chronic glomerulonephritis as the research object,and randomly divided into observation group and control group.To observe group compound nephritis joint shel that captopril treatment,control group simply use that captopril treatment,compared two groups of clinical curative ef ect. Results Treatment group total ef ective rate was 88.4%,the control group was 65.4%,the clinical curative ef ect of observation group was bet er than control group,and ( P0.05);No difference between the two groups of adverse situation( P>0.05).Conclusion Compound nephritis joint shel that split curative effect is the treatment of chronic glomerulonephritis,and safe and reliable,and is worth promoting.

  12. Comparison of renal function and cardiovascular risk following acute myocardial infarction in patients with and without diabetes mellitus

    DEFF Research Database (Denmark)

    Anavekar, Nagesh S; Solomon, Scott D; McMurray, John J V

    2008-01-01

    and nonfatal cv outcomes independent of treatment assignment. In conclusion, although dm is associated with higher risk of renal dysfunction and adverse cv outcomes, patients without dm had a relation between renal function and cv risk similar to that for patients with dm after high-risk acute myocardial......Renal dysfunction is an independent risk factor for cardiovascular (cv) disease and its associated complications. Diabetes mellitus (dm) is a common cause of renal dysfunction. Whether the presence or absence of dm modifies the relation between renal dysfunction and cv disease is unclear....... The valiant trial identified 14,527 patients with acute myocardial infarction complicated by either clinical or radiologic signs of heart failure and/or left ventricular dysfunction for whom baseline creatinine was measured. Patients were randomly assigned to receive captopril, valsartan, or both. Glomerular...

  13. [Arteriosclerosis obliterans. Treatment with angiotensin-converting enzyme inhibitors].

    Science.gov (United States)

    Orea, A; Valdés, R; Niebla, L; Rivas, R; Camacho, B

    1990-01-01

    We compare the effects of two of the main angiotensin convertase enzyme inhibitors, captopril and enalapril, aiming to evaluate their effects in the arterial circulation performance, micro-circulation, and changes in regional blood flow, assuming their property of lowering the angiotensin II blood levels, a very strong peripheral vasoconstrictor. We studied 22 patients: all of them with hypertension and/or skin ulcerations, dropping out those who had venous. They were evaluated periodically, clinically and with photoelectric plethysmography of lower extremities. To interpret the traces we designed an ideogram which gathered the plethysmographic behavior before and after the treatment. Nearly 80% showed considerable improvement in pain, functional capacity and plethysmographic traces patterns. healing of the ulcerations was achieved in all case. We propose some hypothesis to explain the good effect that we have observed.

  14. Posterior reversible encephalopathy syndrome and acute post-streptococcal glomerulonephritis mimicking breakthrough seizures

    Directory of Open Access Journals (Sweden)

    Kamille Abdool

    2015-05-01

    Full Text Available We report the case of a 14-year-old boy with a past history of primary generalized seizures, who had been seizure-free for 2 years on sodium valproate and presented with generalized tonic clonic seizures suggestive of breakthrough seizures. Examination revealed hypertension, impetiginous lesions of the lower limbs, microscopic hematuria, elevated antistreptolysin O titre and low complement levels consistent with acute post-streptococcal glomerulonephritis. Cranial magnetic resonance imaging (MRI demonstrated changes consistent with posterior reversible encephalopathy syndrome. Hypertension was controlled with intravenous nitroglycerin followed by oral captopril and amlodipine. Brain MRI changes returned normal within 2 weeks. The nephritis went in to remission within 2 months and after 8 months the patient has been seizure free again. Posterior reversible encephalopathy syndrome appeared to have neither short nor intermediate effect on seizure control in this patient. The relationship between posterior reversible encephalopathy syndrome and seizures is reviewed.

  15. EFFECTS OF PDGF-BB ON INTRACELLULAR CALCIUM CONCENTRATION AND PROLIFERATION IN CULTURED GLOMERULAR MESANGIAL CELLS

    Institute of Scientific and Technical Information of China (English)

    WEN Li-ping; ZHANG Chong; BIAN Fan; ZOU Jun; JIANG Geng-ru; ZHU Han-wei

    2006-01-01

    Objective To investigate the relationship between the alteration of intracellular calcium concentration and proliferation in cultured glomerular mesangial cells. Methods Rat mesangial cells were cultured.Intracellular calcium concentrations were measured by confocal Laser Scanning Microscopy and Fura-3 fluorescence dyeing techniques. Cell growth was measured by MTT assay. Results PDGF-BB increased intracellular calcium concentrations in a dose-dependent manner, and at the same time promote the proliferation of mesangial cells. After preincubation with calcium channel blocker nifedipine or angiotensin converting enzyme inhibitor captopril, both the increase of intracellular calcium concentrations and cell proliferations induced by PDGF-BB were inhibited. Tripterigium Wilfordii Glycosides (TMG) significantly inhibited the mesangial cell proliferations, but it had no significant effect on intracellular calcium concentrations. Conclusion There was a positive relationship between the elevation of intracellular calcium concentration and cell proliferation in glomerular mesangial cells, but the increase of in- tracellular calcium concentrations wasn't the only way for proliferation.

  16. Modified Eu-doped Y2 O3 nanoparticles as turn-off luminescent probes for the sensitive detection of pyridoxine.

    Science.gov (United States)

    Zobeiri, Eshagh; Bayandori Moghaddam, Abdolmajid; Gudarzy, Forugh; Mohammadi, Hadi; Mozaffari, Shahla; Ganjkhanlou, Yadolah

    2015-05-01

    Europium-doped yttrium oxide nanoparticles (Y2 O3 :Eu NPs) modified by captopril were prepared in aqueous solution. In this study, we report the effect of pyridoxine hydrochloride on the photoluminescence intensity of Y2 O3 :Eu NPs in pH 7.2 buffer solution. By increasing the pyridoxine concentration, the luminescence intensity of Y2 O3 :Eu NPs is quenched. The results show that this method demonstrates high sensitivity for pyridoxine determination. A linear relationship is observed between 0.0 and 62.0 μM with a correlation coefficient of 0.995 and a detection limit of 0.023 μM.

  17. Amlodipine-induced gingival overgrowth in a child after liver transplant

    Science.gov (United States)

    Guollo, André; Vivas, Ana Paula Molina; Lopes, Rodrigo Nascimento; Porta, Gilda

    2016-01-01

    Drug-induced gingival overgrowth (GO) has been associated with phenytoin, cyclosporine, and calcium channel blocker therapies. This study reports the case of an 11-year-old girl who was referred for evaluation of GO, which had occurred over the last 6 months. Her medical history included a liver transplant due to biliary atresia 3 years ago, immunosuppressive therapy, and hypertension, which is why she was started on a daily intake of amlodipine. The intraoral examination showed generalized GO, and the treatment consisted of a gingivectomy. Subsequently, amlodipine was replaced with captopril and oral hygiene instructions. There was no recurrence of GO after 28 months of follow-up. Although GO may be related to the chronic use of amlodipine, such an association is uncommon in pediatrics, and the treatment consists of the replacement of medication combined with a surgical approach and plaque control. PMID:27818959

  18. Transplante cardíaco em Campo Grande - MS. Redução significativa de lesão coronária pós transplante: relato de caso

    Directory of Open Access Journals (Sweden)

    Marcos Vinícius R. P. CALDAS

    1997-04-01

    Full Text Available No Serviço de Cirurgia Cardíaca da Santa Casa de Campo Grande/MS - foi realizado, em 23 de setembro de 1994, um transplante cardíaco ortotópico no paciente C.A.D., 27 anos, portador de miocardiopatia dilatada idiopática, o qual transcorreu sem anormalidades. O paciente recebeu alta da UTI com 7 dias e alta hospitalar no 40º dia de pós-operatório, recebendo ciclosporina, azatioprina e prednisona para manutenção do enxerto, captopril, furosemida e aspirina. Apresentou no 1º ano de seguimento 2 episódios de rejeição, leve e moderada, sendo modificada a posologia dos imunossupressores. Em setembro de 1995, nos exames de seguimento, foi detectada, na coronariografia, lesão obstrutiva de 50% em artéria coronária direita. Decidiu-se modificar a terapêutica do paciente, iniciando diltiazen substituindo o captopril, e associando-se complexo vitamínico (betacaroteno, C e E mais selênio, na tentativa de evitar progressão da lesão obstrutiva. Foi também realizada orientação dietética por nutricionista. Após 12 meses com a nova terapêutica, a coronariografia mostrou redução significativa da lesão obstrutiva em artéria coronária direita. Durante todo o período de seguimento o paciente apresentou níveis normais no lipidograma. Hoje o paciente encontra-se no terceiro ano de seguimento, assintomático e tendo suas atividades habituais sem intercorrências.The Cardiac Surgery Service of Campo Grande, Santa Casa/MS performed on September 23 rd, 1994 an orthotopic cardiac transplantation in a 27 year-old man with idiopathic dilated cardiomyopathy, which elapsed without abnormalities. The patient left the ICU in 7 days and was discharged at 40 th postoperative day, receiving cyclosporine, azathioprine and prednisone for graft support; captopril, furosemide and aspirin. Presented at one year follow-up, 2 rejection episodes, mil and moderate, when the immunesupressivet herapy dose was modified. On September 1995, at follow up, an

  19. Endothelial function impairment in chronic venous insufficiency: effect of some cardiovascular protectant agents.

    Science.gov (United States)

    Carrasco, Omar F; Ranero, Alejandra; Hong, Enrique; Vidrio, Horacio

    In segments of human varicose veins, endothelial function was assessed by measuring relaxation induced by acetylcholine in noradrenaline-precontracted preparations. In addition, concentration-response curves to acetylcholine were obtained before and after incubation with the arterial endothelium protectant agents captopril, losartan, troglitazone, pravastatin, or simvastatin. The antivaricose agent escin was also tested. Mean acetylcholine-induced relaxation of varicose venous rings was about 13%, approximately one third of that reported for control saphenous veins. Concentration-response curves to acetylcholine were ''u'' shaped, the result of endothelium-mediated relaxation at low concentrations, superseded by subsequent smooth muscle contractile responses. Relaxation was enhanced by the endothelium-protecting agents and by escin, troglitazone being the least, and simvastatin the most effective. It was concluded that endothelial dysfunction is present in varicose veins, that this anomaly can be reverted by cardiovascular protecting agents, and that it can play a role in the pathogenesis and treatment of chronic venous insufficiency.

  20. Effects of felodipine combined with puerarin on ACE2-Ang (1-7)-Mas axis in renovascular hypertensive rat.

    Science.gov (United States)

    Bai, Song; Huang, Zheng-Gui; Chen, Li; Wang, Jiang-Tao; Ding, Bo-Ping

    2013-06-10

    This study aimed to investigate the effect of combination of felodipine+puerarin on ACE2-Ang (1-7)-Mas axis, and to explore the protective effect of the combination against kidney in renovascular hypertensive rats. Goldblatt rats were randomly divided into 5 groups as follows: 4 groups which were treated with felodipine (Felo), puerarin (Pue), Felo+Pue, and Felo+captopril (Cap), respectively, and a control group of animals that were administrated with distilled water. Contents of Ang II and Ang (1-7) in renal tissues were determined by ELISA kit. The mRNA expression of ACE2/Mas and ACE/AT1 in kidneys was analyzed by RT-PCR. After 8weeks of treatment, compared with Goldblatt group, Felo+Pue reduced SBP, DBP and HR (pword, a combination of Felo+Pue has a more efficient therapeutic effect on DBP and HR, and contributes to a better protection against renal interstitial fibrosis.

  1. [Risk factors and subjective symptoms of drug-induced leucopenia].

    Science.gov (United States)

    Hayashi, Kyoko; Ohtsu, Fumiko; Yano, Reiko; Sakakibara, Jinsaku; Goto, Nobuyuki

    2011-01-01

    The present study investigated risk factors and subjective symptoms associated with drug-induced leucopenia. We selected 248 patients with drug-induced leucopenia from the Case Reports of Adverse Drug Reactions and Poisoning Information System (CARPIS) database of over 47000 case reports of adverse drug reactions and assigned them to a case group. We also randomly selected 743 cases of adverse drug reactions not associated with leucopenia as a control group. A comparison of patient characteristic data between the two groups using logistic-regression analysis revealed that female sex, autoimmune disease and renal damage were background risk factors for drug-induced leucopenia. In addition, thiamazole, ritodrine, propylthiouracil, ticlopidine, allopurinol, minocycline and captopril administration significantly increased the risk of drug-induced leucopenia. A significant association was also found for fever, chills and pharyngeal abnormalities. Based on these findings, we developed two estimated regression equations to help prevent drug-induced leucopenia in the community pharmacy setting.

  2. Probiotic-fermented purple sweet potato yogurt activates compensatory IGF‑IR/PI3K/Akt survival pathways and attenuates cardiac apoptosis in the hearts of spontaneously hypertensive rats.

    Science.gov (United States)

    Lin, Pei-Pei; Hsieh, You-Miin; Kuo, Wei-Wen; Lin, Yueh-Min; Yeh, Yu-Lan; Lin, Chien-Chung; Tsai, Fuu-Jen; Tsai, Chang-Hai; Huang, Chih-Yang; Tsai, Cheng-Chih

    2013-12-01

    Apoptosis is recognized as a predictor of adverse outcomes in subjects with cardiac diseases. The aim of this study was to explore the effects of probiotic-fermented purple sweet potato yogurt (PSPY) with high γ-aminobutyric acid (GABA) content on cardiac apoptosis in spontaneously hypertensive rat (SHR) hearts. The rats were orally adminsitered with 2 different concentrations of PSPY (10 and 100%) or captopril, 15.6 mg/kg, body weight (BW)/day. The control group was administered distilled water. DAPI and TUNEL staining were used to detect the numbers of apoptotic cells. A decrease in the number of TUNEL-positive cardiac myocytes was observed in the SHR-PSPY (10 and 100%) groups. In addition, the levels of key components of the Fas receptor- and mitochondrial-dependent apoptotic pathways were determined by western blot analysis. The results revealed that the levels of the key components of the Fas receptor- and mitochondrial-dependent apoptotic pathway were significantly decreased in the SHR-captopril, and 10 and 100% PSPY groups. Additionally, the levels of phosphorylated insulin-like growth factor‑I receptor (p-IGF‑IR) were increased in SHR hearts from the SHR-control group; however, no recovery in the levels of downstream signaling components was observed. In addition, the levels of components of the compensatory IGF-IR-dependent survival pathway (p-PI3K and p-Akt) were all highly enhanced in the left ventricles in the hearts form the SHR-10 and 100% PSPY groups. Therefore, the oral administration of PSPY may attenuate cardiomyocyte apoptosis in SHR hearts by activating IGF‑IR-dependent survival signaling pathways.

  3. Antioxidant and ACE Inhibitory Bioactive Peptides Purified from Egg Yolk Proteins

    Directory of Open Access Journals (Sweden)

    Marwa Yousr

    2015-12-01

    Full Text Available Protein by-products from the extraction of lecithin from egg yolk can be converted into value-added products, such as bioactive hydrolysates and peptides that have potential health enhancing antioxidant, and antihypertensive properties. In this study, the antioxidant and angiotensin converting enzyme (ACE inhibitory activities of peptides isolated and purified from egg yolk protein were investigated. Defatted egg yolk was hydrolyzed using pepsin and pancreatin and sequentially fractionated by ultrafiltration, followed by gel filtration to produce egg yolk gel filtration fractions (EYGF. Of these, two fractions, EYGF-23 and EYGF-33, effectively inhibited the peroxides and thiobarbituric acid reactive substance (TBARS in an oxidizing linoleic acid model system. The antioxidant mechanism involved superoxide anion and hydroxyl radicals scavenging and ferrous chelation. The presence of hydrophobic amino acids such as tyrosine (Y and tryptophan (W, in sequences identified by LC-MS as WYGPD (EYGF-23 and KLSDW (EYGF-33, contributed to the antioxidant activity and were not significantly different from the synthetic BHA antioxidant. A third fraction (EYGF-56 was also purified from egg yolk protein by gel filtration and exhibited high ACE inhibitory activity (69% and IC50 value (3.35 mg/mL. The SDNRNQGY peptide (10 mg/mL had ACE inhibitory activity, which was not significantly different from that of the positive control captopril (0.5 mg/mL. In addition, YPSPV in (EYGF-33 (10 mg/mL had higher ACE inhibitory activity compared with captopril. These findings indicated a substantial potential for producing valuable peptides with antioxidant and ACE inhibitory activity from egg yolk.

  4. Chronic excitotoxic lesion of the dorsal raphe nucleus induces sodium appetite

    Directory of Open Access Journals (Sweden)

    Cavalcante-Lima H.R.

    2005-01-01

    Full Text Available We determined if the dorsal raphe nucleus (DRN exerts tonic control of basal and stimulated sodium and water intake. Male Wistar rats weighing 300-350 g were microinjected with phosphate buffer (PB-DRN, N = 11 or 1 µg/0.2 µl, in a single dose, ibotenic acid (IBO-DRN, N = 9 to 10 through a guide cannula into the DRN and were observed for 21 days in order to measure basal sodium appetite and water intake and in the following situations: furosemide-induced sodium depletion (20 mg/kg, sc, 24 h before the experiment and a low dose of dietary captopril (1 mg/g chow. From the 6th day after ibotenic acid injection IBO-DRN rats showed an increase in sodium appetite (12.0 ± 2.3 to 22.3 ± 4.6 ml 0.3 M NaCl intake whereas PB-DRN did not exceed 2 ml (P < 0.001. Water intake was comparable in both groups. In addition to a higher dipsogenic response, sodium-depleted IBO-DRN animals displayed an increase of 0.3 M NaCl intake compared to PB-DRN (37.4 ± 3.8 vs 21.6 ± 3.9 ml 300 min after fluid offer, P < 0.001. Captopril added to chow caused an increase of 0.3 M NaCl intake during the first 2 days (IBO-DRN, 33.8 ± 4.3 and 32.5 ± 3.4 ml on day 1 and day 2, respectively, vs 20.2 ± 2.8 ml on day 0, P < 0.001. These data support the view that DRN, probably via ascending serotonergic system, tonically modulates sodium appetite under basal and sodium depletion conditions and/or after an increase in peripheral or brain angiotensin II.

  5. Effect of pharmaceutical intervention on AT1R, AT2R, ERK and JNK activity in chronic hibernating myocardium in rabbits

    Institute of Scientific and Technical Information of China (English)

    Dongye Li; Weiwei Li; Yong Xia; Wenhao Qian; Hong Zhu; Tongda Xu; Defeng Pan

    2008-01-01

    Objective: To investigate in chronic hibernating myocardium in rabbits and the influence and significance of captopril, betaloc,valsartan in angiotensin Ⅱ subtype 1 receptor(AT1R), angiotensin Ⅱ subtype 2 receptor(AT2R), extracellular signal regulated kinase 1/2 (ERK1/2), c-Jun N-terminal kinase(JNK). Methods: The model of chronic hibernating myocardium(CHM) was established.The changes of AT1R, AT2R, ERK1/2, JNK in different groups were assessed by western blotting and immunohistochemistry. Results:The amount of AT1R decreased while AT2R increased in the CON group compared with in sham group, and both AT1R and AT2R decreased in drug groups compared with the CON group. The content of ERK had no change in each group, while that of "expression" p-ERK increased in CON group compared with in sham group, and was lower in drug intervention groups than in CON and sham groups. The contents of JNK and p-JNK decreased in CON and drug intervention groups compared with in sham group. The protein levels of JNK, p-JN K in drug intervention groups were lower than in the CON group. Three drugs can inhibit interstitial fibrosis and reduce apoptotic cells. The expression levels in the groups(with different doses) had statistical difference as well as between groups of captopril and other drugs; however the results between betaloc and valsartan had no significant difference. Conclusion: AT1R, AT2R may be the upper stream receptor of ERK and JNK and may participate in generation and evolution of CHM. Captepril, valsartan and betaloc may preserve CHM by inhibiting AT1R, AT2R and JNK activity.

  6. FACTORES RELACIONADOS CON LA URGENCIA HIPERTENSIVA EN UN ÁREA DE SALUD URBANA DE SANTA CLARA / Factors linked to hypertensive emergency in an urban health area of Santa Clara

    Directory of Open Access Journals (Sweden)

    Alexis López Casanova

    2009-12-01

    Full Text Available Introduction and objectives: Arterial hypertension manifest itself in many individuals with the appearance of an acute event, the hypertensive emergency, which takes place many times in hypertensive individuals who have not been diagnosed or who have been incorrectly treated. The aim of this research is to characterize the factors linked to the hypertensive emergency. Method: A descriptive, cross-sectional study in a sample formed by 150 patients presenting the above mentioned condition who were treated at the Emergency Department of the Santa Clara Polyclinic during the period from January 2007 to January 2008. The clinical and epidemiological variables were gathered by means of interviews with the patients. Chi square was used in the statistical analysis. Results: There was a predominance of male patients (54 %, the age group between 46 and 60 years of age (54 % and the white race in both sexes (57,4 %. The most common associated illnesses were ischemic heart disease (18.6 % and diabetes mellitus (14 %. Captopril was the first therapeutic choice in 82,7 percent of the cases, presenting a high resolution rate (80,6 %. It was determined that 49 percent of the patients were not correctly controlled, and that the adherence to the pharmacologic treatment was moderate in 49,3 percent and bad in 30 percent of the cases. Conclusions: The hypertensive emergency prevailed in males and in the age group between 46 and 60 years of age. Ischemic heart disease and diabetes mellitus were the most common associated illnesses; as well as a family history of arterial hypertension, smoking and obesity as atherosclerotic risk factors. Arterial hypertension and diabetes mellitus were associated with a higher lack of response to standard therapy. Captopril was the most commonly usedmedication, showing a high resolution rate. The lack of adherence to the treatment and the inadequate control prevailed.

  7. Beneficial effects of Acer okamotoanum sap on L-NAME-induced hypertension-like symptoms in a rat model.

    Science.gov (United States)

    Yang, Hyun; Hwang, Inho; Koo, Tae-Hyoung; Ahn, Hyo-Jin; Kim, Sun; Park, Mi-Jin; Choi, Won-Sil; Kang, Ha-Young; Choi, In-Gyu; Choi, Kyung-Chul; Jeung, Eui-Bae

    2012-02-01

    The sap of Acer okamotoanum has been termed 'bone-benefit-water' in Korea owing to its mineral and sugar content. In particular, the calcium (Ca) and potassium (K) concentrations of the sap of Acer okamotoanum are 40- and 20-times higher, respectively, than commercial spring water. In the present study, we examined whether Acer okamotoanum sap improves or prevents hypertension-like symptoms in a rat model. Male Sprague-Dawley rats (8-weeks-old) were provided commercial spring water supplemented with 25, 50 or 100% Acer okamotoanum sap, 3% potassium ions (K+) or captopril, and treated daily for 2 weeks with NG-nitro-L-arginine methyl ester (L-NAME; 100 mg/kg/day) by subcutaneous injection, in order to induce hypertensive symptoms. Rats were euthanized 6 h following the final injection. To assess the effect of the sap on hypertension-like symptoms, we examined the mean blood pressure (BP), protein levels and localization of endothelial nitric oxide synthase (eNOS) in the descending aorta of the rats. BP levels were significantly lower in hypertensive rats received 25, 50 and 100% sap compared with rats who were administered only commercial spring water. Protein levels of eNOS were repressed in L-NAME-only-treated rats, but were elevated in the descending aorta of rats administered captopril, K+ water and Acer okamotoanum sap (25, 50 and 100%) up to the level of the sham group provided commercial spring water, and then injected with dimethyl sulfoxide for the same period of time. Localized eNOS protein was abundantly expressed in the perivascular descending aorta adipose tissue of the rats. Taken together, these results demonstrated that the sap of Acer okamotoanum ameliorated high BP induced by L-NAME treatment in a rat model.

  8. Use of oral antihypertensive medication preceding blood pressure elevation in hospitalized patients

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    Macedo Cristiano Ricardo Bastos de

    2001-01-01

    Full Text Available OBJECTIVE: To evaluate the frequency of oral antihypertensive medication preceding the increase in blood pressure in patients in a university hospital, the drug of choice, and the maintained use of antihypertensive medication. METHODS: Data from January to June 1997 from the University Hospital Professor Edgard Santos Pharmacy concerning the prescriptions of all inpatients were used. Variables included in the analysis were: antihypertensive medication prescription preceding increase in blood pressure, type of antihypertensive medication, gender, clinical or surgical wards, and the presence of maintained antihypertensive medication. RESULTS: The hospital admitted 2,532 patients, 1,468 in surgical wards and 818 in medical wards. Antihypertensive medication prescription preceding pressure increase was observed in 578 patients (22.8%. Nifedipine was used in 553 (95.7% and captopril in 25 (4.3%. In 50.7% of patients, prescription of antihypertensive medication was not associated with maintained antihypertensive medication. Prescription of antihypertensive drugs preceding elevation of blood pressure was significantly (p<0.001 more frequent on the surgical floor (27.5%; 405/1468 than on the medical floor (14.3%; 117/818. The frequency of prescription of antihypertensive drugs preceding elevation of blood pressure without maintained antihypertensive drugs and the ratio between the number of prescriptions of nifedipine and captopril were greater in surgical wards. CONCLUSION: The use of antihypertensive medication, preceding elevation of blood pressure (22.8% observed in admitted patients is not supported by scientific evidence. The high frequency of this practice may be even greater in nonuniversity hospitals.

  9. Renal oxygen content is increased in healthy subjects after angiotensin-converting enzyme inhibition

    Directory of Open Access Journals (Sweden)

    Anna Stein

    2012-07-01

    Full Text Available OBJECTIVE: The association between renal hypoxia and the development of renal injury is well established. However, no adequate method currently exists to non-invasively measure functional changes in renal oxygenation in normal and injured patients. METHOD: R2* quantification was performed using renal blood oxygen level-dependent properties. Five healthy normotensive women (50±5.3 years underwent magnetic resonance imaging in a 1.5T Signa Excite HDx scanner (GE Healthcare, Waukesha, WI. A multiple fast gradient-echo sequence was used to acquire R2*/T2* images (sixteen echoes from 2.1 ms/slice to 49.6 ms/slice in a single breath hold per location. The images were post-processed to generate R2* maps for quantification. Data were recorded before and at 30 minutes after the oral administration of an angiotensin II-converting enzyme inhibitor (captopril, 25 mg. The results were compared using an ANOVA for repeated measurements (mean + standard deviation followed by the Tukey test. ClinicalTrials.gov: NCT01545479. RESULTS: A significant difference (p<0.001 in renal oxygenation (R2* was observed in the cortex and medulla before and after captopril administration: right kidney, cortex = 11.08 ± 0.56ms, medulla = 17.21 ± 1.47ms and cortex = 10.30 ± 0.44ms, medulla = 16.06 ± 1.74ms, respectively; and left kidney, cortex= 11.79 ± 1.85ms, medulla = 17.03 ± 0.88ms and cortex = 10.89 ± 0.91ms, medulla = 16.43 ± 1.49ms, respectively. CONCLUSIONS: This result suggests that the technique efficiently measured alterations in renal blood oxygenation after angiotensin II-converting enzyme inhibition and that it may provide a new strategy for identifying the early stages of renal disease and perhaps new therapeutic targets.

  10. β-Dystroglycan cleavage by matrix metalloproteinase-2/-9 disturbs aquaporin-4 polarization and influences brain edema in acute cerebral ischemia.

    Science.gov (United States)

    Yan, W; Zhao, X; Chen, H; Zhong, D; Jin, J; Qin, Q; Zhang, H; Ma, S; Li, G

    2016-06-21

    Dystroglycan (DG) is widely expressed in various tissues, and throughout the cerebral microvasculature. It consists of two subunits, α-DG and β-DG, and the cleavage of the latter by matrix metalloproteinase (MMP)-2 and -9 underlies a number of physiological and pathological processes. However, the involvement of MMP-2/-9-mediated β-DG cleavage in cerebral ischemia remains uncertain. In astrocytes, DG is crucial for maintaining the polarization of aquaporin-4 (AQP4), which plays a role in the regulation of cytotoxic and vasogenic edema. The present study aimed to explore the effects of MMP-2/-9-mediated β-DG cleavage on AQP4 polarization and brain edema in acute cerebral ischemia. A model of cerebral ischemia was established via permanent middle cerebral artery occlusion (pMCAO) in male C57BL/6 mice. Western blotting, real-time polymerase chain reaction (PCR), immunohistochemical staining, immunofluorescent staining, electron microscopy, and light microscopy were used. Captopril was applied as a selective MMP-2/-9 inhibitor. Recombinant mouse MMP (rmMMP)-2 and -9 were used in an in vitro cleavage experiment. The present study demonstrated evidence of β-DG cleavage by MMP-2/-9 in pMCAO mouse brains; this cleavage was implicated in AQP4 redistribution and brain edema in cerebral ischemia. In addition, captopril exacerbated cytotoxic edema and ameliorated vasogenic edema at 24h after pMCAO, and alleviated brain edema and neurological deficit at 48h and 72h. In conclusion, this study provides novel insight into the effects of MMP-2/-9-mediated β-DG cleavage in acute cerebral ischemia. Such findings might facilitate the development of a therapeutic strategy for the optimization of MMP-2/-9 targeted treatment in cerebral ischemia.

  11. Minoxidil-associated anorexia in an infant with refractory hypertension.

    Science.gov (United States)

    Vesoulis, Zachary A; Attarian, Stephanie J; Zeller, Brandy; Cole, Francis Sessions

    2014-12-01

    Minoxidil is a potent antihypertensive used as an adjunctive agent in refractory hypertension. It exerts an antihypertensive effect through two mechanisms: selective arterial vasodilation by activation of potassium channels in the vascular smooth muscle and stimulation of carotid and aortic baroreceptors, leading to downstream release of renin and norepinephrine. Although frequently cited in reviews of antihypertensive agents, limited data about the use of minoxidil in neonates are available. We describe an infant girl, born at 35 weeks of gestation, who was diagnosed with idiopathic hypertension after extensive diagnostic evaluation. Adequate blood pressure control was not achieved with captopril, amlodipine, and clonidine. Oliguria secondary to captopril and rapid-onset congestive heart failure due to persistent hypertension led to the introduction of intravenous agents labetalol and nitroprusside. Although adequate blood pressure control was achieved, attempts to transition back to oral agents were unsuccessful, prompting the use of minoxidil as an alternative agent. Although good blood pressure control was achieved, the infant's oral intake plummeted from 210 to 63 ml/kg/day. The anorexia quickly resolved after stopping minoxidil, and she was discharged home at 5 months of age receiving propranolol, amlodipine, and doxazosin. Use of the Naranjo adverse drug reaction probability scale indicated a definite relationship (score of 10) between the patient's development of anorexia and minoxidil therapy. To our knowledge, there have been no previous reports of minoxidil-associated anorexia in preterm or term infants. Clinicians should be aware that anorexia is a possible adverse effect of minoxidil in this patient population when initiating the drug in similar patients.

  12. Dexamethasone reduces tachykinin but not ACh airway hyperreactivity after O[sub 3

    Energy Technology Data Exchange (ETDEWEB)

    Murlas, C.G.; Lang, Z.; Chodimella, V. (Rush Univ., Chicago, IL (United States))

    1993-01-01

    We investigated whether dexamethasone pretreatment affected the acute increase in airway reactivity produced by high-level ozone exposure. Reactivity to intravenous IV substance P (SP), IV acetylcholine (ACh), or aerosolized capsaicin (CAP) before and 1 hr after ozone exposure (3 ppm for 2 hr) was determined by measuring specific airway resistance in anesthetized, spontaneously breathing guinea pigs, half of whom had been pretreated for 2 days pre-ozone with dexamethasone (2 mg/kg intramuscularly [IM] daily). The amount of IV SP, IV ACh, or inhaled capsaicin necessary to increase baseline specific airway resistance by 100% (ED200ACh or ED200SP) or 35% (ED135CAP) was determined by interpolation from dose-response curves. Compared to their pre-ozone status on the day of exposure, we found that dexamethasone-pretreated animals manifested significantly less of an increase in airway reactivity postozone to IV SP or inhaled CAP than did untreated animals. Changes in logEDs of the pretreated group were 0.18 +/- 0.03 (mean +/- SE) for SP and 2.20 +/- 0.11 for CAP compared to 0.27 +/- 0.04 and 3.38 +/- 0.34, respectively, for the untreated groups post-ozone (p < 0.05 and n = 4 for each). In contrast, dexamethasone pretreatment had no effect on IV ACh reactivity postozone: changes in logED200ACh were 0.27 +/- 0.08 and 0.28 +/- 0.04 for the pretreated and untreated groups, respectively (n = 4). In animals pretreated with captopril to block possible dexamethasone stimulation of angiotensin-converting enzyme synthesis that could influence tachykinin reactivity, we found that the corticosteroid effect on post-ozone SP reactivity was as marked as that seen in animals without captopril (n = 4). These reactivity studies were consistent with the possibility that dexamethasone may ameliorate ozone-induced, tachykinin hyperreactivity by stimulating airway neutral endopeptidase (NEP).

  13. 基于1H-NMR代谢组学分析研究平肝方药对高血压大鼠大脑额叶皮质区的影响%Study on Effects of Pingan Prescription on Frontal Cortex of SHR with 1H-NMR-based Metabolic Technology

    Institute of Scientific and Technical Information of China (English)

    解君; 蒋海强; 李运伦

    2013-01-01

    目的:采用核磁共振氢谱(1H-NMR)结合模式识别方法研究高血压模型及平肝方药干预后大鼠大脑额叶皮质区组织代谢组学变化,探讨高血压病和大脑损伤间有价值信息,为平肝方药的作用机制研究提供科学依据。方法:随机将大鼠分为4组:正常对照组、高血压模型组、卡托普利组和平肝方药组,连续给药14天后取各组大鼠额叶组织。采用1H-NMR方法结合模式识别技术检测分析四组大鼠额叶区组织,分别寻找其特征性代谢产物。结果:主成分分析及偏最小二乘判别分析结果显示,卡托普利组和平肝方药组明显异于高血压模型组,且平肝方药组与卡托普利组大鼠样本分类趋势明显,提示平肝方药能显著改善大鼠机体的整体代谢;4种代谢产物鉴定为葡萄糖、半乳糖、多巴胺和琥珀酸。结论:高血压损伤额叶组织可能主要表现在能量代谢和神经损伤方面,而平肝方药在有效降压同时,通过影响其代谢产物来缓解疾病引起的物质代谢异常。%This article applied 1H-NMR-based metabolic technology combined with pattern recognition method to study metabolic changes of brain frontal cortex among spontaneously hypertensive rats ( SHR ) and evaluate Pingan prescription treatment effect . It was aimed to explore the valuable information between hypertension and brain damage in order to provide a scientific basis for the mechanism of Pingan prescription . Rats were ran-domly divided into four groups , which were the normal control group , hypertension model group , captopril group and the Pinggan prescription group . Medications were administered continuously for 14 days . Then , the frontal lobe tissues of rats in each group were removed . The 1H-NMR based metabolic technology combined with pattern recognition method were used in the detection and analysis of frontal lobe tissues of rats from four group in order to find

  14. xy9902抗大鼠心肌重构作用的实验研究%Experimental study of xy9902 on rat myocardial remodeling

    Institute of Scientific and Technical Information of China (English)

    曾菊绒; 胥晓丽; 侯进; 弥曼; 熊晓云; 徐天娇; 于晓江; 臧伟进

    2012-01-01

    Aim To investigate the effects and mechanisms of xy9902 on myocardial remodeling induced by pressure overload in rats. Methods Abdominal aortic constriction ( AAC ) method was applied to establish myocardial remodeling models. Captopril (10 mg · kg-01· d-1 ) and xy9902 ( 10 mg · kg-1 · d-1 ) were administered intragastrically for treatment. Collagen content in myocardium was determined by reforming Mallory' s staining. Superoxide dismutase ( SOD ) activity and malonicdialdehyde ( MDA ) content were determined by xanthine oxidase and 2-thiobarbituric acid respectively. Results Myocardial cells distributed disorder, filaments breakage, and collagen hyperplasia in AAC group, but these phenomenon turned to better in Captopril and xy9902 groups. Compared with sham group, SOD activity was down-regulated but MDA content was up-regulated in AAC group( P <0. 01 ); however, SOD activity was up-regulated but MDA content was down-regulated in Captopril and xy9902 groups( P < 0. 01 ). Furthermore, Correlation analysis showed that CVF was negatively correlated with the ratio of SOD/MDA( r = - 0. 801, P < 0. 01 ). Conclusion Xy9902 can prevent myocardial remodeling, and the disproportion of SOD and MDA may be one of the molecular mechanisms.%目的 研究新型选择性雌激素受体调节剂(SERMs)xy9902对大鼠心肌重构的干预作用,并初步探讨其机制.方法 腹主动脉缩窄复制压力负荷增高致大鼠心肌重构动物模型,术后2周存活动物分为模型组 (AAC)、卡托普利组(Cap)及xy9902组(xy9902),另设假手术组(Sham).Mallory三色染色观察心肌组织胶原纤维含量的变化.黄嘌呤氧化酶法测定心肌组织SOD活性,硫代巴比妥酸法测定MDA含量.结果 与Sham组比较,AAC组心脏指数HMI及LVMI增加,心肌细胞排列紊乱、增粗,细胞间隙明显增宽,可见大量异常胶原纤维堆积,CVF增大,然而Cap组和xy9902组明显好转.AAC组心肌SOD活性下降,MDA含量增加,Cap组和xy9902组与AAC组

  15. Efeitos da angiotensina-I e isquemia na recuperação funcional em corações isolados

    Directory of Open Access Journals (Sweden)

    Ubirajara Oliveira de Oliveira

    2011-11-01

    Full Text Available FUNDAMENTO: A ressuscitação de parada cardíaca pode apresentar disfunção miocárdica determinada pelo tempo da isquemia, e a inibição da enzima conversora de angiotensina (ECA pode reduzir a disfunção cardíaca durante a reperfusão. OBJETIVO: Investigar os efeitos da angiotensina-I e diferentes períodos de isquemia na recuperação funcional em corações de ratos isolados. MÉTODOS: Os corações isolados de ratos Wistar (n = 45; 250-300 g foram submetidos a diferentes períodos de isquemia global (20, 25 ou 30 min e reperfundidos (30 min com o tampão Krebs-Henseleit, ou com a adição de 400 nmol/L de angiotensina-I, ou com 400 nmol/L de angiotensina-I + 100 µmol/L de captopril durante o período de reperfusão. RESULTADOS: A derivada positiva máxima de pressão (+dP/dt max e o produto frequência-pressão foram reduzidos nos corações expostos à isquemia de 25 min (~ 73% e à isquemia de 30 min (~ 80% vs. isquemia de 20 min. A pressão diastólica final do ventrículo esquerdo (PDFVE e a pressão de perfusão (PP foram aumentadas nos corações expostos à isquemia de 25 min (5,5 e 1,08 vezes, respectivamente e à isquemia de 30 min (6 e 1,10 vezes, respectivamente vs. isquemia de 20 min. A angiotensina-I ocasionou uma diminuição no +dP/dt max e no produto frequência-pressão (~ 85-94% em todos os períodos de isquemia e um aumento na PDFVE e na PP (6,9 e 1,25 vezes, respectivamente apenas na isquemia de 20 min. O captopril foi capaz de reverter parcial ou completamente os efeitos da angiotensina-I na recuperação funcional nas isquemias de 20 e 25 min CONCLUSÃO: Os dados sugerem que a angiotensina-II participa direta ou indiretamente no dano pós-isquêmico e que a capacidade de um inibidor da ECA atenuar esse dano depende do tempo de isquemia.

  16. Características da clientela atendida por crise hipertensiva na emergência de um hospital municipal de Fortaleza, Estado do Ceará = Characteristics of the clientele assisted for hypertensive crisis in the emergency of a municipal hospital in Fortaleza, Ceará State

    Directory of Open Access Journals (Sweden)

    Ione Cavalcante Lacerda

    2010-01-01

    Full Text Available Objetivou-se descrever as características da clientela com crise hipertensiva. A pesquisa, quantitativa, descritiva e documental foi realizada em um hospital municipal de Fortaleza, Estado do Ceará em 2006. Na análise de 790 fichas de atendimento, observamos que 48,2% dos pacientes que apresentavam crise hipertensiva, encontravam-se na faixa etária de 40 a 59 anos e a maioria dos indivíduos era de casados (57,5%. Os principais sintomas encontrados foram cefaleia (35,7% e dor precordial (12.3% e, em 36,8% das fichas, não houve registro de sinais e sintomas. As medicações mais prescritas foram o captopril (90,6% e furosemida (53%. Conclui-se que a crise hipertensiva acomete muitos adultos, a maioria casados e que geralmente vão à emergência para fazer avaliação clínica de algum sinal/sintoma. Ressalta-se a necessidade de se alertar os profissionais de saúde quanto à importância do registro para conhecimento e compreensão das características dessa clientela para o controle e a prevenção da crise hipertensiva.The objective was to describe the characteristics of the clientele with hypertensive crisis. The research, which was quantitative, descriptive and documentary, was conducted at a municipal hospital in Fortaleza, Ceará Estate in 2006. In the analysis of 790 patient files, we found that 48.2% of patients presenting hypertensive crisis were in the age group between 40 and 59 years old. Most of the individuals were married (57.5%. The main symptoms were headache (35.7% and chest pain (12.3%, and in 36.8% of files there was no record of signs and symptoms. The most prescribed medications were captopril (90.6% and furosemide (53%. We conclude that hypertensive crisis affects many adults, most married and who usually go to the emergency room for clinical evaluation of a sign/symptom. We emphasize the need to alert health professionals about the importance of records for knowledge and understanding of the characteristics of that

  17. Características da clientela atendida por crise hipertensiva na emergência de um hospital municipal de Fortaleza, Estado do Ceará - DOI: 10.4025/actascihealthsci.v32i1.5746 Characteristics of the clientele assisted for hypertensive crisis in the emergency of a municipal hospital in Fortaleza, Ceará State - DOI: 10.4025/actascihealthsci.v32i1.5746

    Directory of Open Access Journals (Sweden)

    Ana Célia Caetano de Souza

    2009-12-01

    Full Text Available Objetivou-se descrever as características da clientela com crise hipertensiva. A pesquisa, quantitativa, descritiva e documental foi realizada em um hospital municipal de Fortaleza, Estado do Ceará em 2006. Na análise de 790 fichas de atendimento, observamos que 48,2% dos pacientes que apresentavam crise hipertensiva, encontravam-se na faixa etária de 40 a 59 anos e a maioria dos indivíduos era de casados (57,5%. Os principais sintomas encontrados foram cefaleia (35,7% e dor precordial (12.3% e, em 36,8% das fichas, não houve registro de sinais e sintomas. As medicações mais prescritas foram o captopril (90,6% e furosemida (53%. Conclui-se que a crise hipertensiva acomete muitos adultos, a maioria casados e que geralmente vão à emergência para fazer avaliação clínica de algum sinal/sintoma. Ressalta-se a necessidade de se alertar os profissionais de saúde quanto à importância do registro para conhecimento e compreensão das características dessa clientela para o controle e a prevenção da crise hipertensiva.The objective was to describe the characteristics of the clientele with hypertensive crisis. The research, which was quantitative, descriptive and documentary, was conducted at a municipal hospital in Fortaleza, Ceará Estate in 2006. In the analysis of 790 patient files, we found that 48.2% of patients presenting hypertensive crisis were in the age group between 40 and 59 years old. Most of the individuals were married (57.5%. The main symptoms were headache (35.7% and chest pain (12.3%, and in 36.8% of files there was no record of signs and symptoms. The most prescribed medications were captopril (90.6% and furosemide (53%. We conclude that hypertensive crisis affects many adults, most married and who usually go to the emergency room for clinical evaluation of a sign/symptom. We emphasize the need to alert health professionals about the importance of records for knowledge and understanding of the characteristics of that

  18. In Vitro Study on Antihypertensive and Antihypercholesterolemic Effects of a Curcumin Nanoemulsion.

    Science.gov (United States)

    Rachmawati, Heni; Soraya, Irene Surya; Kurniati, Neng Fisheri; Rahma, Annisa

    2016-01-01

    Atherosclerosis and hypertension can potentially progess into dangerous cardiovascular diseases such as myocardial infarction and stroke. Statins are widely used to lower cholesterol levels while antihypertensive agents such as captopril are widely prescribed to treat high blood pressure. Curcumin, a phenolic compound isolated from Curcuma domestica, has been proven effective for a broad spectrum of diseases, including hypertension and hypercholesterolemia. Therefore, curcumin is quite promising as an alternative therapeutic compound. Our previous studies have proven a significant increase in physical properties, bioavailability, and stability of curcumin when encapsulated in a nanoemulsion. The purpose of this study was to assess the ability of the nanoemulsion in enhancing curcumin activity as a antihypertensive and antihypercholesterolemic agent. The formulation and preparation method of the curcumin nanoemulsion have been developed in our previous study. Physical characterization was performed, including measurement of droplet size, polidispersity index, zeta potential, entrapment efficiency, and loading capacity. Antihypertensive activity of curcumin was evaluated by determining Angiotensin Converting Enzyme (ACE) inhibition in vitro. A substrate for ACE, hippuryl-L-histidyl-L-leucine was allowed to react with ACE, resulting in hippuric acid formation as the product. The degree of ACE inhibition by curcumin was represented by the amount of hippuric acid formed. Antihypercholesterolemic activity of curcumin was studied using the HMG-CoA reductase assay equipped with a 96-well UV plate. This assay was based on the spectrophotometric measurement of the decrease in absorbance which represents the oxidation of NADPH by the catalytic subunit of 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) in the presence of the substrate HMG-CoA. Curcumin is known to have no significant difference in inhibiting ACE compared to Captopril, but when it was incorporated in the self

  19. Targeting Angiotensin II Type-1 Receptor (AT1R) Inhibits the Harmful Phenotype of Plasmodium-Specific CD8+ T Cells during Blood-Stage Malaria

    Science.gov (United States)

    Silva-Filho, João L.; Caruso-Neves, Celso; Pinheiro, Ana A. S.

    2017-01-01

    CD8+ T-cell response is critical in the pathogenesis of cerebral malaria during blood-stage. Our group and other have been shown that angiotensin II (Ang II) and its receptor AT1 (AT1R), a key effector axis of renin-angiotensin system (RAS), have immune regulatory effects on T cells. Previously, we showed that inhibition of AT1R signaling protects mice against the lethal disease induced by Plasmodium berghei ANKA infection However, most of the Ang II/AT1R actions were characterized by using only pharmacological approaches, the effects of which may not always be due to a specific receptor blockade. In addition, the mechanisms of action of the AT1R in inducing the pathogenic activity of Plasmodium-specific CD8+ T cells during blood-stage were not determined. Here, we examined how angiotensin II/AT1R axis promotes the harmful response of Plasmodium-specific CD8+ T-cell during blood-stage by using genetic and pharmacological approaches. We evaluated the response of wild-type (WT) and AT1R−/− Plasmodium-specific CD8+ T cells in mice infected with a transgenic PbA lineage expressing ovalbumin; and in parallel infected mice receiving WT Plasmodium-specific CD8+ T cells were treated with losartan (AT1R antagonist) or captopril (ACE inhibitor). Both, AT1R−/− OT-I cells and WT OT-I cells from losartan- or captopril-treated mice showed lower expansion, reduced IL-2 production and IL-2Rα expression, lower activation (lower expression of CD69, CD44 and CD160) and lower exhaustion profiles. AT1R−/− OT-I cells also exhibit lower expression of the integrin LFA-1 and the chemokine receptors CCR5 and CXCR3, known to play a key role in the development of cerebral malaria. Moreover, AT1R−/− OT-I cells produce lower amounts of IFN-γ and TNF-α and show lower degranulation upon restimulation. In conclusion, our results show the pivotal mechanisms of AT1R-induced harmful phenotype of Plasmodium-specific CD8+ T cells during blood-stage malaria. PMID:28261571

  20. Possíveis interações medicamentosas entre os antihipertensivos e antidiabéticos em participantes do Grupo HIPERDIA de Parobé, RS (Uma análise teórica

    Directory of Open Access Journals (Sweden)

    Deise Margarete Duarte do Amaral

    2012-01-01

    Full Text Available Devido à alta incidência simultânea de hipertensão arterial sistêmica e diabetes mellitus, é comum encontrar pacientes que usam anti-hipertensivos e antidiabéticos simultaneamente. Desta forma, tornase importante identificar as possíveis interações medicamentosas no tratamento da hipertensão arterial e do diabetes e realizar manejo farmacoterapêutico adequado para evitar efeitos adversos graves ou até a morte. Este trabalho teve como objetivo identificar possíveis interações com os medicamentos antihipertensivos e antidiabéticos em participantes idosos do grupo HIPERDIA no município de Parobé/RS. Trata-se de um estudo quantitativo, observacional e transversal e foi realizado através de um questionário estruturado aplicado em 45 (39 idosos, 37 com interações medicamentosas participantes do programa HIPERDIA. Foram identificadas 144 possíveis interações medicamentosas, sendo 30% desejáveis e 70% indesejáveis. Destas indesejáveis, 85% classificadas como moderada com maior ocorrência da associação de captopril e ácido acetilsalicílico, 5% grave (interação de diurético de alça com digitálico e 10% leves. Das desejáveis, a associação de captopril e hidroclorotiazida teve maior ocorrência. Este estudo revelou um alto índice de possíveis interações medicamentosas em idosos participantes do programa HIPERDIA. A maioria das interações pode comprometer a segurança do paciente, evidenciando a relevância deste tema e a necessidade de avaliar e monitorar a terapêutica medicamentosa no idoso, no sentido de prevenir e diminuir as consequências dos efeitos decorrentes de potenciais interações medicamentosas.

  1. COMPORTAMIENTO DE LAS REACCIONES ADVERSAS A MEDICAMENTOS EN CUBA. AÑO 2007

    Directory of Open Access Journals (Sweden)

    Ashley Chao Cardeso

    2009-01-01

    Full Text Available Introducción. La farmacovigilancia es una actividad de salud pública destinada a la identificación, evaluación y prevención de los riesgos asociados a los medicamentos una vez comercializados. En Cuba existe un sistema de Farmacovigilancia con una tasa elevada de reporte de efectos adversos por medicamentos (7000 a 10 000 casos anuales. Desarrollo. Se realizó un estudio farmacovigilancia, descriptivo, transversal y retrospectivo, que utilizo la Metodología y Procedimientos de Trabajo de la Unidad Coordinadora Nacional de Farmacovigilancia, donde se analizaron todos los reportes de RAM llegados a la unidad durante el 2007 procedentes de todo el país. Resultados: Se analizaron 6928 notificaciones de reacciones adversas medicamentosas (RAM, notificándose 12963 RAM a razón de 1.9 RAM por notificación, de ellas 4251 fueron reacciones importantes (61.3% según criterios establecidos por la unidad coordinadora nacional de farmacovigilancia de Cuba. Los sistemas de órganos más afectados durante el año fueron piel y anejos (1774, 25.6% seguido del tracto gastrointestinal (1438, 20.7%. Entre los fármacos con mayor numero de reportes se encontró captopril (418/6.03%, el ibuprofeno 289 / 4.2% y ciprofloxacina 259/3.7%. Predominaron las RAM probables (68.7% y moderadas 47.1% y las más frecuentes fueron erupción cutánea, vómitos y fiebre. Entre las asociaciones fármaco - RAM muy importantes y con baja frecuencia de aparición se reportaron en total unas 2953 (35.9% en el año, de ellas el 9.1% fueron reacciones no descritas en la literatura revisada. Conclusiones: se detectaron entre una o dos reacciones adversas a medicamentos por cada notificación realizada. Dejando claro la importancia en la selección de los medicamentos y su uso racional. Los fármacos más asociados a las reacciones adversas notificadas fueron captopril, ciprofloxacina e ibuprofeno, la piel y el sistema digestivo fueron los sistemas más afectados y las reacciones

  2. Extent of dispensing prescription-only medications without a prescription in community drug retail outlets in Addis Ababa, Ethiopia: a simulated-patient study

    Science.gov (United States)

    Erku, Daniel Asfaw; Mekuria, Abebe Basazn; Surur, Abdrrahman Shemsu; Gebresillassie, Begashaw Melaku

    2016-01-01

    Purpose This study was aimed at assessing the extent of dispensing prescription-only medications without a prescription in community drug retail outlets (CDROs) of Addis Ababa, Ethiopia. Methods A descriptive cross-sectional observational study design was used to sample 31 pharmacies, 25 drug stores, and two rural drug vendors from August 11, 2015, to October 21, 2015, through a simple random sampling method. A simulated-patient method of visit was implemented to collect data. Requests of six tracer prescription-only medicines (amoxicillin + clavulanic acid capsule, amitriptyline, captopril, glibenclamide [also known as glyburide], omeprazole capsule, and sildenafil citrate) and upper respiratory tract infection were selected as the simulated clinical scenario. Results Amoxicillin–clavulanic acid capsule was dispensed when requested in 87.93% of the dispensaries. All of the CDROs dispensed omeprazole upon request. Sildenafil citrate (Viagra) was in stock in 96.55% of the CDROs, all of which issued the requested number of tablets without asking why or for whom the drug was needed. Amitriptyline, captopril, and glibenclamide (glyburide) were dispensed in 84.48%, 89.65%, and 87.93% of CDROs upon the provision of an empty container. Antibiotics were obtained from 75.86% of CDROs for presentation of upper respiratory tract infection symptoms. Among the dispensed antibiotics, the most common was amoxicillin (93.18%), followed by amoxicillin–clavulanic acid capsule (72.72%), and azithromycin (50%). Only 4.5% of the dispensaries asked about drug allergies, and 15.9% of the CDROs informed the simulated patient about the possible side effects of the drugs. Conclusion This study revealed a very high rate of dispensing of prescription-only medicines without a prescription. Antimicrobials and drugs for chronic diseases were obtained with ease from almost all of the randomly sampled CDROs. Putting good dispensing practice into effect and adhering to the existing national

  3. Síndrome nefrótica primária grave em crianças: descrição clínica e dos padrões histológicos renais de seis casos Severe primary nephrotic syndrome in children: description of clinical aspects and of the renal histological patterns of six cases

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    Márcia Camegaçava Riyuzo

    2006-10-01

    Full Text Available Os autores relatam os casos de seis crianças com síndrome nefrótica primária grave de padrão histológico renal incomum na rotina cotidiana dos nefrologistas e patologistas. O diagnóstico da doença foi realizado nas faixas etárias de 3 a 9 meses de idade (n = 4, aos 2 anos e 4 meses (n = 1 e aos 11 anos (n = 1. Um paciente foi prematuro, duas pacientes eram irmãs e seus pais eram primos de primeiro grau. Todos apresentavam edema generalizado; dois pacientes apresentavam desnutrição e hipotireoidismo e dois apresentavam hipertensão arterial e insuficiência renal. A histologia renal mostrou esclerose mesangial difusa (n = 3, proliferação mesangial (n = 2 e síndrome nefrótica do tipo finlandês (n = 1. Quatro pacientes faleceram, as causas de óbito foram infecção (n = 2, insuficiência renal (n = 1 e acidose metabólica (n = 1. Entre os sobreviventes, um paciente foi tratado com vitaminas, tiroxina, captopril e indometacina, apresentando aumento da albumina sérica e melhora do crescimento. O outro paciente apresentava insuficiência renal terminal, sendo tratado com diálise e transplante renal.The authors report six children with severe primary nephrotic syndrome with unusual renal histological patterns in the daily routine of nephrologists and pathologists. The diagnosis of the disease was made at the age between 3 to 9 months (n = 4, at 2 years and 4 months (n = 1 and at 11 years (n = 1. One patient was born prematurely; two patients were sisters and their parents were first-degree cousins. All patients presented generalized edema, two patients presented malnutrition and hypothyroidism; two patients presented hypertension and renal failure. The renal histology showed diffuse mesangial sclerosis (n = 3; diffuse mesangial hypercellularity (n = 2 and nephrotic syndrome of the Finnish type (n = 1. Four patients died, causes of death were infection (n = 2, renal failure (n = 1 and metabolic acidosis (n = 1. Among the survivors

  4. 联合用药治疗原发性高血压临床效果分析%Clinical Effect Analysis of Primary Hypertension Treated With Combined Medication

    Institute of Scientific and Technical Information of China (English)

    陶巍

    2015-01-01

    目的:探究原发性高血压治疗过程中联合用药的治疗效果。方法随机抽取我院2013年11月~2014年11月接收的70例原发性高血压患者,随机将其分成A组合B组,A组使用联合用药,分别为硝苯地平缓释片和卡托普利片,B组单独使用卡托普利片,对比两组的降压效果。结果治疗效果相比,A组总体有效率为94.3%,B组的总体有效率为74.3%,两组差异具有统计学意义(P<0.05)。结论治疗原发性高血压的降压过程中,联合使用硝苯地平缓释片和卡托普利片,能够实现突出的降压作用,且临床治疗有效率更高。%Objective To explore the process of combination drug therapy in essential hypertension treatment effect. Methods 70 cases of primary hypertension patients in group A, the use of combination therapy, group B used alone Captopril Tablets, antihypertensive effects of two groups were compared. Results In A group, the overall efifciency of 94.3%, the total rate in group B was 74.3%, with a signiifcant difference between two groups (P<0.05). Conclusion The step-down process in the treatment of essential hypertension, the combined use of Extended Release Nifedipine Tablets and Captopril Tablets, the clinical effective rate of the treatment of higher.

  5. Extent of dispensing prescription-only medications without a prescription in community drug retail outlets in Addis Ababa, Ethiopia: a simulated-patient study

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    Erku DA

    2016-07-01

    Full Text Available Daniel Asfaw Erku,1 Abebe Basazn Mekuria,2 Abdrrahman Shemsu Surur,1 Begashaw Melaku Gebresillassie3 1Department of Pharmaceutical Chemistry, 2Department of Pharmacology, 3Department of Clinical Pharmacy, School of Pharmacy, University of Gondar, Gondar, Ethiopia Purpose: This study was aimed at assessing the extent of dispensing prescription-only medications without a prescription in community drug retail outlets (CDROs of Addis Ababa, Ethiopia.Methods: A descriptive cross-sectional observational study design was used to sample 31 pharmacies, 25 drug stores, and two rural drug vendors from August 11, 2015, to October 21, 2015, through a simple random sampling method. A simulated-patient method of visit was implemented to collect data. Requests of six tracer prescription-only medicines (amoxicillin + clavulanic acid capsule, amitriptyline, captopril, glibenclamide [also known as glyburide], omeprazole capsule, and sildenafil citrate and upper respiratory tract infection were selected as the simulated clinical scenario.Results: Amoxicillin–clavulanic acid capsule was dispensed when requested in 87.93% of the dispensaries. All of the CDROs dispensed omeprazole upon request. Sildenafil citrate (Viagra was in stock in 96.55% of the CDROs, all of which issued the requested number of tablets without asking why or for whom the drug was needed. Amitriptyline, captopril, and glibenclamide (glyburide were dispensed in 84.48%, 89.65%, and 87.93% of CDROs upon the provision of an empty container. Antibiotics were obtained from 75.86% of CDROs for presentation of upper respiratory tract infection symptoms. Among the dispensed antibiotics, the most common was amoxicillin (93.18%, followed by amoxicillin–clavulanic acid capsule (72.72%, and azithromycin (50%. Only 4.5% of the dispensaries asked about drug allergies, and 15.9% of the CDROs informed the simulated patient about the possible side effects of the drugs.Conclusion: This study revealed a very high

  6. Screening of inhibitors of angiotensin-converting enzyme (ACE) employing high performance liquid chromatography-electrospray ionization triple quadrupole mass spectrometry (HPLC-ESI-QqQ-MS).

    Science.gov (United States)

    Musharraf, Syed Ghulam; Bhatti, Muhammad Salman; Choudhary, Muhammad Iqbal; Rahman, Atta-Ur

    2017-04-01

    Angiotensin-converting enzyme (ACE) plays a key role in regulating blood pressure in the body by converting the angiotensin I (AI) into angiotensin II (AII). Angiotensin II is a potent vaso-active peptide that causes arterioles to constrict, resulting in increased blood pressure. A rapid and sensitive method for the identification of inhibitors of ACE was developed, and optimized employing HPLC-ESI-QqQ-MS. In this assay, angiotensin I substrate was converted into the product angiotensin II with the catalytic action of ACE. A calibration curve for depleting concentration of angiotensin I was developed and linearity of R(2)=0.999 with a remarkably low concentration of substrate range 20-200nM. The limit of detection and quantification of angiotensin I was found to be 1.93 and 5.84nM, respectively. The enzymatic reaction was optimized for incubation time, concentration, and volume of enzyme and substrate. All reactions were performed at 37°C at pH7.5 with standard incubation time of 20min. Two standard inhibitors, Captopril and Lisinopril, were checked through the newly developed method for their inhibitory potential, and their IC50 values were found to be 3.969 and 0.852μM, respectively. Reproducibility and precision analysis of different experiments showed <9.9% RSD. The developed method can be used for the identification of new ACE inhibitors.

  7. In vivo antihypertensive and antidyslipidemic effects of the crude extracts and fractions of Moringa stenopetala (Baker f. Cufod. leaves in rats.

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    Bekesho eGeleta

    2016-04-01

    Full Text Available Moringa stenopetala (Baker f. Cufod. is a medicinal plant that has been used in Ethiopian traditional medicine as a remedy for treatment of hypertension and diabetes. The aim of this study was to evaluate antihypertensive and antihyperlipidemic effect in fructose induced hypertensive rats.Rats were randomly divided into control and treatment groups (n=6. Treatment groups were given daily extracts (250, 500, and 1000 mg/kg orally with fructose. Whereas, positive, negative and normal control groups were received captopril (20 mg/kg/day with fructose, only fructose (66% w/v ad libitum and distilled water ad libitum for 15 days, respectively. The blood pressure was measured every 5th day using tail cuff blood pressure analyzer, and on the 16th day the blood was sampled to evaluate antihyperlipidemic effect using clinical chemistry analyzer. The study showed that aqueous and 70% ethanol extracts significantly prevented blood pressure increment in a dose dependent manner comparable to that of the standard drug. Similarly, the extracts suppressed increment in lipid profile (cholesterol, glucose and triglycerides compared with negative control. The biochemical test revealed that extracts produced a rise in liver but no effect on kidney function indicators compared with normal control.These findings revealed that both crude extracts of Moringa stenopetala (Baker f. Cufod. possess antihypertensive and antihyperlipidemic effect.

  8. KAJIAN INTERAKSI OBAT ANTIHIPERTENSI PADA PASIEN HEMODIALISIS DI BANGSAL RAWAT INAP RSU PKU MUHAMMADIYAH YOGYAKARTA PERIODE TAHUN 2010

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    Siti Rahmiati

    2012-05-01

    Full Text Available Drug interactions are one of the Drug Related Problems (DRPs that may affect patient treatment outcomes. Hypertension occurs in approximately 10% to 81.5% of hemodialysis patients. The purpose of this study was to determine the incidence of antihypertensive drug interactions in hemodialysis patients in the inpatient wards PKU Muhammadiyah Hospital of Yogyakarta period in 2010. This study descriptive design. Data retrieved retrospectively. Data retrieval were done by taking all the data that meet the criteria of existing research on the medical records of hemodialysis patients in PKU Muhammadiyah Hospital of Yogyakarta who received antihypertensive with above normal blood pressure (= 130/80 mmHg. Data were analyzed based on the descriptive level of significance, onset, and severity. The results showed that there were 54.79% (40 patients of 73 hemodialysis patients potentially experienced drug interactions. Antihypertensive drugs most widely used in hemodialysis patients were ACEI, CCB, and diuretics. Incidence of antihypertensive drug interactions 27 cases (45.76% were most common at a significance level 3, 48 cases (81.36% were onset delayed, and the severity minor of 44 cases (74.58%. The mechanism of interactions pharmacodynamic were 37 cases (62.71% of the total 59 events that have drug interactions. Drugs often interactions were furosemide and captopril.

  9. Case Report: A case report of acromegaly associated with primary aldosteronism [v1; ref status: indexed, http://f1000r.es/2ny

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    Joanna Matrozova

    2014-02-01

    Full Text Available We describe a patient with a rare combination of acromegaly and primary aldosteronism. A 37 year-old female patient was diagnosed with acromegaly on the basis of typical clinical, hormonal and image characteristics. She presented also with one of the most common co-morbidities – arterial hypertension. The patient has been regularly followed-up and after three surgical interventions, irradiation and adjuvant treatment with a dopamine agonist, acromegaly was finally controlled in 2008 (20 years after diagnosis. Arterial hypertension however, remained a therapeutic problem even after prescription of four antihypertensive drugs. She had normal biochemical parameters, except for low potassium levels 3.2 (3.5-5.6 mmol/l. This raised the suspicion of primary hyperaldosteronism, confirmed by a high aldosterone to plasma rennin activity ratio, high aldosterone level after a Captopril challenge test and visualization of a 35 mm left adrenal nodule on a CT scan. After an operation, the patient recovered from hypokalemia and antihypertensive therapy was reduced to a small dose of a Ca blocker. Co-morbid arterial hypertension is common in acromegaly, though it is rare for this to be caused by Conn’s adenoma. The association of Conn’s adenoma with acromegaly has been interpreted in two lines: as a component of multiple endocrine neoplasia type (MEN1 syndrome or as a direct mitogenic effect of hyperactivated GH-IGF1 axis.

  10. Ethanolic extracts and isolated compounds from small-leaf grape (Vitis thunbergii var. taiwaniana) with antihypertensive activities.

    Science.gov (United States)

    Lin, Yin-Shiou; Lu, Yeh-Lin; Wang, Guei-Jane; Chen, Lih-Geeng; Wen, Chi-Luan; Hou, Wen-Chi

    2012-08-01

    This study aimed to investigate the antihypertensive effects of ethanolic extracts (EE) and compounds isolated from the small-leaf grape (Vitis thunbergii var. taiwaniana, VTT). The highest antiangiotensin-converting enzyme (anti-ACE) was found in stem-EE (IC50 was 69.5 μg/mL). In spontaneously hypertensive rats (SHRs), stem-EE effectively reduced blood pressure 24 h after administration of a single oral dose or when administered daily for 4 weeks. The isolated compounds, including (+)-vitisin A, ampelopsin C, and (+)-ε-viniferin, were shown to have anti-ACE and vasodilating effects against phenylephrine-induced tensions in an endothelium-intact aortic ring, with (+)-vitisin A being the most effective compound. Compared to control rats, SHRs showed significantly reduced systolic and diastolic blood pressures 24 h after a single oral dose of (+)-vitisin A (10 mg/kg) or captopril (2 mg/kg). These results suggest that the development of functional foods with VTT extracts may be beneficial for regulating blood pressure.

  11. Clinical Observation on Breviscapine in Treating Hypertension Patients Complicated with Micro-albuminuria of Renal Impairment

    Institute of Scientific and Technical Information of China (English)

    WEI Ling; TAN Jie

    2005-01-01

    Objective:To evaluate the efficacy of Breviscapine on essential hypertension (EH) patients complicated with micro-albuminuria of renal impairment. Methods: Seventy-six EH patients were randomly assigned to the control group and the treated group, the former was given amlodipine, captopril/uropidil and the latter was given in addition Breviscapine intravenously dripped for 2 treatment courses. The indexes of serum creatinine (Cr), blood urea nitrogen (BUN), blood and urinary β2-microglobulin (β2-MG), and quantitative determination of 24 hrs urinary protein were evaluated before and after treatment. Results: In the control group, compared with before treatment, the quantitative determination of 24 hrs urinary protein got reduced significantly (P<0.05), while in the treated group, both urinary β2-MG and quantitative determination of 24 hrs urinary protein got lowered significantly (P<0.05 and P<0.01). But after treatment, compared with the control group, urinary β2-MG and quantitative determination of 24 hrs urinary protein in the treated group were obviously reduced (P<0.05). Conclusion: Besides lowering blood pressure effectively, Breviscapine could improve the renal function significantly and reduce the urinary micro-albuminuria, hence showing promising effect on renal protection.

  12. The restoration of kidney mitochondria function by inhibition of angiotensin-II production in rats with acute adriamycin-induced nephrotoxicity.

    Science.gov (United States)

    Taskin, Eylem; Ozdogan, Kalender; Kunduz Kindap, Elvan; Dursun, Nurcan

    2014-05-01

    Adriamycin (ADR) is commonly used for many solid tumor treatments. Its clinical utility is, however, largely limited by the adverse reactions, are known to be nephrotoxic. The mechanism by which it induces kidney damage is still not completely understood, but its nephrotoxicity might relate to increase reactive oxidant status (ROS), mitochondrial dysfunction. Until now, neurohormonal activation of it is unclear. ADR might activate the renin angiotensin system. Angiotensin-II also induced ROS and mitochondrial dysfunction. The aim of this study was to investigate whether angiotensin-II production inhibition has the protective effect on attenuation of mitochondrial function in rats with acute ADR-nephrotoxicity or not. Rats were divided into five groups as a control, ADR, co-treated ADR with captopril (CAP), co-treated ADR with Aliskren, co-treated ADR with both CAP and Aliskren groups. Creatinine kinase (CK) levels were measured at the end of treatment period. The kidneys were homogenized and biochemical measurements were made in mitochondria, cytosol. Mitochondria membrane potential (MMP) and ATP levels were determined. ADR increased CK levels and oxidative stress in mitochondria too (pinduced nephrotoxicity via the restoration of MMP and ATP production and prevention of mitochondrial damage in vivo.

  13. Eritadenine from Edible Mushrooms Inhibits Activity of Angiotensin Converting Enzyme in Vitro.

    Science.gov (United States)

    Afrin, Sadia; Rakib, Md Abdur; Kim, Boh Hyun; Kim, Jeong Ok; Ha, Yeong Lae

    2016-03-23

    The inhibition of angiotensin converting enzyme (ACE) activity was determined in vitro by mushroom-derived eritadenine (EA), which was analyzed in 11 principal Korean edible mushrooms. EA inhibited ACE activity with 0.091 μM IC50, whereas the IC50 of captopril (CP), which is a reference compound, was 0.025 μM. Kinetic measurements of ACE reaction in the substrate of hippuryl-l-histidyl-l-leucine (HHL) with or without EA revealed that the Vmax (0.0465 O.D/30 min) was unchanged, but the the Km increased from 2.063 to 3.887 mM, indicating that EA competes with HHL for the active site. When EA was analyzed by HPLC, Lentinus edodes with a soft cap contained the highest amount EA (642.8 mg%); however, Phellinus linteus with a hard cap contained the least amount of EA (9.4 mg%). These results indicate that EA was a strong competitive inhibitor for ACE, and edible mushrooms with soft caps contained a significant amount of EA.

  14. The Effects of Velvet Antler of Deer on Cardiac Functions of Rats with Heart Failure following Myocardial Infarction

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    Ming-Jing Shao

    2012-01-01

    Full Text Available Velvet antler of deer (VAD is a commonly-used kidney-Yang supplementing traditional Chinese medication. According to the heart-kidney-related theory, heart Yang originates in kidney Yang and heart failure due to heart Yang deficiency can be treated by tonifying kidney Yang. In this study, we investigated therapeutic effects of VAD on cardiac functions in rats with heart failure following myocardial infarction. Forty-eight male Wistar rats were subjected either to left coronary artery ligation (N=36 or to sham operation (N=12. One week after the surgery, rats with heart failure received daily treatment of double-distilled water, captopril or VAD by gavage for consecutively four weeks, while sham-operated animals were given double-distilled water. Ultrasonic echocardiography was adopted to examine cardiac structural and functional parameters and serum brain natriuretic peptide (BNP concentration was measured using radioimmunoassay. We found that VAD partially reversed changes in cardiac functional parameters and serum BNP levels in rats with heart failure. These results provide further evidence for the heart-kidney-related theory and suggest that VAD might be a potentially alternative and complementary medicine for the treatment of heart failure.

  15. A liver metalloendopeptidase which degrades the circulating hypotensive peptide hormones bradykinin and atrial natriuretic peptide

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    Carvalho K.M.

    1999-01-01

    Full Text Available A new metalloendopeptidase was purified to apparent homogeneity from a homogenate of normal human liver using successive steps of chromatography on DEAE-cellulose, hydroxyapatite and Sephacryl S-200. The purified enzyme hydrolyzed the Pro7-Phe8 bond of bradykinin and the Ser25-Tyr26 bond of atrial natriuretic peptide. No cleavage was produced in other peptide hormones such as vasopressin, oxytocin or Met- and Leu-enkephalin. This enzyme activity was inhibited by 1 mM divalent cation chelators such as EDTA, EGTA and o-phenanthroline and was insensitive to 1 µM phosphoramidon and captopril, specific inhibitors of neutral endopeptidase (EC 3.4.24.11 and angiotensin-converting enzyme (EC 3.4.15.1, respectively. With Mr 85 kDa, the enzyme exhibits optimal activity at pH 7.5. The high affinity of this endopeptidase for bradykinin (Km = 10 µM and for atrial natriuretic peptide (Km = 5 µM suggests that it may play a physiological role in the inactivation of these circulating hypotensive peptide hormones.

  16. Echocardiographic Study on Experimental Coronary Artery Spasm and Spasmolysis%实验性冠状动脉痉挛及缓解痉挛的超声心动图研究

    Institute of Scientific and Technical Information of China (English)

    姚克纯; 刘朝中; 江一清; 王文清; 李德芬

    1995-01-01

    以麦角新碱诱发实验犬的冠状动脉痉挛(痉挛组)及巯甲丙脯酸缓解冠状动脉痉挛(治疗组)进行了超声心动图研究.结果表明,痉挛组左室扩大,室壁运动呈节段性减弱或不协调,心功能下降;治疗组左室轻度扩大,室壁运动幅度减弱及心功能下降逐渐恢复正常;痉挛组和治疗组各项指标均相差非常显著(P<0.01).%This peper reports the study of ergonovineinduced coronary artery spasm of experimental dogs(spasm group)and release of coronary artery spasm(cured group)by captopril by using the echocardiography.The results showed that left ventricular dilatation,wall segments motion hypokinesia or asynergy and decrease in cardiac function of spasm group were found by echocardiography,while the left ventricular mild dilatation,wall motion range and cardiac function of cured group were all gradually recovered to normal.Left ventricular size,wall motion range and cardiac function were significant differences between spasm group and cured group(P<0.01).

  17. Interactions between drugs and drug-nutrient in enteral nutrition: a review based on evidences

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    Renata Ferreira Silva

    Full Text Available Introduction: Enteral nutrition (EN provides calories, macronutrients and micronutrients in adequate quantity and quality to meet the patient's needs. Some drugs when crushed and diluted may have their properties altered, including the reduction of bioavailability causing the reduction of the serum concentration of the drug; tube obstruction; drug-drug interaction or drug-nutrient interaction. Methods: The study was conducted through review of submitted articles in the databases of the Virtual Health Library (VHL: MEDLINE (National Library of Medicine, USA, Lilacs (Latin American and Caribbean Literature on Health Sciences PUBMED - NCBI (National Center for Biotechnology Information and COCHRANE. Results: For this survey, 42 articles were identified during database searching. After applying the inclusion and exclusion criteria, 08 articles were selected, obtained from the MEDLINE and Lilacs. Discussion: Some interactions were found such as the aluminium hydroxide and lactulose with the enteral nutrition, which may result in a precipitation and reduction of drug bioavailability. Mineral oil will alter the absorption of fat-soluble vitamins and reduces the tube light. Others results were found as phenytoin, warfarin, captopril and furosemide with enteral nutrition may reduce the maximum serum concentration. Conclusion: Drug interactions are more common in day-to-day activities than health professionals may suppose. Knowledge on the matter may also assist in reducing cases of obstruction of tubes, through which enteral nutrition and medications are administered. Thus, the multidisciplinary team, acting together, may have more beneficial effects to the patient.

  18. QGQS Granule in SHR Serum Metabonomics Study Based on Tools of UPLC-Q-TOF and Renin-Angiotensin-Aldosterone System Form Protein Profilin-1

    Science.gov (United States)

    2017-01-01

    QGQS granule is effective for the therapeutic of hypertension in clinic. The aim of this research is to observe the antihypertension effect of QGQS granule on SHR and explain the mechanism of its lowering blood pressure. 30 SHR were selected as model group, captopril group, and QGQS group, 10 WKYr were used as control group, and RBP were measured on tail artery consciously. And all the serum sample analysis was carried out on UPLC-TOF-MS system to determine endogenous metabolites and to find the metabonomics pathways. Meanwhile, ELISA kits for the determination pharmacological indexes of PRA, AngI, AngII, and ALD were used for pathway confirmatory; WB for determination of profilin-1 protein expression was conducted for Ang II pathway analysis as well. It is demonstrated that QGQS granule has an excellent therapeutic effect on antihypertension, which exerts effect mainly on metabonomics pathway by regulating glycerophospholipid, sphingolipid, and arachidonic acid metabolism, and it could inhibit the overexpression of the profilin-1 protein. We can come to a conclusion that RAAS should be responsible mainly for the metabonomics pathway of QGQS granule on antihypertension, and it plays a very important role in protein of profilin-1 inhibition.

  19. Duodenal pseudomelanosis (pseudomelanosis duodeni: a rare endoscopic finding

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    Aloísio Felipe-Silva

    2011-12-01

    Full Text Available Duodenal pseudomelanosis (or pseudomelanosis duodeni is a rare benigncondition characterized by black-brown speckled pigmentation of the duodenalmucosa. Collections of pigment−laden macrophages are found in the tips ofduodenal villi. The pigment is thought to be mostly composed of ferrous sulfide.Histochemichal stains for iron (Perl’s prussian blue or melanin (Masson-Fontana may be positive, but are usually negative or unpredictable. Duodenalpseudomelanosis occurs predominantly in middle-aged to old adults andmore commonly in females. It is associated with chronic renal failure, arterialhypertension, diabetes mellitus and gastrointestinal bleeding. Medications suchas ferrous sulfate, hydralazine, propranolol, hydrochlorothiazide and furosemideare thought to play a role as well. We report a case of a 86-year-old femalewho presented with a history of watery diarrhea and melena. The patient had ahistory of high blood pressure and ischemic stroke episodes. She was on multiplemedication including hidralazine, captopril, hydrochlorthiazide and aspirin. She wasdehydrated, her blood pressure was 96 × 60 mmHg and neurologic examinationshowed complete left hemiplegia with central VII nerve palsy. Laboratory testsshowed normal serum electrolytes and renal function. Hemoglobin level was10.7 g%. An upper endoscopy showed multiple diminutive black spots throughoutthe distal duodenal bulb and second portion. Histology showed multiple foci ofa brown-black granular pigment inside macrophages within the tips of the villi(pseudomelanosis. Stains for iron and melanin were negative. She was treatedwith omeprazol, parenteral fluid replacement with saline and partial fasting. Aftercomplete recovery she was discharged for ambulatory follow up.

  20. Role of Regulatory Peptide in Pathogenesis of Shock

    Institute of Scientific and Technical Information of China (English)

    董林旺; 常英姿; 佟利家; 汤健; 苏静怡; 唐朝枢

    1994-01-01

    The present study evaluated the pathogenetic roles of three kinds of regulatory peptide. The results showed that (i) plasma endothelin(ET) level elevated significantly in septic shock rats, persistent intravenous drip of low doses ET caused development of shock state in normal rats and the irreversible outcome of light hemorrhagic shock. Furthermore, i. v. administration of specific ET-antiserum was significantly effective to septic shock rats, (Ⅱ) Plasma calcitonin gene-related peptide (CGRP) increased by 260% in septic shock rats, i. v. drip of low doses CGRP both in early and late sepsis were effective to shock rats, (Ⅱi) An-giotensin-Ⅱ (ANG-Ⅱ) contents of heart and aorta increased dramatically both in early and late septic shock, and inhibiting its increase with Captopril in late sepsis significantly improved the shock state, but results were inverse in early sepsis. It could be concluded that ET was one of the most important factors participating in the pathogenesis of shock, CGRP had a compens

  1. Metabolomic profiles of myocardial ischemia under treatment with salvianolic acid B

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    Lu Yonghai

    2012-03-01

    Full Text Available Abstract Background Radix Salvia miltiorrhiza (Danshen has been used as a principal herb in treating cardiovascular diseases in Chinese medicine. Salvianolic acid B (SA-B, a water-soluble active component of Danshen, was found to have anti-myocardial ischemia (anti-MI effect. This study aims to investigate mechanisms of SA-B on MI. Methods Five conventional Western medicines (isosorbide dinitrate, verapamil, propranolol, captopril and trimethazine with different mechanisms for treating cardiovascular diseases were selected as positive references to compare with SA-B in changing of the metabolomic profiles in MI rats under treatment. Potential mechanisms of SA-B were further investigated in H9C2 cell line. Results The metabolomic profiles between SA-B- and propranolol-treated MI rats were similar, since there was a big overlap between the two groups in the PLS-DA score plot. Finally, it was demonstrated that SA-B exhibited a protective effect on MI mainly by decreasing the concentration of cyclic adenosine monophosphate (cAMP and Ca2+ and inhibiting protein kinase A (PKA. Conclusion SA-B and propanolol exhibited similar metabolomic profiles, indicating that the two drugs might have a similar mechanism.

  2. Vasopressin contributes to maintenance of arterial blood pressure in dehydrated baboons.

    Science.gov (United States)

    Ryan, K L; Thornton, R M; Proppe, D W

    1989-02-01

    This study primarily sought to determine whether the role of vasopressin (VP) in maintenance of arterial blood pressure is enhanced in awake, chronically instrumented baboons after 68-72 h of dehydration. This question was approached by pharmacologically blocking vasopressin V1-receptors in euhydrated and dehydrated baboons with or without a normally functioning renin-angiotensin system (RAS). VP blockade during dehydration produced a rapidly occurring (within 5 min), statistically significant (P less than 0.05) decrease in mean arterial pressure (MAP) of 5 +/- 1 mmHg in the RAS-intact condition and an identical decline in MAP (5 +/- 1 mmHg) during blockade of the RAS by captopril, an angiotensin I-converting enzyme inhibitor. At 15 min after induction of VP blockade, heart rate was elevated by 9 +/- 2 beats/min in the RAS-intact condition and by 20 +/- 5 beats/min in the RAS-blocked condition. In addition, VP blockade in the dehydrated state produced small and equal increases in hindlimb vascular conductance in RAS-intact and RAS-blocked conditions. None of these cardiovascular changes were produced by VP blockade in the euhydrated state. RAS blockade produced modest declines in MAP in both hydration states, but the fall was larger by 7 +/- 4 mmHg in the dehydrated state. Thus both VP and the RAS contribute to the maintenance of arterial blood pressure during dehydration in the conscious baboon.

  3. Chemistry and pharmacological properties of some natural and synthetic antioxidants for heavy metal toxicity.

    Science.gov (United States)

    Flora, S J S; Shrivastava, Rupal; Mittal, Megha

    2013-01-01

    Heavy metals are known to cause oxidative deterioration of bio-molecules by initiating free radical mediated chain reaction resulting in lipid per-oxidation, protein oxidation and oxidation of nucleic acid like DNA and RNA. The development of effective dual functioning antioxidants, possessing both metal-chelating and free radical-scavenging properties should bring into play. Administration of natural and synthetic antioxidants like, quercetin, catechin, taurine, captopril, gallic acid, melatonin, N-acetyl cysteine, α- lipoic acid and others have been recognized in the disease prevention and clinical recovery against heavy metal intoxication. These antioxidants affect biological systems not only through direct quenching of free radicals but also via chelation of toxic metal(s). These antioxidants also, have the capacity to enhance cellular antioxidant defense mechanism by regenerating endogenous antioxidants, such as glutathione and vitamin C and E. They also influence cellular signaling and trigger redox sensitive regulatory pathways. The reactivity of antioxidants in protecting against heavy metal induced oxidative stress depends upon their structural properties, their partitioning abilities between hydrophilic and lipophilic environment and their hydrogen donation antioxidant properties. Herein, we review the structural, biochemical and pharmacological properties of selected antioxidants with particular reference to their ability to (i) chelate heavy metals from its complex (ii) ameliorate free radical (iii) terminate heavy metal induced free radical chain reaction (iv) regenerate endogenous antioxidants and, (v) excretion of metal without its redistribution.

  4. RU28318, an Aldosterone Antagonist, in Combination with an ACE Inhibitor and Angiotensin Receptor Blocker Attenuates Cardiac Dysfunction in Diabetes

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    Ibrahim F. Benter

    2013-01-01

    Full Text Available Aims. We evaluated the effects of RU28318 (RU, a selective mineralocorticoid receptor (MR antagonist, Captopril (Capt, an angiotensin converting enzyme inhibitor, and Losartan (Los, an angiotensin receptor blocker, alone or in combination with ischemia/reperfusion- (I/R- induced cardiac dysfunction in hearts obtained from normal and diabetic rats. Methods. Isolated hearts were perfused for 30 min and then subjected to 30 min of global ischemia (I followed by a period of 30 min of reperfusion (R. Drugs were administered for 30 min either before or after ischemia. Drug regimens tested were RU, Capt, Los, RU + Capt, RU + Los, Capt + Los, and RU + Capt + Los (Triple. Recovery of cardiac hemodynamics was evaluated. Results. Recovery of cardiac function was up to 5-fold worse in hearts obtained from diabetic animals compared to controls. Treatment with RU was generally better in preventing or reversing ischemia-induced cardiac dysfunction in normal hearts compared to treatment with Capt or Los alone. In diabetic hearts, RU was generally similarly effective as Capt or Los treatment. Conclusions. RU treatment locally might be considered as an effective therapy or preventative measure in cardiac I/R injury. Importantly, RU was the most effective at improving -dP/dt (a measure of diastolic function when administered to diabetic hearts after ischemia.

  5. Case Report: A case report of acromegaly associated with primary aldosteronism [v2; ref status: indexed, http://f1000r.es/3ke

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    Joanna Matrozova

    2014-06-01

    Full Text Available We describe a patient with a rare combination of acromegaly and primary aldosteronism. A 37 year-old female patient was diagnosed with acromegaly on the basis of typical clinical, hormonal and image characteristics. She presented also with one of the most common co-morbidities – arterial hypertension. The patient has been regularly followed-up and after three surgical interventions, irradiation and adjuvant treatment with a dopamine agonist, acromegaly was finally controlled in 2008 (20 years after diagnosis. Arterial hypertension however, remained a therapeutic problem even after prescription of four antihypertensive drugs. She had normal biochemical parameters, except for low potassium levels 3.2 (3.5-5.6 mmol/l. This raised the suspicion of primary hyperaldosteronism, confirmed by a high aldosterone to plasma rennin activity ratio, high aldosterone level after a Captopril challenge test and visualization of a 35 mm left adrenal nodule on a CT scan. After an operation, the patient recovered from hypokalemia and antihypertensive therapy was reduced to a small dose of a Ca blocker. Co-morbid arterial hypertension is common in acromegaly, though it is rare for this to be caused by Conn’s adenoma. The association of Conn’s adenoma with acromegaly has been interpreted in two lines: as a component of multiple endocrine neoplasia type (MEN1 syndrome or as a direct mitogenic effect of hyperactivated GH-IGF1 axis.

  6. How to Give TCM Differential Treatment for Senile Severe Hypertension?

    Institute of Scientific and Technical Information of China (English)

    2007-01-01

    @@ Senile severe hypertension refers to the condition in patients over 60 years old who have a diastolic pressure ≥ 14.7 kPa (110 mmHg) and a systolic pressure ≥ 26.7 kPa (200mmHg). Usually, the course of illness is long, and accompanied with various degrees of visceral lesions of the heart, brain and kidney. It has been proved by clinical experience that the blood pressure can't be made to decrease too fast nor decrease too slow so as to prevent the severe complications which may happen after a long-term high blood pressure. In addition to small dosage of such western drugs as Nifepine (10mg), Captopril (12.5mg) and Atenolol (12.5mg), Chinese herbal drugs can be prescribed based on TCM differentiation of the syndromes for lowering the blood pressure, improving the blood supply of the heart and brain, and relieving the clinical symptoms. The TCM differential treatment can be given for the following 3 patterns of syndromes.

  7. A quantitative peptidomics approach to unravel immunological functions of angiotensin converting enzyme in Locusta migratoria.

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    Duressa, Tewodros Firdissa; Boonen, Kurt; Huybrechts, Roger

    2016-09-01

    Locusta migratoria angiotensin converting enzyme (LmACE) is encoded by multiple exons displaying variable number of genomic duplications. Treatments of lipopolysaccharide (LPS) as well as peptidoglycan but not β-1-3 glucan resulted in enhanced expression of angiotensin converting enzyme in hemocytes of Locusta migratoria. No such effect was observed in fat body cells. Differential peptidomics using locust plasma samples post infection with LPS in combination with both an LmACE transcript knockdown by RNAi and a functional knockdown using captopril allowed the identification of 5 circulating LPS induced peptides which only appear in the hemolymph of locust having full LmACE functionality. As these peptides originate from larger precursor proteins such as locust hemocyanin-like protein, having known antimicrobial properties, the obtained results suggest a possible direct or indirect role of LmACE in the release of these peptides from their precursors. Additionally, this experimental setup confirmed the role of LmACE in the clearance of multiple peptides from the hemolymph.

  8. Effects of hydrogen peroxide treatment on thiol contents in fresh-cut asparagus (Asparagus officinalis) spears.

    Science.gov (United States)

    Demrkol, Omca

    2009-01-01

    In this work, the impact of hydrogen peroxide (H2O2) was investigated on the thiol content of asparagus. Fresh-cut asparagus was treated with H2O2 at varied oxidant concentrations and contact times. A significant decrease (alpha=0.05) was observed in N-acetylcysteine levels treated with 2.5% H2O2 for 10 min and with 5% H2O2 for 3, 5 and 10 min. Captopril and cysteine levels significantly decreased (alpha=0.05) in all and most treatment conditions, respectively. Glutathione levels only significantly decreased with 2.5% and 5% H2O2 for 10 min treatment. In order to determine whether asparagus undergoes oxidative stress, a well-known oxidative stress indicator-the glutathione/oxidized glutathione ratio-was calculated. This study showed that the common use of H2O2 as a disinfectant/sterilizer by the food industry could markedly diminish the important biothiols and develop oxidative stress in asparagus, and potentially in other vegetables as well.

  9. Ginkgo biloba extract suppresses hypertrophy and extracellular matrix accumulation in rat mesangial cells

    Institute of Scientific and Technical Information of China (English)

    Jian-yun WANG; Xiao-xing YIN; Yun-ming WU; Dao-quan TANG; Yuan-yuan GAO; Mei-rong WAN; Xiao-yu HOU; Bei ZHANG

    2006-01-01

    Aim: To observe the effects of Ginkgo biloba extract (EGb) on the hypertrophy of mesangial cells and the accumulation of extracellular matrix (ECM) in mesangial cells. Methods: Cultured mesangial cells were allotted into 7 groups: normal group, solvent control group, high glucose group, low dose of EGb group, moderate dose of EGb group, high dose of EGb group, and captopril group. Activities of cell antioxidases, S phase percentage and G0/G1 phase percentage, collagen Ⅳ and laminin, Smad2/3 and Smad7, TGF-β1, Mrna were measured by different methods. Results: For EGb-treated groups, when compared with high glucose group, the cell percentage of S phase was raised and the percentage of G0/G1 was lowered. The intensity of oxidative stress was weakened. The expression of Smad2/3 was greatly decreased and Smad7 was increased. Collagen Ⅳ, laminin and TGF-β1 Mrna were also reduced. Conclusion: EGb can suppress cell hypertrophy and the accumulation of ECM in rat mesangial cells, which means it could play a vital role in the delay of glomerulosclerosis in diabetic nephropathy.

  10. Inhibition of angiotensin Ⅱ and blockade of endothelin receptors reduce arterial calcification in rats

    Institute of Scientific and Technical Information of China (English)

    Juxiang LI; Shengying WU; Chunshui PAN; Yongfen QI; Bin GENG; Xiuhua LIU; Chaoshu TANG

    2004-01-01

    Objective To examine whether the two vascular paracrine/autocrine factors, angiotensin Ⅱ (Ang Ⅱ) and endothelin, participate in the pathogenesis of arterial calcification. Methods Nicotine and vitamin D3 treated rats were studied. Vascular calcification was confirmed by using Von Kossa staining, measurement of calcium content,45Ca2+ uptake assay and alkaline phosphatase (ALP) activity. The plasma and vascular Ang Ⅱ and endothelin levels were measured by using radioimmunoassay. Angiotensinogen and endothelin mRNA levels were determined by RTPCR. Results The arterial calcium content, 45Ca2+ uptake and ALP activity were increased in calcification groups compared with control ( P < 0.01 ). Administration of the angiotensin receptor antagonist losartan, the endothelin receptor antagonist bosentan, and the angiotensin-converting enzyme inhibitor captopril reduced significantly the arterial calcium content, 45Ca2+ uptake and ALP activity. In addition, the plasma and aortic Ang Ⅱ and endothelin contents, and vascular angiotensinogen and endothelin mRNA expression were significantly up-regulated ( P <0.05).Conclusions These findings suggest that functional renin-angiotensin system and endothelin pathway are involved in vascular calcification, and that activation of these systems could potentiate pathogenesis of arterial calcification. ( J Geriatr Cardiol 2004;1(2) :108-113. )

  11. EVALUATION OF THE RELATIVE INCIDENCE OF ADVERSE EFFECTS LEADING TO TREATMENT DISCONTINUATION OF RECOMMENDED ANTIHYPERTENSIVE DRUGS

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    Yakubu Sani Ibn

    2013-06-01

    Full Text Available This study aimed at evaluating the incidence of adverse effects leading to treatment discontinuation of antihypertensive drugs within the same therapeutic class. Individual medical records were searched to identify those hypertensive patients who had been commenced on antihypertensive therapy during a 24-month period and who had subsequently for a reason(s discontinued the therapy. The results showed variation in discontinuation rates for drugs within same class, and that might be related to the relative frequency of specific adverse effects. Cough was the reason cited for discontinuation of angiotensin converting enzyme inhibitors, with linosopril appearing to be better tolerated than captopril (39% vs 48% ; peripheral oedema with calcium channel blockers, with amlodipine appearing to be better tolerated than nifedipine (29% vs 38% and bradycardia with beta adrenergic receptor blockers, with propranolol better tolerated than atenolol (0% vs 48%. Diuretics showed the lowest discontinuation rate (3.3% mainly due to hypokalemia, with thiazide better tolerated than frusemide (11% vs 43%. Prescribers should verify their use of antihypertensive drugs to ensure that they prescribe drugs with lower adverse effect rates, in order that patients with hypertension continue using the medication in the long term, thereby reducing the risk of developing cardiovascular complications associated with uncontrolled blood pressure.

  12. Inhibition of Urease by Disulfiram, an FDA-Approved Thiol Reagent Used in Humans

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    Ángel Gabriel Díaz-Sánchez

    2016-11-01

    Full Text Available Urease is a nickel-dependent amidohydrolase that catalyses the decomposition of urea into carbamate and ammonia, a reaction that constitutes an important source of nitrogen for bacteria, fungi and plants. It is recognized as a potential antimicrobial target with an impact on medicine, agriculture, and the environment. The list of possible urease inhibitors is continuously increasing, with a special interest in those that interact with and block the flexible active site flap. We show that disulfiram inhibits urease in Citrullus vulgaris (CVU, following a non-competitive mechanism, and may be one of this kind of inhibitors. Disulfiram is a well-known thiol reagent that has been approved by the FDA for treatment of chronic alcoholism. We also found that other thiol reactive compounds (l-captopril and Bithionol and quercetin inhibits CVU. These inhibitors protect the enzyme against its full inactivation by the thiol-specific reagent Aldrithiol (2,2′-dipyridyl disulphide, DPS, suggesting that the three drugs bind to the same subsite. Enzyme kinetics, competing inhibition experiments, auto-fluorescence binding experiments, and docking suggest that the disulfiram reactive site is Cys592, which has been proposed as a “hinge” located in the flexible active site flap. This study presents the basis for the use of disulfiram as one potential inhibitor to control urease activity.

  13. Gallic acid isolated from Spirogyra sp. improves cardiovascular disease through a vasorelaxant and antihypertensive effect.

    Science.gov (United States)

    Kang, Nalae; Lee, Ji-Hyeok; Lee, WonWoo; Ko, Ju-Young; Kim, Eun-A; Kim, Jin-Soo; Heu, Min-Soo; Kim, Gwang Hoon; Jeon, You-Jin

    2015-03-01

    In this study, we investigated the vasorelaxant and antihypertensive effects of gallic acid (GA), a polyphenol isolated from the green alga Spirogyra sp., to assess its suitability as a therapeutic for cardiovascular diseases (CVDs). We examined the effect of GA on endothelium-dependent vasorelaxation in human umbilical vein endothelial cells (HUVECs). GA increased nitric oxide (NO) levels by increasing phosphorylation of endothelial nitric oxide synthase (eNOS), and its effect on NO production was attenuated by pretreatment with the eNOS inhibitor N(G)-nitro-L-arginine methyl ester (L-NAME). We also investigated its antihypertensive effect by examining GA-mediated inhibition of angiotensin-I converting enzyme (ACE). GA inhibited ACE with a half-maximal inhibitory concentration (IC50) value of 37.38 ± 0.39 μg/ml. In silico simulations revealed that GA binds to the active site of ACE (PDB: 1O86) with a binding energy of -270.487 kcal/mol. Furthermore, GA clearly reduced blood pressure in spontaneously hypertensive rats (SHR) to an extent comparable to captopril. These results suggest that GA isolated from Spirogyra sp. exerts multiple therapeutic effects and has potential as a CVD treatment.

  14. Management of Cyclosporine and Nifedipine-Induced Gingival Hyperplasia

    Science.gov (United States)

    Dilber, Erhan; Aral, Kübra; Sarica, Yagmur; Sivrikoz, Oya Nermin

    2015-01-01

    Gingival enlargements modified by medications are becoming more common because of the increased use of inducing drugs, and may create speech, mastication, tooth eruption, periodontal, and aesthetic problems. We hereby present a case of a 54-year-old man with 12-month history of generalized gingival enlargement in the keratinized gingiva was referred to our clinic. The patient had a history of kidney transplant and was under medication of cyclosporine and nifedipine. After medical consultation, cyclosporine was changed to tacrolimus and nifedipine was changed to captopril. Gingivectomy was performed using a diode laser, and scaling and root planning were performed. At five months postoperative, the gingival enlargements relapsed and diode laser-assisted surgery was repeated. The patient was followed-up on second postoperatively at 18 months and no relapse was seen. Diode laser-assisted gingivectomy was found to be useful for coagulation during surgery and decreased postoperative bleeding. Recurrence risk of cyclosporine and nifedipine-induced gingival overgrowth is high, thus, there is a great need for prolonged care of patients following treatment and prosthetic restoration. PMID:26812935

  15. Efecto vasodilatador mediado por óxido nítrico del extracto hidroalcohólico de Zea mays L. (maíz morado en anillos aórticos de rata Vasodilator effect mediated by nitric oxide of the Zea mays L (andean purple corn hydroalcoholic extract in aortic rings of rat

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    Oscar Moreno-Loaiza

    2010-12-01

    Full Text Available Objetivo. Evaluar la respuesta vasodilatadora e inhibidora de la vasoconstricción del extracto hidroalcohólico de Zea mays L. (maíz morado y determinar si esta respuesta es mediada por óxido nítrico (NO. Materiales y métodos. Se obtuvo un extracto de las corontas de maíz morado maceradas durante ocho días en etanol al 70%, y posterior concentración del producto. Se trabajó con anillos aórticos de rata en cámara de órganos aislados, bañada con solución Krebs-Hensleit (K-H y se registró la actividad vasomotora con un transductor de tensión isométrica. Se produjo una contracción basal con KCl 120 mM sobre la cual determinó el efecto vasodilatador de tres dosis del extracto: 0,1; 0,5 y 1,0 mg/mL. Se utilizó L-NG-Nitroarginina metil ester (L-NAME para comprobar que la vasodilatación depende de la óxido nítrico sinteasa (NOs. Luego se comparó la inhibición de la contracción vascular tras la incubación durante 30 minutos, con extracto de maíz morado y captopril 10-5 M. Resultados. Se observó una reducción de la contracción máxima (100% a 85,25 ± 2,60%, 77,76 ± 3,23% y 73,3 ± 4,87%, para las dosis de 0,1; 0,5 y 1,0 mg/mL, respectivamente. La vasodilatación fue inhibida por la incubación previa con L-NAME. El extracto de maíz morado no inhibió la contracción vascular, a diferencia del captopril (reducción a 75,27 ± 8,61%. Conclusión. El extracto hidroalcohólico de Zea mays L produce vasodilatación dependiente de la síntesis de NO.Objective: To evaluate the vasodilator response of the hydroalcoholic extract of Zea mays L. (Andean purple corn and to determine if this response is mediated by nitric oxide (NO. Material and methods: We obtained an extract by maceration for eight days of Andean purple corn cobs in 70% ethanol and subsequent concentration of the product. Thoracic aortic rings were evaluated in an isolated organ chamber, bathed with Krebs-Hensleit solution (KH, and vasomotor activity was recorded

  16. TRATAMENTO FARMACOLÓGICO DA HIPERTENSÃO ARTERIAL EM UNIDADE DE TERAPIA INTENSIVA CORONARIANA

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    Gilmara Holanda da Cunha

    2010-01-01

    Full Text Available La administración de fármacos es una de las actividades realizadas por el equipo de enfermería. Teniendo esto en cuenta, el objetivo fue describir el tratamiento farmacológico de la hipertensión arterial en una unidad de cuidados intensivos coronarios. Estudio transversal realizado en un hospital de referencia en Fortaleza-CE, entre mayo y noviembre de 2008. Se analizaron 62 historiales médicos, verificándose que un 54,8% de los pacientes era del sexo masculino con edad entre 50 y 79 años. Fueron indicados 12 fármacos antihipertensivos, destacándose el captopril. La terapia con tres (3 medicamentos fue la más frecuente, con una correlación significativa (p <0,001 entre las variables rango de edad y tipo de terapia. En todos los casos estudiados, las dosis de los fármacos eran adecuadas. La principal vía de administración fue oral. Se concluyó que para llevar a cabo la administración de antihipertensivos es necesario conocer el mecanismo de acción, las interacciones medicamentosas y reacciones adversas, tema a ser constantemente actualizado por los enfermeros.

  17. Evaluation of the pharmacological treatment of arterial hypertension associated to heart failure in Camarones town.

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    Pedro Miguel Milián Vázquez.

    2006-12-01

    Full Text Available Background: Arterial hypertension is a risk factor for many cardiovascular and cerebrovascular diseases. Objective: To evaluate the pharmacological treatment in patients with arterial hypertension, also suffering from heart failure. Methods: A descriptive-prospective study was carried out, this consisted in the use of prescription-indication drugs through a simple random sample study of 43 patients, representing the 35.2 % in six Family Clinical Units of the urban area of Camarones’ Communitarian Policlinic, Palmira, Cienfuegos, during the first semester of 2004. Results: the 51.2 % of the patients were included in the class II of the New York Heart Asociation’s classification, and the 55.8% were considered hypertense class II. The hypertensive drugs more used were the captopril and the clortalidone, and among the drugs associated to the hypertensive ones it was included the isosorbide dinitrate, the digoxin and the acetylsalicylic acid. The 87.3 % of the patients received a correct dose, and in the 88.9% it was followed an adequate administration interval. The prescription was considered adequate in the 65.1 % of the studied patients. Conclusions: the advances in the treatment of these diseases are due to different factors, even though the study shows that the treatment of the patient of the series is adecuate, it should be bettered as long as possible.

  18. 桃红四物汤对大鼠心梗后心肌间质胶原重构的影响%Influence of Taohong Siwu Decoction on Myocardium Interstitial Collagen Reconstitution after Acute Myocardial Infarction in Rats

    Institute of Scientific and Technical Information of China (English)

    周迎春; 刘彬; 王娇; 孙学刚; 黄桂琼; 曾研津; 陈婧

    2011-01-01

    Objective: To investigate the effects of Taohong Siwu Decoction on myocardium interstitial collagen reconstitution in the non-infarction regions of left ventricle in rats after acute myocardial infarction.Method: Male Wistar SPF rats were used. The ventricle remodeling was induced by ligating the left main coronary artery. Ventricle remodeling rats were divided into 4 groups: Model group,Taohong Siwu Decoction group, captopril group,sham group( n = 12, each). Taohong Siwu Decoction group was orally given the decoction of 4. 86 g· kg-1.Captopril group was given captopril suspension at 0.2 g· kg- 1 with free drinking of water. Sham group and model control groups were given the same volume of drinking water. All the rats were continuously treated for 12 weeks.Afterwards,the rats were killed, the myocardial tissues were sampled and then pathologically observed through Masson trichrome staining. The proteins of myocardial tissue collagen Ⅰ and collagen Ⅲ were determined through immunohistochemical methods. Result: Myocardial myofibril and myofilament in Taohong Siwu Decoction group were in good order,normal morphology, evenly and thinly distributed collagenous fibers, myocardial mesenchyme fibrosis obviously decreased compared with those in the model comparison group. The content of myocardium collagen and the ratio of myocardial collagen type Ⅰ to Ⅲ collagen protein in model control group were obviously higher than that in the sham operation group. The content of myocardium collagen and the ratio of myocardial collagen type Ⅰ to Ⅲ collagen protein in Taohong Siwu group and captopril group were lower than those in model control group.Conclusion: Taohong Siwu Decoction can inhibit proliferation of myocardium interstitial collagenous fibers and expression of collagen protein after acute myocardial infarction in rats, cut down the ratio of myocardial collagen type Ⅰ to Ⅲ collagen protein in the non-infarction regions of left ventricle,relief collagen

  19. Magistral drugs in hospitalized newborns and children

    Science.gov (United States)

    Pereira, Agueda Cabral de Souza; Miranda, Elaine Silva; de Castilho, Selma Rodrigues; Futuro, Débora Omena; Teixeira, Lenise Arneiro; de Paula, Geraldo Renato

    2016-01-01

    Abstract Objective: Study the use of magistral oral solutions and suspensions in infants and children at a university hospital. Methods: This is a descriptive study based on the analysis of the assessed hospital's magistral drug request forms regarding the patients in the neonatal ICU, Obstetrics, Pediatrics and Pediatric Emergency from January 2012 to December 2013. The frequency of drug requests and dispensation was evaluated and the consumption of each active ingredient of the preparations was expressed as number of “infant defined daily dose” (iDDD) and of iDDD/100 bed-days. Results: A total of 657 forms were analyzed - a monthly average of 27 pediatric preparations. The neonatal ICU accounted for 69.6% of these requests. Twenty-one drug items were used, of which the most common were folinic acid (88 requests), sulfadiazine (85) and captopril (73). The consumption of the active principle in these preparations varied in number of iDDD, from 7.5 (hydralazine) to 16,520.0 (folic acid), and in number of iDDD/100 bed-days in the neonatal ICU, from 0.1 (zinc sulfate) to 146.1 (folic acid). Conclusions: The constant consumption of magistral oral solutions and suspensions by newborns and children of the assessed hospital indicates the need for such preparations as a pediatric therapeutic alternative in this hospital. PMID:27131897

  20. Three dimensional structural insight of laser drilled orifices in osmotic pump tablets.

    Science.gov (United States)

    Wu, Li; Wang, Lebing; Wang, Shuxia; Xiao, Tiqiao; Chen, Min; Shao, Qun; York, Peter; Singh, Vikaramjeet; Yin, Xianzhen; Gu, Jingkai; Zhang, Jiwen

    2016-10-10

    The orifice drilled in the membrane as a channel for drug delivery is the key functional part of the osmotic pumps for a controlled drug release system. Reported conventional microscopic evaluations of these orifices have been limited to measurement of two-dimensional cross-section diameters. This study was aimed at establishing a novel method to measure quantitatively the three-dimensional architectures of orifices based on synchrotron radiation X-ray microcomputed tomography (SR-μCT). Quantitative analysis of architectures extracted from captopril osmotic pumps drilled by a range of operating parameters indicated that laser power correlated with the cross section area, volume, surface area and depth of the orifices, while scanning speed of laser beam showed inverse relationships with the above structure characters. The synchrotron radiation based Fourier transform infrared microspectroscopy mapping showed that there was no apparent chemical change in the surrounding area of the orifice compared with the normal membrane region. Thus SR-μCT was successfully applied to marketed felodipine osmotic pumps for architectural evaluation of the orifices. In conclusion, the first three-dimensional structural insight of orifices in osmotic pump tablets by SR-μCT and structural reconstruction for the architectures has provided deeper insight into improving the design of advanced osmotic pumps for controlled drug release.

  1. Dutch guideline for the management of hypertensive crisis -- 2010 revision.

    Science.gov (United States)

    van den Born, B J H; Beutler, J J; Gaillard, C A J M; de Gooijer, A; van den Meiracker, A H; Kroon, A A

    2011-05-01

    Hypertensive crises are divided into hypertensive urgencies and emergencies. Together they form a heterogeneous group of acute hypertensive disorders depending on the presence or type of target organs involved. Despite better treatment options for hypertension, hypertensive crisis and its associated complications remain relatively common. In the Netherlands the number of patients starting renal replacement therapy because of 'malignant hypertension' has increased in the past two decades. In 2003, the first Dutch guideline on hypertensive crisis was released to allow a standardised evidence-based approach for patients presenting with a hypertensive crisis. In this paper we give an overview of the current management of hypertensive crisis and discuss several important changes incorporated in the 2010 revision. These changes include a modification in terminology replacing 'malignant hypertension' with 'hypertensive crisis with retinopathy and reclassification of hypertensive crisis with retinopathy under hypertensive emergencies instead of urgencies. With regard to the treatment of hypertensive emergencies, nicardipine instead of nitroprusside or labetalol is favoured for the management of perioperative hypertension, whereas labetalol has become the drug of choice for the treatment of hypertension associated with pre-eclampsia. For the treatment of hypertensive urgencies, oral administration of nifedipine retard instead of captopril is recommended as first-line therapy. In addition, a section on the management of hypertensive emergencies according to the type of target organ involved has been added. Efforts to increase the awareness and treatment of hypertension in the population at large may lower the incidence of hypertensive crisis and its complications.

  2. In vivo Antihypertensive and Antihyperlipidemic Effects of the Crude Extracts and Fractions of Moringa stenopetala (Baker f.) Cufod. Leaves in Rats

    Science.gov (United States)

    Geleta, Bekesho; Makonnen, Eyasu; Debella, Asfaw; Tadele, Ashenif

    2016-01-01

    Background: Moringa stenopetala (Baker f.) Cufod. is a medicinal plant that has been used in Ethiopian traditional medicine as a remedy for treatment of hypertension and diabetes. The aim of this study was to evaluate antihypertensive and antihyperlipidemic effect in fructose induced hypertensive rats. Methods: Rats were randomly divided into control and treatment groups (n = 6). Treatment groups were given daily extracts (250, 500, and 1000 mg/kg) orally with fructose. Whereas, positive, negative and normal control groups were received captopril (20 mg/kg/day with fructose), only fructose (66% w/v ad libitum) and distilled water ad libitum for 15 days, respectively. The blood pressure was measured every 5th day using tail cuff blood pressure analyzer, and on the 16th day the blood was sampled to evaluate antihyperlipidemic effect using clinical chemistry analyzer. Results: The study showed that aqueous and 70% ethanol extracts significantly prevented blood pressure increment in a dose dependent manner comparable to that of the standard drug. Similarly, the extracts suppressed increment in lipid profile (cholesterol, glucose, and triglycerides) compared with negative control. The biochemical test revealed that extracts produced a rise in liver but no effect on kidney function indicators compared with normal control. Conclusion: These findings revealed that both crude extracts of M. stenopetala (Baker f.) Cufod. possess antihypertensive and antihyperlipidemic effect. PMID:27148056

  3. Prediction of Clinically Relevant Safety Signals of Nephrotoxicity through Plasma Metabolite Profiling

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    W. B. Mattes

    2013-01-01

    Full Text Available Addressing safety concerns such as drug-induced kidney injury (DIKI early in the drug pharmaceutical development process ensures both patient safety and efficient clinical development. We describe a unique adjunct to standard safety assessment wherein the metabolite profile of treated animals is compared with the MetaMap Tox metabolomics database in order to predict the potential for a wide variety of adverse events, including DIKI. To examine this approach, a study of five compounds (phenytoin, cyclosporin A, doxorubicin, captopril, and lisinopril was initiated by the Technology Evaluation Consortium under the auspices of the Drug Safety Executive Council (DSEC. The metabolite profiles for rats treated with these compounds matched established reference patterns in the MetaMap Tox metabolomics database indicative of each compound’s well-described clinical toxicities. For example, the DIKI associated with cyclosporine A and doxorubicin was correctly predicted by metabolite profiling, while no evidence for DIKI was found for phenytoin, consistent with its clinical picture. In some cases the clinical toxicity (hepatotoxicity, not generally seen in animal studies, was detected with MetaMap Tox. Thus metabolite profiling coupled with the MetaMap Tox metabolomics database offers a unique and powerful approach for augmenting safety assessment and avoiding clinical adverse events such as DIKI.

  4. Organ distribution of quantum dots after intraperitoneal administration, with special reference to area-specific distribution in the brain

    Energy Technology Data Exchange (ETDEWEB)

    Kato, Shingo; Itoh, Kyoko; Yaoi, Takeshi; Tozawa, Takenori; Fushiki, Shinji [Department of Pathology and Applied Neurobiology, Graduate School of Medical Science, Kyoto Prefectural University of Medicine, Kyoto (Japan); Yoshikawa, Yutaka; Yasui, Hiroyuki [Department of Analytical and Bioinorganic Chemistry, Kyoto Pharmaceutical University, Kyoto (Japan); Kanamura, Narisato [Department of Dental Medicine, Graduate School of Medical Science, Kyoto Prefectural University of Medicine, Kyoto (Japan); Hoshino, Akiyoshi; Manabe, Noriyoshi; Yamamoto, Kenji, E-mail: sfushiki@koto.kpu-m.ac.jp [The International Clinical Research Center, Research Institute, International Medical Center of Japan, Tokyo (Japan)

    2010-08-20

    Quantum dots (QDs) are well known for their potential application in biosensing, ex vivo live-cell imaging and in vivo animal targeting. The brain is a challenging organ for drug delivery, because the blood brain barrier (BBB) functions as a gatekeeper guarding the body from exogenous substances. Here, we evaluated the distribution of bioconjugated QDs, i.e., captopril-conjugated QDs (QDs-cap) following intraperitoneal injection into male ICR mice as a model system for determining the tissue localization of QDs, employing ICP-MS and confocal microscopy coupled with spectrometric analysis. We have demonstrated that intraperitoneally administered QDs-cap were delivered via systemic blood circulation into liver, spleen, kidney and brain at 6 h after injection. QDs-cap were located predominantly inside the blood vessels in the liver, kidney and brain, but a few were distributed in the parenchyma, especially noteworthy in the brain. Careful studies on acute as well as chronic toxicity of QDs in the brain are required prior to clinical application to humans.

  5. Blood pressure-decreasing effect of etamicastat alone and in combination with antihypertensive drugs in the spontaneously hypertensive rat.

    Science.gov (United States)

    Igreja, Bruno; Pires, Nuno Miguel; Bonifácio, Maria João; Loureiro, Ana Isabel; Fernandes-Lopes, Carlos; Wright, Lyndon Christopher; Soares-da-Silva, Patrício

    2015-01-01

    Hyperactivation of the sympathetic nervous system has an important role in the development and progression of arterial hypertension. This study evaluated the efficacy of etamicastat, a dopamine-β-hydroxylase (DβH) inhibitor, in controlling high blood pressure in the spontaneously hypertensive rat (SHR), either alone or in combination with other classes of antihypertensives. SHRs were administered with etamicastat by gavage, and its pharmacodynamic and pharmacokinetic properties were evaluated. Etamicastat induced a time-dependent decrease in noradrenaline-to-dopamine ratios in the heart and kidney, and had no effect on catecholamine levels in the frontal cortex of SHRs. Cardiovascular pharmacodynamic effects following administration of etamicastat alone or in combination with other classes of antihypertensive drugs were assessed by telemetry. Etamicastat was evaluated in combination with captopril, losartan, hydrochlorothiazide, metoprolol, prazosin and/or diltiazem. Etamicastat monotherapy induced a dose-dependent reduction in blood pressure without reflex tachycardia. Combination therapy amplified the antihypertensive effects of all tested drugs. In conclusion, inhibition of peripheral DβH with etamicastat, as a monotherapy or combination therapy, may constitute a valid alternative treatment for high blood pressure.

  6. Radionuclides in nephrology

    Energy Technology Data Exchange (ETDEWEB)

    Lausanne, A.B.D.

    1987-01-01

    In 47 expert contributions, this volume provides a summary of the latest research on radionuclides in nephro-urology together with current and new clinical applications especially in renovascular hypertension, kidney transplantation, and metabolic and urological diseases. In addition, attention is given to aspects of basic renal physiology and function and possible applications of nuclear magnetic resonance and spectroscopy in nephro-urology. New testing procedures which promise to improve diagnosis, and new radiopharmaceuticals are described. The reports are divided into eight sections, the first of which features studies on the renin-angiotensin system, cisplatin, atrial natriuretic factor and determining plasma oxalate. Four papers describe a number of new radiopharmaceuticals which have the potential to replace hippuran. In the third section, radionuclide methods for the measurement of renal function parameters are discussed. The book then focuses on the potential role of captopril in the improved diagnosis of renovascular hypertension. Applications of nuclear magnetic resonance and spectroscopy are demonstrated in the diagnosis of acute pyelonephritis, kidney assessment after lithotripsy, kidney evaluation prior to transplantation, and in monitoring renal ischemia during hypotension.

  7. Endocrine functional diagnosis in primary aldosteronism%原发性醛固酮增多症的内分泌功能诊断

    Institute of Scientific and Technical Information of China (English)

    张妮娅; 郑仁东; 刘超

    2012-01-01

    原发性醛固酮增多症(原醛症)是继发性高血压最常见的原因之一,以低肾素和高醛固酮血症为特征,血浆醛固酮/肾素比值(ARR)是筛查原醛症的可靠指标.而口服高钠负荷试验、生理盐水试验、氟氯可的松抑制试验或卡托普利试验中的任何一项均可作为ARR阳性患者的确诊试验;肾上腺静脉插管采血(AVS)是原醛症分型诊断的金标准.%Primary aldosteronism is one of the most common causes of secondary hypertension,which is characterized by low plasma renin and high aldosterone,and a major reliable tool for screening primary aldosteronism is the plasma aldosterone/renin activity ratio (ARR).Any of the four confirmatory tests such as oral sodium loading,intravenous saline infusion,captopril challenge and fludrocortisone administration plus sodium loading may carry out in patients who have positive ARR.And adrenal vein sampling (AVS) is recommended as the golden standard to diagnose primary aldosteronism.

  8. Acute Childhood Cardiorenal Syndrome and Impact of Cardiovascular Morbidity on Survival

    Directory of Open Access Journals (Sweden)

    Wasiu A. Olowu

    2011-01-01

    Full Text Available Cardiorenal syndrome (CRS clinical types, prevalence, aetiology, and acute cardiovascular morbidity impact on the outcome of acute kidney function perturbation were determined. Forty-seven of 101 (46.53% patients with perturbed kidney function had CRS. Types 3 and 5 CRS were found in 10 and 37 patients, respectively. Type 3 CRS was due to acute glomerulonephritis (AGN; =7, captopril (=1, frusemide (=1, and hypovolaemia (=1. Malaria-associated haemoglobinuria (=20, septicaemia (=11, lupus nephritis (=3, tumour lysis syndrome (=2, and acute lymphoblastic leukaemia (=1 caused Type 5 CRS. The cumulative mortality in hypertensive CRS was similar to nonhypertensive CRS (51.4% versus 40.9%; =.119. Mortality in CRS and non-CRS was similar (45.7% versus 24.5%; =.053. Type 5 survived better than type 3 CRS (66.7% versus 12.5%; =.001. Risk factors for mortality were Type 3 CRS (=.001, AGN-associated CRS (=.023, dialysis requiring CRS (=.008, and heart failure due to causes other than anaemia (=.003. All-cause-mortality was 34.2%. Preventive measures aimed at the preventable CRS aetiologies might be critical to reducing its prevalence.

  9. Minimal sufficient balance-a new strategy to balance baseline covariates and preserve randomness of treatment allocation.

    Science.gov (United States)

    Zhao, Wenle; Hill, Michael D; Palesch, Yuko

    2015-12-01

    In many clinical trials, baseline covariates could affect the primary outcome. Commonly used strategies to balance baseline covariates include stratified constrained randomization and minimization. Stratification is limited to few categorical covariates. Minimization lacks the randomness of treatment allocation. Both apply only to categorical covariates. As a result, serious imbalances could occur in important baseline covariates not included in the randomization algorithm. Furthermore, randomness of treatment allocation could be significantly compromised because of the high proportion of deterministic assignments associated with stratified block randomization and minimization, potentially resulting in selection bias. Serious baseline covariate imbalances and selection biases often contribute to controversial interpretation of the trial results. The National Institute of Neurological Disorders and Stroke recombinant tissue plasminogen activator Stroke Trial and the Captopril Prevention Project are two examples. In this article, we propose a new randomization strategy, termed the minimal sufficient balance randomization, which will dually prevent serious imbalances in all important baseline covariates, including both categorical and continuous types, and preserve the randomness of treatment allocation. Computer simulations are conducted using the data from the National Institute of Neurological Disorders and Stroke recombinant tissue plasminogen activator Stroke Trial. Serious imbalances in four continuous and one categorical covariate are prevented with a small cost in treatment allocation randomness. A scenario of simultaneously balancing 11 baseline covariates is explored with similar promising results. The proposed minimal sufficient balance randomization algorithm can be easily implemented in computerized central randomization systems for large multicenter trials.

  10. Metabolomic profiles of myocardial ischemia under treatment with salvianolic acid B

    Science.gov (United States)

    2012-01-01

    Background Radix Salvia miltiorrhiza (Danshen) has been used as a principal herb in treating cardiovascular diseases in Chinese medicine. Salvianolic acid B (SA-B), a water-soluble active component of Danshen, was found to have anti-myocardial ischemia (anti-MI) effect. This study aims to investigate mechanisms of SA-B on MI. Methods Five conventional Western medicines (isosorbide dinitrate, verapamil, propranolol, captopril and trimethazine) with different mechanisms for treating cardiovascular diseases were selected as positive references to compare with SA-B in changing of the metabolomic profiles in MI rats under treatment. Potential mechanisms of SA-B were further investigated in H9C2 cell line. Results The metabolomic profiles between SA-B- and propranolol-treated MI rats were similar, since there was a big overlap between the two groups in the PLS-DA score plot. Finally, it was demonstrated that SA-B exhibited a protective effect on MI mainly by decreasing the concentration of cyclic adenosine monophosphate (cAMP) and Ca2+ and inhibiting protein kinase A (PKA). Conclusion SA-B and propanolol exhibited similar metabolomic profiles, indicating that the two drugs might have a similar mechanism. PMID:22409910

  11. Traditional Chinese medicine suppresses left ventricular hypertrophy by targeting extracellular signal-regulated kinases signaling pathway in spontaneously hypertensive rats

    Science.gov (United States)

    Xiong, Xingjiang; Yang, Xiaochen; Duan, Lian; Liu, Wei; Zhang, Yun; Liu, Yongmei; Wang, Pengqian; Li, Shengjie; Li, Xiaoke

    2017-01-01

    Chinese herbal medicine Bu-Shen-Jiang-Ya decoction (BSJYD) is reported to be beneficial for hypertension. Over expression of extracellular signal regulated kinases (ERK) pathway plays an important role in left ventricular hypertrophy (LVH). This study aimed to observe effects of BSJYD on LVH in spontaneously hypertensive rats (SHRs) and explore its possible mechanism on regulation of ERK pathway. Sixty 12-week-old SHRs were randomly allocated into 5 groups: BSJYD high dose group, middle dose group, low dose group, captopril group, and control group. Besides, a control group of Wistar-Kyoto rats was established. All rats were treated for 8 weeks. Systolic blood pressure (SBP), heart rate (HR), pathology, and left ventricular mass index (LVMI) were measured. Western blotting and Real-time PCR were used to assess the expressions of BDNF, Ras, ERK1/2, and c-fox levels. SBP and HR were significantly decreased compared with the control group and LVMI was markedly improved by BSJYD treatment in a dose-dependent manner. BSJYD inhibited the expression of BDNF, Ras, ERK1/2, and c-fox mRNA in LVH. In conclusion, BSJYD suppressed hypertension-induced cardiac hypertrophy by inhibiting the expression of ERK pathway. These changes in gene expression may be a possible mechanism by which BSJYD provides myocardial protection from hypertension. PMID:28225023

  12. Marketing research on the angiotensin-converting enzyme inhibitors antihypertensive medicines

    Science.gov (United States)

    BOBOIA, ANAMARIA; GRIGORESCU, MARIUS RAREŞ; TURCU - ŞTIOLICĂ, ADINA

    2017-01-01

    Background and aims The research aimed at investigating sales trends of angiotensin-converting enzyme inhibitors antihypertensive medicines, both in terms of quantity and value, in ten community pharmacies, for a period of three years. The research on the antihypertensive medicines consumption is important for highlighting the ever increasing impact of hypertension among the population. Methods The methods used in this research were the following: marketing research, method of sampling, descriptive methods, retrospective analysis, method of comparison. Results The results showed that the drugs containing the active substances of the angiotensin converting enzyme inhibitors class had had significant increases in quantitative and value sales, bringing substantial revenues to pharmacies. From the quantitative perspective, the best-selling products were those containing Enalaprilum, while in terms of value, the best-selling medicines were those containing Perindoprilum. We evidenced that spectacular sales were also achieved for products that have Lisinoprilum, respectively Captoprilum, as active substances. The largest quantities were marketed for the Captopril Terapia® product and the highest earnings were recorded for the Prestarium® medicine. Conclusion This paper approaches an interesting and topical issue, which can be helpful to professionals (pharmacists, doctors) and other categories, such as economists, statisticians, representatives of companies manufacturing medicines, as well as to hypertensive patients, as it could be used to warn population regarding the incidence of cardiovascular diseases, and, at the same time, trace sales trends in order to accomplish profitable business plans. PMID:28246502

  13. Moxonidine into the lateral parabrachial nucleus modifies postingestive signals involved in sodium intake control.

    Science.gov (United States)

    Gasparini, S; Menani, J V; Daniels, D

    2015-01-22

    The activation of α2-adrenoceptors with bilateral injections of moxonidine (α2-adrenoceptor and imidazoline receptor agonist) into the lateral parabrachial nucleus (LPBN) increases 1.8% NaCl intake induced by treatment with furosemide (FURO)+captopril (CAP) subcutaneously. In the present study, we analyzed licking microstructure during water and 1.8% NaCl intake to investigate the changes in orosensory and postingestive signals produced by moxonidine injected into the LPBN. Male Sprague-Dawley rats were treated with FURO+CAP combined with bilateral injections of vehicle or moxonidine (0.5 nmol/0.2 μl) into the LPBN. Bilateral injections of moxonidine into the LPBN increased FURO+CAP-induced 1.8% NaCl intake, without changing water intake. Microstructural analysis of licking behavior found that this increase in NaCl intake was a function of increased number of licking bursts from 15 to 75 min of the test (maximum of 49±9 bursts/bin, vs. vehicle: 2±2 bursts/bin). Analysis of the first 15 min of the test, when most of the licking behavior occurred, found no effect of moxonidine on the number of licks/burst for sodium intake (24±5 licks/burst, vs. vehicle: 27±8 licks/burst). This finding suggests that activation of α2-adrenoceptors in the LPBN affects postingestive signals that are important to inhibit and limit sodium intake by FURO+CAP-treated rats.

  14. Insights into the Hypertensive Effects of Tityus serrulatus Scorpion Venom: Purification of an Angiotensin-Converting Enzyme-Like Peptidase

    Directory of Open Access Journals (Sweden)

    Daniela Cajado-Carvalho

    2016-11-01

    Full Text Available The number of cases of envenomation by scorpions has grown significantly in Brazil since 2007, with the most severe cases being caused by the Tityus serrulatus scorpion. Although envenomed patients mostly suffer neurotoxic manifestations, other symptoms, such as hypertension, cannot be exclusively attributed to neurotoxins. Omics analyses have detected plentiful amounts of metalloproteases in T. serrulatus venom. However, the roles played by these enzymes in envenomation are still unclear. Endeavoring to investigate the functions of scorpion venom proteases, we describe here for the first time an Angiotensin I-Converting Enzyme-like peptidase (ACE-like purified from T. serrulatus venom. The crude venom cleaved natural and fluorescent substrates and these activities were inhibited by captopril. Regarding the serum neutralization, the scorpion antivenom was more effective at blocking the ACE-like activity than arachnid antivenom, although neither completely inhibited the venom cleavage action, even at higher doses. ACE-like was purified from the venom after three chromatographic steps and its identity was confirmed by mass spectrometric and transcriptomic analyses. Bioinformatics analysis showed homology between the ACE-like transcript sequences from Tityus spp. and human testis ACE. These findings advance our understanding of T. serrulatus venom components and may improve treatment of envenomation victims, as ACE-like may contribute to envenomation symptoms, especially the resulting hypertension.

  15. Antinuclear antibody-negative, drug-induced lupus caused by lisinopril.

    Science.gov (United States)

    Carter, J D; Valeriano-Marcet, J; Kanik, K S; Vasey, F B

    2001-11-01

    The clinical symptoms of drug-induced lupus (DIL) are similar to those of idiopathic systemic lupus erythematosus. The literature indicates that in patients with DIL, sera generally contain antinuclear antibodies (ANAs); however, ANA-negative DIL has been reported. The list of medications implicated as etiologic agents in DIL continues to grow. This list includes two different types of angiotensin-converting enzyme inhibitors--captopril and enalapril. We report the first case of DIL caused by lisinopril. Our patient had negative results on ANA testing and had histone antibodies (IgG anti-[H2A-H2B]-DNA) mirroring the disease course. Antibodies to the (H2A-H2B)-DNA complex are seen in more than 90% of patients with active DIL, excluding those with DIL due to hydralazine. Thus, it is important to recognize the clinical significance of IgG anti-(H2A-H2B)-DNA antibodies and that negative ANA test results do not preclude the diagnosis of DIL.

  16. Layered double hydroxides as supports for intercalation and sustained release of antihypertensive drugs

    Science.gov (United States)

    Xia, Sheng-Jie; Ni, Zhe-Ming; Xu, Qian; Hu, Bao-Xiang; Hu, Jun

    2008-10-01

    Zn/Al layered double hydroxides (LDHs) were intercalated with the anionic antihypertensive drugs Enalpril, Lisinopril, Captopril and Ramipril by using coprecipitation or ion-exchange technique. TG-MS analyses suggested that the thermal stability of Ena -, Lis - (arranged with monolayer, resulted from X-ray diffraction (XRD) and Fourier transform infrared spectra (FT-IR) analysis was enhanced much more than Cap - and Ram - (arranged with bilayer). The release studies show that the release rate of all samples markedly decreased in both pH 4.25 and 7.45. However, the release time of Ena -, Lis - were much longer compared with Cap -, Ram - in both pH 4.25 and 7.45, it is possible that the intercalated guests, arranged with monolayer in the interlayer, show lesser repulsive force and strong affinity with the LDH layers. And the release data followed both the Higuchi-square-root law and the first-order equation well. Based on the analysis of batch release, intercalated structural models as well as the TG-DTA results, we conclude that for drug-LDH, stronger the affinity between intercalated anions and the layers is, better the thermal property and the stability to the acid attack of drug-LDH, and the intercalated anions are easier apt to monolayer arrangement within the interlayer, were presented.

  17. Insights into the Hypertensive Effects of Tityus serrulatus Scorpion Venom: Purification of an Angiotensin-Converting Enzyme-Like Peptidase

    Science.gov (United States)

    Cajado-Carvalho, Daniela; Kuniyoshi, Alexandre Kazuo; Duzzi, Bruno; Iwai, Leo Kei; de Oliveira, Úrsula Castro; Junqueira de Azevedo, Inácio de Loiola Meirelles; Kodama, Roberto Tadashi; Portaro, Fernanda Vieira

    2016-01-01

    The number of cases of envenomation by scorpions has grown significantly in Brazil since 2007, with the most severe cases being caused by the Tityus serrulatus scorpion. Although envenomed patients mostly suffer neurotoxic manifestations, other symptoms, such as hypertension, cannot be exclusively attributed to neurotoxins. Omics analyses have detected plentiful amounts of metalloproteases in T. serrulatus venom. However, the roles played by these enzymes in envenomation are still unclear. Endeavoring to investigate the functions of scorpion venom proteases, we describe here for the first time an Angiotensin I-Converting Enzyme-like peptidase (ACE-like) purified from T. serrulatus venom. The crude venom cleaved natural and fluorescent substrates and these activities were inhibited by captopril. Regarding the serum neutralization, the scorpion antivenom was more effective at blocking the ACE-like activity than arachnid antivenom, although neither completely inhibited the venom cleavage action, even at higher doses. ACE-like was purified from the venom after three chromatographic steps and its identity was confirmed by mass spectrometric and transcriptomic analyses. Bioinformatics analysis showed homology between the ACE-like transcript sequences from Tityus spp. and human testis ACE. These findings advance our understanding of T. serrulatus venom components and may improve treatment of envenomation victims, as ACE-like may contribute to envenomation symptoms, especially the resulting hypertension. PMID:27886129

  18. 降钙素基因相关肽对实验性心肌肥厚的影响%The Impact of Calcitonin Gene Related Peptide on Experiment Cardiac Hypertrophy

    Institute of Scientific and Technical Information of China (English)

    张欣; 刘玉龙; 张海峰; 李春跃; 王美玲

    2011-01-01

    ) , captopril groups (N = 10). One week after surgery,CGRP group received CGRP 8 |xg/( kg ? D -1 ) and captopril group was given captopril 30 mg/( kg ? D -1 ). The rats were killed 4 weeks later. The indicators were detected. Changes in ventricular structure were observed in the light microscope and ET, NO levels of ventricular muscle were measured respectively with radioimmunoassay and nitric acid reduction method. It is compared with control group, SBP, LVW / BW and myocardial ET levels of rats in constriction group were significantly higher (P < 0. 05 ) and NO significantly decreased ( P < 0. 05 ). Compared with the constriction group, SBP, LVW / BW and myocardial ET levels were significantly lower in the intervention group (P <0. 05) and level of NO in the myocardium (P <0. 05) were higher. There was a positive correlation between myocardial NO-a,ET and left ventricular mess index. The observations in the light microscope; compared with the control group, in the constriction group, myocardial fiber diameter was significantly thicker, nuclear hypertrophy, deep staining, abnormal and myocardial fiber gap widened. And the fibrous connective tissue of stroma increased. In CGRP group and captopril group, myocardial fiber diameter and nucleus were narrower than the constriction group. The degree of proliferation of quality significantly decreaed in the constriction group . Patterns have been similar to the control group. It is conclused that: (1) Reduction in the level of NO in the myocardium and increased level of ET may be involved in the development of pressure overload cardiac hypertrophy. (2) CGRP has a certain reversal effect of hypertensive cardiac hypertrophy and the effect is similar to captopri, the commonly used anti-hypertensive drugs in clinic.

  19. ACE-inhibition and angiotensin II receptor blockers in chronic heart failure: pathophysiological consideration of the unresolved battle.

    Science.gov (United States)

    Simko, F; Simko, J; Fabryova, M

    2003-05-01

    Reducing the effects of angiotensin II by blockade of AT1-receptors may be superior to inhibition of angiotensin II formation by angiotensin converting enzyme (ACE) inhibitors in chronic heart failure (CHF) patients. However, the results of several trials did not fulfil this expectation. In both ELITE II with symptomatic CHF patients and in OPTIMAAL involving high risk patients after acute myocardial infarction, angiotensin II type I (AT1) receptor blocker (ARB) losartan did not prove to be superior to captopril. There are several potential reasons, why ARBs did not fare better than ACE inhibitors. Although AT1-receptor blockade may block the effects of non-ACE pathways of tissue angiotensin II formation, no clinical evidence is available that a more powerful inhibition of the tissue renin-angiotensin system brings improved survival. The choice of patients for clinical trials of HF therapy is not based on the level of neurohumoral activation. Thus, the more effective attenuation of angiotensin II action with ARBs may not bring additional benefits. The potential antiremodeling effect of ARBs through the stimulation of AT2 receptors by angiotensin II could be counterbalanced by a failure of AT1-receptor blockers to enhance bradykinin, nitric oxide and prostacyclin formation with antigrowth properties. Although ACE-inhibitors seem to have slightly better results at present than AT1 blockers in the battle on heart failure patient, future trials will decide which is the definitive winner.

  20. Rapid recovery following fulminant meningococcemia complicated by myocarditis in a 15-year-old Nepalese girl: a case report

    Directory of Open Access Journals (Sweden)

    Shrestha P

    2013-08-01

    Full Text Available Pratyush Shrestha,1 Nabin K Shrestha,2 Smith Giri31Department of Surgery, College of Medical Sciences, Bharatpur, Nepal; 2Department of Internal Medicine, BP Koirala Institute of Health Sciences, Dharan, Nepal; 3Department of Internal Medicine, Tribhuvan University Teaching Hospital, Kathmandu, NepalIntroduction: Fulminant meningococcemia is a relatively rare life-threatening disease caused by Neisseria meningitidis. The clinical presentation is varied, but, when associated with myocarditis, it carries a particularly poor prognosis. We report a case of a patient with fulminant meningococcemia who subsequently developed severe myocardial dysfunction and successfully recovered within a period of 14 days of hospitalization.Case presentation: A 15-year-old girl presented with headache, fever, body ache, and diarrhea for 1 day, and ecchymotic rash over her body for 4 hours. Blood cultures confirmed infection with N. meningitidis. After 6 days in the hospital, the patient developed anasarca, elevated jugular venous pressure, and shock. The patient was managed with intravenous ceftriaxone and captopril. Over the next 3 days the patient rapidly improved and started walking.Conclusion: Meningococcemia complicated by myocarditis has an extremely poor prognosis with high mortality. Our case suggests that recovery from a severe myocardial dysfunction can occur rapidly within a few days. Prompt recognition and management in this case might have contributed to the patient's rapid recovery from myocarditis.Keywords: Neisseria meningitidis, Nepal, recovery, shock

  1. CATETERES EM TERAPIA INTENSIVA

    Directory of Open Access Journals (Sweden)

    Carolina de Deus Lisboa

    2014-01-01

    Full Text Available Pesquisa com os objetivos de identificar falhas na administração de medicamentos por sondas e caracterizar a interrupção ou não da nutrição no caso de medicamentos que exigem jejum relativo. Estudo epidemiológico, transversal, observacional, numa terapia intensiva, com amostra de 350 doses administradas por 56 técnicos de enfermagem. Resultados mostraram que não houve pausa entre a administração do medicamento e a infusão de dieta enteral em 116 (33,14% doses de medicamentos que necessitavam de jejum relativo, entre os quais captopril, varfarina sódica, levotiroxina sódica, digoxina e fenitoína sódica. A irrigação das sondas não ocorreu na maioria dos casos (94,28%. Conclui-se que é possível que os medicamentos citados tenham tido sua biodisponibilidade sérica reduzida, comprometendo sua eficácia terapêutica e que a falta da prática de irrigar sondas com água estéril, antes de administrar medicamentos, configura-se como a ausência de um cuidado específico fundamental para evitar a obstrução das mesmas.

  2. 高脂饮食叙利亚金黄地鼠胰岛局部血管紧张素Ⅱ的生成途径研究%Pathways of local angiotensin II generation in islets of Langerhans in Syrian golden hamster fed with high-fat diet

    Institute of Scientific and Technical Information of China (English)

    叶文慧; 孙侃; 孙嘉; 张桦; 陈宏; 蔡德鸿

    2011-01-01

    AIM : To investigate the diverse pathways of local angiotensin Ⅱ ( Ang Ⅱ ) generation in islets of Langerhans in Syrian golden hamsters with dyslipidemia.METHODS : The Syrian golden hamsters were fed with high - fat diet to induce dyslipidemia.Purified islet cells from dyslipidemia and normal Syrian hamsters were prepared and divided into control group, captopril group, chymotrypsin endostatin group, aprotinin group, α - antitrypsin group and captopril +chymotrypsin endostatin group by adding respective reagents into the cultured cells after treated with angiotensin Ⅰ.The Ang Ⅱ levels in the supernatants of each group were examined hy ELISA.RESULTS : Compared with the c:ontrol animals, Ang Ⅱ levels decreased in all groups with interventions.Compared with the normal hamsters islet cells, the Ang Ⅱ levels in captopril group, chymotrypsin endostatin group, α - antitrypsin group, aprotinin group and captopril + chymotrypsin endostatin group were decreased by 39.98% , 50.10% ( P< 0.01 ), 23.04%, 20.85% ( P < 0.05 ) and 82.78% ( P <0.01 ), respectively.Compared with high - fat group, the corresponding data were 42.12% , 56.96% ( P < 0.01 ),26.11% . 22.68% ( P < 0.05 ) and 83.59% ( P <0.01 ), respectively.The levels of Ang Ⅱ in chymotrypsin group between normal and high - fat diet hamsters were significantly different ( P < 0.05 ).CONCLUSION : Under the condition of dyslipidemia, the classic angiotensin - converting enzyme - based pathway and chymotrypsin pathway are still the main approaches of producing Ang Ⅱ in male Syrian hamster islet to produce angiotensin.The effect of chymotrypsin endostatin is comparatively stronger in inhibiting the production of local Ang Ⅱ than the effect of angiotensin - converting enzyme inhihitor.%目的:观察不同抑制剂阻断局部肾素血管紧张素系统(RAS)后,对血脂谱异常血症叙利亚金黄地鼠胰岛细胞生成血管紧张素Ⅱ(AngⅡ)的影响,探讨高脂饮

  3. COMPORTAMIENTO DEL USO DE HIPOTENSORES EN EL POLICLÍNICO CAPITÁN ROBERTO FLEITES / Use of hypotensive medications at Capitán Roberto Fleites Polyclinic

    Directory of Open Access Journals (Sweden)

    Fernando Martínez Fernández

    2013-04-01

    Full Text Available Resumen: Introducción y objetivos: El uso racional de los medicamentos debe tomar como base la información científica disponible acerca de su eficacia, seguridad, comodidad de administración y costo. El objetivo de este estudio fue caracterizar el comportamiento del uso de fármacos hipotensores. Método: Se realizó una investigación de utilización de medicamentos, de tipo indicación-prescripción, en diez consultorios médicos de la familia del área de salud perteneciente al policlínico Capitán "Roberto Fleites", en el período entre julio y diciembre de 2011. La muestra estuvo constituida por 431 pacientes hipertensos, a los que se les hicieron 680 prescripciones de fármacos hipotensores controlados por certificados de medicamentos. Las variables analizadas fueron: edad, sexo, grupos farmacológicos, fármacos hipotensores, estrategia terapéutica y su clasificación. Resultados: El sexo femenino (54,29 % y los pacientes mayores de 65 años (46,17 % fueron los mayores consumidores de fármacos antihipertensivos, los grupos farmacológicos más utilizados fueron los inhibidores de la enzima conversora de angiotensina (68,68 % y los diuréticos (64,03 %; y como fármacos específicos, el captopril (26,47 % y la hidroclorotiazida (22,35 %. Predominó el tratamiento combinado de la hipertensión arterial (63,11 % y los errores de prescripción encontrados fueron principalmente en la pauta de administración de los medicamentos. Conclusiones: La población geriátrica del sexo femenino fue la mayor consumidora de fármacos antihipertensivos. El tratamiento combinado con dos o más fármacos fue lo más frecuente y los inhibidores de la enzima conversora de angiotensina y los diuréticos, los más utilizados. Los errores de prescripción más frecuentes fueron en la pauta de administración de los medicamentos. / Abstract: Introduction and Objectives: The rational use of medicines should be based on the scientific information available

  4. Medicamentos e sondas de nutrição Drugs and feeding tubes

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    Milton Luiz Gorzoni

    2010-01-01

    Full Text Available OBJETIVO: Definir a prevalência de medicamentos incompatíveis com esta via em internados em instituição de longa permanência para idosos (ILPI e em uso de sondas de nutrição. MÉTODOS: Análise de prescrições de internados em ILPI e em uso de sonda de nutrição há mais de 48 horas. Compararam-se os princípios ativos dos medicamentos prescritos, formas de apresentação e possibilidade de trituração com dados de literatura sobre viabilidade de fármacos por essa via. RESULTADOS: Observou-se sondas de nutrição em 57 pacientes (11,2% do total de leitos, idade média de 65,6 ± 16,0 anos, 32 mulheres e 25 homens. Média de fármacos por via enteral: 5,6 ± 2,2. Itens medicamentosos nas prescrições: 316 divididos em 64 fármacos, sendo 129 itens (40,8% do total e 23 fármacos (35,4% impróprios para essa via. Medicamentos impróprios mais prescritos: captopril, fenitoína, ranitidina, omeprazol e complexo B. Apresentações alternativas foram encontradas para 15 (65,2% dos 23 fármacos inadequados por essa via. CONCLUSÃO: Sondas de nutrição, como via de administração medicamentosa em ILPI, apresentam significativo risco de prescrições incompatíveis com elas.OBJECTIVE: Define the prevalence of drugs that are not compatible with this way of administration for inpatients in long term care facilities (LTCF, and their use in feeding tubes. METHODS: Analysis of prescriptions for LTCF inpatient who are using feeding tubes for more than 48 hours. The active ingredients, presentation and possibility of pulverizing drugs prescribed were compared to data in literature regarding the feasibility of enteral administration of drugs. RESULTS: Feeding tubes were observed in 57 patients (11.2% of the total of inpatients, mean age of 65.6 ± 16.0 years, 32 women and 25 men. Mean number of drugs administered enterally: 5.6 ± 2.2. Medication items in prescriptions: 316 divided into 64 drugs, with 129 items (40.8% of the total, and 23 drugs (35

  5. Evaluation of the pharmacological treatment of arterial hypertension associated to heart failure in Camarones town. Evaluación del tratamiento farmacológico de la hipertensión arterial asociada a insuficiencia cardiaca en el poblado de Camarones.

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    Lidia Vázquez Montero

    2006-12-01

    Full Text Available Background: Arterial hypertension is a risk factor for many cardiovascular and cerebrovascular diseases. Objective: To evaluate the pharmacological treatment in patients with arterial hypertension, also suffering from heart failure. Methods: A descriptive-prospective study was carried out, this consisted in the use of prescription-indication drugs through a simple random sample study of 43 patients, representing the 35.2 % in six Family Clinical Units of the urban area of Camarones’ Communitarian Policlinic, Palmira, Cienfuegos, during the first semester of 2004. Results: the 51.2 % of the patients were included in the class II of the New York Heart Asociation’s classification, and the 55.8% were considered hypertense class II. The hypertensive drugs more used were the captopril and the clortalidone, and among the drugs associated to the hypertensive ones it was included the isosorbide dinitrate, the digoxin and the acetylsalicylic acid. The 87.3 % of the patients received a correct dose, and in the 88.9% it was followed an adequate administration interval. The prescription was considered adequate in the 65.1 % of the studied patients. Conclusions: the advances in the treatment of these diseases are due to different factors, even though the study shows that the treatment of the patient of the series is adecuate, it should be bettered as long as possible.
    Fundamento: La hipertensión arterial constituye un factor de riesgo para muchas enfermedades cardio y cerebrovasculares. Objetivo: Evaluar el tratamiento farmacológico en pacientes con hipertensión arterial que padecen además, de insuficiencia cardiaca. Métodos: Se realizó un estudio descriptivo retrospectivo, de utilización de medicamentos de tipo indicación prescripción, a través de un muestreo aleatorio simple, con una

  6. Therapeutic adherence in outpatients with heart failure registered with a community pharmacy

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    Rosario Megret Despaigne

    2012-03-01

    Full Text Available A transverse descriptive study was carried out, according to the classification of therapeutic compliance, to evaluate adherence in 250 patients with a diagnosis of Heart Failure, registered with the health department of the municipality of Santiago de Cuba in 2009. The sample characterization was studied, with an assessment of adherence level and possible associated factors for sex, age and toxic habits. As an instrument for the work, data extraction was scheduled and the interview was carried out at patients' homes; the results were expressed in percentage and level of influence for associated factors. This was determined using the chi-square test. In the investigated population, adherence was greater for females, for age group 67-82 years, and toxic habits were found to have prevalence. Prevailing pharmacoterapies were digoxin, chlortalidone, captopril and isosorbide dinitrate, and a high level of adherence was found, both for the pharmacological and non-pharmacological treatments, in the studied sample. A good level of therapeutic adherence was found for 63.6% of the patients, regular level of adherence was found for 32% and only 4.4% or patients presented with poor adherence. Influencing factors were: knowledge of the treatment, number of medications, frequency of administration, and satisfaction with the service of pharmaceutical care.Realizou-se estudo descritivo transversal, de acordo com a classificação de adesão à terapêutica, para avaliar a adesão em 250 pacientes com diagnóstico de disfunção cardíaca, registrada no departamento de saúde do município de Santiago de Cuba, em 2009. A caracterização da amostra foi estudada, com a avaliação do nível de adesão e possíveis fatores associado a sexo, idade e hábitos tóxicos. Como instrumento para o trabalho, esquematizou-se aa extração de dados e realizou-se a entrevista nas moradias dos pacientes. Os resultados foram expressos em porcentagem e em nível de influ

  7. Penggunaan Obat Antihipertensi pada Pasien Hipertensi Esensial di Poliklinik Ginjal Hipertensi RSUP DR. M. Djamil Tahun 2011

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    Heri Fitrianto

    2014-01-01

    Full Text Available AbstrakPenyakit hipertensi tidak dapat disembuhkan dan berkaitan erat dengan penurunan usia harapan hidup. Penderita hipertensi juga sering kali disertai oleh penyakit penyerta. Umumnya, golongan obat antihipertensi yang dikenal yaitu, diuretik, ACE Inhibitor, Angiotensin Reseptor Bloker, Canal Calcium Blocker, and Beta Blocker. Terapi yang diberikan pada penderita hipertensi tanpa penyakit penyerta dan dengan penyakit penyerta tentunya berbeda. Tujuan penelitian ini adalah mengetahui penggunaan obat antihipertensi antara pasien hipertensi esensial dengan penyakit penyerta dan yang tidak disertai dengan penyakit penyerta di poliklinik RSUD Dr. M. Djamil, Padang. Metode penelitian yang digunakan adalah deskriptif dengan mengambil data dari rekam medik. Data dari 380 pasien yang dikumpulkan selama periode Januari 2011 sampai dengan Desember 2011. Jumlah subjek ditentukan dengan teknik total sampling. Dari data penelitian didapatkan bahwa 277 pasien hipertensi tanpa penyakit penyerta dan sebanyak 103 pasien hipertensi dengan penyakit penyerta. Komposisi dari 103 pasien hipertensi dengan penyakit penyerta yaitu 63 pasien dengan diabetes melitus, 13 pasien dengan PJK, 13 pasien dengan stroke, 7 pasien dengan gagal jantung, 4 pasien dengan pasca infark miokard, 3 pasien dengan gagal ginjal kronik. Berdasarkan data penelitian didapatkan penggunaan obat antihipertensi yang sering digunakan yaitu Hidroklortiazid (35,5%, Captopril (26,2%, Valsartan (20,6%, Amlodipin (15,2%, dan obat antihipertensi lain (2,5%. Berdasarkan hasil penelitian disimpulkan bahwa hipertensi dengan penyakit penyerta terbanyak adalah diabetes melitus dan penggunaan obat terbanyak berasal dari golongan diuretik yaitu penggunaan Hidroklortiazid.Kata kunci: obat antihipertensi, hipertensi, diuretikAbstractHypertension can not be cured and is closely related to a decrease in life expectancy. Patients with hypertension are also often accompanied by complience indication. Generally

  8. Multivariate Analysis of Pulmonary Hypertensive Crisis after Cardiac Surgery in Patients with Congestive Pulmonary Arterial Hypertension%肺动脉高压心脏手术后危象多因素分析

    Institute of Scientific and Technical Information of China (English)

    陈光献; 梁孟亚; 唐白云; 张金涛; 吴钟凯; 张希

    2009-01-01

    目的 探讨肺动脉高压(pulmonary arterial hypertension,PAH)左向右分流型先天性心脏病(left-to-right shunt congenital heart diseases,L-RCHD)影响心脏手术术后肺高压危象的重要因素.方法 对229例心脏手术同时合并肺动脉高压患者的可能导致术后肺高压危象的影响因素进行回顾性分析.结果 术后肺高压危象26例次,死亡6例,死亡率为23.08%.术前呼吸道感染、术前吸氧、术前卡托普利、手术时间、通气频率、再次插管和术后一氧化氮(nitrogen monoxidum,NO)治疗对肺动脉高压患者术后出现肺高压危象的影响差异有统计学意义(P<0.05).术前呼吸道感染、手术时间和再次插管为危险因素;术前吸氧、术前卡托普利、通气频率和术后NO治疗为保护因素.结论 术前呼吸道感染、手术时间和再次插管为肺动脉高压患者心脏外科手术术后肺高压危象的危险因素;术前吸氧、术前卡托普利、通气频率和术后NO治疗为保护因素.%Objective To investigate the risk factors that influence the morbidity of pulmonary hypertensive crisis(PHC) after surgical treatment in left-to-right shunt congenital heart diseases(L-RCHD) patients with congestive pulmonary arterial hyperten-sion(PAH). Methods 229 cases of L-RCHD with congestive PAH who underwent surgical treatment were eligible for entry into the study. The influence factors were analyzed retrospectively. Results There were 26 cases of PHC, six died, the mortality was 23.08%. Effects of preoperative respiratory infection, supplemental oxygen and administration of captopril, operational time, fre-quency of ventilation, repeated intubation and the postoperative NO had statistically significant on the morbidity of PHC in L-RCHD with congestive PAH after surgical treatment( P< 0.05 ). Conclusion Preoperative respiratory infection,operational time and repeated intubation are risk factors, while preoperative supplemental oxygen, the preoperative

  9. ACESSO A MEDICAMENTOS ESSENCIAIS EM FARMÁCIAS E DROGARIAS DO MUNICÍPIO DE ARARAQUARA.

    Directory of Open Access Journals (Sweden)

    Cesar Rente Ferreira

    2010-11-01

    Full Text Available

    O levantamento teve como objetivo avaliar a disponibilidade de 20 medicamentos essenciais para doenças importantes da atenção básica a saúde, pela presença e o preço nas as farmácias e drogarias do setor privado do município de Araraquara/SP. O estudo foi realizado utilizando-se dois formulários, preconizados pela OMS, um para disponibilidade e outro para os preços. Os medicamentos mais disponíveis nas farmácias e drogarias foram o propranolol (90,5%, captopril (96% e ranitidina (96%, e os menos disponíveis foram sulfato ferroso (27%, beclometasona (33,8% e ibuprofeno (41,9%. Os medicamentos que apresentaram maior variação entre os preços praticados foram propranolol (97,1%, hidroclorotiazida 96,4% e glibenclamida (95,0%, e os de menor variação foram salbutamol (30,8% e sulfametoxazol + trimetoprima (30,2%. Metade dos medicamentos avaliados (10 o menor preço era do medicamento genérico. Os indicadores de acesso por capacidade de aquisição para o tratamento das principais doenças no nível de atenção básica demonstrou que nenhum estabelecimento continha todos os medicamentos avaliados e evidenciaram grandes variações de preços, comprometendo o seu acesso aos usuários que a única forma de adquiri-los é em farmácias e drogarias. Palavras-chave: Preço de medicamento. Economia Farmacêutica. Medicamentos Genéricos.Farmacoepidemiologia. ABSTRACT A survey to determine the availability of 20 essential medicines for the diseases with highest prevalence in primary health care was conducted in the city of Araraquara. The presence and the price of these medicines in private sector pharmacies and drugstores of the city were recorded. Two forms, recommended by the WHO, were used in the survey, one for availability and the other for prices. The drugs most commonly available in pharmacies and drugstores were: propranolol (90.5%, captopril (96% and ranitidine (96%, while the least available were ferrous

  10. RP-HPLC-UV波长切换法同时测定复方吡拉西坦尼莫地平胶囊中3种成分的含量%Simultaneous Determination of Three Components in Compound Piracetam and Nimodipine Capsules by RP-HPLC-UV Wavelength Switching Method

    Institute of Scientific and Technical Information of China (English)

    赵建颖

    2015-01-01

    Objective:To establish a RP-HPLC-UV wavelength switching method for the simultaneous determination of captopril, aspirin and nimodipine in compound piracetam and nimodipine capsules. Methods:The separation was carried out on a YMC-Pack Pro-C18 column(250 mm × 4. 6 mm,5μm) with acetonitrile-water(adjusting pH to 2. 5 with phosphpric acid)as the mobile phase with gra-dient elution. The flow rate was 1. 0 ml·min-1 . During 0-4. 3 min, the detection wavelength was 215 nm, during 4. 3-11. 0 min, the detection wavelength was 276 nm and during 11. 0-18. 0 min, the detection wavelength was 235 nm. The column temperature was 40℃. Results:The linear range of captopril, aspirin and nimodipine was 0. 054 7-1. 641 8 μg(r=0. 999 9),0. 055 3-1. 654 8 μg(r=0. 999 9) and 0. 077 7-2. 331 6 μg(r=0. 999 7), and the average recovery was 100. 69%(RSD=0. 69%,n=6),101. 04%(RSD=1. 05%,n=6)and 102. 56%(RSD=1. 14%,n=6), respectively. Conclusion: The method is simple, rapid and accurate, and can be used in the content determination of compound piracetam and nimodipine capsules.%目的::建立同时测定复方吡拉西坦尼莫地平胶囊中卡托普利、阿司匹林、尼莫地平含量的HPLC法。方法:采用YMC-Pack Pro-C18色谱柱(250 mm ×4.6 mm,5μm),以乙腈为流动相A、水(磷酸调节pH至2.5)为流动相B进行梯度洗脱,流速:1.0 ml·min-1,柱温:40℃,检测波长:215 nm(0~4.3 min),276 nm(4.3~11.0 min),235 nm(11.0~18.0 min)。结果:卡托普利、阿司匹林、尼莫地平分别在0.0547~1.6418μg(r =0.9999),0.0553~1.6548μg(r =0.9999),0.0777~2.3316μg(r=0.9997)范围内线性良好,平均加样回收率分别为100.69%(RSD=0.69%,n=6),101.04%(RSD=1.05%,n=6),102.56%(RSD=1.14%,n=6)。结论:该分析方法简便、快速、准确、重复性好,可用于复方吡拉西坦尼莫地平胶囊中卡托普利、阿司匹林、尼莫地平的含量测定。

  11. Evaluation of Divided Doses of Scored Tablets and Non-scored Tablets Produced by Different Manufacturers%不同厂家刻痕片及非刻痕片分剂量评价

    Institute of Scientific and Technical Information of China (English)

    刘元江; 缪经纬; 杨亚勇; 詹金陶; 刘其东

    2012-01-01

    目的:评价对不同厂家复方卡托普利片和复方对乙酰氨基酚片(Ⅱ)的刻痕片及非刻痕片采用3种方法的分剂量情况,促进合理用药.方法:以分剂量准确性、期望重量与实际重量差值(d)、重量损失百分比、等分片脆碎度为指标,采用手掰、剪刀、切药器3种方法对A厂(有刻痕)、B厂(无刻痕)的复方卡托普利片及C厂(无刻痕)、D厂(有刻痕)的复方对乙酰氨基酚片(Ⅱ)进行分剂量评价.结果:除D厂(3种方法)、C厂(切药器法)外,其余厂家或方法分剂量准确性均不符合《欧洲药典》第6版的规定.与手掰法比较,C厂剪刀法d值明显降低(P<0.05);与剪刀法比较,D厂切药器法d值明显降低(P<0.01).3种方法间比较分剂量后重量损失百分比均具有统计学意义(P均<0.01),其中剪刀法>切药器法(除B厂外)>手掰法.等分片脆碎度结果表明,A厂切药器法不合格,B厂3种方法均不合格,其余厂家或方法均合格.结论:刻痕片较非刻痕片更适合分剂量,具体分剂量方法需根据药片物理参数情况进行选择.%OBJECTIVE: To evaluate the subdivision of scored tablets and non-scored tablet of Compound captopril tablets and Compound paracetamol tablets ( II ) from different manufacturers with 3 methods, to promote the rational use of medicines. METHODS: Using subdivision accuracy, difference between expected mass and real mass (d value), loss of mass and friability as index, the subdivision of Compound captopril tablets from manufacturer A (scored tablet) and manufacturer B (non-scored tablet) and Compound paracetamol tablets (II) from manufacturer C (non-scored tablet) and manufacturer D (scored tablet) were evaluated with hand, scissors and tablet cutters. RESULTS: Except manufacturer D (3 methods) and manufacturer C (tablet cutter), others could not comply with the specification of Ph. Eur. (6th edition). Compared with manual splitting, d value of manufacturer C decreased

  12. Gastrointestinal Endogenous Protein-Derived Bioactive Peptides: An in Vitro Study of Their Gut Modulatory Potential

    Science.gov (United States)

    Dave, Lakshmi A.; Hayes, Maria; Mora, Leticia; Montoya, Carlos A.; Moughan, Paul J.; Rutherfurd, Shane M.

    2016-01-01

    A recently proposed paradigm suggests that, like their dietary counterparts, digestion of gastrointestinal endogenous proteins (GEP) may also produce bioactive peptides. With an aim to test this hypothesis, in vitro digests of four GEP namely; trypsin (TRYP), lysozyme (LYS), mucin (MUC), serum albumin (SA) and a dietary protein chicken albumin (CA) were screened for their angiotensin-I converting (ACE-I), renin, platelet-activating factor-acetylhydrolase (PAF-AH) and dipeptidyl peptidase-IV inhibitory (DPP-IV) and antioxidant potential following simulated in vitro gastrointestinal digestion. Further, the resultant small intestinal digests were enriched to obtain peptides between 3–10 kDa in size. All in vitro digests of the four GEP were found to inhibit ACE-I compared to the positive control captopril when assayed at a concentration of 1 mg/mL, while the LYS < 3-kDa permeate fraction inhibited renin by 40% (±1.79%). The LYS < 10-kDa fraction inhibited PAF-AH by 39% (±4.34%), and the SA < 3-kDa fraction inhibited DPP-IV by 45% (±1.24%). The MUC < 3-kDa fraction had an ABTS-inhibition antioxidant activity of 150 (±24.79) µM trolox equivalent and the LYS < 10-kDa fraction inhibited 2,2-Diphenyl-1-picrylhydrazyl (DPPH) by 54% (±1.62%). Moreover, over 190 peptide-sequences were identified from the bioactive GEP fractions. The findings of the present study indicate that GEP are a significant source of bioactive peptides which may influence gut function. PMID:27043546

  13. Modified spectrophotometric method for assay of angiotensin I-converting enzyme inhibitory activity of food derived peptides%改进的分光光度计法测定食源性多肽血管紧张素转化酶的抑制活性

    Institute of Scientific and Technical Information of China (English)

    高丹丹; 曹郁生; 麦曦

    2011-01-01

    在传统检测食源性多肽血管紧张素转化酶(ACE)抑制肽体外活性方法的基础上,结合纸层析测定马尿酸的方法对其进行改进,建立了一种新的分光光度法用于测定样品中ACE的抑制活性.结果表明:该方法确定的显色反应吸收波长为459 nm;最佳显色温度为40℃;最佳显色时间为30 min;最佳显色剂质量分数为0.5%;用卡托普利和有ACE抑制活性的棉籽蛋白肽作为样品进行检测验证,结果表明,此方法简便、灵敏、准确、重复性好,可用于筛选食源性ACE抑制肽.%A modified spectrophotometric assay was developed for determination of angiotensin I-converting enzyme (ACE) inhibitory activity of peptides derived from plant protein, which was based on the classical paper chromatography determination of hippuric acid (HA) content in the urine. By using the modified method, the maximum absorbance of HA was measured at 459 nm, and the optimum chromogenic reaction conditions were as follows: temperature of 40 ℃, time for 30 min, and the DAB concentration of 0. 5%. Captopril and cottonseed protein peptides showing antihypertensive activity as inhibitors of ACE were detected by this modified spectrophotometric assay. The result showed that the modified method was proved to be convenient, sensitive, accurate and reproducible, and it could be used for the screening of ACE inhibitory peptides derived from food proteins.

  14. 高血压治疗的现代观念%Modern concept of hypertension therapy

    Institute of Scientific and Technical Information of China (English)

    林金秀

    2007-01-01

    过去7年,相继发表了9项重要高血压临床试验:高血压的合理治疗(hypertension optimal treatment,HOT)、卡托普利预防试验(captopril prevention project,CAPPP)、瑞典老人高血压试验-2(Swedish trial in old patients with hypertension 2,STOP-2)、抗高血压药和调血脂药预防心脏病发作试验(antihypertensive and lipid-lowering treatment to prevent heart attack trial,ALLHAT)、北欧地尔硫(艹卓)试验(Nordic diltiazem study,NORDIL)、高血压治疗目标(intervention as a goal in hypertension treatment,INSIGHT)、氯沙坦对高血压试验终点的干预(losartan intervention for endpoint reduction in hypertension study,LIFE)、缬沙坦长期使用评估(valsartan antihypertensive long-term use evaluation,VALUE)、英国人和斯堪的那维亚人心脏试验-降血压篇(Anglo-Scandinavian cardiac outcomes trial-blood pressure lowering arm,ASCOT-BPLA),使高血压治疗观念和策略发生日新月异变化.可概括为早期、快速、平稳、联合、综合.

  15. Renin-angiotensin system stimulates erythropoietin secretion in chronic hemodialysis patients.

    Science.gov (United States)

    Vlahakos, D V; Balodimos, C; Papachristopoulos, V; Vassilakos, P; Hinari, E; Vlachojannis, J G

    1995-01-01

    A series of observations suggests an interrelationship between the renin-angiotensin system (RAS) and erythropoietin (EPO) secretion. To further evaluate the role of RAS in erythropoiesis of chronic hemodialysis patients, we studied two groups of such patients: Group A consisted of 16 patients (14 male and 2 female, 54.7 +/- 3.3 years old), who maintained a target hematocrit value of 0.30 (0.32 +/- 0.01), without recombinant human EPO (rhEPO) supplementation. Group B consisted of 14 patients (7 male and 7 female, 50 +/- 5.3 years old), who required subcutaneous injections of rhEPO (90.8 +/- 10 IU.kg-1.week-1), to maintain the same target hematocrit value of 0.30 (30 +/- 0.01). Plasma renin activity (PRA) was found to be the major feature to distinguish patients in these two Groups and it was five times higher in Group A (10 +/- 2 ng.ml-1.h-1) compared to Group B patients (1.8 +/- 0.6 ng.ml-1.h-1) (p < 0.001). Moreover, activation of RAS in Group A patients by volume depletion (2.2 +/- 0.2 l) during hemodialysis resulted in a 118 +/- 33 percent increment of PRA (p < 0.01) which was accompanied by a 69 +/- 25 percent increment of serum EPO levels (p < 0.05). Repetition of the same protocol after inhibiting the converting enzyme with 50 mg of Captopril prior to dialysis session, resulted in a 315 +/- 64 percent increment of PRA (p < 0.001), while at the same time completely blocked the expected rise in serum EPO levels (1.25 +/- 12.5 percent increment).(ABSTRACT TRUNCATED AT 250 WORDS)

  16. Effects of angiotensin-converting enzyme inhibitors and angiotensin II type 1 receptor blockers on lymphangiogenesis of gastric cancer in a nude mouse model

    Institute of Scientific and Technical Information of China (English)

    WANG Liang; CAI Shi-rong; ZHANG Chang-hua; HE Yu-long; ZHAN Wen-hua; WU Hui; PENG Jian-jun

    2008-01-01

    Background Angiotensin-converting enzyme inhibitors (ACEI) and angiotensin II type 1 receptor blockers (ARB) can inhibit tumor growth by inhibition of angiogenesis.This study was designed to study the anticancer effects of ACEI and ARB on tumor growth and lymphangiogenesis in an implanted gastric cancer mouse model.Methods A model of gastric cancer was established by subcutaneously inoculating human gastric cancer cell line SGC-7901 into 60 nude mice.One week later,all mice were randomly divided into 5 groups.A control group received physiologic saline once daily for 21 days.Mice in the 4 treatment groups received one of the following agents by gavage once daily for 21 days:perindopril,2 mg/kg;captopril,5 mg/kg;Iosartan,50 mg/kg;or valsartan,40 mg/kg.Twenty-one clays after treatment,all the mice were sacrificed and the tumors were removed.Tumor sections were processed,and immunohistochemical methods were used to observe the expressions of vascular endothelial growth factor C (VEGF-C),matrix metalloproteinase 7 (MMP-7),and lymphatic microvessel density (LMVD).Results Tumor volume was significantly inhibited in all ACEI and ARB groups,compared with the control group (all P <0.01).LMVD in the ACEI and ARB groups was also significantly lower than that of the control group (all P<0.01).In the ACEI groups,the expressions of VEGF-C and MMP-7 were both significantly decreased,compared with the control group (all P<0.05).In the ARB groups,expression of VEGF-C was significantly decreased compared with the control group (all P<0.05).However,no significant difference was found in the expression of MMP-7 between ARB groups and the control group.Conclusion In a mouse model,ACEI and ARB might inhibit gastric cancer tumor growth by suppressing lymphangiogenesis.

  17. In vivo hypotensive effect and in vitro inhibitory activity of some Cyperaceae species

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    Monica Lacerda Lopes Martins

    2013-12-01

    Full Text Available In 1820, French naturalist August Saint Hillaire, during a visit in Espírito Santo (ES, a state in southeastern Brazil, reported a popular use of Cyperaceae species as antidote to snake bites. The plant may even have a hypotensive effect, though it was never properly researched. The in vitro inhibitory of the angiotensin converting enzyme (ACE activity of eigth ethanolic extracts of Cyperaceae was evaluated by colorimetric assay. Total phenolic and flavonoids were determined using colorimetric assay. The hypotensive effect of the active specie (Rhychonospora exaltata, ERE and the in vivo ACE assay was measured in vivo using male Wistar Kyoto (ERE, 0.01-100mg/kg, with acetylcholine (ACh as positive control (5 µg/kg, i.v.. The evaluation of ACE in vivo inhibitory effect was performed comparing the mean arterial pressure before and after ERE (10 mg/kg in animals which received injection of angiotensin I (ANG I; 0,03, 03 and 300 µg/kg, i.v.. Captopril (30 mg/kg was used as positive control. Bulbostylis capillaris (86.89 ± 15.20% and ERE (74.89 ± 11.95%, ERE were considered active in the in vitro ACE inhibition assay, at 100 µg/mL concentration. ACh lead to a hypotensive effect before and after ERE's curve (-40±5% and -41±3%. ERE showed a dose-dependent hypotensive effect and a in vivo ACE inhibitory effect. Cyperaceae species showed an inhibitory activity of ACE, in vitro, as well as high content of total phenolic and flavonoids. ERE exhibited an inhibitory effect on both in vitro and in vivo ACE. The selection of species used in popular medicine as antidotes, along with the in vitro assay of ACE inhibition, might be a biomonitoring method for the screening of new medicinal plants with hypotensive properties.

  18. Renal effects of Mammea africana Sabine (Guttiferae stem bark methanol/methylene chloride extract on L-NAME hypertensive rats

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    Nguelefack-Mbuyo Elvine

    2010-01-01

    Full Text Available Objective : The present study aims at evaluating the effects of methanol/methylene chloride extract of the stem bark of Mammea africana on the renal function of L-NAME treated rats. Material and Methods : Normotensive male Wistar rats were divided into five groups respectively treated with distilled water, L-NAME (40 mg/kg/day, L-NAME + L-arginine (100 mg/kg/day, L-NAME + captopril (20 mg/kg/day or L-NAME + M. africana extract (200 mg/kg/day for 30 days. Systolic blood pressure was measured before and at the end of treatment. Body weight was measured at the end of each week. Urine was collected 6 and 24 h after the first administration and further on day 15 and 30 of treatment for creatinine, sodium and potassium quantification, while plasma was collected at the end of treatment for the creatinine assay. ANOVA two way followed by Bonferonni or one way followed by Tukey were used for statistical analysis. Results : M. africana successfully prevented the rise in blood pressure and the acute natriuresis and diuresis induced by L-NAME. When given chronically, the extract produced a sustained antinatriuretic effect, a non-significant increase in urine excretion and reduced the glomerular hyperfiltration induced by L-NAME. Conclusions : The above results suggest that the methanol/methylene chloride extract of the stem bark of M. africana may protect kidney against renal dysfunction and further demonstrate that its antihypertensive effect does not depend on a diuretic or natriuretic activity.

  19. [Simultaneous determination of erdosteine and its active metabolite in human plasma by liquid chromatography-tandem mass spectrometry with pre-column derivatization].

    Science.gov (United States)

    Jin, Jing; Chen, Xiao-Yan; Zhang, Yi-Fan; Ma, Zhi-Yu; Zhong, Da-Fang

    2013-03-01

    A sensitive, rapid and accurate liquid chromatography-tandem mass spectrometric (LC-MS/MS) method with pre-column derivatization was developed for the simultaneous determination of erdosteine and its thiol-containing active metabolite in human plasma. Paracetamol and captopril were chosen as the internal standard of erdosteine and its active metabolite, respectively. Aliquots of 100 microL plasma sample were derivatized by 2-bromine-3'-methoxy acetophenone, then separated on an Agilent XDB-C18 (50 mm x 4.6 mm ID, 1.8 microm) column using 0.1% formic acid methanol--0.1% formic acid 5 mmol x L(-1) ammonium acetate as mobile phase, in a gradient mode. Detection of erdosteine and its active metabolite were achieved by ESI MS/MS in the positive ion mode. The linear calibration curves for erdosteine and its active metabolite were obtained in the concentration ranges of 5-3 000 ng x mL(-1) and 5-10 000 ng x mL(-1), respectively. The lower limit of quantification of erdosteine and its active metabolite were both 5.00 ng x mL(-1). The pharmacokinetic results of erdosteine and its thiol-containing active metabolite showed that the area under curve (AUC) of the thiol-containing active metabolite was 6.2 times of that of erdosteine after a single oral dose of 600 mg erdosteine tables in 32 healthy volunteers, The mean residence time (MRT) of the thiol-containing active metabolite was (7.51 +/- 0.788) h, which provided a pharmacokinetic basis for the rational dosage regimen.

  20. Maitake Mushroom Extracts Ameliorate Progressive Hypertension and Other Chronic Metabolic Perturbations in Aging Female Rats

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    Harry G. Preuss, Bobby Echard, Debasis Bagchi, Nicholas V. Perricone

    2010-01-01

    Full Text Available Objective: We assessed the ability of two commercially-available fractions labeled SX and D derived from the edible maitake mushroom to overcome many age-associated metabolic perturbations such as progressive, age-related elevation of blood pressure, over activity of the renin-angiotensin system (RAS, decreased insulin sensitivity, and inflammation in an in vivo laboratory model. Design and Method: We divided forty mature, female Sprague-Dawley rats (SD into five groups of eight. SD ingested regular rat chow containing added sucrose (20% w/w. The groups received baseline diet alone (control or baseline diet containing captopril, niacin-bound chromium, maitake fraction SX, or maitake fraction D. In addition to blood pressure readings, the following procedures were implemented: losartan and insulin challenges, evaluation of serum ACE activity, glucose tolerance testing, blood chemistries, LNAME challenge, and measurement of various circulating cytokines. Results: We found that implementation of all test conditions stopped the gradual elevation of systolic blood pressure (SBP in the SD over the four months of study, even reversing some of the previous elevation that occurred over time. In general, the treatment groups showed decreased activity of the RAS estimated by less lowering of SBP after losartan challenge and decreased serum ACE activity and were more sensitive to exogenous insulin challenge. TNFa levels decreased in all four test groups suggesting a lessening of the inflammatory state. Conclusions: We believe our data suggest that maitake mushroom fractions lessen age-related hypertension, at least in part, via effects on the RAS; enhance insulin sensitivity; and reduce some aspects of inflammation -- actions that should lead to a longer, healthier life span.

  1. Efeito de um programa de manejo farmacoterapêutico em um grupo de idosos com hipertensão em Aracaju-Sergipe

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    D. P. LYRA JúNIOR

    2009-08-01

    Full Text Available O presente estudo visou avaliar o efeito de um programa de manejo farmacoterapêutico no atendimento de idosos com hipertensão arterial sistêmica assistidos em unidade básica de saúde no município de Aracaju-Sergipe. Foram selecionados 30 idosos portadores de hipertensão, entre 60 e 75 anos de ambos os gêneros. Foi realizado um estudo de intervenção. Ao longo do estudo foram avaliadas as mudanças referentes ao manejo da farmacoterapia, de janeiro de 2007 a agosto de 2008. As variáveis analisadas foram: perfil sócio-demográfico e farmacoterapêutico e freqüência de comorbidades. A média de idade foi 69 ± 4 anos, com prevalência do gênero feminino. Os dados obtidos mostraram freqüência das comorbidades, especialmente nos sistema cardiovascular (100% e músculo-esquelético (90%. Com relação ao perfil farmacoterapêutico foram identificados 76 diferentes tipos de especialidades farmacêuticas. Os medicamentos mais consumidos foram a hidroclorotiazida (53,3% e o captopril (30%. Além disso, as intervenções reduziram o uso de AINEs (25,3% para 10% e de polifarmácia (de nove para seis pacientes. O levantamento do perfil farmacoterapêutico forneceu elementos relevantes para compreender o uso de medicamentos em uma unidade de saúde, bem como, para eleger prioridades no cuidado aos idosos com hipertensão e elaborar estratégias em que o farmacêutico possa intervir de modo a reduzir e prevenir problemas farmacoterapêuticos. Palavras-chave: Idoso. Hipertensão arterial sistêmica. Farmacoterapia.

  2. Comparative Efficacy and Safety of Antihypertensive Agents for Adult Diabetic Patients with Microalbuminuric Kidney Disease: A Network Meta-Analysis

    Science.gov (United States)

    Huang, Rongzhong; Feng, Yuxing; Wang, Ying; Qin, Xiaoxia; Melgiri, Narayan Dhruvaraj; Sun, Yang; Li, Xingsheng

    2017-01-01

    Background Antihypertensive treatment mitigates the progression of chronic kidney disease. Here, we comparatively assessed the effects of antihypertensive agents in normotensive and hypertensive diabetic patients with microalbuminuric kidney disease. Methods MEDLINE, EMBASE, and the Cochrane Central Register of Controlled Trials were systematically searched for randomized controlled trials (RCTs) comparing oral antihypertensive agents in adult diabetic patients with microalbuminuria. The primary efficacy outcome was reduction in albuminuria, and the primary safety outcomes were dry cough, presyncope, and edema. Random-effects pairwise and Bayesian network meta-analyses were performed to produce outcome estimates for all RCTs, only hypertensive RCTs, or only normotensive RCTs. Surface under the cumulative ranking (SUCRA) probability rankings were calculated for all outcomes. Sensitivity analyses on type 2 diabetes status, age, or follow-up duration were also performed. Results A total of 38 RCTs were included in the meta-analyses. The angiotensin-converting enzyme inhibitor-calcium channel blocker (ACEI-CCB) combination therapy of captopril+diltiazem was most efficacious in reducing albuminuria irrespective of blood pressure status. However, the ACEI-angiotensin receptor blocker (ACEI-ARB) combination therapy of trandolapril+candesartan was the most efficacious in reducing albuminuria for normotensive patients, while the ACEI-CCB combination therapy of fosinopril+amlodipine was the most efficacious in reducing albuminuria for hypertensive patients. The foregoing combination therapies displayed inferior safety profiles relative to ACEI monotherapy with respect to dry cough, presyncope, and edema. With respect to type 2 diabetic patients with microalbuminuria, the Chinese herbal medicine Tangshen formula followed by the ACEI ramipril were the most efficacious in reducing albuminuria. Conclusions Trandolapril+candesartan appears to be the most efficacious intervention

  3. Potential prescription patterns and errors in elderly adult patients attending public primary health care centers in Mexico City

    Science.gov (United States)

    Corona-Rojo, José Antonio; Altagracia-Martínez, Marina; Kravzov-Jinich, Jaime; Vázquez-Cervantes, Laura; Pérez-Montoya, Edilberto; Rubio-Poo, Consuelo

    2009-01-01

    Introduction Six out of every 10 elderly persons live in developing countries. Objective To analyze and assess the drug prescription patterns and errors in elderly outpatients attending public health care centers in Mexico City, Mexico. Materials and methods A descriptive and retrospective study was conducted in 2007. Fourteen hundred prescriptions were analyzed. Prescriptions of ambulatory adults aged >70 years who were residents of Mexico City for at least two years were included. Prescription errors were divided into two groups: (1) administrative and legal, and (2) pharmacotherapeutic. In group 2, we analyzed drug dose strength, administration route, frequency of drug administration, treatment length, potential drug–drug interactions, and contraindications. Variables were classified as correct or incorrect based on clinical literature. Variables for each drug were dichotomized as correct (0) or incorrect (1). A Prescription Index (PI) was calculated by considering each drug on the prescription. SPSS statistical software was used to process the collected data (95% confidence interval; p <0.05). Results The drug prescription pattern in elderly outpatients shows that 12 drugs account for 70.72% (2880) of prescribed drugs. The most prescribed drugs presented potential pharmacotherapeutic errors (as defined in the present study). Acetylsalicylic acid–captopril was the most common potential interaction (not clinically assessed). Potential prescription error was high (53% of total prescriptions). Most of the prescription errors were due to omissions of dosage, administration route, and length of treatment and may potentially cause harm to the elderly outpatients. Conclusions A high number of potential prescription errors were found, mainly due to omissions. The drug prescription pattern of the study population is mainly constituted by 12 drugs. The results indicate that prescription quality depends on the number of prescribed drugs per prescription (p < 0

  4. Inverse relation between aldosterone and venous capacitance in chronically treated congestive heart failure.

    Science.gov (United States)

    Rietzschel, E; Duprez, D A; De Buyzere, M L; Clement, D L

    2000-04-15

    The purpose of this study was to examine if there is a relation between the aldosterone escape phenomenon and venous capacitance of the upper and lower limbs in patients with long-term congestive heart failure (CHF) receiving chronic treatment with angiotensin-converting enzyme (ACE) inhibitors. The study group consisted of 16 subjects with ischemic CHF in New York Heart Association functional class II (age 59 +/-2 years, ejection fraction 24+/-4%), stabilized under a constant drug regimen comprising furosemide, captopril 50 mg 3 times daily, and digoxin for at least 3 months. Thirteen apparently healthy volunteers, aged 50+/-4 years acted as controls. Forearm and calf venous capacitances were measured simultaneously by venous occlusion plethysmography using mercury-in-silastic strain gauges. The equilibration technique was used to derive venous capacitance from the recorded pressure-volume curves. Active renin, angiotensin II, and aldosterone levels were determined on venous blood samples obtained in the supine position. Angiotensin II (paldosterone (paldosterone escape phenomenon). In CHF, forearm venous capacitance was 2.19+/-0.18 ml/100 ml; calf venous capacitance was 2.83+/-0.27 ml/100 ml. Aldosterone significantly and inversely correlated with venous capacitance in both upper (r = -0.586; p = 0.017) and lower (r = -0.625; p = 0.01) limbs. No correlations were found between forearm or calf venous capacitance and renin or angiotensin II. In patients with heart failure chronically treated with diuretics and full ACE inhibition, venous capacitance is inversely correlated with aldosterone through the mechanism of aldosterone escape, creating the potential for further deterioration of the CHF process.

  5. Activation of μ opioid receptors in the LPBN facilitates sodium intake in rats.

    Science.gov (United States)

    Pavan, Carolina G; Roncari, Camila F; Barbosa, Silas P; De Paula, Patrícia M; Colombari, Débora S A; De Luca, Laurival A; Colombari, Eduardo; Menani, José V

    2015-07-15

    Important inhibitory mechanisms for the control of water and sodium intake are present in the lateral parabrachial nucleus (LPBN). Opioid receptors are expressed by LPBN neurons and injections of β-endorphin (nonspecific opioid receptor agonist) in this area induce 0.3M NaCl and water intake in satiated rats. In the present study, we investigated the effects of the injections of endomorphin-1 (μ opioid receptor agonist) alone or combined with the blockade of μ, κ or δ opioid receptors into the LPBN on 0.3M NaCl and water intake induced by subcutaneous injections of the diuretic furosemide (FURO) combined with low dose of the angiotensin converting enzyme inhibitor captopril (CAP). Male Holtzman rats with stainless steel cannulas implanted bilaterally in the LPBN were used. Bilateral injections of endomorphin-1 (0.1, 0.25, 0.5, 1.0, 2.0 and 4.0nmol/0.2μl) into the LPBN increased 0.3M NaCl and water intake induced by FURO+CAP. The previous blockade of μ opioid receptor with CTAP (1.0nmol/0.2μl) into the LPBN reduced the effect of endomorphin-1 on FURO+CAP-induced 0.3M NaCl. GNTI (κ opioid receptor antagonist; 2.0nmol/0.2μl) and naltrindole (δ opioid receptor antagonist; 2.0nmol/0.2μl) injected into the LPBN did not change the effects of endomorphin-1 on FURO+CAP-induced 0.3M NaCl. The results suggest that μ opioid receptors in the LPBN are involved in the control of sodium intake.

  6. Delayed emergence of effects of memory-enhancing drugs: implications for the dynamics of long-term memory.

    Science.gov (United States)

    Mondadori, C; Hengerer, B; Ducret, T; Borkowski, J

    1994-01-01

    Many theories of memory postulate that processing of information outlasts the learning situation and involves several different physiological substrates. If such physiologically distinct mechanisms or stages of memory do in fact exist, they should be differentially affected by particular experimental manipulations. Accordingly, a selective improvement of the processes underlying short-term memory should be detectable only while the information is encoded in the short-term mode, and a selective influence on long-term memory should be detectable only from the moment when memory is based on the long-term trace. Our comparative study of the time course of the effects of the cholinergic agonist arecoline, the gamma-aminobutyric acid type B receptor antagonist CGP 36742, the angiotensin-converting enzyme inhibitor captopril, and the nootropic oxiracetam, four substances with completely different primary sites of action, show that the memory-enhancing effects consistently come into evidence no sooner than 16-24 h after the learning trial. On the one hand, this finding suggests that all these substances act by way of the same type of mechanism; on the other hand, it demonstrates that the substrate modulated by the compounds forms the basis of memory only after 16-24 h. From the observation that animals also show clear signs of retention during the first 16 h--i.e., before the effects of the substances are measurable--it can be inferred that retention during this time is mediated by other mechanisms that are not influenced by any of the substances. Images PMID:8134347

  7. IRMPD spectroscopy of protonated S-nitrosocaptopril, a biologically active, synthetic amino acid.

    Science.gov (United States)

    Coletti, Cecilia; Re, Nazzareno; Scuderi, Debora; Maître, Philippe; Chiavarino, Barbara; Fornarini, Simonetta; Lanucara, Francesco; Sinha, Rajeev K; Crestoni, Maria Elisa

    2010-11-07

    S-Nitrosocaptopril, a biologically active S-nitrosothiol, is generated as protonated species and isolated in the gas phase by electrospray ionization coupled to Fourier Transform Ion Cyclotron Resonance (FT-ICR) or ion-trap mass spectrometry. The structural and IR spectroscopic characterization of protonated S-nitrosocaptopril (SNOcapH(+)) is aided by the comparative study of the parent species lacking the NO feature, namely protonated captopril. The study is accomplished by methodologies based on tandem mass spectrometry, namely by energy resolved collision-induced dissociation and infrared multiple-photon dissociation (IRMPD) spectroscopy, backed by density functional theory calculations. IRMPD spectra have been obtained both in the 1000-1900 cm(-1) fingerprint range, using a beamline of the infrared free electron laser (IR-FEL) at the Centre Laser Infrarouge d'Orsay (CLIO), and in the O-H and N-H stretching region (2900-3700 cm(-1)) using the tunable IR radiation of a tabletop parametric oscillator/amplifier (OPO/OPA) laser source. The structural features of the ion have been ascertained by comparison of the experimental IRMPD spectra with the IR transitions calculated for the lowest energy isomers. Evidence is obtained that protonation occurs at the amide carbonyl oxygen which is found to be the thermodynamically most basic site. However, SNOcapH(+) is present as a thermally equilibrated mixture of low-energy structures, with a major contribution of the most stable isomer characterized by a trans relationship of the positively charged OH group with respect to the carboxylic acid functionality on the adjacent proline ring and by an anti conformation at the S-N (partial) double bond, though the energy difference with the analogous trans-syn isomer is less than 1 kJ mol(-1). The highly diagnostic N-O stretching mode has been unambiguously identified, which may be regarded as an informative probe for S-nitrosation features in more complex, biologically active

  8. AVALIAÇÃO DA ADESÃO AO TRATAMENTO MEDICAMENTOSO E NÃO MEDICAMENTOSO DE PACIENTES HIPERTENSOS ATENDIDOS NO PSF GUARITÁ, ITAPERUNA-RJ

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    Raphael Laiber BONADIMAN

    2015-12-01

    Full Text Available Foi realizada uma pesquisa durante os meses de agosto e setembro de 2010, com 108 pacientes hipertensos atendidos no PSF (Programa Saúde da Família Guaritá, localizado no bairro Vinhosa, no município de Itaperuna, estado do Rio de Janeiro. O objetivo do estudo foi verificar o grau de adesão ao tratamento medicamentoso e não medicamentoso nos quadros de hipertensão arterial bem como avaliar os níveis pressóricos dos pacientes. Os resultados indicaram que 63,9% dos pacientes não seguem dieta alimentar específica para hipertensão arterial e 75% dos pacientes não praticam exercícios físicos.  Em relação ao tratamento medicamentoso, o anti-hipertensivo mais utilizado foi a hidroclorotiazida, presente no tratamento de 63,9% dos pacientes avaliados, seguido do captopril (61,1% dos pacientes, propranolol (27,8%, dentre outros prescritos para menos de 25% dos pacientes.  A avaliação da adesão ao tratamento medicamentoso indicou que 69,4% dos pacientes apresentam adesão plena, 17,6% relataram omissão de doses e apenas 13% relataram não adesão ao tratamento. Um total de 87,9% dos pacientes apresentou níveis pressóricos acima dos limites de normalidade. De acordo com os resultados pode-se concluir que os pacientes possuem alta adesão ao tratamento farmacológico e baixa adesão ao tratamento não farmacológico, o que pode ser responsável pela dificuldade de controle dos níveis da pressão arterial.

  9. A novel dipeptidyl aminopeptidase in rat brain membranes. Its isolation, purification, and characterization.

    Science.gov (United States)

    Hui, K S

    1988-05-15

    A new type of dipeptidyl aminopeptidase, which releases basic aminoacyl dipeptides from the NH2-terminal end of oligopeptides, was purified about 2100-fold with 6.8% recovery from rat brain membranes by column chromatography on Cellex D, Arg-Tyr-AH-Sepharose 4B, hydroxylapatite, and Sephadex G-75, after the membranes were solubilized with Nonidet P-40. Activity was assayed by high performance liquid chromatography (HPLC) using Arg0-Met5-enkephalin (Arg0-enk)* as substrate in the presence of bestatin, thiorphan, and captopril. In sodium dodecyl sulfate-polyacrylamide gel electrophoresis, the purified enzyme is apparently homogeneous with a mass of 64,000 daltons. This thiol enzyme is optimally active at pH 7 and is selectively activated by Mn(II). It loses 94% of its activity after EDTA treatment and can be reactivated by Mn(II), Co(II), and Zn(II). It splits Arg0-enk into equimolar amounts of Arg-Tyr and Gly-Gly-Phe-Met with a Km of 100 microM, and Vmax of 3.8 mumol/mg of protein/min. Dipeptidyl aminopeptidase does not hydrolyze model substrates for dipeptidyl aminopeptidases I, II, III, and IV, aminoacyl beta-naphthylamides, actin, desmin, tubulin, glial fibrillary acidic protein, and cytoskeletal neurofilament proteins. The enzyme is insensitive to puromycin, but is inhibited by several neuropeptides. Angiotensin III is the most potent with a Ki of 0.3 microM. Substrate specificity, pH optimum, molecular weight, activators, and catalytic site demonstrate that this enzyme is distinct from dipeptidyl aminopeptidases previously described.

  10. Prevalence of cough among patients treated with angiotensin converting enzyme inhibitors

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    Gebrehiwot Teklay

    2014-12-01

    Full Text Available Purpose: The aim of this study was to assess the prevalence of cough, its causality and impact on patient adherence in patients taking angiotensin converting enzyme inhibitors. Methods - A cross sectional study was conducted in Ayder Referral Hospital, northern Ethiopia from April to June 2014. Patients who started either captopril or enalapril were interviewed for the occurrence of cough and its characteristics. Data were entered to EPI-info and analyzed using SPSS for windows version 16 statistical software. Logistic regression model was used to analyze variations in occurrence of cough among different factors. P value of less than 0.05 was considered statistically significant. Results - One hundred two patients were participated in this study. Of which, 54(52.9% were females. About half of the respondents (53% were between the ages of 40 to 60. Cough was observed in 30 (29.4% patients. According to World Health Organizations causality scale, the reported cough was certain (drug induced in 5 (7.1% patients; possible in 10 (25% patients; probable in 12 (10.7% patients and unlikely in 3 (57.1% patients. Significant statistical difference was observed between occurrence of cough and durations of treatment (P<0.05. There was no statistically significant difference in occurrence of cough with age, sex, ethnicity, residence, dose and type of ACEI. Conclusion – In this study, dry cough was more prevalent among patients on angiotensin converting enzyme inhibitors. Troublesome cough may affect patient’s sleep and overall adherence to treatment. Health professionals should aware of the characteristics cough and manage accordingly.

  11. Angiotensin II receptors in the gonads

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    Aguilera, G.; Millan, M.A.; Harwood, J.P.

    1989-05-01

    The presence of components of the renin-angiotensin system in ovaries and testes suggests that angiotensin II (AII) is involved in gonadal function, and thus we sought to characterize receptors for AII in rat and primate gonads. In the testes, autoradiographic studies showed receptors in the interstitium in all species. In rat interstitial cells fractionated by Percoll gradient, AII receptors coincided with hCG receptors indicating that AII receptors are located on the Leydig cells. In Leydig cells and membranes from rat and rhesus monkey prepuberal testes, AII receptors were specific for AII analogues and of high affinity (Kd=nM). During development, AII receptor content in rat testes decreases with age parallel to a fall in the ratio of interstitial to tubular tissue. In the ovary, the distribution of AII receptors was dependent on the stage of development, being high in the germinal epithelium and stromal tissue between five and 15 days, and becoming localized in secondary follicles in 20-and 40-day-old rats. No binding was found in primordial or primary follicles. In rhesus monkey ovary, AII receptors were higher in stromal tissue and lower in granulosa and luteal cells of the follicles. Characterization of the binding in rat and monkey ovarian membranes showed a single class of sites with a Kd in the nmol/L range and specificity similar to that of the adrenal glomerulosa and testicular AII receptors. Receptors for AII were also present in membrane fractions from PMSG/hCG primed rat ovaries. Infusion of AII (25 ng/min) or captopril (1.4 micrograms/min) during the PMSG/hCG induction period had no effect on ovarian weight or AII receptor concentration in the ovaries.

  12. Ritonavir and Disulfiram May Be Synergistic in Lowering Active Interleukin-18 Levels in Acute Pancreatitis, and thereby Hasten Recovery

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    Richard Eric Kast

    2008-05-01

    Full Text Available This short note reviews the role of interleukin-18 (IL-18 in acute pancreatitis. IL-18 is a narrow yet important aspect of acute pancreatitis. Narrow because many other inflammatory mediators are active in acute pancreatitis, but important because: a many of the other inflammatory mediators arise secondary to IL-18; and B we happen to have several medicines, in use for other purposes for decades, that pre-clinical and murine studies have indicated happily have ability to lower active IL-18 formation. Also giving IL-18 particular importance is: c the cause of early mortality in acute pancreatitis is mostly due to systemic inflammation, for which IL-18 is an important driving force [1, 2, 3]. Alcohol abuse and cholelithiasis account for 90% of acute pancreatitis, with autoimmune, genetic, hyperlipidemia, obesity and other factors as less common predisposing factors [1, 2, 3]. Diverse secondary morbidity is seen, with chronic pain as a common sequela. Mortality rate is not trivial by multiorgan dysfunction that in extreme forms leads to multiorgan failure[1, 2, 3]. The clinical picture is dominated by fierce pain, hypotension, and susceptibility to secondary infection. Hepatitis and pneumonia are common. Endoscopic or surgical decompression procedures, necrotic tissue removal can help. Medical interventions seem limited to supportive measures, antibiotics for secondary infection, etc. and have not changed much in the last 50 years [1, 2, 3]. This short note presents data indicating that three old drugs, ritonavir, disulfiram, and captopril, have potential to lower IL-18 and may therefore be of benefit in treating pancreatitis.

  13. Modulation of cutaneous inflammation by angiotensin-converting enzyme.

    Science.gov (United States)

    Scholzen, Thomas E; Ständer, Sonja; Riemann, Helge; Brzoska, Thomas; Luger, Thomas A

    2003-04-01

    Cutaneous neurogenic inflammation is a complex biological response of the host immune system to noxious stimuli. Present evidence suggests that zinc metalloproteases may play an important role in the regulation of neurogenic inflammation by controlling the local availability of neuropeptides, such as substance P (SP), that are capable of initiating or amplifying cutaneous inflammation after release from sensory nerves. To address the hypothesis that the dipeptidyl carboxypeptidase angiotensin-converting enzyme (ACE) is capable of modulating skin inflammation, we have analyzed murine allergic contact dermatitis (ACD) and irritant contact dermatitis (ICD) using wild-type C57BL/6J (ACE(+/+)) or genetically engineered mice with a heterozygous deletion of somatic ACE (ACE(+/-)). In 2,4-dinitro-1-fluorobenzene-sensitized ACE(+/-) mice, ACD was significantly augmented in comparison to ACE(+/+) controls as determined by the degree of ear swelling after exposure to hapten. Likewise, systemic treatment of ACE(+/+) mice with the ACE inhibitor captopril before sensitization or elicitation of ACD significantly augmented the ACD response. In contrast, local damage and neuropeptide depletion of sensory nerves following capsaicin, injection of a bradykinin B(2), or a SP receptor antagonist before sensitization significantly inhibited the augmented effector phase of ACD in mice with functionally absent ACE. However, in contrast to ACD, the response to the irritant croton oil was not significantly altered in ACE(+/-) compared with ACE(+/+) mice. Thus, ACE by degrading bradykinin and SP significantly controls cutaneous inflammatory responses to allergens but not to irritants, which may explain the frequently observed exacerbation of inflammatory skin disease in patients under medication with ACE inhibitors.

  14. Angiotensin I conversion to angiotensin II stimulates cortical collecting duct sodium transport.

    Science.gov (United States)

    Komlosi, Peter; Fuson, Amanda L; Fintha, Attila; Peti-Peterdi, János; Rosivall, Laszlo; Warnock, David G; Bell, Phillip Darwin

    2003-08-01

    Angiotensin (Ang) II directly stimulates epithelial sodium channel activity in the rabbit cortical collecting duct. Because Ang I and converting enzyme analogues might be present in the distal nephron, this raises the possibility of intraluminal generation of Ang II. Conversion of Ang I to Ang II was monitored by Ang II-dependent changes in intracellular sodium concentration as a reflection of sodium transport across the apical membrane. This involved imaging-based fluorescence microscopy with sodium-binding benzofuran isophthalate in isolated, perfused, cortical collecting-duct segments from rabbit kidney. Principal and intercalated cells were differentiated by rhodamine-conjugated peanut lectin. Control principal cell intracellular sodium concentration, during perfusion with 25 mmol/L NaCl and zero sodium in the bath plus monensin (10(-5) mol/L) averaged 5.8+/-0.14 mmol/L (n=156). The increase in intracellular sodium concentration, when luminal NaCl was increased from 25 to 150 mmol/L, was elevated by 3.5-fold in the presence of intraluminal Ang I (10(-6) mol/L). Also, the effects of Ang I on sodium transport were not significantly different from the effects of Ang II (10(-9) mol/L). Ang I was used in micromolar concentrations to ensure that there was sufficient substrate available for conversion to Ang II. Inhibition of the angiotensin-converting enzyme with captopril reduced the stimulatory effect of Ang I. These results suggest that intraluminal conversion of Ang I to Ang II can occur in the cortical collecting duct, resulting in enhanced apical sodium entry.

  15. Imaging the renin-angiotensin system: an important target of anti-hypertensive therapy.

    Science.gov (United States)

    Kang, Jung Julie; Toma, Ildikó; Sipos, Arnold; McCulloch, Fiona; Peti-Peterdi, János

    2006-09-15

    Multiphoton fluorescence microscopy allows visualization, manipulation, and quantification of the structure-function relationships between pharmacological interventions and their physiological effects. The application of these methods to live animals permits direct observation of acute physical responses that lack chemically detectable signals in the blood or urine and would otherwise remain unknown. With the use of special fluorescent dyes, chemical/hormonal responses may also be detected. The delivery and site-specific effects of drugs can be monitored in real-time. The capacity to simultaneously visualize both proximal and distal segments of the nephron permits observation of the dynamic processes within the living kidney and a quantitative assessment of the various operations. Consequently, a clinically valuable and pending application for multi-photon microscopy will be to provide real-time, quantitative imaging of basic organ functions and their responses to therapeutic intervention. Imaging of the intra-renal renin content and enzymatic activity of renin in situ and in real-time is a new, more informative measure of RAS activity. Direct visualization of the molecular and cellular components of renin release signals and the interactions between the vascular endothelium, tubular epithelium, local mediators, and the renin producing cells provides great insight for drug development. Examples of how the effects of various RAS inhibitors can be visualized in the intact kidney are provided: including angiotensin converting enzyme inhibition (captopril), angiotensin II type 1 receptor blockade (olmesartan), and renin inhibition (aliskiren). The site-specific actions of diuretics, like furosemide, have also been visualized. Quantitative imaging of basic renal functions in health and disease can provide key information to assess the delivery and effects of pharmaceutical interventions.

  16. Immunolocalization of a microsomal prostaglandin E synthase in rabbit kidney.

    Science.gov (United States)

    Fuson, Amanda L; Komlosi, Peter; Unlap, Tino M; Bell, P Darwin; Peti-Peterdi, János

    2003-09-01

    PGE2, the major cyclooxygenase (COX) metabolite of arachidonic acid, is an important paracrine regulator of numerous tubular and vascular functions in the kidney. To date, COX activity has been considered the key step in prostaglandin synthesis and is well characterized. However, much less is known about the recently cloned microsomal PGE2 synthase (mPGES), the terminal enzyme of PGE2 synthesis, which converts COX-derived PGH2 to the biologically important PGE2. Present studies provide the detailed localization of mPGES protein in the rabbit kidney using immunohistochemistry. In the cortex, strong mPGES labeling was found in the macula densa (MD) and principal cells of the connecting segment and cortical collecting tubule but not in intercalated cells. The medulla was abundant in mPGES-positive structures, with heavy labeling in the collecting duct system. In descending thin limbs and renal medullary interstitial cells, mPGES expression was less intense, and it was below the limits of detection in the vasa recta. Expression of MD mPGES, similarly to COX-2, was greatly increased in response to low-salt diet and angiotensin I-converting enzyme inhibition by captopril. These findings suggest autocrine regulation of renal salt and water transport by PGE2 in descending thin limb and collecting tubule and a paracrine effect of PGE2 on the glomerular and medullary vasculature. Similar to other organs, mPGES in the kidney is an inducible enzyme and may be similarly regulated and acts in concert with COX-2.

  17. Role of α{sub 2}-adrenoceptors in the lateral parabrachial nucleus in the control of body fluid homeostasis

    Energy Technology Data Exchange (ETDEWEB)

    Andrade, C.A.F.; Andrade-Franzé, G.M.F.; De Paula, P.M.; De Luca, L.A. Jr.; Menani, J.V. [Departamento de Fisiologia e Patologia, Faculdade de Odontologia, Universidade Estadual Paulista, Araraquara, SP (Brazil)

    2014-01-10

    Central α{sub 2}-adrenoceptors and the pontine lateral parabrachial nucleus (LPBN) are involved in the control of sodium and water intake. Bilateral injections of moxonidine (α{sub 2}-adrenergic/imidazoline receptor agonist) or noradrenaline into the LPBN strongly increases 0.3 M NaCl intake induced by a combined treatment of furosemide plus captopril. Injection of moxonidine into the LPBN also increases hypertonic NaCl and water intake and reduces oxytocin secretion, urinary sodium, and water excreted by cell-dehydrated rats, causing a positive sodium and water balance, which suggests that moxonidine injected into the LPBN deactivates mechanisms that restrain body fluid volume expansion. Pretreatment with specific α{sub 2}-adrenoceptor antagonists injected into the LPBN abolishes the behavioral and renal effects of moxonidine or noradrenaline injected into the same area, suggesting that these effects depend on activation of LPBN α{sub 2}-adrenoceptors. In fluid-depleted rats, the palatability of sodium is reduced by ingestion of hypertonic NaCl, limiting intake. However, in rats treated with moxonidine injected into the LPBN, the NaCl palatability remains high, even after ingestion of significant amounts of 0.3 M NaCl. The changes in behavioral and renal responses produced by activation of α{sub 2}-adrenoceptors in the LPBN are probably a consequence of reduction of oxytocin secretion and blockade of inhibitory signals that affect sodium palatability. In this review, a model is proposed to show how activation of α{sub 2}-adrenoceptors in the LPBN may affect palatability and, consequently, ingestion of sodium as well as renal sodium excretion.

  18. The vascular renin-angiotensin system contributes to blunted vasodilation induced by transient high pressure in human adipose microvessels.

    Science.gov (United States)

    Durand, Matthew J; Phillips, Shane A; Widlansky, Michael E; Otterson, Mary F; Gutterman, David D

    2014-07-01

    Increased intraluminal pressure can reduce endothelial function in resistance arterioles; however, the mechanism of this impairment is unknown. The purpose of this study was to determine the effect of local renin-angiotensin system inhibition on the pressure-induced blunting of endothelium-dependent vasodilation in human adipose arterioles. Arterioles (100-200 μm) were dissected from fresh adipose surgical specimens, cannulated onto glass micropipettes, pressurized to an intraluminal pressure of 60 mmHg, and constricted with endothelin-1. Vasodilation to ACh was assessed at 60 mmHg and again after a 30-min exposure to an intraluminal pressure of 150 mmHg. The vasodilator response to ACh was significantly reduced in vessels exposed to 150 mmHg. Exposure of the vessels to the superoxide scavenger polyethylene glycol-SOD (100 U/ml), the ANG II type 1 receptor antagonist losartan (10(-6) mol/l), or the angiotensin-converting enzyme inhibitor captopril (10(-5) mol/l) prevented the pressure-induced reduction in ACh-dependent vasodilation observed in untreated vessels. High intraluminal pressure had no effect on papaverine-induced vasodilation or ANG II sensitivity. Increased intraluminal pressure increased dihydroethidium fluorescence in cannulated vessels, which could be prevented by polyethylene glycol-SOD or losartan treatment and endothelial denudation. These data indicate that high intraluminal pressure can increase vascular superoxide and reduce nitric oxide-mediated vasodilation via activation of the vascular renin-angiotensin system. This study provides evidence showing that the local renin-angiotensin system in the human microvasculature may be pressure sensitive and contribute to endothelial dysfunction after acute bouts of hypertension.

  19. Availability, price and affordability of cardiovascular medicines: A comparison across 36 countries using WHO/HAI data

    Directory of Open Access Journals (Sweden)

    Cameron Alexandra

    2010-06-01

    Full Text Available Abstract Background The global burden of cardiovascular disease (CVD continues to rise. Successful treatment of CVD requires adequate pharmaceutical management. The aim was to examine the availability, pricing and affordability of cardiovascular medicines in developing countries using the standardized data collected according to the World Health Organization/Health Action International methodology. Methods The following medicines were included: atenolol, captopril, hydrochlorothiazide, losartan and nifedipine. Data from 36 countries were analyzed. Outcome measures were percentage availability, price ratios to international reference prices and number of day's wages needed by the lowest-paid unskilled government worker to purchase one month of chronic treatment. Patient prices were adjusted for inflation and purchasing power, procurement prices only for inflation. Data were analyzed for both generic and originator brand products and the public and private sector and summarized by World Bank Income Groups. Results For all measures, there was great variability across surveys. The overall availability of cardiovascular medicines was poor (mean 26.3% in public sector, 57.3% private sector. Procurement prices were very competitive in some countries, whereas others consistently paid high prices. Patient prices were generally substantially higher than international references prices; some countries, however, performed well. Chronic treatment with anti-hypertensive medication cost more than one day's wages in many cases. In particular when monotherapy is insufficient, treatment became unaffordable. Conclusions The results of this study emphasize the need of focusing attention and financing on making chronic disease medicines accessible, in particular in the public sector. Several policy options are suggested to reach this goal.

  20. Platelet-derived growth factor receptor-β in myocyte was upregulated by angiotensin II

    Institute of Scientific and Technical Information of China (English)

    2002-01-01

    To observe the regulation of platelet-derived growth factor (PDGF) receptor-βin myocyte stimulated by angiotensin II (AngII) at both integrated and cellular levels and reveal the signal transduction mechanism in cell, two kidneys, one clip (2K1C) renal hypertension were performed by placing a sliver clip around the left renal artery. Blood pressure and the ratio of left ventricular weight to body weight were measured at 4 and 8 weeks after operation. The content of AngII in heart was detected by radioimmunology assay; the protein level of PDGF receptor-βin heart was measured by Western blot analysis. The alteration of PDGF receptor-βstimulated by AngII and several inhibitors was observed on cultured neonatal rat ventricular myocyte (NRVM). The content of AngII in heart of 2K1C renal hypertensive rat at 4 and 8 weeks after operation was increased. Compared with sham group, 4 and 8 weeks after operation, PDGF receptor-βin heart of 2K1C group was upregulated by 100.3% and 127.1% (P < 0.05), respectively. This upregulation could be inhibited by captopril. For cultured myocyte, PDGF receptor-βwas increased by 47.1% after being stimulated by AngII and this upregulation could be inhibited by losartan which was an inhibitor of AT1 receptor. PLC inhibitor (U73122) and MEK inhibitor (PD98059) could partly inhibit PDGF receptor-βupregulation induced by AngII. These results suggested that AngII could upregulate PDGF receptor-βin myocyte by its AT1 receptor and this effect was at least partly dependent on PLC and extracellular signal-regulated kinase (ERK).

  1. Metabolic considerations in the choice of therapy for the patient with hypertension.

    Science.gov (United States)

    Black, H R

    1991-02-01

    The objective of treating patients with hypertension is not simply to reduce blood pressure but rather to prevent the associated morbidity and mortality. Recent assessments of clinical trials have shown that while the risk of stroke is consistently lower with antihypertensive therapy, the same degree of success has not been demonstrated for coronary artery disease (CAD). Although there are many explanations of why we have not done as well in preventing CAD, one possibility is that the therapy used in clinical trials, primarily thiazide diuretics and beta-adrenoreceptor blockers, has increased the patient's risk of developing coronary atherosclerosis or lethal arrhythmias. Four classes of antihypertensive agents are recommended for initial therapy--thiazide diuretics, beta-adrenoreceptor blockers, angiotensin-converting enzyme (ACE) inhibitors, and calcium entry blockers. The metabolic effects of thiazide diuretics include electrolyte disturbances (hypokalemia, hypomagnesemia, and hyponatremia), dyslipidemia (increased triglycerides), abnormalities of glucose metabolism (hyperglycemia, hyperinsulinemia, and peripheral insulin resistance), and hyperuricemia. beta-Adrenoreceptor blockers have many of the same metabolic adverse reactions. beta-Adrenoreceptor blockers without intrinsic sympathomimetic activity (ISA) also cause dyslipidemias (lowered high-density lipoprotein cholesterol and increased triglycerides) and abnormalities of glucose metabolism (hyperglycemia, hyperinsulinemia, and peripheral insulin resistance). beta-Adrenoreceptor blockers with ISA and third-generation beta-blockers with selective partial agonist activity (celiprolol and dilevalol) do not cause dyslipidemia and to date do not appear to induce abnormalities in glucose metabolism. ACE inhibitors may decrease triglycerides and increase high-density lipoprotein cholesterol, and captopril may improve insulin sensitivity. Calcium entry blockers are metabolically neutral.(ABSTRACT TRUNCATED AT 250

  2. Uso contínuo de medicamentos e condições de trabalho entre motoristas de caminhão

    Directory of Open Access Journals (Sweden)

    Edmarlon Girotto

    Full Text Available Resumo Os motoristas de caminhão têm sido pouco explorados quanto aos problemas de saúde que os acometem e, principalmente, quanto ao seu perfil de consumo de medicamentos. Este estudo teve o objetivo de determinar o uso contínuo de medicamentos, por motoristas de caminhão, e identificar as características profissionais associadas. Para a sua realização, conduziu-se um estudo transversal com motoristas de caminhão estacionados no Pátio de Triagem do Porto de Paranaguá, Paraná, Brasil. Realizou-se uma entrevista com obtenção de dados socioeconômicos, problemas de saúde, condições de trabalho e uso contínuo de medicamentos. Dos motoristas avaliados (n = 665, 21,1% referiram utilizar algum medicamento continuamente, com destaque para o captopril (10,7%, metformina (10,3%, omeprazol (6,2% e sinvastatina (6,2%. Motoristas com dezesseis anos ou mais de experiência profissional (RP 1,67; IC 95% 1,11-2,51, proprietários do próprio caminhão (RP 1,38; IC 95% 1,03-1,86 e que não possuíam vínculo empregatício formal (RP 1,49; IC 95% 1,11-2,00 apresentaram maior prevalência de uso contínuo de medicamentos. Observa-se que algumas condições de trabalho têm importante papel do uso contínuo de medicamentos pelos motoristas de caminhão.

  3. Mechanisms of the regional hemodynamic effects of a mu-opioid receptor agonist microinjected into the hypothalamic paraventricular nuclei of conscious unrestrained rats.

    Science.gov (United States)

    Bachelard, H; Pître, M; Lessard, A

    1997-01-01

    The present study was undertaken to characterize the mechanisms of the hemodynamic responses to microinjection of the selective mu-opioid receptor agonist [D-Ala2,MePhe4,Gly5-ol]enkephalin (DAMGO) into the paraventricular nucleus of the hypothalamus, in conscious rats chronically instrumented with pulsed Doppler flow probes. We found that i.v. pretreatment with phentolamine had no effect on the tachycardia elicited by DAMGO (1 nmol); however, the pressor response was reversed to a state of hypotension, the renal and superior mesenteric vasoconstrictions were attenuated and the hindquarter vasodilation was potentiated. In the presence of propranolol, the pressor response and renal vasoconstriction were unchanged, whereas the superior mesenteric vasoconstriction was reduced and the hindquarter vasodilation was abolished. Moreover, in those animals we observed bradycardia followed by tachycardia. Combined i.v. pretreatment with phentolamine and propranolol abolished the pressor and heart rate responses to DAMGO but had no effect on the renal and superior mesenteric vasoconstrictions, although the hindquarter vasodilation was reduced. Intravenous pretreatment with a vasopressin V1 receptor antagonist or captopril had no effect on the cardiovascular responses to DAMGO. Together, these results indicate that the hypertension observed after injection of DAMGO into the paraventricular nucleus of the hypothalamus was secondary to alpha adrenoceptor-mediated vasoconstrictions in renal and superior mesenteric vascular beds and to beta adrenoceptor-mediated vasodilation in the hindquarter vascular bed, whereas the involvement of circulating vasopressin or angiotensin seems less obvious from the present findings. However, we cannot exclude the possibility that nonadrenergic, nonvasopressinergic and nonangiotensinergic vasoconstrictor mechanisms were acting in the renal and superior mesenteric vascular beds.

  4. Effects of multi-intervention RAAS on ventricular remodeling and serum K+ concentration in the chronic cardiac insufficiency rats%多重干预RAAS对大鼠慢性心功能不全心室重构及血钾的影响

    Institute of Scientific and Technical Information of China (English)

    陈斗佳; 陈娅; 吴伦宽

    2011-01-01

    目的 探讨多重干预RAAS对大鼠慢性心功能不全心室重构及血钾的影响.方法 实验采用缩窄大鼠腹主动脉法建立慢性压力负荷致心功能不全动物模型,选6周龄20只雌性SD大鼠,随机分4组(每组5只),B组(手术模型组)、C组(卡托普利组)、D组(卡托普利+缬沙坦组)、E组(卡托普利+缬沙坦+螺内酯组),另随机抽取5只同龄雌性SD大鼠假手术作为对照(A组).给药8周后用Doppler超声心动图检测大鼠心脏结构和心功能各项参数的变化,放射免疫法测定血浆Ang Ⅱ,ALDO浓度,并生化检测血钾水平.结果 腹主动脉结扎后第9周,与A组比较,B组舒张末期室间隔厚度(IVSTD)、舒张末期左室后壁厚度(LVPWTD)、相对室壁厚度(RWT)、左室重量(LVM)、左室重量与体重比(LVM/BW)均显著提高(P<0.05);C、D、E组与B组相比,LVM,LVM/BW下降显著(P<0.05).各药物干预组(C、D、E)血浆Ang Ⅱ,ALDO水平明显低于B组(P<0.05),以联合应用螺内酯组明显.各药物干预组与A组和B组相比较,血钾水平差异无显著性(P>0.05).结论 联合应用卡托普利、缬沙坦及螺内酯多重干预RAAS能明显改善大鼠慢性心功能不全心室重构,对血钾无明显影响.%Objective To explore the effects of multi-intervention RAAS on ventricular remodeling and serum K+ concentration in the chronic pressure overload heart due to cardiac insufficiency in rats. Methods To establish chronic cardiac insufficiency animal models with suprarenal abdominal aortic banding in rats. Six-week old female Sprague-Dawley rats were enrolled and the suprarenal abdominal aorta was ligated by 4-0 nylon suture against a needle (outer diameter 0. 7 mm). Twenty female rats were randomized into four groups (n = 5), including operated rats (group B), and Captopriltreated rats ( group C), Captopril + Valsartan treatment rats ( group D) and Captopril + Valsartan + Spironolactone treatment rats (group E), which were treated by

  5. Preços e disponibilidade de medicamentos no Programa Farmácia Popular do Brasil Precios y disponibilidad de medicamentos en el Programa Farmacia Popular de Brasil Medicine prices and availability in the Brazilian Popular Pharmacy Program

    Directory of Open Access Journals (Sweden)

    Cláudia Du Bocage Santos Pinto

    2010-08-01

    Full Text Available OBJETIVO: Analisar o desempenho do Programa Farmácia Popular do Brasil perante os setores público e privado, em relação a: disponibilidade, preço e custo, para o paciente, de medicamentos para hipertensão e diabetes. MÉTODOS: Foi utilizada a metodologia desenvolvida pela Organização Mundial da Saúde em conjunto com a Ação Internacional para Saúde, para comparação de preços e disponibilidade de medicamentos. A pesquisa foi aplicada em maio de 2007, em estabelecimentos de diferentes setores [público, privado e as modalidades própria (FPB-P e expansão (FPB-E do Programa], em 30 municípios do Brasil. Os quatro medicamentos analisados foram: captopril 25mg e hidroclorotiazida 25mg, para hipertensão, e metformina 500mg e glibenclamida 5mg, para diabetes. RESULTADOS: O FPB-E apresentou maior disponibilidade de medicamentos e o setor público, a menor. Tanto no setor público quanto na FPB-P o percentual de disponibilidade de similares foi maior que o de genéricos. A comparação de preços entre os setores mostrou menor preço de aquisição no FPB-E, seguido pelo FPB-P. O FPB-E apresentou economia superior a 90% em relação ao setor privado. O número de dias de trabalho necessários para aquisição de tratamentos para hipertensão e diabetes foi menor no FPB-E. CONCLUSÕES: A menor disponibilidade encontrada no setor público pode ser uma das justificativas para migração dos usuários do setor público para o FPB. Os altos preços praticados pelo setor privado também contribuem para que o Programa seja uma alternativa de acesso a medicamentos no País.OBJETIVO: Analizar el desempeño del Programa Farmacia Popular de Brasil frente a los sectores público y privado, con relación a: disponibilidad, precio y costo para el paciente, de medicamentos para hipertensión y diabetes. MÉTODOS: Fue utilizada la metodología desarrollada por la Organización Mundial de la Salud en conjunto con la Acción Internacional para Salud, para

  6. 滋肾活血方在抗肾纤维化中对HA、LN、TGF-β1干预作用的实验研究%An experimental study of intervention effect of the Zishen Huoxue recipe against HA, LN, TGF-β1 in anti-renal fibrosis

    Institute of Scientific and Technical Information of China (English)

    曹秋彩

    2013-01-01

      目的:探讨滋肾活血方对慢性肾病肾纤维化的防治作用及机制。方法:采用右侧肾切除加重复尾静脉注射阿霉素制备肾纤维化大鼠模型[1]。设滋肾活血方治疗组、卡托普利对照组、模型组、空白组。8周后观察各组大鼠24h蛋白定量、血清尿素氮(Bun)、肌肝(Scr)、透明质酸(HA)、层粘蛋白(LN)和肾组织中转化生长因子β1(TGF-β1)表达的变化。结果:滋肾活血方能够减少阿霉素肾纤维化大鼠尿蛋白的排泄,降低血清Bun、Scr、HA、LN的含量,抑制肾组织中TGF-β1的过度表达。结论:滋肾活血方能够延缓肾纤维化的进程,具有保护肾功能的作用。%  Objective:To investigate the effect of Zishen Huoxue recipe anti-chronicity nephropathy renal fibrosis preventive and therapeutic effect and mechanism. Methods:According to reference documents[1], we reproduced the rat model of adriamycin nephrosis by having right nephrectomy adding to injecting repeatedly ADR through the vein of tail. The rats were divided into four groups for the bland contral group, the Zishen Huoxue recipe group, the captopril group and the model group. We observe quantity of 24h urinary protein excretion, blood urea nitrogen and creatinine, HA , laminin and tranforming growth factorβ1 in kidney tissues after 8 weeks. Results:The Zishen Huoxue recipe can decrease quantity of 24h urinary protein excretion, degrade blood serum hyaluronic acid and laminin contents, depress tranforming growth factorβ1 over expression in kidney tissues. Conclusion:Zishen Huoxue recipe can prevent process of the renal fibrosis, to have preserve effect of the renal function.

  7. Consumo de medicamentos por idosos segundo prescrição médica em Jaú-SP

    Directory of Open Access Journals (Sweden)

    A. C. Marques

    2009-01-01

    Full Text Available

    Realizou-se este trabalho com o objetivo de conhecer as interações medicamentosas mais freqüentemente ocorridas no consumo de medicamentos por prescrição médica entre os idosos atendidos na rede municipal de saúde de Jaú-SP. Sabe-se que são os idosos que convivem mais freqüentemente com problemas crônicos de saúde, o que os leva a uma maior utilização de serviços de saúde e a um elevado consumo de medicamentos. Na presença de doenças concomitantes e na conseqüente prática da politerapia, aumenta a probabilidade de ocorrência de reações adversas e interações medicamentosas. A população estudada foi de 148 idosos com 65 anos ou mais, que compareceram à farmácia do Núcleo de Gestão Assistencial (NGA-25 da cidade de Jaú, no período de agosto a dezembro de 2004. Os dados foram coletados através da prescrição médica e as variáveis estudadas foram o sexo e a idade. Quanto aos medicamentos foram classificados, segundo a classe farmacológica e as interações medicamentosas.Como resultados observouse que consumo de medicamentos segundo o sexo foi de 3,8 medicamentos entre as mulheres e 3,9 entre os homens. Quanto a idade, o maior consumo foi no grupo de 75 a 84 anos, com 4,2 medicamentos. As classes terapêuticas mais prescritas, em ordem decrescente de ocorrência, foram: anti-hipertensivos, 25,0%, cardioterápicos, 15,5%, diuréticos, e antidiabéticos, 10,7%. Concluiu-se que as classes terapêuticas mais envolvidas com interações foram os cardioterápicos, diuréticos e antihipertensivos. Os princípios ativos mais problemáticos foram digoxina, amiodarona, furosemida, captopril, propranolol e nifedipina. Palavras-chave: Consumo medicamento, prescrição medicamento, idosos, interações medicamentos.

  8. Therapeutic possibilities of Bothrops jararaca in high dilution

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    Eduardo Costa Gaia Nazareth

    2011-09-01

    Full Text Available Introduction: The knowledge and use of the venom of Bothrops jararaca in high dilutions is still quite limited. One of the important properties is the use of one of its components, bradykinin, for the development of antihypertensive medication known as captopril. Other situations, such as clinical, local and systemic should receive more depth to the composition of Materia Medica related to various medical actions on the man and mammals in general. The systemic action of the bite of this snake, includes hemostasis disorders, culminating as bleeding gums, in addition to sweating, hypertension, and hypothermia. The action includes local pain and swelling with bruising, bleeding and often blistering and tissue necrosis. The action on the immune system, through action on the complement C3 and other complement components may show its possible use in cases of bacterial infections, including mycobacteria, as presented in the study of 1970 Vanessa Birdsey, "Interactions of poisons toxic with the addition, "the journal of Immunology 1971. Today, this poison has a toxicology published by Anibal Melgarejo, "Venomous Animals of Brazil", 2003, which subsidizes the development of study for its use in high dilutions, and a comprehensive study of the biology of the animal itself. Published studies on biomolecular analysis add more details about the relations of the poison and mammals. All these characteristics suggest the use of poison as a homeopathic remedy. Objective: To investigate the therapeutic possibilities in high dilutions of the venom of the snake Bothrops jararaca, expanding its clinical use. Methodology: Methodological description of this poison in contemporary bases including: Origin, physical description chemistry, toxicology, pharmacology and medicine in preparation of high dilution, general action, specific actions on systems or organs, sensations, modalities, concomitants, etiological indications relations main clinics. Results: Defining

  9. ABC gene-ranking for prediction of drug-induced cholestasis in rats

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    Yauheniya Cherkas

    2016-01-01

    drugs that behaved very differently, and were distinct from both non-cholestatic and cholestatic drugs (ketoconazole, dipyridamole, cyproheptadine and aniline, and many postulated human cholestatic drugs that in rat showed no evidence of cholestasis (chlorpromazine, erythromycin, niacin, captopril, dapsone, rifampicin, glibenclamide, simvastatin, furosemide, tamoxifen, and sulfamethoxazole. Most of these latter drugs were noted previously by other groups as showing cholestasis only in humans. The results of this work suggest that the ABC procedure and similar statistical approaches can be instrumental in combining data to compare toxicants across toxicogenomics databases, extract similarities among responses and reduce unexplained data varation.

  10. Regulation of urinary ACE2 in diabetic mice.

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    Wysocki, Jan; Garcia-Halpin, Laura; Ye, Minghao; Maier, Christoph; Sowers, Kurt; Burns, Kevin D; Batlle, Daniel

    2013-08-15

    Angiotensin-converting enzyme-2 (ACE2) enhances the degradation of ANG II and its expression is altered in diabetic kidneys, but the regulation of this enzyme in the urine is unknown. Urinary ACE2 was studied in the db/db model of type 2 diabetes and stretozotocin (STZ)-induced type 1 diabetes during several physiological and pharmacological interventions. ACE2 activity in db/db mice was increased in the serum and to a much greater extent in the urine compared with db/m controls. Neither a specific ANG II blocker, telmisartan, nor an ACE inhibitor, captopril, altered the levels of urinary ACE2 in db/db or db/m control mice. High-salt diet (8%) increased whereas low-salt diet (0.1%) decreased urinary ACE2 activity in the urine of db/db mice. In STZ mice, urinary ACE2 was also increased, and insulin decreased it partly but significantly after several weeks of administration. The increase in urinary ACE2 activity in db/db mice reflected an increase in enzymatically active protein with two bands identified of molecular size at 110 and 75 kDa and was associated with an increase in kidney cortex ACE2 protein at 110 kDa but not at 75 kDa. ACE2 activity was increased in isolated tubular preparations but not in glomeruli from db/db mice. Administration of soluble recombinant ACE2 to db/m and db/db mice resulted in a marked increase in serum ACE2 activity, but no gain in ACE2 activity was detectable in the urine, further demonstrating that urinary ACE2 is of kidney origin. Increased urinary ACE2 was associated with more efficient degradation of exogenous ANG II (10(-9) M) in urine from db/db compared with that from db/m mice. Urinary ACE2 could be a potential biomarker of increased metabolism of ANG II in diabetic kidney disease.

  11. A Comparative Effectiveness Meta-Analysis of Drugs for the Prophylaxis of Migraine Headache.

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    Jeffrey L Jackson

    Full Text Available To compare the effectiveness and side effects of migraine prophylactic medications.We performed a network meta-analysis. Data were extracted independently in duplicate and quality was assessed using both the JADAD and Cochrane Risk of Bias instruments. Data were pooled and network meta-analysis performed using random effects models.PUBMED, EMBASE, Cochrane Trial Registry, bibliography of retrieved articles through 18 May 2014.We included randomized controlled trials of adults with migraine headaches of at least 4 weeks in duration.Placebo controlled trials included alpha blockers (n = 9, angiotensin converting enzyme inhibitors (n = 3, angiotensin receptor blockers (n = 3, anticonvulsants (n = 32, beta-blockers (n = 39, calcium channel blockers (n = 12, flunarizine (n = 7, serotonin reuptake inhibitors (n = 6, serotonin norepinephrine reuptake inhibitors (n = 1 serotonin agonists (n = 9 and tricyclic antidepressants (n = 11. In addition there were 53 trials comparing different drugs. Drugs with at least 3 trials that were more effective than placebo for episodic migraines included amitriptyline (SMD: -1.2, 95% CI: -1.7 to -0.82, -flunarizine (-1.1 headaches/month (ha/month, 95% CI: -1.6 to -0.67, fluoxetine (SMD: -0.57, 95% CI: -0.97 to -0.17, metoprolol (-0.94 ha/month, 95% CI: -1.4 to -0.46, pizotifen (-0.43 ha/month, 95% CI: -0.6 to -0.21, propranolol (-1.3 ha/month, 95% CI: -2.0 to -0.62, topiramate (-1.1 ha/month, 95% CI: -1.9 to -0.73 and valproate (-1.5 ha/month, 95% CI: -2.1 to -0.8. Several effective drugs with less than 3 trials included: 3 ace inhibitors (enalapril, lisinopril, captopril, two angiotensin receptor blockers (candesartan, telmisartan, two anticonvulsants (lamotrigine, levetiracetam, and several beta-blockers (atenolol, bisoprolol, timolol. Network meta-analysis found amitriptyline to be better than several other medications including candesartan, fluoxetine, propranolol, topiramate and valproate and no different than

  12. 四逆汤含药血清对心肌毒性大鼠乳鼠血清Bcl-2 Bax水平影响的研究%To Study of Effection of Blood Serum of Decoction for Treating Yang Exhaustion on Serum Baxand Bcl-2in Adriamycin Induced Cardio-toxicity in Myocardial Cell of Rat

    Institute of Scientific and Technical Information of China (English)

    王睿; 费洪新; 石小芳; 刘文华; 黄小义; 杨德助; 张腾腾

    2009-01-01

    目的:探讨四逆汤含药血清抗心肌毒性的疗效及其作用机制.方法:采用盐酸阿霉素(ADB)损伤Wistar大鼠乳鼠心肌导致心肌毒性为模型.随机分为正常组、心脏毒性ADR模型对照组、卡托普利组、四逆汤含药血清组.测定大鼠乳鼠血清Bcl-2、Bax水平,并应用光镜观察心肌组织的病理变化.结果:与正常组比较,阿霉素致心肌毒性大鼠乳鼠血清Bax水平显著降低.血清Bcl-2水平明显升高,四逆汤及卡托普利均能降低Bcl-2水平,升高Bax水平(P<0.05).光镜显示,四逆汤含药血清治疗组心肌细胞损伤程度明显低于模型组.结论:四逆汤含药血清能调节改善心肌毒性大鼠乳鼠的神经内分泌功能,拮抗过度激活的神经内分泌系统.%Objective:To explore the clinical effect and machenism of blood serum of decoction for treating yang ex-haustion on adriamycin induced cardio-toxicity in myocardial cell. Methods: Wistar rats were used to make cardio-toxicity in myocardial cell of rat model by injection of adriamyc into the peritoneum. The other 10 Wistar mrs were divided into the normal group. Model rats were randomly divided into model control group. Captopril group and blood serum of decoction for treating yang exhaustion group. Results : Compared with the normal group, serum baxlevel significantly decreased and Bcl -2level significantly increased. Compared with the model failure group, serum Bcl -2level significantly decreased and the level of baxsignificantly increased in the blood serum of decoction for treating yang exhaustion group and the Captopfil group(P < 0. 05). The degree of mycardial damage in the blood serum of decoction for treating yang exhaustion group was obviously lower than that in the model group. Conclusion: Blood senun of decoction for treating yang exhaustion can modify the nerval endocrine function of cardio - toxicity in myocardial cell failure rat and can antagonize the hyperactive nerval endocrine system.

  13. [Pharmacological study on blood pressure in rats with bone disorders].

    Science.gov (United States)

    Shamoto, T

    1989-12-01

    To evaluate the relationship between the elevation of blood pressure and altered bone metabolism, the changes of systolic blood pressure in six experimental models for bone disorders were investigated. Rats used were either parathyroidectomized, ovariectomized, fed with a calcium-deficient diet, fed with a vitamin D-deficient diet, treated with HEBP (1-Hydroxyethylidene-1, 1-bisphosphonate) or treated with streptozotocin. Hypertension developed in 5-week-old male rats fed with a calcium-deficient diet for 2 weeks, which evoked hypocalcemia and nutritional hyperparathyroidism. The blood pressure returned to normal when fed with a normal calcium diet. In parathyroidectomized rats receiving a normal calcium diet, the blood pressure did not rise, though the plasma calcium level decreased to an extent similar to the rats fed with the calcium-deficient diet. These findings seem to indicate that hyperparathyroidism, but not hypocalcemia, was involved in the elevation of blood pressure in rats fed with a calcium-deficient diet. Hypertension was not observed in rats fed with a vitamin D-deficient diet or treated with streptozotocin. These rats showed not only an increase in parathyroid hormone (PTH) but also a decrease in 1,25 (OH)2 D3. These results may suggest that the presence of 1,25 (OH)2D3 as well as the enhanced parathyroid function is necessary for the development of hypertension. The elevated blood pressure was reduced by a calcium antagonist, nifedipine, or by calcium supplementation, but not by an inhibitor of angiotensin-converting enzyme, captopril, or by calcitonin. This may indicate that hypertension due to nutritional hyperparathyroidism responds to the calcium antagonist nifedipine and to calcium supplementation, but does not depend on renin or salt. Furthermore, an acute hypotensive effect by human PTH (1-34) was not observed in the hypertension of calcium-deficient rats, suggesting the difference between acute and chronic effects of PTH. The hypertension

  14. Renovascular hypertension in children with neurofibromatosis type 1

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    Peco-Antić Amira

    2003-01-01

    Full Text Available Arterial hypertension in pediatric patients with neurofibromatosis type 1 (NF 1 is usually due to renal artery stenosis (RAS mainly involving the proximal part of the vessel. The treatment modalities are highly individualized. In severe and/or bilateral RAS, antihypertensive drugs are either ineffective or have the potential risk for acute renal failure, while percutaneous transluminal angioplasty (PTA has limited success due to the ostial localization of RAS and the tough fibrotic tissue involved that is refractory to dilatation Renal autotransplantation has potential advantages when medical control and PTA/or bypass techniques failed. Here we report 5 year-old girl with NF 1 and hyponatremic hypertensive syndrome due to severe bilateral disease, occluded proximal part of the right artery and ostial stenosis (80% of the left one. Only left kidney was identified on 99 in Tc DTP A, but the right one was visualized on the renal ultrasonography and in the late phase of arterial renography due to well developed collateral circulation. Multiple antihyper-tensive drugs (nifedipine, labetolol and minoxidil in maximal doses and PTA failed to normalize BP while short term therapy with ACEIwith NF1 and hyponatremic hypertensive syndrome due to severe bilateral renovascular disease; occluded proximal part of the right renal artery and ostial stenosis (80% of the left one. Only left kidney was identified on 99m Tc DTPA, but the right one was visualized on the renal ultrasonography and in the late phase of arterial renography due to well developed collateral circulation. Multiple antyphypertensive drugs (nifedipine, labetolol and minoxidil in maximal doses and PTA failed to normalize BP while. short term therapy with ACEI, captopril induced transient acute renal failure. Autotransplantation of right kidney saved its function and improved BP control. Our current case Autotransplantation of right kidney saved its function and improved BP control. Our current

  15. Effects of angiotensin II on leptin and downstream leptin signaling in the carotid body during acute intermittent hypoxia.

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    Moreau, J M; Messenger, S A; Ciriello, J

    2015-12-03

    Angiotensin II (ANG II) is known to promote leptin production and secretion. Although ANG II type 1 receptors (AT1Rs) and leptin are expressed within the carotid body, it is not known whether AT1R and leptin are co-expressed in the same glomus cells nor if these peptides are affected within the carotid body by intermittent hypoxia (IH). This study was done to investigate whether ANG II modulated leptin signaling in the carotid body during IH. Rats were treated with captopril (Capt) or the AT1R blocker losartan (Los) in the drinking water for 3days prior to being exposed to IH (8h) or normoxia (8h). IH induced increases in plasma ANG II and leptin compared to normoxic controls. Capt treatment abolished the plasma leptin changes to IH, whereas Los treatment had no effect on the IH induced increase in plasma leptin. Additionally, carotid body glomus cells containing both leptin and the long form of the leptin receptor (OB-Rb) were found to co-express AT1R protein, and IH increased the expression of only AT1R protein within the carotid body in both Capt- and non-Capt-treated animals. On the other hand, Los treatment did not modify AT1R protein expression to IH. Additionally, Capt and Los treatment eliminated the elevated carotid body leptin protein expression, and the changes in phosphorylated signal transducer and activator of transcription three protein, the short form of the leptin receptor (OB-R100), suppressor of cytokine signaling 3, and phosphorylated extracellular-signal-regulated kinase 1/2 protein expression induced by IH. However, Capt elevated the expression of OB-Rb protein, whereas Los abolished the changes in OB-Rb protein to IH. These findings, taken together with the previous observation that ANG II modifies carotid body chemosensitivity, suggest that the increased circulating levels of ANG II and leptin induced by IH act at the carotid body to alter leptin signaling within the carotid body which in turn may influence chemoreceptor function.

  16. The right choice of antihypertensives protects primary human hepatocytes from ethanol- and recombinant human TGF-β1-induced cellular damage

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    Ehnert S

    2013-03-01

    Full Text Available Sabrina Ehnert,1 Teresa Lukoschek,2 Anastasia Bachmann,2 Juan J Martínez Sánchez,1 Georg Damm,3 Natascha C Nussler,4 Stefan Pscherer,5 Ulrich Stöckle,1 Steven Dooley,2 Sebastian Mueller,6 Andreas K Nussler11Eberhard Karls Universität Tübingen, BG Trauma Center, Tübingen, Germany; 2Mol Hepatology - Alcohol Associated Diseases, Department of Medicine II, Medical Faculty, Mannheim, Germany; 3Department of General, Visceral, and Transplantation Surgery, Charité University Medicine, Berlin, Germany; 4Clinic for General, Visceral, Endocrine Surgery and Coloproctology, Clinic Neuperlach, Städtisches Klinikum München GmbH, Munich, Germany; 5Department of Diabetology, Klinikum Traunstein, Kliniken Südostbayern AG, Traunstein, Germany; 6Department of Medicine, Salem Medical Center, Ruprecht-Karls-Universität, Heidelberg, GermanyBackground: Patients with alcoholic liver disease (ALD often suffer from high blood pressure and rely on antihypertensive treatment. Certain antihypertensives may influence progression of chronic liver disease. Therefore, the aim of this study is to investigate the impact of the commonly used antihypertensives amlodipine, captopril, furosemide, metoprolol, propranolol, and spironolactone on alcohol-induced damage toward human hepatocytes (hHeps.Methods: hHeps were isolated by collagenase perfusion. Reactive oxygen species (ROS were measured by fluorescence-based assays. Cellular damage was determined by lactate-dehydrogenase (LDH-leakage. Expression analysis was performed by reverse-transcription polymerase chain reaction and Western blot. Transforming growth factor (TGF-β signaling was investigated by a Smad3/4-responsive luciferase-reporter assay.Results: Ethanol and TGF-β1 rapidly increased ROS in hHeps, causing a release of 40%–60% of total LDH after 72 hours. All antihypertensives dose dependently reduced ethanol-mediated oxidative stress and cellular damage. Similar results were observed for TGF-β1-dependent

  17. Potential prescription patterns and errors in elderly adult patients attending public primary health care centers in Mexico City

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    José Antonio Corona-Rojo

    2009-08-01

    Full Text Available José Antonio Corona-Rojo1, Marina Altagracia-Martínez1, Jaime Kravzov-Jinich1, Laura Vázquez-Cervantes1, Edilberto Pérez-Montoya2, Consuelo Rubio-Poo31Division of Biological Sciences and Health, Metropolitan Autonomous University, Campus Xochimilco (UAM-X, Xochimilco, México; 2National Polytechnical Institute (IPN, México DF; 3Faculty of Higher Studies – Zaragoza (FES-Zaragoza, National Autonomous University of México (UNAM, México City, MéxicoIntroduction: Six out of every 10 elderly persons live in developing countries.Objective: To analyze and assess the drug prescription patterns and errors in elderly outpatients attending public health care centers in Mexico City, Mexico.Materials and methods: A descriptive and retrospective study was conducted in 2007. Fourteen hundred prescriptions were analyzed. Prescriptions of ambulatory adults aged >70 years who were residents of Mexico City for at least two years were included. Prescription errors were divided into two groups: (1 administrative and legal, and (2 pharmacotherapeutic. In group 2, we analyzed drug dose strength, administration route, frequency of drug administration, treatment length, potential drug–drug interactions, and contraindications. Variables were classified as correct or incorrect based on clinical literature. Variables for each drug were dichotomized as correct (0 or incorrect (1. A Prescription Index (PI was calculated by considering each drug on the prescription. SPSS statistical software was used to process the collected data (95% confidence interval; p < 0.05.Results: The drug prescription pattern in elderly outpatients shows that 12 drugs account for 70.72% (2880 of prescribed drugs. The most prescribed drugs presented potential pharmacotherapeutic errors (as defined in the present study. Acetylsalicylic acid–captopril was the most common potential interaction (not clinically assessed. Potential prescription error was high (53% of total prescriptions. Most

  18. Potential drug-drug interactions in prescriptions to patients over 45 years of age in primary care, southern Brazil.

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    Jorge Juarez Vieira Teixeira

    Full Text Available BACKGROUND: Few cross-sectional studies involving adults and elderly patients with major DDIs have been conducted in the primary care setting. The study aimed to investigate the prevalence of potential drug-drug interactions (DDIs in patients treated in primary care. METHODOLOGY/PRINCIPAL FINDINGS: A cross-sectional study involving patients aged 45 years or older was conducted at 25 Basic Health Units in the city of Maringá (southern Brazil from May to December 2010. The data were collected from prescriptions at the pharmacy of the health unit at the time of the delivery of medication to the patient. After delivery, the researcher checked the electronic medical records of the patient. A total of 827 patients were investigated (mean age: 64.1; mean number of medications: 4.4. DDIs were identified in the Micromedex® database. The prevalence of potential DDIs and major DDIs was 63.0% and 12.1%, respectively. In both the univariate and multivariate analyses, the number of drugs prescribed was significantly associated with potential DDIs, with an increasing risk from three to five drugs (OR = 4.74; 95% CI: 2.90-7.73 to six or more drugs (OR = 23.03; 95% CI: 10.42-50.91. Forty drugs accounted for 122 pairs of major DDIs, the most frequent of which involved simvastatin (23.8%, captopril/enalapril (16.4% and fluoxetine (16.4%. CONCLUSIONS/SIGNIFICANCE: This is the first large-scale study on primary care carried out in Latin America. Based on the findings, the estimated prevalence of potential DDIs was high, whereas clinically significant DDIs occurred in a smaller proportion. Exposing patients to a greater number of prescription drugs, especially three or more, proved to be a significant predictor of DDIs. Prescribers should be more aware of potential DDIs. Future studies should assess potential DDIs in primary care over a longer period of time.

  19. 抗高血压药在我院应用的合理性分析

    Institute of Scientific and Technical Information of China (English)

    张颖菊

    2013-01-01

    Objective:To investigate the antihypertensive drugs used in our hospital. Method to my courtyard in 2008-2010 years of antihypertensive drugs in the class,the prescribing frequency were compared,the application of drug utilization index (DUI)in our hospital medication administration reasonableness analysis. Results of the calcium ion antagonist(CCB ),an-giotensin II receptor antagonists(ARB),diuretics,beta blockers prescribing frequency increase trend. Angiotensin converting enzyme inhibitors(ACEI)decreased the prescribing frequency. Spironolactone,metoprolol,amlodipine,enalapril,losartan potassium prescribing frequency in their respective categories of drugs in the first place. Captopril,benazepril,culture Duopuli, nifedipine,irbesartan DUI is greater than 1,other antihypertensive drugs DUI were less than 1. Conclusion:in addition to cap-topril,benazepril,culture Duopuli,nifedipine,irbesartan,my courtyard other antihypertensive drugs in outpatient and emer-gency use is basic and reasonable,norms,no abuse.%  目的探讨抗高血压药在我院应用的合理性.方法对我院2008年-2010年抗高血压药物在类别、处方频度进行比较,应用药物利用指数(DUI)对我院医师用药的合理性进行分析.结果钙离子拮抗剂(CCB)、血管紧张素Ⅱ受体拮抗剂(ARB)、利尿剂、β受体阻滞剂处方频度呈递增趋势.血管紧张素转换酶抑制剂(ACEI)处方频度呈递减趋势.螺内酯、美托洛尔、依那普利、左旋氨氯地平、氯沙坦钾的处方频度在各自所属类别药物中位居第一.卡托普利、贝那普利、培朵普利、硝苯地平、厄贝沙坦的DUI大于1.0,其它抗高血压药的DUI均小于1.0.结论除卡托普利、贝那普利、培朵普利、硝苯地平、厄贝沙坦外,我院其它抗高血压药在门急诊的使用基本合理、规范,无滥用现象.

  20. Fixed-dose combination vs monotherapy in hypertension: a meta-analysis evaluation.

    Science.gov (United States)

    Hilleman, D E; Ryschon, K L; Mohiuddin, S M; Wurdeman, R L

    1999-07-01

    Fixed-dose combination antihypertensive therapy has received interest since the publication of the JNC-VI report. Relatively few head-to-head comparative studies between fixed-dose combinations and first-line monotherapies for hypertension have been published. The objective of this study was to conduct a meta-analysis of various first-line monotherapies and the fixed-dose combination of amlodipine/benazepril. The results of the meta-analysis were used to compare the efficacy and safety of the first-line monotherapies with amlodipine/benazepril. The meta-analysis included 82 studies that included 110 treatment groups (cohorts). The study compared nine different monotherapies and one combination therapy (amlodipine/benazepril). Of the 82 studies, 22 were placebo-controlled and 60 were active treatment controlled. The mean absolute decrease in supine diastolic blood pressure (BP) ranged from 9.7 to 13.3 mm Hg with verapamil showing the greatest effect and captopril the least (13.3 +/- 3.0 mm Hg; 9.7 +/- 2.9 mm Hg, respectively). When studies were weighted by sample size, atenolol, verapamil, lisinopril and amlodipine/benazepril showed the greatest BP effect. When studies were weighted by variance, amlodipine/benazepril and atenolol showed the greatest BP effect. The percentage of patients controlled on therapy ranged from 54% to 79%. Lisinopril and amlodipine/benazepril showed the greatest percent controlled. The overall incidence of adverse effects ranged from 12.1% to 41.8% with lisinopril having the lowest and nifedipine having the highest incidence. The overall incidence of adverse effects resulting in drug discontinuance ranged from 1.3% to 10.7%, with amlodipine/benazepril having the lowest and nifedipine having the highest incidence. The results of the meta-analysis indicate that amlodipine/benazepril produces above average reductions in BP with a lower than average incidence of overall side effects and the lowest incidence of adverse effects resulting in drug

  1. Análise da prescrição de medicamentos de pacientes hipertensos atendidos pelo SUS da rede municipal de saúde de Rincão – SP

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    L. L. Veronez

    2009-01-01

    Full Text Available

    O estudo foi desenvolvido com o objetivo de identificar os principais fármacos utilizados no tratamento de hipertensão no Centro de Saúde da cidade de Rincão e as principais interações medicamentosas decorrentes das associações, incluindo não só os medicamentos anti-hipertensivos, mas também, aqueles mais utilizados em conjunto. A população estudada compreendeu 725 pacientes hipertensos cadastrados no Centro Municipal de Saúde e que faziam acompanhamento médico trimestral. Foram coletados dados sobre a idade, sexo, presença de diabetes, tabagismo, sedentarismo e sobrepeso para traçar um perfil da população hipertensa. Todos tinham fichas de controle na farmácia da unidade, onde retiravam os medicamentos mensalmente. O paciente, na sua maioria, constituiu de mulheres (62% com idade entre 50 a 70 anos (57%; 21%, eram tabagistas; 43% sedentários. Quanto às prescrições, 33% eram constituídas de monoterapia e 66% de politerapia. Quanto à utilização de medicamentos de outras classes terapêuticas, além dos antihipertensivos, 50% dos pacientes faziam uso e dentre estes, 34% utilizam três ou mais medicamentos anti-hipertensivos, enquanto 66% utilizavam apenas, dois medicamentos anti-hipertensivos e 47% das prescrições apresentaram interações medicamentosas. O captopril foi o medicamento que mais apresentou interações com outros medicamentos representando 54% das interações medicamentosas, a hidroclorotiazida apresentou 27%, seguido da furosemida, com 14%, o propranolol, 4% e a nifedipina, 1%. Concluiuse que o consumo de medicamentos pelos pacientes é elevado e consequentemente apresentaram também um elevado número de interações medicamentosas. Palavras chaves: prescrição de medicamentos; SUS; farmacoepidemiologia, interação medicamentos; hipertensão arterial.

  2. 拉曼光谱快速鉴别品牌药与仿制药的研究%Rapid Screening of the branded and generic drugs by Raman Spectroscopy

    Institute of Scientific and Technical Information of China (English)

    陈辉; 王晓钰; 李丹; 陆峰; 褚克丹

    2015-01-01

    In this paper, Raman spectroscopy in combination with Random forest method were used to distinguish the differences between the same drugs of different manufacturers efficiently. The captopril tablets were used as the experimental samples, and one of them was branded version, the others were generic drug manufacturers. Additionally, the pretreatment methods of spectra wavelength range cutting, smoothing, and baseline correcting, mean-centralizing and so on. After optimization of parameters, the prediction model was established by method of Principal component analysis (PCA) and Random forests (RF). The results show that PCA cannot differentiate the branded version and six generic drug manufacturers, while the RF characterized the differences very well. So one can draw a conclusion that the application of RF can make a great contribution to Raman spectroscopy for the drug fast screening efficiently and accurately.%本文用拉曼光谱结合随机森林法很好的区分了相同药品不同厂家之间差异,为拉曼光谱用于快速区分仿制药和品牌药奠定基础。选用了1个品牌药厂家和6个仿制药厂家生产的卡托普利片作为实验研究对象,经过截取拉曼波长范围、光谱平滑、背景扣除、中心化等预处理,优化参数后,用随机森林法和主成分分析投影判别分别建立分析模型。计算结果表明:随机森林法所建立的分类模型可以区分卡托普利片的品牌药与仿制药厂家间的差异性,结果优于的主成分分析降维后不同主成分数下的投影判别分析效果。因此结合随机森林法能为拉曼光谱在药品快检中的高效、快速、无损分析提供有力保障。

  3. Analysis on the Clinical Efficacy of Metoprolol for the Treatment of Early Acute Myocardial Infarction%美托洛尔用于急性心肌梗死早期的临床疗效分析

    Institute of Scientific and Technical Information of China (English)

    陈悦; 宋涛; 霍阳; 初巍巍

    2013-01-01

    Objective To discuss the effect of metoprolol for the treatment of early acute myocardial infarction. Methods From March,2010 to November 2011 ,98 patients in Liaoning Armed Police Corps Hospital with early acute myocardial infarction were randomly divided into trial group( 51 cases ) and control group( 47 cases ). The trial group was given metoproloK 12. 5-100mg ) combined with captopril,2 times per day taken orally; and the control group was given captopriK 2. 5-20 mg ),2 times per day taken orally. The other methods were the same in the two groups. After the treatment, the curative effects were compared statistically between the two groups. Results The survival rate and left ventricular remodeling delaying of the trial group was apparently higher than the control group With statistically significant difference( P <0. 05 ). Conclusion Metoprolol as the treatment of the patients with early acute myocardial infarction can significantly reduce the mortality and delay the ventricular remodeling, which is of great clinical significance.%目的 探讨美托洛尔用于急性心肌梗死早期的临床疗效.方法 选取2010年3月至2011年11月因急性心肌梗死而在武警辽宁省总队医院进行治疗的患者98例,随机分为试验组(51例)和对照组(47例),对照组患者心肌梗死早期给予卡托普利2.5 ~20 mg,每日2次,口服;试验组在对照组治疗的基础上加入美托洛尔12.5 ~100 mg,每日2次,口服.两组患者的其他治疗方法相同,统计分析两组治疗方法的临床效果.结果 试验组患者的生存率及左心室重构延缓的程度明显高于对照组,比较差异有统计学意义(均P<0.05).结论 将美托洛尔应用于心肌梗死早期患者能够显著降低患者病死率,同时能延缓心室重构,临床意义重大.

  4. Clinical Study on the Real-time Efficacy of Balance Acupuncture in Treating Primary Hypertension%平衡针治疗原发性高血压即刻疗效的临床研究

    Institute of Scientific and Technical Information of China (English)

    徐国峰; 余惠萍; 李敏

    2015-01-01

    Objective To observe the real-time efficacy of balance acupuncture in treating primary hypertension. Method Totally 160 patients with primary hypertension were randomized into a treatment group and a control group, 80 in each group. The treatment group was intervened by balance acupuncture, while the control group was by oral administration of Captopril. The blood pressure and symptom score were observed before and after intervention. Result There were no significant differences in comparing the total effective rate at different time points between the two groups (P>0.05). There was a significant difference in comparing the headache score in male patients at 30 min after treatment between the two groups (P<0.05). Conclusion Balance acupuncture is an effective method in treating primary hypertension, and can release headache of the patients.%目的:观察平衡针治疗原发性高血压的即刻疗效。方法将160例原发性高血压患者随机分为治疗组和对照组,每组80例。治疗组采用平衡针治疗,对照组采用口服卡托普利治疗。观察两组治疗前后血压及症状积分变化。结果两组患者各时段总有效率比较,差异均无统计学意义(P>0.05)。治疗组男性患者治疗后30 min 头痛积分与对照组男性患者比较,差异具有统计学意义(P<0.05)。结论平衡针是一种治疗原发性高血压的有效方法,并能缓解患者头痛症状。

  5. Fatores associados à adesão ao tratamento antihipertensivo por idosos na atenção primária

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    Lorena Flor da Rosa Santos Silva

    2014-04-01

    Full Text Available A adesão ao tratamento anti-hipertensivo é fundamental para o manejo dos pacientes portadores de hipertensão arterial, o que contribui para a redução da morbimortalidade por esta enfermidade. Desta forma, este estudo teve como objetivo determinar a adesão ao tratamento anti-hipertensivo e fatores associados em idosos hipertensos cadastrados em uma Unidade de Saúde da Família, Londrina-PR. Desenvolveu-se um estudo transversal com idosos (60 anos ou mais, selecionados a partir do Sistema de Informação da Atenção Básica. As variáveis de interesse (socioeconômicas e demográficas, hábitos de vida, acesso aos serviços de saúde e adesão ao tratamento medicamentoso foram obtidas pela aplicação de um formulário semiestruturado através de um inquérito domiciliar. A adesão foi avaliada por meio do Teste de Morisky-Green e o controle pressórico. Dos 117 idosos investigados, 54,7% foram identificados como aderentes ao tratamento anti-hipertensivo e 61,4% apresentaram pressão arterial controlada. A média de medicamentos anti-hipertensivos utilizados foi de 1,97, destacando-se hidroclorotiazida (30,8%, enalapril (24,8% e captopril (14,5%. A adesão ao tratamento farmacológico apresentou-se associada ao sexo feminino (61,8%; p<0,05 e a idade entre 60 e 79 anos (67,9%; p<0,01. O controle pressórico mostrou-se associado à menor escolaridade (75,6%; p<0,05 e não possuir trabalho remunerado (69,4%; p<0,02. Os resultados observados indicam moderada adesão ao tratamento anti-hipertensivo e ao controle pressórico. Além disso, detectou-se que as variáveis socioeconômicas e demográficas mostraram-se mais fortemente associadas à adesão e controle pressórico.

  6. Estudio de las fracciones lipídicas de colesterol y triglicéridos en pacientes de dos consultorios médicos de la familia

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    José Luis Cusidó Carralero

    2014-11-01

    Full Text Available La segunda causa de muerte en la provincia de Las Tunas son las enfermedades del corazón, estas se asocian a múltiples factores de riesgo, como, por ejemplo, los niveles elevados de colesterol y triglicéridos. La alta frecuencia de valores patológicos de colesterol y triglicéridos en pacientes de los Consultorios Médicos de la Familia (CMF 19-01 y 20-01 en el Policlínico Docente “Manuel Fajardo Rivero” motivó a la realización de este trabajo, que tiene como objetivo evaluar el comportamiento de las fracciones lipídicas de colesterol y triglicéridos en pacientes de estos CMF, durante el período comprendido entre enero y junio de 2014. Las variables analizadas fueron: rango de valores de colesterol y triglicéridos, edad, sexo, antecedentes patológicos personales, diagnóstico clínico y tratamiento médico. Se incluyeron los pacientes mayores de 20 años de ambos consultorios, los diabéticos, hipertensos, cardiópatas; se excluyeron de la investigación las gestantes, enfermos hospitalizados o con ingreso domiciliario. Se obtuvo como resultado que casi la mitad de los pacientes presentó valores elevados en las fracciones lipídicas de colesterol y triglicéridos, las edades más afectadas fueron los adultos de 41 a 60 años, con predominio del sexo masculino. En la revisión de historias clínicas se tabularon como principales antecedentes patológicos personales que más de la mitad de los pacientes con alteraciones lipídicas son fumadores y un cuarto de ellos consumen alcohol. En el diagnóstico clínico y tratamiento médico registrado en la historia clínica de los pacientes afectados se constató que dos tercios de ellos son hipertensos y utilizan el captopril, enalapril y atenolol y casi un tercio son diabéticos, que se medican con los hipoglucemiantes, insulina y glibenclamida

  7. Study on The Protective Effects and Its Mechanism of Rutin on Experimental Diabetic Nephropathy Rat%芦丁对糖尿病肾病大鼠的保护作用及其机制探讨

    Institute of Scientific and Technical Information of China (English)

    王素琴; 汤玲君; 王艳

    2012-01-01

    Objective To study rutin's preventive and therapeutic effects on early stage of diabetic nephropathy (DN) in rats. Methods The DN rats model was established by intraperitoneal injection of streptozotocin. Then rats were randomly divied 6 groups: normal group(NS) , DN model group, low dose of rutin group (RL, lOmg/kg) , moderate dose of rutin group (RM, 30mg/kg) , high dose of rutin group (RH, 90mg/kg) , and captopril group (CAP, lOmg/kg). Every group was housed in a SPF environment suitable for breeding specific pathogen -free grade animals for 12 weeks, and they were allowed free access to food and water. Finally the leves of blood glucose (Glu) , urine protein, creatinine (Cr) and blood urea nitrogen (BUN) were detected. Renal morphological changes were observed by HE dyeing method. Results The Glu, 24h urine protein,kidney index, BUN, Cr and glomerular morphology of DN rat were all improved significantly after being administrated rutin. Conclusion Rutin has the protective effects on early stage of diabetic nephropathy (DN) in rats.%目的 研究芦丁对糖尿病肾病(diabetic nephropathy,DN)大鼠的保护作用.方法 采用腹腔注射链脲霉素(streptozotocin,STZ)的方法复制DN大鼠模型,分为正常组(NS组),DN模型组(DN组)、芦丁低剂量治疗组(RL组,10mg/kg)、芦丁中剂量治疗组(RM组,30mg/kg)、芦丁高剂量治疗组(RH组,90mg/kg)、卡托普利对照组(CAP组,剂量为10mg/kg),每组10只,灌胃给药,12周后测定空腹血糖、尿白蛋白、肾脏指数、尿素氮、肌酐、观察肾脏组织形态学改变.结果 芦丁能明显改善糖尿病肾病模型大鼠的血糖(Glu)、24h尿白蛋白、肾脏指数、尿素氮、肌酐以及肾小球组织形态.结论 芦丁对糖尿病肾病大鼠具有好的保护作用.

  8. 芝麻素对自发性高血压大鼠心肌氧化应激损伤的保护作用%Effect of sesamin on the protein iNOS and c-fos expression in myocardia of spontaneously hypertensive rats

    Institute of Scientific and Technical Information of China (English)

    李伟; 杨解人; 李文星; 张俊秀; 唐丽娟; 杨慧; 熊莺

    2015-01-01

    目的:观察芝麻素对自发性高血压大鼠( spontaneously hypertensive rat ,SHR)心肌iNOS和c-fos蛋白表达来探讨其可能保护机制。方法:SHR 35只,随机分为SHR模型组、芝麻素[40、80、160 mg/(kg· d)]组、卡托普利[30 mg/(kg· d)]组及WKY阴性组,每天灌胃给药1次,连续16周。末次给药后,称体质量,HE染色观察心肌病理变化;化学比色法测心肌组织中T-SOD的含量;免疫组化法检测心肌诱导型一氧化氮合酶( inducible nitric oxide synthase ,iNOS)和原癌基因( cellular oncogene fos,c-fos)阳性蛋白表达。结果:SHR组心肌细胞增生肥大且排列紊乱,组织中可见大量炎性细胞和脂肪组织浸润,心肌T-SOD的含量明显减少( P<0.01),心肌iNOS和c-fos蛋白表达显著增加( P<0.01),芝麻素和卡托普利组上述病理变化则有不同程度的改善;心肌T-SOD明显增加( P<0.01), iNOS和c-fos蛋白表达明显下调( P<0.01)。结论:芝麻素具有下调SHR心肌iNOS和c-fos蛋白表达,增强T-SOD能力,保护心肌损伤的作用。%Objective:To observe the effects of sesamin on the protein iNOS and c-fos expression in myocardia of spontaneously hypertensive rats( SHR) , and explore the potential protective mechanisms.Methods:Thirty-five SHRs were randomly divided into group of SHR model ,sesamin treatment in diverse dosage[40 ,80 and 160 mg/(kg · d)]and captopril intervention [30 mg/(kg· d)],and 7 Wistar-Kyoto rats(WKY) were included as negative controls. All rats were intragastrically administrated with the drugs once a day for consecutive 16 weeks.After the final intervention,the body weight (BW) was measured,and histopathological changes of the myocardia were observed by HE staining.Colorimetric analysis was performed to measure the contents of myocardial T-SOD,and immunohitochemical method was used to determine the expression of inducible nitric oxide

  9. Hipertensão arterial sistêmica no setor de emergência: o uso de medicamentos sintomáticos como alternativa de tratamento Systemic hypertension at emergency units: the use of symptomatic drugs as choice for management

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    Sandro Gonçalves de Lima

    2005-08-01

    Full Text Available OBJETIVO: Comparar a resposta terapêutica dos pacientes atendidos no Setor de Emergência com sintomas e pressão arterial (PA elevada, ao tratamento com medicação sintomática ou anti-hipertensiva. MÉTODOS: Ensaio clínico randomizado, cego, envolvendo 100 pacientes atendidos na Emergência Cardiológica do Hospital Universitário Oswaldo Cruz com sintomas associados à pressão arterial sistólica (PAS entre 180 e 200 mmHg e/ou pressão arterial diastólica (PAD entre 110 e 120 mmHg. Os pacientes foram randomizados para tratamento com medicação sintomática (dipirona ou diazepam ou anti-hipertensiva (captopril. Aqueles portadores de qualquer condição clínica associada, que necessitassem de tratamento imediato na Unidade de Emergência, foram excluídos do estudo. Atingiram o critério de alta os pacientes que, ao final do período de observação de noventa minutos, tornaram-se assintomáticos e tiveram seus níveis tensionais sistólicos reduzidos para abaixo de 180 mmHg e diastólicos para aquém de 110 mmHg. RESULTADOS: A idade média da população estudada foi 54,4 anos. A maioria dos pacientes era do sexo feminino, hipertensos crônicos em tratamento farmacológico irregular, com baixa taxa de aderência às medidas não farmacológicas e classificados quanto ao índice de massa corpórea (IMC, em sobrepeso e obesos grau I. Cefaléia, dor torácica tipo D (não anginosa e dispnéia foram as queixas mais freqüentes. A proporção de pacientes tratados com medicação sintomática que atingiu o critério de alta foi semelhante àquela de pacientes medicados com anti-hipertensivo (p=0,165. Não foi encontrada associação entre o diagnóstico prévio de hipertensão arterial sistêmica (HAS (p=0,192, tratamento farmacológico (p=0,687 e não-farmacológico e o critério de alta. CONCLUSÃO: Uma maior proporção (não significativa de pacientes tratados com medicação sintomática obtiveram redução da PA aquém dos n

  10. A propósito de un caso: ¿Sirven los genéricos para moderar el gasto en hipertensión? Apropos of a case: do generic drugs help control expenditure on hypertension?

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    Antonio J. García

    2004-04-01

    Full Text Available Objetivo: Se analiza desde la perspectiva del pagador (Sistema Nacional de Salud [SNS] la influencia que tienen los genéricos en el gasto en medicamentos en la hipertensión arterial, examinándose el subgrupo terapéutico de mayor consumo y utilización, los inhibidores de la enzima de conversión de la angiotensina (IECA y antagonistas de los receptores de la angiotensina II (ARA II. Métodos: Partiendo de los datos de facturación al SNS de todas las oficinas de farmacia del Área de Salud de Málaga, se explora el consumo (envases y gasto de los fármacos IECA, IECA + especialidades farmacéuticas genéricas (EFG y ARA II, desde 1999 hasta 2002, así como el precio medio (ponderando según ventas y el porcentaje de desviación de prescripción de un grupo a otro. Resultados: El incremento en envases del subgrupo C09 fue del 20,79%, muy superior para los ARA II (136% y los IECA + EFG (177%. El gasto total creció en más del 42%. Se redujo el gusto en IECA en casi el 7%, a pesar del incremento en gasto de los IECA + EFG, mientras que los ARA II lo aumentaron en más del 154%. El precio medio ponderado según las ventas de este subgrupo terapéutico se incrementó en cerca del 18%. Se produjo un descenso en el precio medio ponderado de los principios activos donde había EFG (captopril y enalapril además de otros (trandolapril, pero entre los ARA II destaca el aumento en el precio medio ponderado según las ventas de irbesartán (9% y valsartán (16%. Conclusiones: Los genéricos usados han originado una disminución en el gasto de IECA y del precio medio ponderado del subgrupo. Pero a pesar del incesante aumento en el consumo de las especialidades farmacéuticas genéricas, no se ha producido el efecto ahorrador pretendido con este tipo de medicamentos por el Ministerio de Sanidad y Consumo. Se apunta como posible causa la desviación de las prescripciones hacia los medicamentos no afectados de sustitución por parte de la oficina de

  11. Diuréticos melhoram a capacidade funcional em pacientes com insuficiência cardíaca congestiva

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    Eterno Francesca Tadeu

    1998-01-01

    Full Text Available OBJETIVO: Quantificar a influência do diurético na capacidade funcional em portadores de insuficiência cardíaca congestiva (ICC descompensada, através do teste de caminhada. MÉTODOS: Estudamos 10 pacientes internados, com idade média de 47 anos, sendo cinco do sexo masculino, com ICC descompensada, em classe funcional III e IV (NYHA, submetidos ao teste de caminhada de 6 e 9min na admissão e alta. Foram obtidos registros na admissão e alta, do peso, do ecocardiograma, sódio, potássio, uréia, creatinina séricos, hematócrito e hemoglobina. O tratamento instituído foi o aumento da dose prévia de furosemida EV e/ou VO, associado ou não a diurético tiazídico, tendo sido mantidas as doses prévias de digital, captopril ou da associação de nitrato e hidralazina. RESULTADOS: O período de compensação variou entre 4 a 30 dias (média 8,7±7,8 dias. Ao ecocardiograma bidimensional apresentaram diâmetro do ventrículo esquerdo que variou de 47 a 81mm e a fração de ejeção de 0,26 a 0,74. A distância caminhada em 6min passou de 193,4±71,5m para 341,8±67,7m (p<0,00002 e em 9min passou de 268,1±119,6m para 518,0±114,8m (p<0,00005 . Não houve diferença estatística entre os valores, na admissão e alta, do hematócrito, hemoglobina, uréia, creatinina e sódio. O potássio sérico médio à admissão era de 4,0±0,91mEq/l e na alta 4,69±1,00mEq/l (p= 0,01 e o peso dos pacientes na admissão e na alta foi de 58,9±6,42kg para 52,9±5,31kg, respectivamente (p<0,0006 . CONCLUSÃO: A compensação da ICC com o uso de diurético induziu a uma melhora importante, a curto prazo, da capacidade física dos pacientes, demonstrada pelo aumento da distância caminhada em 6 e 9min. O diurético melhorou significativamente o desempenho físico.

  12. 黄芪多糖对压力超负荷诱导的大鼠心肌肥大的影响%Effect of Astragalus polysaccharides on cardiac hypertrophy induced by pressure overload in rat

    Institute of Scientific and Technical Information of China (English)

    李素娟; 吴伟平; 李杰锋; 张贵平; 魏毅; 宜全; 罗健东; 刘英华

    2012-01-01

    目的:探讨黄芪多糖(astragalus polysaccharides,APS)对压力超负荷所致大鼠心肌肥大的抑制作用.方法:SD大鼠随机分为5组:假手术手组、模型组、APS低剂量组(AP1)、APS高剂量组(AP2)和卡托普利组.给药8周后,分别进行心脏超声和HE染色检测心脏肥大指数及形态学改变.结果:超声检测发现,与假手术组相比,模型组左右心室质量比明显增加,舒张期左心室容量、左心室射血分数和左心室短轴缩短速率均明显降低;AP2组与模型组相比,以上指标均有显著性改善,而AP1组和模型组比较无明显差异.HE染色显示,模型组肌细胞排列疏松、肥大,AP1组和AP2组细胞排列整齐,有少量肥大细胞夹杂.结论:高剂量APS对压力超负荷大鼠的心肌肥大有明显保护作用.%Objective To investigate the inhibition of the astragalus polysaccharides (APS) on cardiac hypertrophy induced by pressure overload in rat. Methods 60 SD rats were randomly divided into 5 groups:Sham, Model, Captopril, low-dose APS and high-dose APS group. All these drugs were administrated for 8 weeks respectively. Echocardiography and cardiac hypertrophy index were detected respectively for the heart function, HE staining was detected to observe the cardiac morphology. Results Echocardiography showed that compared with the sham group, left and right ventricular mass ratio (LVM/RVM) of the model group significantly increased, diastolic left ventricular volume (LV Vol, d), left ventricular ejection fraction (EF) and left ventricular fractional shortening rate (FS) of the model group decreased significantly. While comparing with the model group, the indexes of the above in APS group significantly improved. HE staining showed that myocardial cells became hypertrophic and arranged loosely in model group, while the myocardial cells in AP2 group arranged in order, and the hypertrophy cells obviously decreased. But there was no significant difference between the API and

  13. 干预高血压、高血脂、高黏滞血症对心脑血管疾患发生率的影响%Impact of intervened hypertension,hyperlipemia ,hyperviscosity syndrome in incidence of card-iovascular and cerebrovascular diseases

    Institute of Scientific and Technical Information of China (English)

    王建文; 王清; 徐培清

    2002-01-01

    Background:According to American Heart Association's report,death composition of cerebrovascular and cerebrovascular disease was increased to 29% in 1996,and now 33% from 25% in 1992.Now,atherosclerosis seriously endanger human's health.Hypertension,hyperlipemia and hyperviscosity syndrome are main risk factors of cardiovascular and cerebrovascular diseases.There conditions often existed simultaneously in elders.Intervention to these diseases can prevent cardiovascular and cerebrovascular events,which is feasible. Objective:To investigate impact of hypertension,hyperlipemia and hyperviscosity syndrome on incidence of cardiovascular and cereborvascular events. Design:Random,controlled study. Unit:Department of Senile Diseases, Qianfoshan Hospital of Shandong. Subjects:In study group, 52 senile subjects with complete hospitalizing data were recruited from 1995~ 2000.Patients with hypertension,hyperlipemia ,hyperviscosity syndrome were included in the current study.13 subjects asked medical help due to hypertension,25 due to hyperlipemia and 14 due to hyperviscosity syndrome.Sometimes blood pressure of hypertension patients was 140~ 160/90~ 100 mmHg.Patients' mean age was 65.21.Ratio of male to female was 13:1.In control group,50 outpatients were included who had similar diseases those in study group.Mean age was 62.34 and ratio of male to female was 17.33:1. Intervention:In study group,calcium antagonist such as adalatcc, nitrendipine, plendil and/or ASCE inhibitor such as perindopril and captopril were given o.s.Blood pressure was con trolled to normal level.Blood lipid regulating drugs such as pravastatin, ticlopidine,and lipanthy were given for hyperlipemia patients.For patients with hyperviscosity syndrome,enteral aspirin or persantine was given,50~ 75 mg/day.Interval of drugs was 1 day to 2 months.Detailed data was unavailable.Red sage root or its compound form injecto was given i.v.,70 mg/day,pueraria root was given i.v.300~ 500 mg

  14. 酚妥拉明与ACEI联用方案治疗婴幼儿重症肺炎合并心力衰竭的临床研究%The clinical research of phentolamine associated with ACEI program in the treatment of infants with severe pneumonia & nbsp;complicated by heart failure

    Institute of Scientific and Technical Information of China (English)

    陆露

    2013-01-01

      目的分析探讨酚妥拉明联合血管紧张素转换酶抑制剂(ACEI)在治疗婴幼儿重症肺炎合并心力衰竭方面的临床效果.方法选取2009年4月-2012年5月间在我院住院治疗的70例重症肺炎合并心力衰竭患儿,将其分为观察组和对照组各35例.对照组采用常规治疗措施,观察组在对照组基础上加用酚妥拉明与血管紧张素转换酶抑制剂卡托普利,比较两组的临床疗效.结果观察组用药24h后总有效率为91.4%,高于对照组的80.0%,组间差异有统计学意义(P <0.05);观察组患儿心衰纠正时间、症状缓解时间、肺部音消失时间以及总的住院时间均明显短于对照组患儿(P <0.05).结论酚妥拉明联合ACEI在治疗婴幼儿重症肺炎合并心力衰竭方面疗效显著,患儿心衰症状改善明显,值得临床推广.%Objective To analyze and explore the clinical effect of phentolamine combined with angiotensin-converting enzyme inhibitors(ACEI) in the treatment of infants with severe pneumonia complicated by heart failure. Methods 70 patients with severe pneumonia complicated by heart failure in children hospitalized in our hospital from April 2011 to May 2012 were chosen, and they were divided into the observation group and the control group. The control group of 35 cases was taken with conventional treatment. The observation group of 35 cases was taken with phentolamine and angiotensin-converting enzyme inhibitor captopril on the basis of the control group. The clinical efficacy of the two groups was compared. Results The total effective rate of children with drug treatment after 24h of the observation group was 91.4%, while the total effective rate of the treatment in the control group was 80.0%. The statistics showed that the total efficiency rate in the two groups of patients were with statistically significant differences(P <0.05). The correct time, remission time, pulmonary disappeared time and total hospitalization

  15. 妊娠期高血压疾病药物降压治疗的临床安全性及有效性分析%Antihypertensive therapyin pregnancy induced hypertension clinical safety and effectiveness

    Institute of Scientific and Technical Information of China (English)

    谢秀媚

    2012-01-01

    目的 分析妊娠期高血压疾病的临床表现以及治疗方法,探讨降压药物在妊高症中应用的安全性及有效性.方法 我院收治的134例妊高症患者作为观察组,酌情给予肼苯哒嗪、利血平、硝苯地平、卡托普利等药物进行降压治疗,选择同期我院分娩的正常产妇134例作为对照组.分析对比两组的凝血功能、产后出血、胎盘早剥、以及有无发生妊高症心脏病等并发症.结果 观察组患者出现凝血功能异常、胎盘早剥、妊高症心脏病以及产后出血的患者分别为9.7%、12.69%、8.21%、8.96%,均多于对照组的1.49%、2.24%、0、1.49%(P< 0.01).结论 妊高症常导致患者出现各种不良并发症,影响母婴健康,降压治疗能够有效地减少并发症的发生,改善患者的生活质量.%Objective Analysis of clinical manifestation and treatment of pregnancy induced hypertension,study of antihypertensive drugs in pregnancyinduced hypertension in the application of safety and effectiveness.Methods 134 patients with pregnancy induced hypertension in our hospital as an observer group,granting hydralazine,reserpine,nifedipine,captopril drug blood pressure treatment,select normal maternal in our hospital childbirth over the same period as the control group.Analysis and comparison of two groups of blood coagulation,postpartum hemorrhage,placental abruption,and there are no complications of pregnancy-induced hypertension patients with heart disease.Results Observer Group in patients with dysfunction of blood coagulation,Placental Abruption,patients with pregnancy-induced hypertension heart disease and patients with postpartum hemorrhage are 9.7%,12.69%,8.21%,8.96%,more than the control group 1.49%,2.24%,0,1.49%,a statistically significant(P < 0.05).Conclusion Complications in patients with pregnancy induced hypertension Syndrome often results in a variety of adverse affect maternal and child health

  16. Simultaneous determination of erdosteine and its active metabolite in human plasma by liquid chromatography-tandem mass spectrometry with pre-column derivatization%柱前衍生化LC-MS/MS法同时测定人血浆中厄多司坦及其活性代谢物

    Institute of Scientific and Technical Information of China (English)

    金经; 陈笑艳; 张逸凡; 马智宇; 钟大放

    2013-01-01

    建立快速、灵敏、准确的柱前衍生化液相色谱-串联质谱(LC-MS/MS)法同时测定人血浆中厄多司坦及其含巯基活性代谢物,并将其应用于厄多司坦片人体药动学研究.厄多司坦及其活性代谢物分别以对乙酰氨基酚和卡托普利为内标.100.L血浆样品经2-溴-3'-甲氧基苯乙酮衍生化处理后以甲醇(含0.1%甲酸)-5 mmol·L-1醋酸铵(含0.1%甲酸)为流动相梯度洗脱,Agilent XDB-C18色谱柱(50 mm×4.6 mm ID,1.8 μm)分离.采用电喷雾电离源,多反应监测方式进行正离子检测.测定人血浆中厄多司坦及其活性代谢物的标准曲线线性范围分别为5~3 000 ng·mL-1和5~10 000 ng·mL-1,定量下限均为5.00 ng·mL-1.厄多司坦片人体药动学研究发现,含巯基活性代谢物曲线下面积(AUC)是原形药物的6.2倍,平均滞留时间(MRT)为(7.51±0.788)h,为合理制订给药方案提供了药动学依据.%A sensitive, rapid and accurate liquid chromatography-tandem mass spectrometric (LC-MS/MS) method with pre-column derivatization was developed for the simultaneous determination of erdosteine and its thiol-containing active metabolite in human plasma. Paracetamol and captopril were chosen as the internal standard of erdosteine and its active metabolite, respectively. Aliquots of 100 μL plasma sample were derivatized by 2-bromine-3'-methoxy acetophenone, then separated on an Agilent XDB-C 18 (50 mm × 4.6 mm ID, 1.8 μm) column using 0.1% formic acid methanol - 0.1% formic acid 5 mmol·L-1 ammonium acetate as mobile phase, in a gradient mode. Detection of erdosteine and its active metabolite were achieved by ESI MS/MS in the positive ion mode. The linear calibration curves for erdosteine and its active metabolite were obtained in the concentration ranges of 5-3 000 ng·mL-1 and 5-10 000 ng·mL-1, respectively. The lower limit of quantification of erdosteine and its active metabolite were both 5.00 ng·mL-1. The pharmacokinetic results of

  17. 化学药片剂生产设备清洁方法的验证%Verification for Chemical Medicine Tablet Production Equipment Cleaning Method

    Institute of Scientific and Technical Information of China (English)

    柴振平; 高鹏; 白亚灵; 何丽娟; 任文学; 黄占周; 李杰

    2015-01-01

    目的:评价化学药片剂生产设备清洁规程的合理性与有效性。方法:选择存在相似生产工艺的几种化学药——琥珀酸美托洛尔缓释片、卡托普利片、单硝酸异山梨酯片、盐酸二甲双胍片中毒性最强的琥珀酸美托洛尔缓释片为验证品种,对其生产设备按清洁规程进行清洁消毒,用棉签擦拭法对最难清洁点进行擦拭取样,验证其擦拭回收率、残留限度的检出限和定量限,评价其结果是否符合规定的限度。结果:经采用棉签擦拭法对最难清洁点进行擦拭取样、检测,结果各取样点均未见可见异物,产品残留量均<29.75μg/棉签、微生物限度均<50 CFU/棉签,各检测项目均符合对该药的规定标准。结论:该清洁方法能有效对生产设备进行清洁,防止产品污染和交叉污染,确保下批产品的质量、疗效和安全性。%OBJECTIVE:To evaluate the rationality and validity of chemical medicine tablet production equipment cleaning pro-cedure. METHODS:Among several chemical medicines prepared by similar production technology as Metoprolol succinate sus-tained-release tablets,Captopril tablets,Isosorbide mononitrate tablet and Metformin hydrochloride tablet,Metoprolol succinate sus-tained-release tablets had strongest toxicity and were included in validation test. The production equipment was cleaned and disinfect-ed according to cleaning procedure. The point which was most difficult to clean could be wiped and sampled by using the cotton swab method. The detection limit and the limit of quantitation of the residue limits were verified as well as the recovery rate of wip-ing,in order to evaluate whether the results meet the requirements. RESULTS:The cotton swab method is adopted to wipe sample and detect the point which is most difficult to clean. The visible foreign body has not been found in each sampling point. The amount of residual drug is <29.75 μg/cotton bud

  18. Evaluation of tablets splitting in NAH treatment for hypertensive patients in primary clinic unit%基层高血压NAH治疗方案片剂分剂量评价

    Institute of Scientific and Technical Information of China (English)

    刘元江; 缪经纬; 詹金陶; 刘其东

    2012-01-01

    AIM To evaluate accuracy and rationality of tablets splitting in nifedipine, atenolol, hydro-chlorothiazide and captopril ( NAH) treatment for hypertensive patients in primary clinical unit. METHODS Tablet cutter was utilized to split these pills into quarter or one eighth, and then European Pharmacopoeia (EP) and other standards was adopted to evaluate the accuracy of tablets spittin, expected weight (EW) and real wegtht (RW), mean weight loss percentage, and friability. RESULTS When these tablets split into quarter, they could not meet the accuracy subdivision of EP standards. There was significant difference when compared EW1/4 with RW1/4, such as nifedipine tablets produced by Xiangxue Pharmaceutical Company, atenolol tablets produced by Zhongyang Pharmaceutical Company or Wanraa Pharmaceutical Company, and hydrochlorothiazide tablets produced by Yunpeng Pharmaceutical Company. All tablets met the mean weight loss percentage ≤3%, however part of tablets could not meet the requirement of friability. When these tablets split into one eighth, they could not meet the accuracy subdivision of EP standards. There was significant difference when compared EW1/8 with RW^, such as nifedipine tablets produced by Xiangxue Pharmaceutical Company and atenolol tablets produced by Wanma Pharmaceutical Company. Meanwhile, mean weight loss percentage and friability could not meet the related regulation. CONCLUSION In the NAH treatment for hypertensive patients in primary clinical unit, the accuracy of tablets spitting and other indicators can not meet the requirements. It should be solved urgently to improve rational drug use.%目的 评价基层高血压硝苯地平、阿替洛尔、氢氯噻嗪和卡托普利(NAH)治疗方案片剂分剂量的准确性、合理性.方法 采用药片切割器对4种片剂四等分和(或)八等分,参照《欧洲药典》及相关参考文献评价分剂量准确性、期望重量(EW)与实际重量(RW)的比较、平均损失百分

  19. Detection of Illegally Added Chemicals in Antihypertensive Traditional Chinese Medicine Preparations and Health Products by UPLC-MS/MS%UPLC-MS/MS法检测降压类中药制剂及保健品中添加的化学药品

    Institute of Scientific and Technical Information of China (English)

    田兰; 张继春; 陈睿; 储忠英; 包综方

    2013-01-01

    Objective: To establish a specific method for the determination of seven chemicals in antihypertensive traditional Chinese medicine preparations and health products. Method: Nifedipine, atenolol, prazosin hydrochloride, reserpine, clonidine hydro-chloride, captopril and hydrochlorothiazide were determined and analyzed by UPLC-MS/MS. An ACQUITY BEH C18 analysis column (2.1 mm×50 mm ,1.7 μm ) was used with the mobile phase of 0. 1 % formic acid and methanol with gradient elution. The flow rate was 0. 3 ml·min-1 . EIS ion source was used with positive and negative ion monitoring. Result: The standard curves of the seven chemicals showed good linearity over the concentration range of 62.5-2 000.0,65.6-2 100.0, 16.6-530.0,34.5-2 210.0,67.1-2 146.0,33.7-2 159.0, 1 637.3-104 790.0 ng·ml-1 , respectively. The average recoveries of the seven chemicals were within 85. 1% and 106.7% . Conclusion: The method is specific, sensitive,simple and quick,and can be used to detect the seven chemicals in antihypertensive traditional Chinese medicine preparations and health products.%目的:建立降压类中药制剂及保健品中非法添加7种化学药品的检测方法.方法:采用超高效液相色谱-串联四级杆质谱,多反应监测(MRM)模式进行定性和定量检测.采用ACQUITY BEH C18色谱柱(2.1 mm×50 mm,1.7 μm),流动相为0.1%甲酸-甲醇梯度洗脱,流速为0.3 ml·min-1;离子源为ESI源,正负离子检测,对中成药及保健品中添加硝苯地平、阿替洛尔、盐酸哌唑嗪、利血平、盐酸可乐定、卡托普利、氢氯噻嗪进行定性、定量检测.结果:7种化学药品测定的线性范围分别为62.5~2 000.0,65.6~2 100.0,16.6~530.0,34.5~2 210.0,67.1~2 146.0,33.7~2 159.0,1 637.3~104 790.0 ng·ml-1,7种化学药品平均回收率在85.1%~106.7%之间.结论:本方法选择性强、灵敏度高、处理方法简单,测定快速,可用于降压类中成药及保健品中添加7种化学药品的测定.

  20. A assistência multidisciplinar e o manejo efetivo do Diabetes Mellitus: desafios atuais - doi:10.5020/18061230.2004.p200

    Directory of Open Access Journals (Sweden)

    Renan Magalhães Montenegro Junior

    2012-01-01

    Full Text Available O presente trabalho objetivou caracterizar o perfil clínico e o atendimento multidisciplinar da clientela diabética assistida no NAMI/UNIFOR, unidade que assiste a comunidade adstrita. Foi realizado um estudo retrospectivo, a partir de dados coletados dos prontuários de 101 pacientes com diagnóstico de diabetes mellitus (DM, selecionados aleatoriamente entre agosto de 2003 e junho de 2004. Todos os pacientes avaliados tinham diagnóstico de DM tipo 2, há 5,7 ± 3,9 anos, sendo 88,1% do sexo masculino e 11,9% do sexo feminino e com uma média de idade de 58,4 ± 12,2 anos. Desse total, 5,9% faziam uso de clorpropramida, 84,1% de glibenclamida, 15,8% de metformina, 7,9% de insulina, 1% de glipizida, 1% de glimepirida e 4,9% nunca fizeram uso de medicações para esse fim. Em 61,4% dos prontuários não havia registro de orientação dietética e, dos demais, 20,8% relatavam seguir as recomendações. Em 82,2% dos prontuários também não havia referência à realização de atividade física. Somente havia registro de glicemias de jejum (187±75 mg/dl, 192±80 mg/dl, 192±75 mg/dl, em três períodos distintos. Verificou-se que 72,3% pacientes eram também hipertensos e 56,4% dislipidêmicos. Dos hipertensos somente 62,4% estavam em tratamento medicamentoso e destes 45,5% faziam uso de inibidores de enzima conversora de angiotensina, sendo o captopril o mais usado. Apresentavam pressão arterial sistólica média de 148±26 mmHg e diastólica de 90±13 mmHg. Em nenhum caso houve menção ao uso de drogas hipolipemiantes e somente 9,9% desses usavam AAS. Esses dados sugerem que os pacientes diabéticos seguidos no NAMI apresentam elevada prevalência de condições mórbidas associadas, encontrando-se, em geral, com o controle metabólico inadequado e com terapêuticas passíveis de melhor adequação. Considerando os benefícios da atuação multidisciplinar no DM e das potencialidades do NAMI, observa-se a necessidade de adoção de novas

  1. 糖尿病合并高血压患者有效降压药物的选择%Selection of effective antihypertensive drugs in patients with diabetes mellitus complicated with hypertension

    Institute of Scientific and Technical Information of China (English)

    周蕾

    2016-01-01

    Objective:To explore the selection of effective antihypertensive drugs in patients with diabetes mellitus complicated with hypertension.Methods:273 cases of diabetic patients with hypertension were selected.We analyzed the use of antihypertensive drugs and the choice of methods.Results:In this study,48 cases(17.6%) took amlodipine besylate;32 cases(11.7%) took nifedipine sustained release tablets;24 cases(8.8%) took felodipine sustained-release tablets;28 patients(10.26%) took candesartan cilexetil;22 cases(8.06% ) took valsartan;15 cases(5.49% ) took irbesartan;20 patients(7.33% ) took enalapril;15 cases(5.49% ) took benazepril;17 cases(6.23%) took captopril;15 cases(5.49%) took indapamide;10 cases(3.66%) took furosemide;27 cases(9.89%) took metoprolol sustained-release tablets.The control of blood pressure in 273 cases was good.After treatment,the patient's systolic blood pressure was (127.4±6.9)mmHg,and diastolic blood pressure was (74.4±7.9)mmHg.Conclusion:The incidence of diabetes mellitus complicated with hypertension was higher,and the difference of different antihypertensive drugs was larger.In the treatment,the patients should adhere to the principle of individuation,pay attention to the dynamic monitoring of blood glucose and blood pressure,timely adjust the treatment plan,improve the clinical treatment effect,and reduce the occurrence of vascular events.%目的:探讨糖尿病合并高血压患者有效降压药物的选择方法。方法:收治糖尿病合并高血压患者273例,分析降压药物的使用情况及选择方法。结果:本次研究中,48例(17.6%)服用苯磺酸氨氯地平,32例(11.70%)服用硝苯地平缓释片,24例(8.8%)服用非洛地平缓释片,28例(10.26%)服用坎地沙坦酯,22例(8.06%)服用缬沙坦,15例(5.49%)服用厄贝沙坦,20例(7.33%)服用依那普利,15例(5.49%)使用贝那普利,17例(6.23%)服用卡托普利,15例(5.49%)服用吲达帕胺,10例(3.66%)服用呋塞米,27例(9

  2. 降压药物在老年高血压病人中的药学特点分析%Analysis of Pharmaceutic Characteristics of Antihypertensive Drugs in El-derly Patients with Hypertension

    Institute of Scientific and Technical Information of China (English)

    王禹

    2016-01-01

    Objective To discuss the pharmaceutic characteristics of antihypertensive drugs in elderly patients with hyper-tension. Methods 120 cases of elderly patients with hypertension admitted and treated in our hospital from January 2015 to January 2016 were selected, and the application types, adverse reactions and blood pressure standard situations of the pa-tients were observed and analyzed. Results In the 120 cases of patients, the blood pressure standard rates of 42 cases tak-ing valsartan, 29 cases taking captopril, 7 cases taking metoprolol, 25 cases taking amlodipine besylate tablets, 12 cases taking benazepril, 3 cases taking indapamide and 2 cases taking furosemide were respectively 78.57%, 72.42%, 71.43%, 68.00%, 66.67%, 66.67% and 50.00%, the standard rate of diastolic pressure of the 120 cases of patients was higher than that of systolic pressure, (85.00%vs 70.83%) and in this group, the incidence rate of adverse reactions caused by benazepril was the highest, which was 3.33%. Conclusion For elderly patients with hypertension, the hypotensive effect of hypotensive drugs for the diastolic pressure is better than that of hypotensive drugs for the systolic pressure, and we should timely adjust the drug dose according to the patient’s blood pressure level thus ensuring the curative effect and safety of medication.%目的:探讨降压药物在老年高血压病人中的药学特点。方法方便选择2015年1月—2016年1月该院收治的120例老年高血压病人,观察分析该组患者降压药物的应用类型、不良反应与血压达标情况。结果该组120例患者中服用缬沙坦42例血压达标率为78.57%、卡托普利72.42%、美托洛尔71.43%、络活喜68.00%、贝那普利66.67%、吲达帕胺66.67%、呋塞米50.00%。该组120例患者中舒张压达标率为85.00%,高于收缩压的70.83%。该组老年高血压用药所致不良反应中以贝那普利(33.33%)最高。结论降压药物对老年高血压病人舒张压的

  3. Application of Amlodipine Hypertension Diabetes that Benazepril Treatment Effect%高血压糖尿病应用氨氯地平贝那普利治疗的效果

    Institute of Scientific and Technical Information of China (English)

    张国权

    2016-01-01

    Objective To analysis of amlodipine in combination with that, the therapeutic effect of captopril treatment of high blood pressure, diabetes. Methods Adopt the method of randomized between January 2015 and January 2015 in our hospital for treatment of 100 patients with hypertension diabetes randomly divided into two groups, the observation group of 50 cases of patients, using a combination of two drugs. 50 patients with the control group, only with the simplex treatment, after treatment to observe the effect of the two groups of patients with high blood pressure step-down. Results After differ-ent ways of treatment, compared two groups of patients before treatment, the systolic and diastolic blood pressure dropped significantly, the difference statistically significant (P<0.05), to compare the effect of two groups of patients, found that the women in the observation group compared with control group, the blood pressure difference is more apparent, with statistical significance(P<0.05). Conclusion The application of the two drugs combination therapy in patients with high blood pressure, diabetes, to reduce the patient's blood pressure has good effect, is worth popularization in clinical.%目的:分析氨氯地平联合贝那普利治疗高血压糖尿病患者的治疗效果。方法采用随机分组的方法把2015年1月-2016年1月来该院接受治疗的100名高血压糖尿病患者随机分成两组,其中观察组患者50例,采用两种药物联合治疗。对照组患者50例,单纯采用贝那普利治疗,在治疗之后对两组患者的高血压降压效果进行观察。结果经过不同方式的治疗之后,两组患者对比治疗之前,其收缩压和舒张压都显著下降,差异有统计学意义(P<0.05),对两组患者的治疗效果进行比较,发现观察组的血压与对照组相比,差异有统计学意义(P<0.05)。结论对高血压糖尿病患者应用两种药物联合治疗,对于降低患者的血压具有

  4. 天钩降压胶囊对麻醉Beagle犬血压及血流动力学的影响%Effects of Tiangou Jiangya capsule on hypertension and hemodynamics in anaesthetized dogs

    Institute of Scientific and Technical Information of China (English)

    李玉洁; 杨庆; 翁小刚; 陈颖; 周淑媛; 李丹; 朱晓新

    2011-01-01

    Objective; To evaluate the effects of Tiangou Jiangya capsule on blood pressure and hemodynamics in anesthetized Beagle dogs. Method; Anesthetized dogs were divided into five groups; Tiangou Jiangya capsule 3-dose groups as 1. 6, 3. 2, 6. 4 g ? Kg-1, positive control group was giving captopril, negative control was giving 0.5% CMC-Na, duodenal administration. The blood pressure and hemodynamic changes were observed. Result: The systolic blood pressure of middle-dose Tiangou Jiangya capsule group was significantly reduced at 30 min after administration. The systolic blood pressure (SAP) and diastolic blood pressure ( DAP) of high-dose group of Tiangou Jiangya capsule was significantly reduced at 15 min to 90 min after administration. High-dose Tiangou Jiangya capsule can also significantly reduce cardiac work (LVW) and total peripheral resistance (TPR). Tiangou Jiangya capsule had no significant effect on the other hemodynamic parameters and myocardial oxygen consumption. Conclusion; Tiangou Jiangya capsule has a significant effect on reducing blood pressure, which is related to the reducing total peripheral resistance and reducing cardiac work. The result can provide a reference to further clarify the Tiangou Jiangya capsule mechanism on reducing blood pressure.%目的:评价天钩降压胶囊对麻醉Beagle犬血压及血流动力学的影响.方法:天钩降压胶囊设置1.6,3.2,6.4g·kg-13个剂量组(按生药计),以卡托普利为阳性对照药,0.5% CMC-Na为阴性对照药,十二指肠给药,观察麻醉犬血压及血流动力学的变化.结果:天钩降压胶囊中剂量组给药30 min后麻醉犬收缩压(SAP)明显降低,高剂量组给药后15 min SAP,舒张压(DAP)即明显降低,作用维持至给药后90 min.给予天钩降压胶囊高剂量能明显降低心脏做功(LVW)和总外周阻力(TPR).天钩降压胶囊对其他血流动力学指标及心肌耗氧量无明显影响.结论:天钩降压胶囊具有明显降压作用,

  5. 肺动脉高压心脏手术后发生肺高压危象的影响因素分析

    Institute of Scientific and Technical Information of China (English)

    陈艳玲; 陈光献; 唐白云

    2011-01-01

    目的 探讨影响肺动脉高压心脏手术后发生肺高压危象的因素.方法 对可能导致肺动脉高压心脏手术后发生肺高压危象的影响因素进行Logistic回归分析.结果 229例肺动脉高压心脏手术患者,术后发生肺高压危象26例,死亡6例,死亡率为23.08%.术前呼吸道感染、术前吸氧、术前使用卡托普利、手术时间、通气频率、再次插管和术后一氧化氮(nitrogen monoxidum,NO)吸入对肺动脉高压患者术后发生肺高压危象具有一定的影响(均P< 0.05).术前呼吸道感染、手术时间和再次插管为肺动脉高压手术后患者发生肺高压危象的危险因素;手术前吸氧、满足通气频率和NO吸入等为保护因素.结论 在对肺动脉高压心脏手术后患者的护理过程中,应尽量避免发生危险因素,以及加强保护因素的措施,对术后预防肺高压危象的发生具有重要的意义.%Objective To explore the influential factors of pulmonary hypertensive crisis after pulmonary artery hypertension cardiac operation. Method The influential factors of pulmonary hypertensive crisis after pulmonary artery hypertension cardiac operation were analyzed by Logistic regression. Results 229 patients undergoing pulmonary artery hypertension cardiac operation had 26 cases of postoperative pulmonary hypertensive crisis and 6 of them died, with a mortality of 23.08%. Such factors as preoperative infection of respiratory tract, preoperative oxygen inhalation, preoperative use of captopril, operation time, ventilation frequency, re-intubation and preoperative inhalation of nitrogen monoxidum were significant factors of pulmonary hypertensive crisis (all P < 0.05). The preoperative infection of respiratory tract, operation duration and re-intubation were the influential factors of pulmonary hypertensive crisis. Preoperative intermittent inhalation of oxygen, ventilation frequency and right treatment with nitrogen monoxidum were preventive

  6. Access to and use of high blood pressure medications in Brazil

    Science.gov (United States)

    Mengue, Sotero Serrate; Bertoldi, Andréa Dâmaso; Ramos, Luiz Roberto; Farias, Mareni Rocha; Oliveira, Maria Auxiliadora; Tavares, Noemia Urruth Leão; Arrais, Paulo Sergio Dourado; Luiza, Vera Lucia; Pizzol, Tatiane da Silva Dal

    2016-01-01

    ABSTRACT OBJECTIVE To analyze the access to and use of medicines for high blood pressure among the Brazilian population according to social and demographic conditions. METHODS Analysis of data from Pesquisa Nacional Sobre Acesso, Utilização e Promoção do Uso Racional de Medicamentos (PNAUM – National Survey on Access, Use and Promotion of Rational Use of Medicines), a nationwide cross-sectional, population-based study, with probability sampling, carried out between September 2013 and February 2014 in urban households in the five Brazilian regions. The study evaluated the access and use of medicines to treat people with high blood pressure. The independent variables were gender, age, socioeconomic status and Brazilian region. The study also described the most commonly used drugs and the percentage of people treated with one, two, three or more drugs. Point estimations and confidence intervals were calculated considering the sample weights and sample complex plan. RESULTS Prevalence of high blood pressure was 23.7% (95%CI 22.8–24.6). Regarding people with this condition, 93.8% (95%CI 92.8–94.8) had indication for drug therapy and, of those, 94.6% (95%CI 93.5–95.5) were using the medication at the time of interview. Full access to medicines was 97.9% (95%CI 97.3–98.4); partial access, 1.9% (95%CI 1.4–2.4); and no access, 0.2% (95%CI 0.1–0.4). The medication used to treat high blood pressure, 56.0% (95%CI 52.6–59.2) were obtained from SUS (Brazilian Unified Health System), 16.0% (95%CI 14.3–17.9) from Popular Pharmacy Program, 25.7% (95%CI 23.4–28.2) were paid for by the patients themselves and 2.3% (95%CI 1.8–2.9) were obtained from other locations. The five most commonly used drugs were, in descending order, hydrochlorothiazide, losartan, captopril, enalapril and atenolol. Of the total number of patients on treatment, 36.1% (95%CI 34.1–37.1) were using two medicines and 13.5% (95%CI 12.3–14.9) used three or more. CONCLUSIONS Access to

  7. Radioprotectors in Radiotherapy

    Energy Technology Data Exchange (ETDEWEB)

    Nair, C.K.K. [Bhabha Atomic Research Centre, Mumbai (India); Parida, D.K.; Nomura, Taisei

    2001-03-01

    This review article focuses on clinically relevant radioprotectors and their mechanisms of radioprotection. Radiotherapy is the most common modality of human cancer therapy. Obtaining optimal results requires a judicious balance between the total dose of radiotherapy delivered and the threshold limit of critical surrounding normal tissues, and the normal tissues need to be protected against radiation injury to obtain better tumor control by using a higher dose. For this reason, radiation-protective agents play an important role in clinical radiotherapy. Radiation-protective agents can be classified into three groups: radioprotectors, adaptogens, and absorbents. The first group generally consists of sulfhydryl compounds and other antioxidants. They include several myelo-, entero-, and cerebro-protectors. Adaptogens act as promotors of radioresistance. They are natural protectors that offer chemical protection against low levels of ionizing radiation. Absorbents protect organs from internal radiation and chemicals. They include drugs that prevent incorporation of radioiodine by the thyroid gland and absorption of radionuclides. This article thoroughly describes the properties, mechanisms of action, and perspectives on clinical application of the following categories of radioprotectors: sulfhydryl compounds (e.g., cysteine, cysteamine, glutathione, AET, WR 2127, and other WR-compounds), antioxidants (e.g., tempace, Hoechst 33342, vitamin A, E, and C, TMG, melatonin), angiotensin-converting enzyme (ACE) inhibitors (e.g., captopril, elanopril, penicillamine, pentoxifylline, L-158, 809), cytoprotective agents (mesna, dexrazoxane, and amifostin), metalloelements (e.g., manganese chloride, cadmium salts, bismuth subnitrate), immunomodulators (gamma-interferon, polysaccharides AM5, AM218, heat-killed lactobacillus cells, broncho-vaxom, trehalose dicorynomycolate, and AS101), lipopolysaccharides and prostaglandins, plant extracts and compounds isolated from plants (curcmin

  8. 前列腺素E2在肾脏球旁器调节肾素分泌中的作用%Role of prostaglandin E2 in regulation of renin secretion at juxtaglomerular apparatus

    Institute of Scientific and Technical Information of China (English)

    陈丽萌; 黄宇宁; 秦岩; 刘冬妍; 李艳; 段琳

    2009-01-01

    Objective To investigate the effect and mechanism of prostaglandin E2 (PGE2) in renin regulation at the juxtaglomerular apparatus (JGA). Methods Macula densa cell line (MMDD1) was cultured on the special filter. In the medium on the apical lateral of the cells, low concentration of sodium chloride, chloride and different doses of angiotensin Ⅱ (Ang Ⅱ) were used to stimulate the PGE2 secretion. The PGE2 concentration was tested by ELISA. In the animal experiment, the response of plasma renin activity (PRA) to acute intraperitoneal administration of captopril (30 mg/kg) was determined, in conscious wild-type (WT) and cyclooxygenase COX-2-/- mice on C57BL/6 genetic backgrounds. PRA was measured in plasma obtained by tail vein puncture. Different concentrations of PGE2 were used to stimulate the renin secretion of primary cultured JGA cells from COX-2-/- mice and wild type mice. In specific Gsα gene delete mice (low renin producing mice), 24 h urine was collected to test the concentration of PGE2. The COX-2 mRNA and protein of the kidney cortex were observed by real-time PCR and immunohistochemicul staining. Results Low chloride could stimulate the PGE2 secretion both at the apical and basement of the macula densa cells. In COX-2-/- mice, the base PRA and were obviously lower than wild type mice. Captopril could stimulate the PRA of (COX)-2-/- mice increasing 32.8 times. But Ang Ⅱ had no effect on PGE2 secretion in macula densa cells. In primary cultured JGA cells, the decreasing renin seretion was partly recovered by PGE2 in cells from COX-2-/- mice. In low renin producing mice, the expression of COX-2 mRNA in the kidney cortex increased by (8.07±1.08) times (n=6, P=0.0022). The COX-2 protein of the kidney cortex and the urine PGE2 increased by several times. Conclusions Low chloride is the primary stimulation messenger of PGE2 secretion in macula densa cells. The PRA in COX-2-/- mice can be stimulated by angiotensin converting enzyme inhibitor, but the Ang

  9. Baoxinkang Formula Combining with Conventional Medicine Therapy in Influencing Cardiac Function and Myocardial ATPase Activity in Rats with Chronic Heart Failure%保心康与常规药物合用对慢性心衰大鼠心功能、心肌ATP酶活性的影响

    Institute of Scientific and Technical Information of China (English)

    洪永敦; 叶子青; 苏一飞; 李小兵; 赵静; 傅思莹

    2014-01-01

    Objective This research is to figure out whether the combination of Baoxinkang formula and conventional medicine therapy is better than conventional medicine therapy only in preservation of ATPase activity in chronic heart failure rat model. Methods Sprague-Dawley rats were randomly divided into 6 groups, the Baoxinkang group, conventional medicine therapy group, the Baoxinkang and conventional medicine therapy group, the trimetazidine and conventional medicine therapy group, control group and sham-operation group. Abdominal aortic constriction was performed to induce chronic heart failure . Baoxinkang(1020 mg·kg-1) in combination with conventional medicine therapy(Metoprolol 10 mg·kg-1, Captopril 5 mg·kg-1, Digoxin 0.0225 mg·kg-1) was administrated for 6 weeks. Echocardiography was performed to evaluate the cardiac function. The activity of Na+-K+-ATPase(NKA), Ca2+-Mg2+-ATPase(CMA) was examined by spectrometry. Results Echocardiography showed that either comparing with the control group or conventional medicine therapy group, Baoxinkang+conventional medicine therapy group had improved enlarged heart, higher ejection fraction, higher cardiac output and lower heart rate. Myocardial ATPase activity in Baoxinkang+conventional medicine therapy group were higher than those in the control group. Comparing with control group, Baoxinkang group has higher CMA activity, but similar NKA activity. No significant difference was observed in ATPase activity between Baoxinkang+conventional medicine therapy group and conventional medicine therapy group. Conclusion Baoxinkang formula could provide better protection to the activity of CMA, modulate the consumption of ATP to improve the cardiac function. The synergistic protection of Baoxinkang formula in combination with conventional medicine therapy may not completely cause by the preservation of ATPase activity. How does the Baoxinkang formula protect the activity of myocardial NKA and CMA needs further study.%目的:观察

  10. Proteinuria in patients with primary aldosteronism%原发性醛固酮增多症患者蛋白尿情况分析

    Institute of Scientific and Technical Information of China (English)

    李南方; 马轩; 王红梅; 李娟; 王新国

    2013-01-01

    . The aldosterone-renin ratio (ARR) was calculated as a screening method, and confirmatory tests were including saline load test and captopril challenge test. Finally, 155 patients were diagnosed as PA (PA group) , and other 246 patients who did not meet the criteria for PA were labeled as EH group. The differences in urinary protein level and proteinuria detection rate between the two groups were analysed. The multivariate linear regression model was used to analyze the potential risk factors for proteinuria in PA patients. Results The 24-hour urinary protein level and proteinuria detection rate in PA group were significantly higher than those in EH group [ (1. 99 ± 0.37) vs (1.85 ± 0. 34)g/24 h, P<0. 01; 14.2% vs 6. 5%, P = 0. 01]. After the adjustment for age, gender, duration of hypertension by logistic regression model, patients with PA also had higher proteinuria detection rate (P = 0. 031) and higher proteinuria risk {OR 2. 152) compared to patients with EH. The serum aldosterone level was a risk factor for proteinuria in patients with PA {β=0. 232, P = 0. 021) after the adjustment for age, blood pressure, duration of hypertension, and PRA. Conclusions The urinary protein level and proteinuria detection rate were higher in patients with PA, and the elevated serum aldosterone level was likely the key pathogenic factor.

  11. 肾上腺静脉采血在原发性醛固酮增多症分型诊断中的价值%Value of adrenal venous sampling in the subtypic diagnosis of primary aldosteronism

    Institute of Scientific and Technical Information of China (English)

    赵家胜; 李颖; 贺铭; 刘琦; 尚鸣异; 王宏保

    2013-01-01

    Objective To assess the diagnostic value of adrenal venous sampling (AVS) in the subtype diagnosis of primary aldosteronism (PA).Methods The diagnosis of PA was made in 36 patients based on an elevated ratio of plasma aldosterone (ALD) to plasma rennin activity (PRA) (ARR) and confirmed tests (saline infusion or captopril challenge) in recent 3 years.All PA patients underwent adrenal computed tomographic scan (CT) and AVS.The diagnostic accuracy of CT and AVS in the subtype differentiation of PA were evaluated by comparing the differences of CT findings,AVS results and clinical outcomes.Results Fifteen of 36 patients (42%) had a final diagnosis of aldosterone-producing adenoma (APA) and aother 21 patients (58%) with bilateral adrenal hyperplasia (BAH).The level of ALD was significantly higher in APA group than that in BAH group (298.9 ± 91.0 vs 226.3-± 59 ng/L,P < 0.05).PRA (ng · ml-1 · h-1) in APA patients were markedly lower than that in BAH counterparts (0.18 ±0.14 vs 0.28-±0.29 ng · ml-1 · h-1,P <0.01).Consequently,ARR in APA group was evidently higher than that in BAH group (2444.7 ± 1405.2 vs 1550.0 ± 1059.8,P < 0.05).Plasma potassium in APA patients was lower than that in those with BAH (2.71 ±0.57 vs 3.17 ±0.40 mmol/L).But there was no statistic significance (P > 0.05).The CT findings were discordant with the AVS results in 27.8% of patients (10/36).The accuracy of adrenal CT scan was only 72.2% in the subtypic diagnosis of PA,provided AVS was the gold standard for distinguishing between APA and BAH.Reliance on CT findings could lead to inappropriate management in 25% of PA patients.Conversely,the AVS results were concordant with the clinical outcomes in 94.4% of all patients.Conclusion CT scan is not a reliable method of differentiating primary aldosteronism.Compared with CT,AVS is more accurate in establishing a correct diagnosis of primary aldosteronism.AVS should be performed routinely before operation in PA patients

  12. Therapeutic effect evaluation on the treatment on acute left heart failure with Shenmai injection and deslanoside%参脉注射液联合去乙酰毛花苷丙注射液治疗急性左心衰竭的疗效分析

    Institute of Scientific and Technical Information of China (English)

    陈元粉; 贾琪; 侯静静

    2014-01-01

    Objective To observe the effect of treating acute left heart failure with Shenmai injection and auxiliary conventional western medicine. Methods 132 patients were randomly divided into a control group and a treatment group, with 66 cases in each group. The control group was treated with lanatoside C, captopril, diuretics, and aminophylline. While the treatment group was additionally treated with Shenmai injection on the basis of the control group. Left ventricular ejection fraction(LVEF), left smothering end-diastolic diameter(LVEDD)value, the index of b-type natriuretic peptide(BNP), and 24 h dynamic electrocardiogram(ecg)were observed in both groups after 1 month’s treatment. Results LVEF and BNP were improved in both groups after the treatment[LVEF and BNP were(40.42 ± 4.32)%, (306.57 ± 201.21)pg/ml in the treatment group and(37.92±3.32)%, (451.51±294.23)pg/ml in the control group before the treatment;(35.28±4.15)%, (540.17±382.23)pg/ml in the treatment group and(35.13±2.35)%, (572.35± 422.21)pg/ml in the control group after the treatment], and the curative effect in the treatment group was better than the control group(P0.05). Conclusion Shenmai injection has good effects in the treatment of acute left heart failure.%目的:观察参脉注射液辅助西医常规疗法治疗急性左心力衰竭的临床疗效。方法采用随机数字表法按1∶1的比例将132例患者随机分为两组各66例,对照组采用西地兰、卡托普利、利尿剂及氨茶碱等治疗。治疗组在对照组治疗基础上静滴参脉注射液,1次/d,两组均治疗1个月后观察患者左室射血分数(LVEF)、左窒舒张末内径(LVEDD)值、B型利钠肽(BNP)指标变化,及两组患者的24 h动态心电图。结果两组患者LVEF值与BNP浓度治疗后[治疗组分别为(40.42±4.32)%、(306.57±201.21)pg/ml,对照组分别为(37.92±3.32)%、(451.51±294.23)pg/ml]均较同组治疗前明显改善[治疗组分别为(35.28±4.15)%

  13. Effects of Schisandra Lignans and Polysaccharides on Ventricular Remodeling Induced by Isoproterenol in Mice%北五味子木脂素和北五味子粗多糖对异丙肾上腺素诱导小鼠心室重构作用的研究

    Institute of Scientific and Technical Information of China (English)

    孙红霞; 陈建光

    2014-01-01

    Objective To study the effects of Schisandra lignans( SCL) and Schisandra chinensis polysaccharides ( SCP ) on ventricular remodeling induced by isoproterenol( ISO) in mice and explore its preliminary mechanism. Methods Ventricular remodeling model was induced by subcutaneous injections of ISO for continuous ten days. Mice were randomly divided into control group,ISO group,positive control drug captopril(CAP) group,low-dose, middle-dose,high-dose SCL groups and SCP group by intragastric administration. Cardiac mass index of mouse was calculated after experiment, the changes of myocardial pathological morphology were observed, myocardial fiber diameter(MD) was measured by HE staining;hydroxyproline(HYP) content,nitric oxide(NO) content, nitric oxide synthase(NOS) activity,superoxide dismutase(SOD) activity and malondialdehyde(MDA) content in myocardial tissue were measured by spectrophotometry. Results Compared with those in the control group,the heart weight index and HYP content in ISO group were significantly increased ( P<0 . 05 or P<0 . 01 ) , the NOS and SOD activity were decreased(P<0. 05 or P<0. 01). Compared with the ISO group,three doses of SCL and SCP could reduce heart weight index obviously ( P<0 . 05 or P<0 . 01 ) , improve the myocardial pathological changes,inhibit HYP content,increase SOD activity and reduce MDA content,and enhance NOS activity and NO level in myocardium ( P<0 . 05 , P<0 . 01 or P<0 . 001 ) . Conclusion Schisandra lignans and Schisandra chinensis polysaccharides have inhibitory effects on ventricular remodeling induced by ISO in mice, its mechanisms may be related to increasing NOS activity and NO level,scavenging oxygen free radicals,enhancing the antioxidant ability.%目的:研究北五味子木脂素( Schisandra lignans, SCL )和北五味子粗多糖( Schisandra chinensis polysaccharides,SCP)对异丙肾上腺素(Isoproterenol,ISO)诱导小鼠心室重构的保护作用,并探讨其初步机制.方法采用连续10 d皮下注

  14. Anti-hypertensive effect and mechanism of sesamin in spontaneously hypertensive rats%芝麻素对自发性高血压大鼠的降压作用及机制

    Institute of Scientific and Technical Information of China (English)

    张俊秀; 杨解人; 李文星; 唐丽娟; 杨慧; 熊莺

    2014-01-01

    Objective:To observe the anti-hypertensive effects of sesamin ( Ses) and its potential mechanism in the spontaneously hypertensive rats (SHR).Methods:Thirty-five SHRs were randomized into groups of SHR model,administration of sesamin in dose of 160,80 and 40 mg/(kg· d) as well as captopril(Cap)in dose of 30 mg/(kg· d).Another 7 Wistar-Kyoto (WKY) rats were added as negative controls.All rats were undergone measurement of the systolic blood pressure( SBP) ,diastolic blood pressure( DBP) and mean blood pressure( MBP) via inserting a cannula into the carotids,and deter-mination of the aortic nitric oxide (NO) and hydrogen peroxide (H2O2) levels with Griess reagent.Reverse transcription polymerase chain reaction(RT-PCR) was performed to determine the expression of aortic eNOS,p22phox and p47phox mRNA.Results:The SBP,DBP and MAP were significantly decreased in groups treated with sesamin in dose of 160 and 80 mg/kg(P<0.01,P<0.05),whereas the aortic NO level was markedly elevated (P<0.01) and eNOS mRNA expression was remarkably up-regulated(P<0.01,P<0.05),and p22phox and p47phox mRNA were significantly down-regulated(P<0.01, P<0.05),as compared with those in the SHR group.In addition,aortic H2O2 levels were reduced in groups treated with diverse dose of sesamin(P<0.01).Conclusion:Sesamin may function in anti-hypertension for SHR through up-regulating the level of eNOS mRNA to facilitate increased synthesis and release of NO in the endothelial cells,while down-regulating the subunits of p22phox and p47phox mRNA expression in aortas to enhance the NO activity.%目的:观察芝麻素(Ses)对自发性高血压大鼠(SHR)的降压作用,并探讨其可能机制。方法:SHR 35只,随机分为SHR模型组、Ses160、80、40 mg/(kg· d)、卡托普利(Cap)30 mg/(kg· d),另设WKY正常对照组,于给药16周后,颈总动脉插管测收缩压(SBP)、舒张压(DBP)及平均血压(MBP),Griess Reagent法测主动脉中一氧化氮

  15. Relatively Strong Heart Piece of Clinical Studies in Patients with Chronic Heart Failure%补益强心片治疗慢性心力衰竭临床研究

    Institute of Scientific and Technical Information of China (English)

    陈绪忠; 陈卓; 陈敬发

    2014-01-01

    目的:探讨补益强心片治疗慢性心力衰竭( CHF)的临床疗效。方法:将86例CHF患者随机分为对照组和观察组,每组各43例。对照组予以盐酸贝那普利片、倍他乐克片、地高辛片、氢氯噻嗪片口服,配合非药物干预治疗。观察组在对照组基础上加用补益强心片,两组疗程均为8周。观察治疗前后Lee氏心力衰竭计分、心室射血分数( LVEF)、心输出量( CO)、心房利钠多肽( ANP)、N末端B型钠尿肽( NT-proBNP)、血管紧张素Ⅱ( AngⅡ)及醛固酮( ALD)水平。结果:观察组Lee氏心力衰竭疗效有效率90.70%,优于对照组的74.42%(P<0.05);治疗后两组Lee氏心力衰竭评分较治疗前下降,观察组低于对照组(P<0.01);治疗后两组LVEF和CO均上升,观察组高于对照组,差异有统计学意义(P<0.01);治疗后观察组血浆ANP、NT-proBNP、AngⅡ及ALD水平低于对照组( P<0.01)。结论:在西医常规治疗的基础上,补益强心片能进一步改善CHF患者心功能,其作用机制可能与其下调RAAS系统及对ANP、NT-proBNP等细胞因子的调节有关。%Objective:To investigate the relatively strong heart piece the clinical curative effect of treatment of chronic heart failure ( CHF). Methods:86 patients with CHF were randomly divided into control group and observation group,43 cases in each group. Control group to hydrochloric acid that captopril and betaloc pills,digoxin,hydrochlorothiazide tablets,cooperate with the drug intervention ther-apy. Based on observation group in the control group with relatively strong heart,two groups of a course of 8 weeks. Score were observed before and after treatment of Lee's heart failure and ventricular ejection fraction( LVEF)and cardiac output( CO),atrial natriuretic polypeptide(ANP),N end of b-type natriuretic peptide(NT-proBNP),angiotensin Ⅱ(Ang Ⅱ)and aldosterone(ALD)level. Re-sults:the curative effect of

  16. 道家认知疗法对冠状动脉粥样硬化性心脏病患者A型行为的干预作用%Interventional effect of Chinese daoistic cognitive therapy on type-A behavior of patients with coronary heart disease

    Institute of Scientific and Technical Information of China (English)

    朱金富

    2006-01-01

    BACKGROUND: Coronary heart disease (CHD) is commonly seen psychosomatic disease of cardiovascular system. Its behavioral characteristics have been closely concerned by scholars at home and abroad. Chinese daoistic cognitive therapy works well in patients with anxiety, but its application in the field of psychosomatic disease needs further development.OBJECTIVE: To probe into the interventional effect of Chinese daoistic cognitive therapy on type-A behavior of patients with coronary heart disease (CHD).DESIGN: A randomized controlled grouping observation.SETTING: Department of Psychology, Xinxiang Medical College.PARTICIPANTS: Totally 206 patients who were retired and received treatment in the Staff Hospitals of Changsha University of Science and Technology and Hunan University between August 2002 and January 2004were recruited. They were randomly divided into psychotherapy group (n=104)and control group (n=104).METHODS: Patients of control group underwent simple drug treatment and those of psychotherapy group underwent drug treatment + daoistic cog nitive therapy. Drug and dosage:①nifedipine 10 mg/d.②betaxolol 25-50mg/d. ③nitrendipine 20-30mg/d. ④captopril 25-50 mg/d. Dapistic cognitive therapy was divided into four parts according to operation procedure: Loose and calm technique, the technique of soft movement, the meeting of analyzing the cause of CHD and the records of health care and what one has learned from study. Psychotherapy group received 3-month treatment with Chinese daoistic therapy and 6-month follow-up and control group only received medical treatment. Both groups were test on a type-A behavior questionnaire (TABQ) and a mental detachment scale. TABQ included three-subscales: L scale is for measuring lie; TH scale for measuring time hurry and CH is for competition hostility. Subjects, whose value of L was equal to or beyond 7, were excluded. Subjects were considered as patients with type-A behavior if their TH+CH value was equal to or beyond

  17. Study of the Detection of Histidine Based on “On-Off” Fluorescence Probe of Carbon Dots%基于碳点“开关”型荧光探针在组氨酸检测中的研究

    Institute of Scientific and Technical Information of China (English)

    陶慧林; 廖秀芬; 孙超; 周素莲; 钟福新; 易忠胜; 陆艳群

    2016-01-01

    An new type of switch “On‐Off” fluorescence probe was constructed based on fluorescence carbon dots as a novel strategy to analyze trace histidine(His) which was proposed for the first time .In water solution with pH 7.6 ,the fluorescence of CDs was quenched with Ru3+ due to the formation of ground state compound through electrostatic attraction ,and the system was thus“turned‐off” .The fluorescence intensity of CDs was “turned‐on” due to the competition between His and Ru towards the surface of CDs .The effect of critical parameters including pH ,buffer solutions ,reaction temperature and time needed to grow the fluorescence intensity of CDs was studied .Results show thatin water solution with pH 7.6 ,and when the temperature was between 20~25 ℃ ,the fluorescence intensity of the released CDs displayed a linear relationship in the range of (6.5~219.3) × 10-6 mol · L -1 of captopril .Lower limit of detection for His ,at the signal‐to‐noise ratio of 3/(3δ) ,was 2.15 × 10-6 mol · L -1 .The methodology was successfully applied for the determination of His in Compound Amino Acid Injections ,with the RSD≤2.07% ,and the recovery rate was between 95.7% ~102.4% .The result of the experiment was satisfactory .On the one hand ,the excellent optical character CDs was acted as “On‐Off” fluorescence probe ,which could be extent the application of CDs ,on the other hand ,the excellent performance of the proposed fluorescence probe shows that this method possesses the po‐tential for practical application .%研究并构建了一种基于荧光碳点(carbon dots ,CDs)的新型“开关”探针,利用CDs荧光强度的变化进行痕量组氨酸(histidine ,His)的检测。在pH 7.6的溶液中,钌(Ru)能与CDs通过静电吸引作用形成弱的基态化合物,导致CDs的荧光猝灭,此时体系处于“关闭”状态。而His与Ru有更强的亲和力,故向体系中加入 His后,Ru从CDs表面竞争中下来

  18. Surgical treatment and perioperative management of congenital heart disease with severe pulmonary hypertension%先心病合并重度肺动脉高压的手术及相关治疗

    Institute of Scientific and Technical Information of China (English)

    陈元恒; 张红超; 于鲁峰; 李令珂; 侯迈; 杨军民; 徐金星

    2009-01-01

    AIM: To review the results and methods of surgical treatment and perioperative management of congenital heart disease (CHD) with severe pulmonary hypertension (PH). METHODS: Thirty-six patients (17 males, 19 females, aging from 1-41 years) of congenital heart disease with severe pulmonary hypertension were included in the study, among whom were 9 cases of atrial septal defect and 20 cases of ventricular septal defect. The saturation of artery oxygen ranged from 0.85-0.94 and echocardiograpby showed left to right slow velocity shunt in 23 cases, double direction shunt in 10 cases and no shunt in 3 cases. The pulmonary pressure was 80 to 130 mmHg(1 mmHg=0.133 kPa), the pulmonary pressure/systemic pressure varied from 0.75-1.0 and the pulmonary resistance was 8-27.2 Wood unit. All the patients were treated with corrective surgery, and one way shunt valve (size 0.5-0.6 cm) from right to left shunt on the repaired patch was created especially for the treatment of extremely severe pulmonary hypertension. The therapy of oxygen inhalation, oral intake of captopril and sildenafil, and intravenous injection of sodium nitroprusside and prostaglandin E1 were routinely administrated perioperatively to reduce pulmonary hyper-tension. Nitric oxide and sildenafil were applied especially for the treatment of extremely severe pulmonary hypertension or pulmonary hypertension crisis. RESULTS: Only one early postoperative death occurred due to low output syndrome, and the other 35 patients were recovered and discharged from the hospital. The 0.5 -7 years follow-up showed that the patients were well recovered with NYHA Ⅰ heart function. CONCLUSION: Satisfactory outcome can be achieved in surgical treatment of CHD with severe pulmonary hypertension by meticulous preoperative analysis of surgical indications, selection of appropriate operative procedures and multiple perioperative therapies.%目的:对36例先心病合并重度肺动脉高压患者手术及综合治疗的经验

  19. Effect of advanced glycation end products on renin-angiotensin system in podocytes%晚期糖基化终产物对足细胞内肾素-血管紧张素系统的影响

    Institute of Scientific and Technical Information of China (English)

    成彩联; 郑振达; 石成钢; 叶增纯; 刘迅; 娄探奇

    2013-01-01

    Objective To investigate the effect and mechanism of advanced glycation end products (AGEs) on the components of renin-angiotensin system (RAS) in the podocytes.Methods Immortalized mouse podocytes were exposed to various concentrations of AGEs for 24 h.The expression levels of renin,angiotensinogen (AGT) and angiotensin Ⅱ type 1 and 2 receptors (AT1R and AT2R),the level of angiotensin Ⅱ (Ang Ⅱ),and the activity of angiotensin-converting enzyme (ACE) were assayed.The levels of Akt and phosphorylated Akt were examined by Western blotting.Cell adhesion was measured in the podocytes pretreated with phosphoinositide 3-kinase (PI3-K) inhibitor LY294002,losartan,captopril and chymostatin,respectively.Results Treatment with AGEs resulted in significant increase in the expression of AGT and AT1R.Moreover,ACE activity and Ang Ⅱ level increased significantly.However,there was no significant change in renin and AT2R expression.AGEs increased the phosphorylation of Akt by 100%.When the podocytes were pretreated with LY294002 (10 μmol/L),the AGEs-induced increase in AGT and AT1R expression reduced remarkably.Likewise,ACE activity and Ang Ⅱ level decreased significantly,and the reduced podocyte adhesive capacity induced by AGEs was improved significantly.Conclusions AGEs activate the RAS via PI3-K/Akt-dependent pathway,and lead to a decrease in podocyte adhesion.%目的 观察晚期糖基化终产物(advanced glycation end products,AGEs)对足细胞内肾素-血管紧张素系统(renin-angiotensin system,RAS)的影响及作用机制.方法 不同浓度的AGEs干预小鼠足细胞24h,分别检测肾素(renin)、血管紧张素原(renin-angiotensin system,AGT)、血管紧张素Ⅱ1型、2型受体(AT1R、AT2R)的表达,血管紧张素转换酶(angiotensin-converting enzyme,ACE)的活性和血管紧张素Ⅱ(angiotensinⅡ,AngⅡ)的浓度,观察蛋白激酶B(Akt)的磷酸化,然后分别加入磷酸肌醇3激酶抑制剂LY294002、Iosartan、captopril和chymastatin,

  20. Research of candesartan on treating young and middle-aged patients with hypertension and protecting target or-gan%坎地沙坦治疗中青年高血压及靶器官保护作用研究

    Institute of Scientific and Technical Information of China (English)

    刘俊勇; 骆淑斐

    2014-01-01

    目的:观察坎地沙坦治疗中青年高血压患者的疗效,并探讨其对靶器官的保护作用。方法将162例中青年高血压患者随机分为两组,对照组80例患者予以卡托普利片25 mg口服,每日二次,治疗疗程为6个月。治疗组82例患者予以坎地沙坦片8 mg口服,每日一次,治疗疗程为6个月。对比观察两组患者治疗前后血压控制有效率,和左心室重量指数(LVMI)、左心室舒张末内径(LVEDd)、左心室后壁舒张末厚度(LVPWT)、室间隔舒张末厚度(IVST)以及肱动脉内皮依赖性舒张功能(FMD)。结果治疗6个月后,治疗组的降压有效率(90.24%)高于对照组(75.32%),差异有统计学意义(χ2=6.27,P<0.05)。两组患者在治疗6个月后LVMI、LVEDd、IVST和LVPWT均见明显改善,差异均有统计学意义(t分别=6.13、2.67、3.15、6.75;5.37、9.83、9.13、10.23,P均<0.05),其中在LVEDd方面,治疗组优于对照组,差异有统计学意义(t=6.13,P<0.05);两组患者治疗后FMD均有提高,两组组内治疗前后的差异有统计学意义(t分别=2.45、3.56,P均<0.05),且治疗组治疗后的FMD明显低于对照组,差异有统计学意义(t=3.36,P<0.05)。结论坎地沙坦治疗中青年高血压,其降压效果优于卡托普利,且能更有效改善血管内皮功能及逆转左心室肥厚。%Objective To observe the curative effect of candesartan on treating hypertension of young and middle-aged and explore its protective effect on target organ. Methods A total of 162 cases of hypertension were randomly divided into two groups with 80 patients in each. The control group was given captopril tablets 25 mg, orally, twice a day. The treat-ment group was given candesartan tablets 8 mg, orally, once a day. The treatment courses of two groups were 6 months. the blood pressure effective controlling rate, left ventricular mass index (LVMI

  1. Mechanisms and protective effect of compound Shanju on renal injury in spontaneously hypertensive rats%复方山菊对自发性高血压大鼠肾脏的保护作用及机制

    Institute of Scientific and Technical Information of China (English)

    李文星; 杨解人; 张俊秀; 唐丽娟; 杨慧; 陈国祥

    2012-01-01

    Objective: To observe the protective effect of compound Shanju on the renal injury in spontaneously hypertensive rats (SHR) and the related protection mechanisms. Methods: Thirty-five SHRs were random-ized into groups of SHR model [distilled water,5 ml/(kg·d)],compound Shanju of high, medium and low dosage [0.05,0.15 and0.45 g/ kg·d) , respectively ] and captopril [ 0.03 g/kg·d), (n = 7 for each]. Another 7 Winstar-Kyoto(WKY) rat? were included as negative control by administration of aqua destillata in a dose of 5 ml/(kg·d) that was daily applied to the groups described above for 16 weeks. Blood pressure was measured in all animals by tail cuff every 2 weeks. After 16 weeks,the primary pathologic changes of glomerulus were observed with HE staining,and collagen fiber alteration by Mason's trichrome staining. In addition,immunohisochemical technique and RT-PCR were used to detect the expression of glomerulus iNOS protein and glomerulus TGF-β1 mRNA, respectively. Results: Compound Shanju resulted in delayed glo-merular mesangial cell and matrix proliferation, checked tubular granular degeneration,gradually repaired renal interstitial inflammatory cell infiltration, reduced fibrosis and deposition of glomerular mesangial collagen with increasing intervention dose. Also, the expression of iNOS and TGF-β1 mRNA were down-regulated in glomeruli. Conclusion, Compound Shanju can significantly reduce the glomerular injury and inhibit the glo-merular mesangial collagen synthesis of SHRs, suggesting that this agent may protect the kidney from injury through down-regulated iNOS and TGF-β1 mRNA expression of SHR glomerulus.%目的:观察复方山菊对自发性高血压大鼠(SHR)肾脏损伤的保护作用并分析其可能机制.方法:SHR大鼠35只,随机分5组,每组7只,分别灌服复方山菊[0.05、0.15、0.45 g/(kg·d)]和卡托普利(0.03 g/kg),WKY大鼠正常对照组7只、SHR模型组灌服等容积蒸馏水(5ml/kg),每日1次,连续16周.尾袖法每两

  2. Clinical analysis of right coronary artery anomalies in 8 children%儿童右冠状动脉畸形8例临床分析

    Institute of Scientific and Technical Information of China (English)

    甄珍; 袁越

    2016-01-01

    excluded),who were admitted into Beijing Children's Hospital Affiliated to Capital Medical University from January 2009 to December 2014.Results A total of 8 medical records of children with right coronary artery anomalies,among whom 5 cases were male and 3 cases were female,with a mean age of (7.06 ± 1.37) years old.In these 8 patients,there were 5 patients with right coronary artery originating from left coronary sinus,1 patient with right coronary artery originating from left wall of aorta,1 patient with single left coronary artery type Lipton L Ⅱ,and 1 patient with right coronary artery absence.The main symptoms included chest distress,chest pain and palpitation in elder children,but in infants,the primary symptom was poor feeding.One case of these patients represented syncope.Electrocardiogram of these patients showed ST-T wave changes,sinoatrial block,and sinus arrest.Ultrasonic cardiogram failed to discover the coronary artery anomalies.Four cases showed enlarged left ventricular end-diastolic diameter,and 1 case showed slight decrease of left ventricular ejection function.All 8 patients were given myocardial tonic with limitation in doing exercise,and clinical follow-up studies were conducted for 6 months.Four patients with enlarged left ventricular were treated with Captopril,and 3 patients of them recovered after 3 to 6 months.Two patients with sinus node malfunction were treated with permanent pacemaker implantation in other hospitals.Conclusions Right coronary artery anomaly in children is rare.Patients with cardiac ischemia and sinus node malfunction should be aware of right coronary malformation.64-section multidetector computerized tomography angiography can diagnose right coronary artery anomalies.To patients with right coronary artery anomalies,vigorou