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Sample records for captopril

  1. Captopril

    Science.gov (United States)

    ... a class of medications called angiotensin-converting enzyme (ACE) inhibitors. It decreases certain chemicals that tighten the blood ... pharmacist if you are allergic to captopril; other ACE inhibitors such as benazepril (Lotensin, in Lotrel), captopril (Capoten), ...

  2. Captopril in the hepatorenal syndrome

    Energy Technology Data Exchange (ETDEWEB)

    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.

  3. 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

  4. Development studies of captopril certified reference material

    Directory of Open Access Journals (Sweden)

    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.

  5. Foam fractionation in recovery of captopril

    OpenAIRE

    Avishek Mandal

    2013-01-01

    Toxic effect caused due to the presence of pharmaceuticals in waste water has been recognized as one of the emerging issue in the presentday environmental pollution. The aim of the present work is to investigate the feasibility of foam fractionation technique in batch mode for the recovery of captopril from dilute aqueous solution and to compare the performance of drug recovery from two feed solutions, one containing pure drug and the other containing formulated drug (tablet). Captopril is an...

  6. Foam fractionation in recovery of captopril

    Directory of Open Access Journals (Sweden)

    Avishek Mandal

    2013-09-01

    Full Text Available Toxic effect caused due to the presence of pharmaceuticals in waste water has been recognized as one of the emerging issue in the presentday environmental pollution. The aim of the present work is to investigate the feasibility of foam fractionation technique in batch mode for the recovery of captopril from dilute aqueous solution and to compare the performance of drug recovery from two feed solutions, one containing pure drug and the other containing formulated drug (tablet. Captopril is an anionic compound used as antihypertensive drug. Presence of this drug can cause aquatic toxicity. The performance of recovery was investigated as a function of gas velocity, pH of feed solution, collector-colligend ratio (j, colligend (drug concentration, feed volume, column height and aliphatic chain length of the collector (surface active agent and finally, optimum condition had been determined. Percentage recovery was enhanced to 90% (approx for pure drug at the optimum pH value of 3.75, j = 4 at an optimum gas velocity. The optimum gas velocity depends on feed volume. Percentage recovery (Rp decreases with increase of chain length. Enrichment ratio (Er was enhanced with the increase of foam height in the column. Rp and Er were found lower in formulated type of captopril in comparison to the pure drug due to the presence of other soluble ingredients in tablet.

  7. The determination of captopril in Solution by Raman spectroscopy

    Science.gov (United States)

    Gao, Junxiang; Gu, Huaimin; Dong, Xiao; liu, fangfang

    2011-01-01

    Captopril, 1-[(2S)-3-mercapto-2-methyl propionyl]-Lproline, is an angiotensin converting enzyme (ACE) inhibitor, which reduces peripheral resistance and lowers blood pressure. It is widely used in the hypertensive ailments and incongestive heart failure treatment. Due to such crucial pharmacological importance, development of simple and accurate methods for the determination of captopril is desired. In this work, the normal Raman spectra of the captopril in different concentrations were studied, and the relationship between the Raman intensity and the concentrations of the captopril was quantificationally analysed. By selecting appropriate characteristic Raman bands of the cptopril, the solution of some captopril purchased in a local pharmacy was quantificationally determined. A quantificational linear relationship between the Raman intensity and the concentrations of captopril was obtained, and it is little affected by other compounds in the solution of captopril. This study provides an effective technique for the quantificational determination of captopril in solutions, and it has a potential application in the analysis of medicament.

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

    Directory of Open Access Journals (Sweden)

    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.

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

    Directory of Open Access Journals (Sweden)

    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

  10. 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.

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

    Directory of Open Access Journals (Sweden)

    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.

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

    Science.gov (United States)

    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. PMID:27468462

  13. Afterload reduction: a comparison of captopril and nifedipine in dilated cardiomyopathy.

    Science.gov (United States)

    Agostoni, P G; De Cesare, N; Doria, E; Polese, A; Tamborini, G; Guazzi, M D

    1986-01-01

    Nifedipine and captopril are potent vasodilators and may be expected to help left ventricular failure by reducing afterload. Nifedipine (20 mg three times a day) and captopril (50 mg three times a day) were added to an optimal regimen of digitalis and diuretics in a double blind crossover trial in 18 cases of dilated cardiomyopathy. New York Heart Association functional class rating symptoms and exercise tolerance times improved on captopril but not on nifedipine. The reduction in pulmonary capillary wedge pressure and the increase of cardiac output on captopril indicated that the augmented functional capacity may have resulted in part from an improved performance of the left ventricle. Although there were comparable decreases in systemic vascular resistance and presumably in impedence to ejection by the left ventricle on both drugs, the dimensions of the ventricular cavity were found to be reduced by captopril and augmented by nifedipine, and only captopril reduced the afterload (wall stress). In addition, the force-length relation (between left ventricular end systolic stress and end systolic diameter) was shifted to the left of baseline by captopril and to the right by nifedipine, suggesting that muscle contractility was reduced by nifedipine and not by captopril. These results suggest that nifedipine and captopril have different effects on afterload and contractility and these may account for the different effects of these drugs on the performance of the heart and clinical responses. PMID:3516187

  14. Mechanical evaluation of matrix type transdermal therapeutic systems containing captopril

    OpenAIRE

    KERİMOĞLU, Oya; Şahbaz, Sevinç; ŞEHİRLİ, Ahmet Özer; Dortunç, Betül; Şener, Göksel

    2015-01-01

    The objective of this study was to evaluate themechanical properties of transdermal therapeuticsystems (TTS) containing captopril together withsynthetic and pH independent polymers, EudragitRL 100 and RS 100. The formulations werecharacterized in terms of their adhesiveness andbioadhesiveness by using texture analyser. Theseoptimum formulations were chosen according to theresults of our previous study regarding in vitrodissolution and ex vivo diffusion rate studies throughexcised human skin b...

  15. 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.

  16. Nifedipine and captopril in hypertensive crisis in children.

    Directory of Open Access Journals (Sweden)

    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

  17. 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

  18. 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. PMID:27163244

  19. Amelioration of radiation nephropathy in rats by postirradiation treatment with dexamethasone and/or captopril

    International Nuclear Information System (INIS)

    Dexamethasone (DEX) and captopril are effective drugs in the treatment of radiation nephropathy in experimental animals. The aim of the present study was to determine the relative effectiveness of the two drugs and to see if their combination is more effective than either drug alone. For this purpose both kidneys of 143 rats were exposed surgically and irradiated with 13-20 Gy γ rays. The surrounding tissues, with the exception of a segment of lumbar cord, were shielded. Each group had free access to acidified drinking water containing either DEX (94 μg/l), captopril (500 mg/l), DEX (94μg/l) + captopril (500 mg/l) or drug-free water. Dexamethasone treatment was stopped after 90 days, but animals continued to receive captopril until death. At approximately monthly intervals the animals were weighed and renal function (PUN, hematocrit, 51Cr-EDTA retention) was measured. A side effect of treatment with DEX and DEX + captopril was a reduced increase in body weight. Paralysis of the hind limbs developed in nine animals that received captopril and/or DEX treatment. The classical histological lesions associated with radiation myelopathy were not evident in these paretic rats. It is therefore suggested that paralysis may be attributed in part to drug-induced neurotoxicity in animals with impaired renal clearance. Macroscopically and histologically, nearly all the animals that survived more than 400 days had evidence of renal tumor development. dexamethasone and/or captopril appear to selectively ameliorate glomerular compared to tubular damage, based on histological findings. All three experimental treatments delayed but did not stop the progression of lethal renal injury as measured by kidney function tests and survival time. Median survival times for nontreated and captopril-DEX- and DEX + captopril-treated animals exposed to 14.5 to 19.0 Gy kidney irradiation were 175,242,261 and 395 days, respectively. 33 refs., 8 figs., 4 tabs

  20. Amelioration of radiation nephropathy in rats by postirradiation treatment with dexamethasone and/or captopril

    Energy Technology Data Exchange (ETDEWEB)

    Geraci, J.P.; Sun, M.C.; Mariano, M.S. [Univ. of Washington, Seattle, WA (United States)

    1995-07-01

    Dexamethasone (DEX) and captopril are effective drugs in the treatment of radiation nephropathy in experimental animals. The aim of the present study was to determine the relative effectiveness of the two drugs and to see if their combination is more effective than either drug alone. For this purpose both kidneys of 143 rats were exposed surgically and irradiated with 13-20 Gy {gamma} rays. The surrounding tissues, with the exception of a segment of lumbar cord, were shielded. Each group had free access to acidified drinking water containing either DEX (94 {mu}g/l), captopril (500 mg/l), DEX (94{mu}g/l) + captopril (500 mg/l) or drug-free water. Dexamethasone treatment was stopped after 90 days, but animals continued to receive captopril until death. At approximately monthly intervals the animals were weighed and renal function (PUN, hematocrit, {sup 51}Cr-EDTA retention) was measured. A side effect of treatment with DEX and DEX + captopril was a reduced increase in body weight. Paralysis of the hind limbs developed in nine animals that received captopril and/or DEX treatment. The classical histological lesions associated with radiation myelopathy were not evident in these paretic rats. It is therefore suggested that paralysis may be attributed in part to drug-induced neurotoxicity in animals with impaired renal clearance. Macroscopically and histologically, nearly all the animals that survived more than 400 days had evidence of renal tumor development. dexamethasone and/or captopril appear to selectively ameliorate glomerular compared to tubular damage, based on histological findings. All three experimental treatments delayed but did not stop the progression of lethal renal injury as measured by kidney function tests and survival time. Median survival times for nontreated and captopril-DEX- and DEX + captopril-treated animals exposed to 14.5 to 19.0 Gy kidney irradiation were 175,242,261 and 395 days, respectively. 33 refs., 8 figs., 4 tabs.

  1. 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 of Captopril on TNF-α contents in serum of rheumatoid arthritis(RA) rats,and to provide the theoretical proofs for clinical application of Captopril in treatments ol rheumatoid diseases.Methods:Fifty Wistar rats were randomly divided into 5 groups,namely.Group A,Group 13.Group C.Group D,Group E with 10 rats in each group.Injection of Freund’s complete adjuvant was employed to establish adjuvant-induced arthritis model in rats.Group A was model group;after model establishment,rats were treated with 20 mL normal saline as placebo(ip.).Rats in Group B were treated with 8 mg/kg cyclophosphamide(ip.).Rats in Group C.D and E were intraperitoneally injected with 30 mg/kg.100 mg/kg and 300 mg/kg Captopril respectively.Rats in each group were subjected to continuous treatment for 3 weeks,and then sacrificed.Eyeballs of rats were excised and blood was collected.TNF- α content in serum were detected using ELISA: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- α content in serum of Group A rats was significantly higher than that of rats in other 4 groups(P<0.05).TNF- α content in serum of Group B rats was significantly lower compared with that of rats in Groups C.D and E.The highest TNF- α content in serum of rats treated with Captopril was found in Group C,followed by Groups D and E(P<0.05).Right ankle arthrocele of rats in Groups B.C.D and E in early stage showed no statistical difference compared with that of Group A rats(P>0.05).From Day 8,ankle arthrocele of rats in Groups B.C.D and E was obviously relieved compared with that of Group A rats:the anti-inflammatory effects were gradually enhanced with the extension of medication time.Treatments of Groups C.D and E showed significant activities against tardive aithrocele

  2. Comparison of captopril and losartan renography for diagnosis of renovascular hypertension

    International Nuclear Information System (INIS)

    Objective: his study was to evaluate clinical value of Captopril and Losartan renography for diagnosis of renovascular hypertension. Methods: Forty-six patients with suspected renovascular hypertension were included. Among them, 15 were men and 31 women, with an average age of 42±16 years. All patients underwent Captopril renography, and Losartan renography within 48 hours from one another. Losartan renography was obtained 4 hours after 25mg Losartan. Contrast renal arteriography was performed in all patients within 7 days of radionuclide renography. Result: Overall, 25 patients had a normal renal arteriography and 21 patients had an abnormal one. Comparison of Captopril and Losartan renography for diagnosing of renovascular hypertension is presented. Conclusions: Losartan renography is an accurate method, and may have a higher sensitivity than Captopril renography for the diagnosing of renovascular hypertension

  3. [Evaluating influence of Captopril therapy on occupational activity of engine operators with hypertension].

    Science.gov (United States)

    Serikov, V V; Kolyagin, V Ya; Bogdanova, V E

    2016-01-01

    The article covers results of study concerning influence of Captopril (25 mg) therapy on occupational activity of locomotive crew workers in real night travels model on training complex "EP1M locomotive operator cabin". Findings are that single use of Captopril (25 mg) in modelled railway activity enabled to increase reliability of occupational activity, that manifested in lower number of errors in locomotive operators' actions at night, and in psychophysiologic regulation of various psychic acts. PMID:27396147

  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. The radioprotective effect and mechanism of captopril on radiation induced lung damage in rat

    International Nuclear Information System (INIS)

    It was reported that Captopril (angiotensin converting enzyme inhibitor) had an effect to reduce the pneumonitis and pulmonary fibrosis induced by radiation in rat. We performed this study to investigate the radioprotective effect and mechanism of Captopril. The comparison was made between the radiation only group and the combined Captopril and radiation group by examining histopathologic findings and immunohistochemical stains (TNF α and TGF β1) at 2 and 8 weeks after irradiation. Each group has 8 to 10 rats (Sprague-Dawley). 12.5 Gy of X-ray was irradiated to the left hemithorax in a single fraction. Captopril (50 mg/kg/d) mixed with water was given per oral and continuously from 1 week prior to irradiation up to 8th week of the experiment. In the combined Captopril and radiation group, the histopathologic changes which were hemorrhage into alveolar space, changes of alveolar epithelium, bronchial epithelium and blood vessels, and perivascular edema were less severe than in the radiation only group at 2 weeks. At 8 weeks, the alveolar epithelial changes and perivascular edema were less prominent in the combined Captopril and radiation group. At 2 weeks, the TNF α expression of the combined Captopril and radiation group was markedly decreased at the alveolar epithelium (p<0.01), lymphoid tissue (p=0.06) and the macrophage of alveolar space (p<0.01) compared with the radiation only group. Furthermore the TGF β1 expression was significantly prominent at the alveolar epithelium (p<0.02) and the macrophage in alveolar space (p< 0.02). At 8 weeks, the expression of TNF α and TGF β 1 of most sites, except TGF β1 of the macrophage of alveolar space (p=0.09), showed no significant difference between 2 groups. This study revealed that early lung damage induced by irradiation was reduced with the addition of Captopril in the latent and early pneumonitis phase. The expression of TNF α and TGF β 1 at 2 weeks and TGF β 1 at 8 weeks was further decreased in the

  6. The radioprotective effect and mechanism of captopril on radiation induced lung damage in rat

    Energy Technology Data Exchange (ETDEWEB)

    Song, Mi Hee; Lee, Kyung Ja; Koo, Hea Soo; Oh, Won Young [College of Medicine, Ewha Women Univ., Seoul (Korea, Republic of)

    2001-06-01

    It was reported that Captopril (angiotensin converting enzyme inhibitor) had an effect to reduce the pneumonitis and pulmonary fibrosis induced by radiation in rat. We performed this study to investigate the radioprotective effect and mechanism of Captopril. The comparison was made between the radiation only group and the combined Captopril and radiation group by examining histopathologic findings and immunohistochemical stains (TNF {alpha} and TGF {beta}1) at 2 and 8 weeks after irradiation. Each group has 8 to 10 rats (Sprague-Dawley). 12.5 Gy of X-ray was irradiated to the left hemithorax in a single fraction. Captopril (50 mg/kg/d) mixed with water was given per oral and continuously from 1 week prior to irradiation up to 8th week of the experiment. In the combined Captopril and radiation group, the histopathologic changes which were hemorrhage into alveolar space, changes of alveolar epithelium, bronchial epithelium and blood vessels, and perivascular edema were less severe than in the radiation only group at 2 weeks. At 8 weeks, the alveolar epithelial changes and perivascular edema were less prominent in the combined Captopril and radiation group. At 2 weeks, the TNF {alpha} expression of the combined Captopril and radiation group was markedly decreased at the alveolar epithelium (p<0.01), lymphoid tissue (p=0.06) and the macrophage of alveolar space (p<0.01) compared with the radiation only group. Furthermore the TGF {beta}1 expression was significantly prominent at the alveolar epithelium (p<0.02) and the macrophage in alveolar space (p< 0.02). At 8 weeks, the expression of TNF {alpha} and TGF {beta} 1 of most sites, except TGF {beta}1 of the macrophage of alveolar space (p=0.09), showed no significant difference between 2 groups. This study revealed that early lung damage induced by irradiation was reduced with the addition of Captopril in the latent and early pneumonitis phase. The expression of TNF {alpha} and TGF {beta} 1 at 2 weeks and TGF {beta} 1 at

  7. Effect of antihypertensive agents - captopril and nifedipine - on the functional properties of rat heart mitochondria

    Science.gov (United States)

    Kancirová, Ivana; Jašová, Magdaléna; Waczulíková, Iveta; Ravingerová, Táňa; Ziegelhöffer, Attila; Ferko, Miroslav

    2016-01-01

    Objective(s): Investigation of acute effect on cellular bioenergetics provides the opportunity to characterize the possible adverse effects of drugs more comprehensively. This study aimed to investigate the changes in biochemical and biophysical properties of heart mitochondria induced by captopril and nifedipine antihypertensive treatment. Materials and Methods: Male, 12-week-old Wistar rats in two experimental models (in vivo and in vitro) were used. In four groups, the effects of escalating doses of captopril, nifedipine and combination of captopril + nifedipine added to the incubation medium (in vitro) or administered per os to rat (in vivo) on mitochondrial ATP synthase activity and membrane fluidity were monitored. Results: In the in vitro model we observed a significant inhibitory effect of treatment on the ATP synthase activity (Pactivity and the membrane fluidity in rats receiving captopril, nifedipine, and combined therapy. Conclusion: In vitro kinetics study revealed that antihypertensive drugs (captopril and nifedipine) directly interact with mitochondrial ATP synthase. In vivo experiment did not prove any acute effect on myocardial bioenergetics and suggest that drugs do not enter cardiomyocyte and have no direct effect on mitochondria.

  8. Facile fabrication of mesoporous ZnO nanospheres for the controlled delivery of captopril

    Energy Technology Data Exchange (ETDEWEB)

    Bakrudeen, Haja Bava [Central Leather Research Institute (Council of Scientific and Industrial Research), Industrial Chemistry Laboratory (India); Tsibouklis, John [University of Portsmouth, School of Pharmacy and Biomedical Sciences (United Kingdom); Reddy, Boreddy S. R., E-mail: induchem2000@yahoo.com [Central Leather Research Institute (Council of Scientific and Industrial Research), Industrial Chemistry Laboratory (India)

    2013-03-15

    In the present study, to formulate captopril in a hierarchical porous structure of ZnO nanospheres by means of the soluble-starch-insertion method, state of drug carrier delivery toward oral route and the mode of delivery in suitable medium. Mesoporous ZnO nanospheres were synthesized by simple soluble-starch-insertion method, followed by loading of captopril using ultrasonic force. The materials were characterized by PXRD, SEM, FESEM, TEM, TGA, FT-IR, and BET analyses, and biocompatibility studies. Captopril-loaded porous ZnO nanospheres were evaluated as in vitro drug-release studies and its kinetic models. Crystallite plane arrangement, functional groups, materials morphology, and porosity of porous ZnO nanospheres were confirmed. Larger surface area and distribution in constrained pores on its surface make the nanospheres suitable for high drug loading of captopril. The ZnO nanocrystallites have given porous properties on the spherical surface leads to the drug adsorption. The loading and release studies (in vitro in simulated gastric and intestinal fluids) have shown that both were affected by the mesoporous nanospheres' surface properties of the ZnO materials and its biocompatibility has also been proved. Therefore, the in vitro experiments have indicated the considerable promise of mesoporous ZnO nanospheres, fabricated by the soluble-starch-insertion method acting as a biocompatible carrier for the controlled delivery of captopril in oral route of administration.Graphical Abstract.

  9. Synergistic Inhibition of Angiogenesis by Artesunate and Captopril In Vitro and In Vivo

    Directory of Open Access Journals (Sweden)

    Benjamin Krusche

    2013-01-01

    Full Text Available Inhibition of angiogenesis represents one major strategy of cancer chemotherapy. In the present investigation, we investigated the synergism of artesunate and captopril to inhibit angiogenesis. Artesunate is an antimalarial derivative of artemisinin from the Chinese medicinal plant, Artemisia annua L., which also reveals profound anticancer activity in vitro and in vivo. Captopril is an angiotensin I-converting (ACE inhibitor, which is well established in Western academic medicine. Both compounds inhibited migration of human umbilical vein endothelial cells (HUVECs in vitro. The combination of both drugs resulted in synergistically inhibited migration. Whereas artesunate inhibited HUVEC growth in the XTT assay, captopril did not, indicating independent modes of action. We established a chorioallantoic membrane (CAM assay of quail embryos (Coturnix coturnix L. and a computer-based evaluation routine for quantitative studies on vascularization processes in vivo. Artesunate and captopril inhibited blood vessel formation and growth. For the first time, we demonstrated that both drugs revealed synergistic effects when combined. These results may also have clinical impact, since cardiovascular diseases and cancer frequently occur together in older cancer patients. Therefore, comorbid patients may take advantage, if they take captopril to treat cardiovascular symptoms and artesunate to treat cancer.

  10. Synergistic inhibition of angiogenesis by artesunate and captopril in vitro and in vivo.

    Science.gov (United States)

    Krusche, Benjamin; Arend, Joachim; Efferth, Thomas

    2013-01-01

    Inhibition of angiogenesis represents one major strategy of cancer chemotherapy. In the present investigation, we investigated the synergism of artesunate and captopril to inhibit angiogenesis. Artesunate is an antimalarial derivative of artemisinin from the Chinese medicinal plant, Artemisia annua L., which also reveals profound anticancer activity in vitro and in vivo. Captopril is an angiotensin I-converting (ACE) inhibitor, which is well established in Western academic medicine. Both compounds inhibited migration of human umbilical vein endothelial cells (HUVECs) in vitro. The combination of both drugs resulted in synergistically inhibited migration. Whereas artesunate inhibited HUVEC growth in the XTT assay, captopril did not, indicating independent modes of action. We established a chorioallantoic membrane (CAM) assay of quail embryos (Coturnix coturnix L.) and a computer-based evaluation routine for quantitative studies on vascularization processes in vivo. Artesunate and captopril inhibited blood vessel formation and growth. For the first time, we demonstrated that both drugs revealed synergistic effects when combined. These results may also have clinical impact, since cardiovascular diseases and cancer frequently occur together in older cancer patients. Therefore, comorbid patients may take advantage, if they take captopril to treat cardiovascular symptoms and artesunate to treat cancer. PMID:24223058

  11. 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.

  12. Effect of antihypertensive agents - captopril and nifedipine - on the functional properties of rat heart mitochondria

    Directory of Open Access Journals (Sweden)

    Ivana Kancirová

    2016-06-01

    Full Text Available Objective(s: Investigation of acute effect on cellular bioenergetics provides the opportunity to characterize the possible adverse effects of drugs more comprehensively. This study aimed to investigate the changes in biochemical and biophysical properties of heart mitochondria induced by captopril and nifedipine antihypertensive treatment. Materials and Methods: Male, 12-week-old Wistar rats in two experimental models (in vivo and in vitro were used. In four groups, the effects of escalating doses of captopril, nifedipine and combination of captopril + nifedipine added to the incubation medium (in vitro or administered per os to rat (in vivo on mitochondrial ATP synthase activity and membrane fluidity were monitored. Results: In the in vitro model we observed a significant inhibitory effect of treatment on the ATP synthase activity (P

  13. The Effect of Captopril on Impaired Wound Healing in Experimental Diabetes

    OpenAIRE

    Ehsan Zandifar; Sajedeh Sohrabi Beheshti; Alireza Zandifar; Shaghayegh Haghjooy Javanmard

    2012-01-01

    We aimed to investigate whether oral administration of captopril modulate wound healing, nitric oxide (NO), and vascular endothelial growth factor (VEGF) concentration in wound fluid of diabetic rats. 48 male Sprague-Dawley rats were divided in four groups (n = 12). The 36 rats were rendered diabetic by streptozotocin. The animals of the first and second groups received 25 and 50 mg/kg/day captopril, respectively, (DM-cap25 and DM-cap50). The animals of the third group were treated by distill...

  14. Captopril in heart failure secondary to a left to right shunt.

    OpenAIRE

    Shaw, N J; Wilson, N.; Dickinson, D F

    1988-01-01

    Captopril was used in 20 infants aged less than 1 year with heart failure secondary to defects with predominantly a left to right shunt that was poorly controlled with digoxin and diuretics. Total daily dose of captopril ranged from 0.88 to 2.5 mg/kg (mean 1.3 mg/kg) in three divided doses. Improvement in the control of heart failure was seen mainly as an increase in the rate of weight gain from a mean of 48 g/week before treatment to 102 g/week on treatment and a decrease in the mean respira...

  15. 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.

  16. 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

  17. Low-dose captopril in the treatment of severe refractory hypertension associated with renal failure

    OpenAIRE

    Bell, G. M.; Doig, A.; Watson, M. L.; Muir, A L; Winney, R. J.

    1982-01-01

    Six patients with severe refractory hypertension and chronic renal failure were treated with a low dose of captopril (mean daily dose 75 mg) in combination with dietary sodium restriction, frusemide and either metoprolol, labetalol or prazosin. Sustained control of blood pressure was achieved in all six patients. Adverse effects noted were severe hyperkalaemia (2 patients), skin rashes (2 patients) and taste disturbance (1 patient).

  18. 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...

  19. 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.

  20. 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.

  1. Validation of a liquid chromatographic method for determination of related substances in a candidate certified reference material of captopril

    Directory of Open Access Journals (Sweden)

    Raquel Nogueira

    2011-06-01

    Full Text Available This paper describes the validation of a reversed-phase high performance liquid chromatography method (RP-HPLC with diode array detection (DAD for determination of related substances (impurities from organic synthesis and degradation products of captopril according to the Brazilian Pharmacopeia IV. The aim of this study was to guarantee the method accuracy for quantification of related substances, an essential requisite to determine, using the mass balance approach, the captopril content in the first Brazilian certified reference material (CRM of an active pharmaceutical ingredient (API, developed by Inmetro. The captopril instability in solution is discussed and the captopril content determined by mass balance is compared to the results from titration and differential scanning calorimetry (DSC.Este artigo descreve a validação de método de cromatografia líquida de alta eficiência em fase reversa (CLAE-RP com detector de fotodiodos (DAD para determinação de substâncias relacionadas (impurezas orgânicas de síntese e produtos de degradação de captopril segundo Farmacopéia Brasileira IV ed. Este estudo teve como objetivo garantir que o método é capaz de quantificar com exatidão o teor de substâncias relacionadas, um requisito essencial para que o teor de captopril seja determinado por balanço de massa no primeiro material de referência certificado (MRC de fármacos brasileiro, o qual foi desenvolvido pelo Inmetro. A instabilidade do captopril em solução é discutida em detalhes e o teor de captopril determinado por balanço de massa é comparado com aqueles obtidos por titulação e por calorimetria exploratória diferencial (DSC.

  2. Participation of kinins in the inhibitory action of captopril on acute hypertension induced by L-NAME in anesthetized rats

    Directory of Open Access Journals (Sweden)

    R. Soares de Moura

    1997-10-01

    Full Text Available The aim of the present study was to investigate the role of bradykinin in the inhibitory action of captopril in hypertension induced by L-NAME in anesthetized rats. Male Wistar rats (260-320 g were anesthetized with chloralose and arterial blood pressure was recorded with a polygraph pressure transducer. The hypertensive effect of L-NAME was studied in rats pretreated with saline, captopril or HOE 140 plus captopril. The effect of captopril was also studied during the sustained pressor effect of L-NAME. The acute pressor effect of L-NAME (10 mg/kg, iv was significantly reduced by iv pretreatment with 2 mg/kg captopril (D increase of 49 ± 4.9 mmHg reduced to 20 ± 5.4 mmHg, P = 0.01. The pressor effect of L-NAME (D increase of 38 ± 4.8 mmHg observed in rats pretreated with captopril and HOE 140 (0.1 mg/kg, iv was not significantly different from that induced by L-NAME in rats pretreated with saline (P = 0.09. During the sustained pressor effect induced by L-NAME (D increase of 49 ± 4.9 mmHg captopril induced a significant (PD decrease of 22 ± 3.0 mmHg. The present results demonstrate that the acute pressor effect of L-NAME is reduced by captopril and this inhibitory effect may be partly dependent on the potentiation of the vasodilator actions of bradykinin

  3. In vitro and in vivo assessment of cellular permeability and pharmacodynamics of S-nitrosylated Captopril, a nitric oxide donor

    OpenAIRE

    Jia, Lee; Wong, Hong

    2001-01-01

    The present studies were aimed at testing the hypothesis that S-nitrosylated captopril (CapNO), a novel crystalline nitric oxide (NO) donor, readily permeates both in vitro and in vivo endothelial monolayers, resulting in its pharmacodynamic effects.CapNO and Captopril (Cap) were added to apical side of endothelial monolayers formed on microporous membranes, and the permeated drugs were collected from basolateral side and detected by a HPLC method. The permeability coefficient (Papp; cm sec−1...

  4. Determination of captopril in pharmaceutical preparation and biological fluids using two- and three-way chemometrics methods

    Institute of Scientific and Technical Information of China (English)

    Nahid Ghasemi; Ali Niazi

    2007-01-01

    Spectrophotometric method has been developed for the direct quantitative determination of captopril in pharmaceutical preparation and biological fluids (human plasma and urine) samples. The method was accomplished based on parallel factor analysis (PARAFAC) and partial least squares (PLS). The study was carried out in the pH range from 2.0 to 12.8 and with a concentration from 0.70 to 61.50 μg mL-1 of captopril. Multivariate calibration models such as PLS at various pH and PARAFAC were elaborated from ultraviolet spectra deconvolution and captopril determination. The best models for this system were obtained with PARAFAC and PLS at pH 2.0. The applications of the method for determination of real samples were evaluated by analysis of captopril in pharmaceutical preparations and biological fluids with satisfactory results. The accuracy of the method, evaluated through the RMSEP, was 0.5801 for captopril with best calibration curve by PARAFAC and 0.6168 for captopril with PLS at pH 2.0 model.

  5. 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.

  6. Captopril for refractory hypertension in patients with chronic renal failure and renal transplantation.

    OpenAIRE

    Hamilton, D V; Evans, D. B.; Maidment, G; Pryor, J S

    1981-01-01

    The converting-enzyme inhibitor, captopril, was given to ten patients with refractory severe hypertension of renal origin: 6 patients had chronic renal failure, 3 patients had hypertension following renal transplantation, and one patient had hypertension and congestive cardiac failure. Control of blood pressure was achieved with doses from 78 to 400 mg/day. Severe hyperkalaemia occurred in one patients, ageusia (dose dependent) in another, and one patients withdrew from treatment because of n...

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

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    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.

  8. Ultrastructural study of renal tubular damage induced by captopril in adult and fetal mice

    Directory of Open Access Journals (Sweden)

    Hamdy H. Swelim and Aleya A.Sakr

    2004-12-01

    Full Text Available The present study has been designed to evaluate the possible nephrotoxicity of the angiotensin converting enzyme inhibitor, captopril on renal tubules of adult and maternally treated fetuses of CD-1 mice. The study included the effect of captopril administration for one month up to three months in adults, while in fetuses, they were exposed to the drug through their mothers in two periods. The first was from 6th-12th days of pregnancy, while the second was from 6th -18th day of pregnancy. The dose used in the present study represents the dose equivalent to the therapeutic daily dose taken by human. All the recorded tissue damage was found to be time dependent. The first remarkable feature noticed in all the treated adult animals was the presence of hyaline casts that obstructed most of the renal tubules. The second remarkable feature was the increase of the intertubular space associated with irregularity of the tubules due to the degeneration and vacuolation of the basal regions of the cells. Renal tubule cells showed large blebs, accumulaton of lipids, degeneration and necrosis. In maternally treated fetuses, the proximal convoluted tubule cells displayed moderate vacuolation and marked increase of lysosomes while some of the distal convoluted tubules revealed atrophy and their cells showed loss of mitochondria. In addition, the collecting tubules showed loss of microprojections. Worthy to mention that there was apparent increase of mesenchymal cells as well as fibroblasts in the fetuses maternally treated with captopril. The significance of these changes was discussed and it should be emphasized that captopril must be taken with caution for pregnant women and those who suffer from renal troubles. Moreover, kidney function should be monitored during therapy .

  9. 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.

  10. Value of renal scintigraphy with captopril test in the exploration of renovascular hypertension: Case report

    International Nuclear Information System (INIS)

    Introduction Dynamic renal scintigraphy with 99mTc-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 99mTc-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)

  11. 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.

  12. Quality by Design approach to understand the physicochemical phenomena involved in controlled release of captopril SR matrix tablets.

    Science.gov (United States)

    Saurí, J; Millán, D; Suñé-Negre, J M; Colom, H; Ticó, J R; Miñarro, M; Pérez-Lozano, P; García-Montoya, E

    2014-12-30

    The aim of this study is to obtain swelling controlled release matrix tablets of captopril using the Quality by Design methodology (ICH Q8) and to know the transport mechanisms involved in captopril release. To obtain the area of knowledge, the design of experiments studying the effect of two components (HPMC K15M and ethylcellulose) at different levels has been applied, with the captopril dissolution profile as the product's most important critical quality attribute (CQA). Different dissolution profiles have been obtained with the design of experiments performed, which is a key factor in the development of controlled release matrix tablets. Kinetic analysis according to the equations of Higuchi and Korsmeyer-Peppas demonstrates that the release mechanism is a mechanism of erosion when the whole percentage of the polymer is ethylcellulose, and a diffusion mechanism when the whole percentage of the polymer is HPMC K15M. The physico-chemical characteristics of the gel layer determine the release rate of captopril. The thickness of the gel layer, the porosity which is formed in the matrix upon contact with water, pore size, the swelling rate, the erosion rate of the matrix, and the physico-chemical characteristics of captopril, are factors related to the kinetic equations described and that allow us to predict the release mechanism of captopril. A new relationship of the kinetic equations governing the in vitro behavior with the physical characteristics of the gel layer of the different formulations has been established. This study shows that the size of water-filled pores and the degree of crosslinking between the chains of HPMC K15M of the matrix are related to the exponent n of the Korsmeyer-Peppas equation and the type of transport of the captopril from within the matrix to the dissolution medium, that is, if the transport is only through water-filled pores, or if a combination of diffusion occurs through water-filled pores with a transport through continuous

  13. 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.

  14. Effects of captopril and a combination of hydralazine and isosorbide dinitrate on myocardial sympathetic tone in patients with severe congestive heart failure.

    OpenAIRE

    Daly, P; Rouleau, J L; Cousineau, D.; Burgess, J H; Chatterjee, K.

    1986-01-01

    Changes in circulating catecholamines and transmyocardial catecholamine balance associated with improved left ventricular function were studied in patients with chronic heart failure after treatment with captopril (10 patients) and hydralazine in combination with isosorbide dinitrate (eight patients). Cardiac performance improved in response to both captopril and hydralazine-nitrate treatment. The systemic haemodynamic effects were also qualitatively similar, but the hydralazine-nitrate combi...

  15. Study of polymorphism of Atenolol and Captopril antihypertensives using x-ray powder diffraction and Rietveld refinement

    Science.gov (United States)

    Sato, Juliana; Ferreira, Fabio

    2013-03-01

    Characterization of bulk drugs has become increasingly important in the pharmaceutical industry. X-ray powder diffractometry is an effective technique for the identification of crystalline solid-phase drugs. The technique is unique, since it combines specificity with a high degree of accuracy for the characterization of pharmaceuticals in solid state and is an especially useful method to describe the possible polymorphic behavior of drugs substances. In this work X-ray diffraction data have been obtained for two well-known antihypertensive drugs currently being administered in tablet form. They include atenolol and captopril. Atenolol and captopril were purchased from drugstore. The characterizations of the atenolol and captopril samples were carried out by FTIR spectroscopy and X-ray powder diffraction (XRPD). We would like to thank the Brazilian agencies CNPq and FAPESP for their financial support.

  16. 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

  17. N-acetylcysteine and captopril protect DNA and cells against radiolysis by fast neutrons

    International Nuclear Information System (INIS)

    N-Acetylcysteine and captopril, respectively mucolytic and antihypertensive drugs, contain free sulfhydryl groups. Since in general thiols have well-established radioprotective abilities, we sought putative radioprotective effects of these drugs against therapeutic fast neutrons. We show that pBR322 plasmid DNA is indeed protected against radiolytic strand breakage by both drugs. The oxygen independent protection is consistent with a hydroxyl radical scavenging mechanism. A clonogenicity assay reveals an increase of the survival of SCL-1 cultured keratinocytes irradiated in the presence of the drugs compared with cells irradiated without drugs. Our results suggest possible interferences between treatment with drugs bearing-SH groups and radiotherapy. (orig.)

  18. Captopril does not interact with the pharmacodynamics and pharmacokinetics of digitoxin in healthy man.

    Science.gov (United States)

    de Mey, C; Elich, D; Schroeter, V; Butzer, R; Belz, G G

    1992-01-01

    The chronic oral administration of 0.07 mg digitoxin o.d. for up to 58 days to 12 healthy volunteers caused a small drop in mean heart rate HR (95% CI: -7.9 to -1.6 beats.min-1), in mean diastolic blood pressure (95% CI: -8.3 to -0.4 mmHg), shortening of the QTc-interval (95% CI: -42 to -19 ms), shortening of the HR-corrected pre-ejection period PEPc (95% CI: -16 to -1 ms) and electromechanical systole QS2c (95% CI: -25 to -1 ms), and an increase in the impedance cardiographic Heather index (dZ/dtmax/RZ, 95% CI: 0.3 to 4.3) relative to the baseline measurements before digitalisation. The concomitant administration of 25 mg oral captopril b.d. did not significantly alter these responses relative to the concomitant double-blind administration of placebo, nor did it alter the pharmacokinetic characteristics of plasma digitoxin at steady state. Thus, no relevant change in the pharmacokinetic and pharmacodynamic characteristics of chronically administered digitoxin were induced by concomitant treatment with captopril. PMID:1451730

  19. A randomized comparative trial of first-dose response to Angiotensin- Converting Enzyme Perindopril and Captopril in Indonesian heart failure patients

    Directory of Open Access Journals (Sweden)

    Lukman H. Makmun

    2002-03-01

    Full Text Available Several large placebo-controlled trials have confirmed that angiotensin converting enzyme (ACE inhibitors significantly reduce mortality aid morbidity in all functional grades of congestive heart failure (CHF, nevertheless only a proportion of patients who may benefit from treatment are priscribed an ACE inhibitor. One of the perceived difficulties is the occurrence of first-dose hypotension in susceptible patients. A double-blind, randomised, single-dose therapy, parallel-group study was conducted with the aim to compare the first-dose responses to low dose ACE inhibitors captopril and perindopril in patients with stable chronic heart failure. Seventy patients (New York Heart Association class I-IV were included. Blood pressure was recorded every 15 minutes 2 hours before starting treatment. The mean of these readings was taken as the baseline blood pressure. Patients were randomised to receive a single-dose of captopril 6.25 mg or perindopril 2 mg. After taking the drug, blood pressure was monitored every 15 minutes for 2 hours, every 30 minutes during 5 hours then hourly after 2 hours. The maximum mean arterial pressure fall from baseline of perindopril was 0.85 mmHg compared to captopril 4.60 mmHg. The maximum mean systolic fall from baseline of perindopril was 3 '31 'mmHg compared to captopril 6.76 mmHg while the maximum mean diastolic fall from baseline of perindopril was 1.08 mmHg compared to captopril 2.63 mmHg. The hypotensive effect of the captopril group started soon after dosing and reached its maximum after 1 to 2 hours while perindopril showed slight reduction of systolic after 1 hour and slight reduction of diastolic after 4 hours. Compared to captopril, perindopril seemed to be less likely to cause first-dose hypotension in patients with heart failure. (Med J Indones 2002; 11: 19-23Keywords: first dose hypotension, perindopril, captopril, chronic heart failure

  20. Conceptuation, formulation and evaluation of sustained release floating tablets of captopril compression coated with gastric dispersible hydrochlorothiazide using 23 factorial design

    OpenAIRE

    Sirisha, Pathuri Lakshmi; Babu, Govada Kishore; Babu, Puttagunta Srinivasa

    2014-01-01

    Ambulatory blood pressure monitoring is regarded as the gold standard for hypertensive therapy in non-dipping hypertension patients. A novel compression coated formulation of captopril and hydrochlorothiazide (HCTZ) was developed in order to improve the efficacy of antihypertensive therapy considering the half-life of both drugs. The synergistic action using combination therapy can be effectively achieved by sustained release captopril (t1/2= 2.5 h) and fast releasing HCTZ (average t1/2= 9.5 ...

  1. Formulation, evaluation and optimization of sustained release matrix tablets of captopril

    Directory of Open Access Journals (Sweden)

    V Pinank Pandya

    2012-01-01

    Full Text Available Sustained release matrix tablet is a delivery system by which the drug can be delivered at a controlled rate for long period of time. The present study aims at formulation, evaluation and optimization of captopril matrix tablets. A 3 2 full factorial design was adopted and all 9 batches were prepared by wet granulation method. Prepared granules and tablets were evaluated for precompression and postcompression characteristics respectively. Check point analysis was applied to the observations and the formula of the tablet was optimized. Optimized formula, F6 showed zero order drug release kinetics for the time period of 24 hours i.e. 17.55% release at the end of 2 hours, 53.4% release at the end of 12 hours and 100.24% release at the end of 24 hours. The results revealed that concentration of matrix forming agent and solution of granulating agent significantly affected in vitro drug release profile.

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

    Directory of Open Access Journals (Sweden)

    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.

  3. Serum levels of renin, angiotensin-converting enzyme and angiotensin II in patients treated by surgical excision, propranolol and captopril for problematic proliferating infantile haemangioma.

    Science.gov (United States)

    Sulzberger, L; Baillie, R; Itinteang, T; de Jong, S; Marsh, R; Leadbitter, P; Tan, S T

    2016-03-01

    The role of the renin-angiotensin system (RAS) in the biology of infantile haemangioma (IH) and its accelerated involution induced by β-blockers was first proposed in 2010. This led to the first clinical trial in 2012 using low-dose captopril, an angiotensin-converting enzyme (ACE) inhibitor, demonstrating a similar response in these tumours. This study aimed to compare serial serum levels of the components of the RAS in patients before and after surgical excision, propranolol or captopril treatment for problematic proliferating IH. Patients with problematic proliferating IH underwent measurements of serum levels of plasma renin activity (PRA), ACE and angiotensin II (ATII) before, and 1-2 and 6 months following surgical excision, propranolol or captopril treatment. This study included 27 patients undergoing surgical excision (n = 8), propranolol (n = 11) and captopril (n = 8) treatment. Treatment with either surgical excision or propranolol resulted in significant decrease in the mean levels of PRA. Surgical excision or captopril treatment led to significant decline in the mean levels of ATII. All three treatment modalities had no significant effect on the mean levels of ACE. This study demonstrates the effect of surgical excision, propranolol and captopril treatment in lowering the levels of PRA and ATII, but not ACE, supporting a mechanistic role for the RAS in the biology of IH. PMID:26612192

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

    Directory of Open Access Journals (Sweden)

    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.

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

    Directory of Open Access Journals (Sweden)

    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

  6. 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

  7. 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 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. PMID:27269004

  8. Effects of curcumin and captopril on the functions of kidney and nerve in streptozotocin-induced diabetic rats: role of angiotensin converting enzyme 1.

    Science.gov (United States)

    Abd Allah, Eman S H; Gomaa, Asmaa M S

    2015-10-01

    Oxidative stress and inflammation are involved in the development and progression of diabetes and its complications. The renin-angiotensin system also plays an important role in the pathogenesis of diabetes and its complications. We hypothesized that curcumin and captopril would restore the kidney and nerve functions of diabetic rats through their angiotensin converting enzyme 1 (ACE1) inhibiting activity as well as their antioxidant and anti-inflammatory effects. Diabetes was induced by a single intraperitoneal injection of streptozotocin (100 mg·kg(-1) body weight). One week after induction of diabetes, rats were treated with 100 mg·kg(-1)·day(-1) curcumin or 50 mg·kg(-1)·day(-1) captopril orally for 6 weeks. Compared with diabetic control rats, curcumin- or captopril-treated diabetic rats had significantly improved blood glucose, lipid profile, kidney/body weight ratio, serum creatinine, blood urea nitrogen (BUN), and pain thresholds assessed by Von Frey filaments, hot plate test, and tail-flick test. Diabetic control rats showed increased levels of total peroxide, renal and neural tumor necrosis factor-α and interleukin-10, and renal ACE1 compared with nondiabetic rats. Although treatment with either curcumin or captopril restored the altered variables, captopril was more effective in reducing these variables. ACE1 was positively correlated with BUN and creatinine and negatively correlated with paw withdrawal threshold, hot plate reaction time, and tail-flick latency, suggesting a possible causal relationship. We conclude that curcumin and captopril protect against diabetic nephropathy and neuropathy by inhibiting ACE1 as well as oxidation and inflammation. These findings suggest that curcumin and captopril may have a role in the treatment of diabetic nephropathy and neuropathy. PMID:26398443

  9. 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.

  10. 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).

  11. 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)

  12. 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.

  13. 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.

  14. Colorimetric microdetermination of captopril in pure form and in pharmaceutical formulations

    Science.gov (United States)

    Shama, Sayed Ahmed; El-Sayed Amin, Alla; Omara, Hany

    2006-11-01

    A simple, rapid, accurate, precise and sensitive colorimetric method for the determination of captopril (CAP) in bulk sample and in dosage forms is described. The method is based on oxidation of the drug by potassium permanganate in acidic medium and determination of the unreacted oxidant by measuring the decrease in absorbance for five different dyes; methylene blue (MB); acid blue 74 (AB), acid red 73 (AR), amaranth dye (AM) and acid orange 7 (AO) at a suitable λmax (660, 610, 510, 520, and 485 nm), respectively. Regression analysis of Beer's plots showed good correlation in the concentration ranges (0.4 12.5, 0.3 10, 0.5 11, 0.4 8.3 and 0.5 9.3 μg ml-1), respectively. The apparent molar absorbtivity, Sandell sensitivity, detection and quantitation limits were calculated. For more accurate results, Ringbom optimum concentration ranges were 0.5 12, 0.5 9.6, 0.6 10.5, 0.5 8.0 and 0.7 9.0 μg ml-1, respectively. The validity of the proposed method was tested by analyzing in pure and dosage forms containing CAP whether alone or in combination with hydrochlorothiazide. Statistical analysis of the results reflects that the proposed procedures are precise, accurate and easily applicable for the determination of CAP in pure form and in pharmaceutical preparations. Also, the stability constant was determined and the free energy change was calculated potentiometrically.

  15. 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

  16. Vasodilatation with captopril and prazosin in chronic heart failure: double blind study at rest and on exercise.

    Science.gov (United States)

    Bayliss, J; Canepa-Anson, R; Norell, M S; Poole-Wilson, P; Sutton, G

    1986-03-01

    A double blind cross over study was performed to compare the long term hormonal, haemodynamic, and clinical responses to specific inhibition of the renin-angiotensin-aldosterone system (captopril) and of the alpha 1 adrenoceptors of the sympathetic system (prazosin) both at rest and during upright exercise in patients with chronic heart failure. Sixteen patients completed one month's treatment with each drug. During conventional diuretic treatment (control) plasma renin activity, aldosterone, and noradrenaline were increased at rest and on exercise. Control left ventricular filling pressures were raised, and correlated significantly with plasma renin activity both at rest and on exercise. Systemic vascular resistance was increased at rest, and its reduction during exercise correlated inversely with the increase in plasma renin activity and plasma noradrenaline. After one month's treatment with captopril there were reductions in plasma aldosterone, weight, left ventricular filling pressure, and systemic vascular resistance at rest and on exercise. Dyspnoea was relieved and exercise capacity increased. The greater fall in systemic vascular resistance on exercise no longer correlated with the increase in plasma renin activity. During treatment with prazosin there were increases in plasma noradrenaline and, transiently, in plasma aldosterone. Fluid retention occurred, and left ventricular filling pressure was unchanged. Compared with control values systemic vascular resistance was reduced at rest but not on exercise. Dyspnoea and exercise capacity did not improve. In chronic heart failure, vasodilatation by inhibition of the alpha adrenergic system with prazosin causes compensatory stimulation of the renin-angiotensin-aldosterone system and does not result in clinical benefit. Inhibition of the renin-angiotensin-aldosterone system with captopril causes secondary vasodilatation at rest and on exercise and results in improvement in symptoms and exercise capacity. PMID

  17. 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.

  18. A comparison of the effects of captopril and enalapril on skin responses to intradermal bradykinin and skin blood flow in the human forearm.

    OpenAIRE

    LI KAM WA, T. C.; Cooke, E D; Turner, P

    1993-01-01

    1. The effects of captopril and enalapril on skin responses to intradermal injections of bradykinin and skin blood flow in the forearm were investigated in this randomised, double-blind, placebo-controlled, cross-over study. 2. Intradermal injections of 0, 1, 2.5 and 5 micrograms of bradykinin in 0.9% sodium chloride were made into the forearm of twelve healthy volunteers before and at 2, 6 and 24 h after single oral doses of 25 mg captopril, 10 mg enalapril or placebo. Forearm skin blood flo...

  19. Pumpkin-seed oil modulates the effect of felodipine and captopril in spontaneously hypertensive rats.

    Science.gov (United States)

    Zuhair, H A; Abd El-Fattah, A A; El-Sayed, M I

    2000-05-01

    Natural products like pumpkin-seed oil (PSO) may modify the potency of the calcium antagonist felodipine (FEL) or angiotensin-converting enzyme inhibitor (ACE-inhibitor), captopril (CPT) in modulating the biochemical derangement in blood, heart and kidney as well as blood pressure and heart rate of spontaneously hypertensive rats (SHR) were investigated. SHR were treated orally with FEL at a dose of 0. 45 mg kg(-1) body wt. or CPT at a dose of 9 mg kg(-1) body wt. once daily for 4 weeks. PSO was administered at a dose of 40 mg kg(-1) body wt. alone or with FEL or CPT in the previous respective dose regimen for the same period to SHR. This study showed that hypertension induced increments the content of malondialdehyde (MDA) by 55% and 38% as well as the activity of glutathione peroxidase (GSH-Px) by 26% and 23% in heart and kidney, respectively, accompanied by reductions in the activity of myocardial superoxide dismutase (SOD) from 3.40+/-0.17 to 2.42+/-0.19 U mg protein(-1)and contents of glutathione (GSH) and protein thiols (PrSHs) in different tissues of SHR as compared to normotensive rats. Treatment of SHR with FEL or CPT monotherapy or combined with PSO produced improvement in the measured free radical scavengers in the heart and kidney. Our results also showed that pretreatment of SHR with PSO for 4 weeks then i.v. administration of FEL or CPT produced a significant beneficial hypotensive action. The results were explained in the light of the antioxidant properties of PSO. Therefore, it is concluded that concomitant administration of FEL or CPT with natural antioxidants can yield a beneficial therapeutic effect and retard the progression of hypertension. PMID:10753555

  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. Comparing the impact of melatonin and captopril on early effects of radiation on the heart tissue by studying glutathione, malondialdehyde, and lactate dehydrogenase enzyme activity in rats

    International Nuclear Information System (INIS)

    Prevention of secondary malignancy while the patient is receiving radiotherapy for the management of primary cancer has been an enormous challenge for biological and medical safety. The aim of the study is to compare protective effects of melatonin and captopril on early effects of radiation on the heart tissue of rats. Forty-eight adult male Wistar rats weighing 180-220 g were used. The rats were divided into six groups and the rats were exposed to 8 Gy whole body dose from Cobalt-60 sources. Thirty minutes prior to irradiation, six animals received melatonin (100 mg/kg body weight), and six animals received captopril (50 mg/kg body weight). All groups were sacrificed 10 days post-irradiation, and hearts were collected. Malondialdehyde (MDA), lactate dehydrogenase (LDH), and glutathione (GSH) were measured to evaluate cellular oxidative stress-induced injury. The biochemical data are presented as mean ± standard error of the mean, and the difference between the groups was analyzed using a two-way variance analysis. Treatment with captopril resulted in a significant increase in LDH and MDA, although the level of GSH was decreased (P < 0.01). MDA and LDH levels were decreased after melatonin treatment while GSH level was increased (P < 0.001). Melatonin has protective effects following radiation, while treatment with captopril post-irradiation seems to be radiosensitizing and does not have protective effects against radiation exposure. (author)

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

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    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

  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. 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

  6. Apamin-Sensitive Small Conductance Calcium-Activated Potassium Channels were Negatively Regulated by Captopril in Volume-Overload Heart Failure Rats.

    Science.gov (United States)

    Hongyuan, Bai; Xin, Dong; Jingwen, Zhang; Li, Gao; Yajuan, Ni

    2016-08-01

    In heart failure (HF), the malignant arrhythmias occur frequently; a study demonstrated that upregulation of I KAS resulted in recurrent spontaneous ventricular fibrillation in HF. However, the regulation of SK channels was poorly understood. The activation of SK channels depended on [Ca(2+)]i and PP2A; studies suggested that angiotensin II can regulate them. So, we hypothesized that in HF, the excess of angiotensin may regulate the SK channels and result in the remodeling of SK channels. To test the hypothesis, we used volume-overload-induced HF rat model, treated with captopril, performed whole-cell patch clamp to record apamin-sensitive currents (I KAS), and I-V curve was studied. The sensitivity of I KAS to [Ca(2+)]i was also explored by setting various [Ca(2+)]i (10, 100, 500, 900, 1000, and 10,000 nM), and the steady-state Ca(2+) response of I KAS was attained and performed Hill fitting with the equation (y = 1/[1 + (EC50/x) (n) ]). Immunofluorescent staining, real-time PCR, Western blot were also carried out to furtherly investigate the underlying molecular mechanisms of the regulation. Captopril significantly decreased the mean density of I KAS when [Ca(2+)]i was 500, 900, 1000, and 10000 nM. The Hill fitting showed significantly different EC50 values and the Hill coefficients and showed captopril significantly shifted rightward the steady-state Ca(2+) response of I KAS. The results of real-time PCR and Western blot demonstrated captopril decreased the mRNA and protein expression of SK3 channels. Captopril significantly downregulated the sensitivity of SK channels to [Ca(2+)]i and the SK3 channels expression in HF, and reversed the SK channels remodeling. PMID:26924798

  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

    Directory of Open Access Journals (Sweden)

    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. Conceptuation, formulation and evaluation of sustained release floating tablets of captopril compression coated with gastric dispersible hydrochlorothiazide using 2(3) factorial design.

    Science.gov (United States)

    Sirisha, Pathuri Lakshmi; Babu, Govada Kishore; Babu, Puttagunta Srinivasa

    2014-04-01

    Ambulatory blood pressure monitoring is regarded as the gold standard for hypertensive therapy in non-dipping hypertension patients. A novel compression coated formulation of captopril and hydrochlorothiazide (HCTZ) was developed in order to improve the efficacy of antihypertensive therapy considering the half-life of both drugs. The synergistic action using combination therapy can be effectively achieved by sustained release captopril (t1/2= 2.5 h) and fast releasing HCTZ (average t1/2= 9.5 h). The sustained release floating tablets of captopril were prepared by using 2(3) factorial design by employing three polymers i.e., ethyl cellulose (EC), carbopol and xanthan gum at two levels. The formulations (CF1-CF8) were optimized using analysis of variance for two response variables, buoyancy and T50%. Among the three polymers employed, the coefficients and P values for the response variable buoyancy and T50% using EC were found to be 3.824, 0.028 and 0.0196, 0.046 respectively. From the coefficients and P values for the two response variables, formulation CF2 was optimized, which contains EC polymer alone at a high level. The CF2 formulation was further compression coated with optimized gastric dispersible HCTZ layer (HF9). The compression coated tablet was further evaluated using drug release kinetics. The Q value of HCTZ layer is achieved within 20 min following first order release whereas the Q value of captopril was obtained at 6.5 h following Higuchi model, from which it is proved that rapid release HCTZ and slow release of captopril is achieved. The mechanism of drug release was analyzed using Peppas equation, which showed an n >0.90 confirming case II transportation mechanism for drug release. PMID:25006552

  10. Hemodynamic and radionuclide effects of acute captopril therapy for heart failure: changes in left and right ventricular volumes and function at rest and during exercise

    International Nuclear Information System (INIS)

    Although the resting hemodynamic effects of captopril in congestive heart failure are known, little information is available about the hemodynamic response to captopril during exercise or about changes in noninvasive measurements of the size and function of both ventricles. In this study, 14 stable New York Heart Association class III patients were given 25 mg of oral captopril. Rest and exercise hemodynamic measurements and blood pool scintigrams were performed simultaneously before and 90 minutes after captopril. The radionuclide studies were analyzed for left and right ventricular end-diastolic volumes, end-systolic volumes, ejection fractions and pulmonary blood volume. The primary beneficial responses at rest were decreases in left and right ventricular end-diastolic volumes from 388 + 81 to 350 + 77 ml (p < 0.01) and from 52 + 26 to 43 + 20 volume units (p < 0.01), respectively, and in their corresponding filling pressures, from 24 + 10 to 17 + 9 mm Hg and 10 + 5 to and + 5 mm Hg (both p < 0.01). Altough stroke volume did not increase significantly, both left and right ventricular ejection fractions increased slightly, from 19 + 6% to 22 + 5% and from 25 + 9% to 29 + 11%, respectively (both p < 0.01). During exercise, similar changes were noted in both hemodynamic and radionuclide indexes. Thus, in patients with moderate symptomatic limitation from chronic heart failure, captopril predominantly reduces ventricular volume and filling pressure, with a less significant effect on cardiac output. These effects persist during exercise, when systemic vascular resistance is already very low. Radionuclide techniques are valuable in assessing the drug effect in these subjects, particularly when ventricular volumes are also measured

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

    Directory of Open Access Journals (Sweden)

    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

  12. 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

  13. Solid and solution NMR studies of the complexation of Ag + with the trans isomer of captopril: Biological activities of this high blood pressure drug along with its Ag + complex

    Science.gov (United States)

    Isab, Anvarhusein A.; Wazeer, Mohamed I. M.

    2006-09-01

    Complexation of Ag + with captopril, 1-[(2 S)-3-mercapto-2-methylpropionyl]- L-proline, has been studied by 1H and 13C-NMR spectroscopy. The equilibrium constants for the trans to cis isomers of captopril bound to Ag + were measured by 1H NMR spectroscopy. It is observed that the trans isomer of the drug binds more strongly to Ag + between pH 5 and 8, as shown by the broadening of the trans isomer's resonances in 13C NMR spectra on complexation. A monodentate complexation of the trans captopril with Ag + via the thiol site is proposed based on the solid-state NMR and IR data. A superior antimicrobial activity is exhibited by the Cap-Ag(I) complex compared to captopril ligand itself against Heterotrotropic Plate Counts (HPC), Pseudomonas aeruginosa and Fecal streptococcus bacteria.

  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. 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.

  16. 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.

  17. Captopril at 50 mg as well as at 100 mg once a day reduces blood pressure for up to 24 h: a double-blind randomized crossover study in mild to moderate hypertensives.

    Science.gov (United States)

    Salvetti, A; Circo, A; Raciti, S; Gulizia, M; Cardillo, R; Miceli, S; Botta, G

    1988-12-01

    The extent and the duration of the antihypertensive effect of captopril, given once a day at a dose of 50 mg, compared with placebo and with the 100 mg once daily dose was studied in 30 mild or moderate uncomplicated essential hypertensives (mean +/- s.e.m. age 52.0 +/- 1.5 years), who responded (mean blood pressure decrease greater than 10%) to a single oral dose (12.5 mg) of captopril. According to a randomized, double-blind, crossover design, they were given 50 mg captopril four times a day, 100 mg captopril four times a day or matched placebo for 1 month. At the end of each treatment period blood pressure and heart rate were measured every 30 min from 3 h before to 2 h after the last dose. Although the heart rate did not change, mean blood pressure after the 50- and 100-mg doses of captopril was consistently significantly (P less than or equal to 0.05) lower than after placebo. The hypotensive effect peaked at the second hour and was still significant 24 h after dosing without any significant differences between the 50- and the 100-mg doses. These findings indicate that captopril, given chronically once a day at a dose of 50 mg to mild to moderate hypertensive responders, exerts its hypotensive effect up to 24 h and that doubling the dose does not increase either the extent or the duration of its action. PMID:3071596

  18. 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.

  19. Effect of captopril and paraquat on expression of p53 and Bcl-2 genes and proteins in rat lung tissue using RT-PCR and immunohistochemistry

    Directory of Open Access Journals (Sweden)

    Azizi E

    2008-10-01

    Full Text Available "n Normal 0 false false false EN-US X-NONE AR-SA MicrosoftInternetExplorer4 /* Style Definitions */ table.MsoNormalTable {mso-style-name:"Table Normal"; mso-tstyle-rowband-size:0; mso-tstyle-colband-size:0; mso-style-noshow:yes; mso-style-priority:99; mso-style-qformat:yes; mso-style-parent:""; mso-padding-alt:0cm 5.4pt 0cm 5.4pt; mso-para-margin:0cm; mso-para-margin-bottom:.0001pt; mso-pagination:widow-orphan; font-size:11.0pt; font-family:"Calibri","sans-serif"; mso-ascii-font-family:Calibri; mso-ascii-theme-font:minor-latin; mso-fareast-font-family:"Times New Roman"; mso-fareast-theme-font:minor-fareast; mso-hansi-font-family:Calibri; mso-hansi-theme-font:minor-latin; mso-bidi-font-family:Arial; mso-bidi-theme-font:minor-bidi;} Background: Paraquat is an herbicide produced and used prevalently worldwide. Studies have shown that lung fibrosis induced by paraquat can be prevented or delayed by certain antioxidants, iron chelating agents, melatonin, and, recently, blood pressure lowering drugs such as captopril."n"n Methods: The protective effects of captopril on paraquat toxicity were studied using RT-PCR and immunohistochemistry to determine the gene and protein expression of p53 and Bcl-2 in lung tissue samples from rats treated with captopril before and after exposure to paraquat."n"n Results: We found no significant difference in the gene and protein expression of p53 in different tissue samples, except for mRNA levels in the lung tissue of captopril-treated rats. However, the protein expression of Bcl-2 is greater in tissue from rats exposed to paraquat alone and paraquat together with pre- and posttreatment with captopril compared to tissue from untreated control rats and from those treated with captopril alone, which can be due to inflammatory responses of lung tissue. By RT-PCR, we were unable to detect Bcl-2 in lung tissue samples."n"n Conclusion: These results show that paraquat does not induce significant DNA damage; therefore, the

  20. 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).

  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. PMID:27638402

  2. Effect of chronic oral administration of a low dose of captopril on sodium appetite of hypothyroid rats: Influence of aldosterone treatment

    OpenAIRE

    Ventura R.R.; Olivares E.L.; Passos Junior D.B.; Ramalho M.J.; Antunes-Rodrigues J.; Reis L.C.

    2001-01-01

    Rats rendered hypothyroid by treatment with methimazole develop an exaggerated sodium appetite. We investigated here the capacity of hypothyroid rats (N = 12 for each group) to respond to a low dose of captopril added to the ration, a paradigm which induces an increase in angiotensin II synthesis in cerebral areas that regulate sodium appetite by increasing the availability of circulating angiotensin I. In addition, we determined the influence of aldosterone in hypothyroid rats during the exp...

  3. 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. PMID:27008813

  4. Comparative study on the ACE inhibitors Quinapril and Captopril for the (Angiotensin converting enzyme) treatment of the decompensated cardiac insufficiency in dog

    International Nuclear Information System (INIS)

    In a randomized study of 52 dogs the efficacy and safety of captopril and quinapril in the treatment of canine heart failure is studied. The drugs were found to be comparably effective. The recommended dosage schedule for the short acting captopril is three times daily 0.5 mg/kg body weight. Quinapril belongs to a newer generation of ACE inhibitors with a longer half life than captopril and the treatment was started with a single dose of 0.5 mg/kg body weight. This dosage schedule was sufficient for the successful therapy of most of the dogs with heart failure phase II (12 of 13), but in 4 of 7 dogs with heart failure phase III and in all of the patients with phase IV the single dose had to be increased and/or the dosing interval of quinapril had to be shortened, because they still showed complaints due to heart failure. We recommend to adjust the dosage schedule of quinapril individually to the severity of heart failure. Therapy should be started once daily with an application of 0,5 mg/kg body weight and the dog should be controlled about one week later. If there are still symptoms of decompensated heart failure, the dosage may be increased gradually until a maximum dosage of 0.5 mg/kg three times daily. Especially for patients with severe heart failure we recommend at least when treatment is started a concomitant diuretic therapy. Echocardiographic evaluation of cardiac function shows if there is an indication for positive inotropic support witha digitalis glycoside. Quinapril, a novel inhibitor of the angiotensin-converting enzyme can ease the management of canine heart failure, because at least in dogs with mild to moderate heart failure dosing interval is longer compared with captopril. Moreover, quinapril is available as 5 mg tablets whereas the smallest captopril tablets contain 12.5 mg agent. It has to be mentioned that expenses for a treatment with ACE inhibitors are significantly higher than for a therapy with digitalis, so frequently above all the

  5. 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.

  6. Modulation of the captopril interference with the activity of some enzymatic biomolecules in monkey kidney vero cells by drug delivery mesoporous silica system

    Directory of Open Access Journals (Sweden)

    Roxana Popovici

    2011-12-01

    Full Text Available The in vitro effect of different formulations of captopril on some cellular enzymatic equipments activities of monkey kidney Vero cells was investigated in the present research. The preparation of the samples of the mesoporous silica nanocomposites, loaded or not with captopril, was described and their effect on membranary Na+-K+-ATP-ase, cell Mg2+-ATP-ase, LDH, Px, GSH-Px, SOD, CAT, ACP, ALP activities were studied. The Vero cells were incubated, for a period of 144 hours, with growing medium renewed twice. When the cells reached confluence in the monolayer stage, the cultures were divided into control cell cultures and other 4 treated groups. To the 12 hours treated cells were added: Cap H2, SBA–15, unfunctionalized SBA-15_CapH2_RT and functionalized SBA-15_APTES_CapH2_80°C nanocomposites, each of them in a dose of 0.4μg./flask. As compared with the control Vero cells, which are characterized by a specific level of the enzymatic activities, the cultures treated with SBA-15 have not presented significant alterations of them. The comparative study of captopril interactions with some membrane bound and intracellular enzymatic biomolecules of monkey kidney Vero cells has revealed either an enhancement of membranary Na+-K+-ATP-ase, intracell total ATP- ase , LDH, ACP , and GSH-Px activities or a repression of cellular CAT, Px and SOD activities. These variations of the enzymatic activities – which induce modifications of the membranary and metabolic processes – could be due to a direct or indirect interaction of captopril with cellular (plasmalemma or subcellular (organelles structures and with intracellular biomolecules (enzymes, DNA, RNA etc.. The association of captoptil with SBA – 15 or SBA – 15 _ APTES mesoporous silica matrices and treatment of Vero cells with these nanocomposites were correlated with modulation of the captopril interference with the activity of investigated enzymatic biomolecules, its sense (stimulation or

  7. 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

  8. 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.

  9. 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)

  10. 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.

  11. [Doppler echocardiographic evaluation of vasodilator treatments in patients with cardiac insufficiency. Contribution to the combination of isosorbide dinitrate and captopril].

    Science.gov (United States)

    Dubourg, O; Jondeau, G; Beauchet, A; Delorme, G; Chikli, F; Weber, S; Bejuit, R; Bourdarias, J P

    1992-04-01

    Hemodynamic evaluation of a vasodilator drug is a difficult exercise in which Doppler echocardiography can be a useful tool. We studied the hemodynamic effect of isosorbide dinitrate (ISDN) by Doppler echocardiography in 7 patients with severe cardiac failure despite prolonged therapy with usually effective doses of captopril. The patients were evaluated before (H0) and 24 hours after treatment by ISDN (120 mg/24 hr) (H24) and 10 minutes after sublingual 0.75 mg of trinitrin (H24 + T). M mode echocardiography did not show any significant changes in chamber dimension as reported after vasodilator therapy in patients without cardiac dilation: in patients with severe left ventricular dilatation a reduction in LV filling pressures causes little if any changes in fractional shortening and ventricular dimensions. Two-dimensional echocardiography showed a reduction in end systolic volume and an increase in ejection fraction, emphasizing the superiority of this technique in cases of abnormal left ventricular function and the sensitivity of indices of systolic function to changes in afterload in these patients. Cardiac output measured by Doppler increased during the study. The maximal acceleration did not change significantly and pulmonary artery pressures were stable after administration of nitrates. ISDN caused a marked change in diastolic mitral flow patterns for which there are several explanations: an effect of ISDN on relaxation or LV compliance or on the conditions of LV filling or on both factors together. The presence of mitral regurgitation and/or atrial arrhythmia prevents the use of Doppler indices for analysis of diastolic LV function.(ABSTRACT TRUNCATED AT 250 WORDS)

  12. 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.).

  13. Which patient benefits from early angiotensin-converting enzyme inhibition after myocardial infarction? Results of one-year serial echocardiographic follow-up from the captopril and thrombolysis study (CATS)

    NARCIS (Netherlands)

    vanGilst, WH; Kingma, JH; Peels, KH; Dambrink, Jan Hendrik Everwijn

    1996-01-01

    Objectives. In this study we sought to investigate the effect of intervention with captopril within 6 h of the onset of myocardial infarction on left ventricular volume and clinical symptoms of heart failure in relation to infarct size during a 1-year follow-up period. Background. Remodeling of the

  14. 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.

  15. 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.

  16. 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. PMID:27591621

  17. Captopril and Hydrochlorothiazide

    Science.gov (United States)

    ... doctor immediately: swelling of the face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs hoarseness difficulty breathing or swallowing fever, sore throat, chills, and other signs of infection yellowing of the skin or eyes dry mouth ...

  18. 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

  19. 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. PMID:23897845

  20. A multicenter, double-blind, randomized, placebo-controlled study of isradipine and methyldopa as monotherapy or in combination with captopril in the treatment of hypertension. The LOMIR-MCT-IH Research Group.

    Science.gov (United States)

    Yodfat, Y; Cristal, N

    1993-03-01

    This multicenter, double-blind, randomized trial of 1 year's duration compared the safety and efficacy of isradipine, methyldopa, and placebo in 368 men, aged 40 to 65 years, with mild-to-moderate essential hypertension. Initial treatment with isradipine (1.25 mg twice daily), methyldopa (250 mg twice daily), or placebo was started after a wash-out and single-blind placebo period. If normotension [diastolic blood pressure (DBP) effect during the first 2 weeks of treatment, monotherapy with isradipine resulted in a higher rate of normalization (more than 64%) compared with 50% in the methyldopa group and 36% in the placebo group. Adding captopril to the treatments of non-responders increased the rate of normalization to 90% in the isradipine group, 84% in the methyldopa group, and 75% in the placebo group. Twenty-one patients dropped-out and 70 patients discontinued the study, the majority because of a lack of efficacy and adverse reactions. The most common adverse reactions reported were cardiovascular and gastrointestinal complaints, headaches, and sleep and sexual disorders, mostly by patients taking methyldopa. Isradipine was well tolerated and the side-effects were minimal. These results indicate that isradipine is superior to methyldopa and, whether as monotherapy or in combination with captopril, highly effective and well tolerated in the treatment of mild-to-moderate hypertension. PMID:8466728

  1. 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.

  2. Study on the Covalent Immobilization of Captopril onto Polymer Microspheres%高分子微球偶联固定卡托普利药物分子的研究

    Institute of Scientific and Technical Information of China (English)

    张妙; 方仕江

    2012-01-01

    The poly (styrene-co-glyeidyl methacrylate) (PSG) latex microspheres were prepared by soap-free emulsion polymerization. The resulted PSG microspheres were further modified with 1,6- hexanediamine as a space arm to get the amino-modified PSGN microsphere. Captopril was coupled onto the surface of PSGN microspheres by the activation with N ethylcarbodiimide hydrochloride (EDC) and polymer microspheres immobilized captopril N-Hydroxysuccinimide ( 3-dimethylaminopropyl )(NHS), so that the affinity was finally obtained. The effects of the ratio and concentration of catalysts, pH, temperature and time on the coupling reaction between the PSGN mierospheres and captopril were examined. It was shown that the effect of immobilization was much better under the condition of 25℃, pH=4.0, m(NHS):m(EDC)=1: 2, m(EDC)=4mg/mL.%采用无皂乳液聚合法制得聚苯乙烯一甲基丙烯酸缩水甘油酯(PSG)乳液微球,然后在微球表面嫁接空间臂分子1,6-己二胺,得到表面含氨基的PSGN微球,接着借助EDC/NHS催化作用将药物分子卡托普利化学偶联到PSGN微球表面,制成固定卡托普利的亲和PSG微球。实验着重考察了PSGN微球偶联固定卡托普利反应过程中催化剂比例和用量、pH值、反应温度和时间等的影响规律。结果表明,在25℃,pH为4.0m(NHS):m(EDC)=1:2,EDC的浓度为4mg/mL的条件下,卡托普利偶联到微球表面的效果较好。

  3. Avaliação do uso do captopril na fibrose peritoneal induzida em ratos pelo uso de solução de glicose a 4,25%

    Directory of Open Access Journals (Sweden)

    Adriana Fátima Menegat Schuinski

    2013-12-01

    Full Text Available INTRODUÇÃO: A Insuficiência Renal Crônica (IRC tem incidência alarmante neste século. A diálise peritoneal, uma das modalidades de terapia renal pode ter complicações, e entre estas a fibrose peritoneal, que ocorre com o decorrer dos anos nestes pacientes. Sua forma mais grave é a chamada peritonite esclerosante encapsulante, levando à mudança de terapia dialítica. OBJETIVO: Estudar a influência do uso do captopril na fibrose peritoneal induzida em ratos pelo uso de solução de glicose a 4,25 %. MÉTODOS: Estudo prospectivo controlado, em ratos Wistar não urêmicos. Foram estudados 20 animais. Os animais foram submetidos diariamente à punção abdominal, sendo infundida solução de diálise peritoneal com glicose a 4,25% na dose de 10 ml/100 g de peso. Os animais foram divididos em 2 grupos: experimental e controle. O grupo experimental recebeu captopril na dose de 30 mg/kg/dia por gavagem. O grupo controle não recebeu nenhuma droga. Foram acompanhados por 21 e 49 dias. Ao final do período foram submetidos à procedimento cirúrgico para retirada de peritônio parietal e visceral. As amostras obtidas foram analisadas histologicamente, usando-se coloração Hematoxilina - Eosina e Sirius Red, para avaliação do grau de fibrose. RESULTADOS: A análise mostrou que a intensidade da fibrose, a espessura do peritônio e o número de células não atingiram diferença estatisticamente significante entre os grupos experimental e controle. CONCLUSÃO: O estudo mostrou que o uso do captopril não foi capaz de alterar a intensidade da fibrose peritoneal induzida pelo uso de solução de diálise em ratos.

  4. Efficacy Observation of Diltiazem Combined with Captopril in the Treatment of Pulmonary Artery Hypertension%地尔硫(卓)联合卡托普利治疗小儿肺动脉高压的疗效观察

    Institute of Scientific and Technical Information of China (English)

    安育林; 周更须; 王辉; 刘宇航

    2012-01-01

    Objective:To observe effectiveness and safety of diltiazem combined with captopril in the treatment of children' s pulmonary artery hypertension (PAH).Methods:62 eligible children were randomly divided into group A,B,C.They were given diltiazem,captopril,combined therapy of diltiazem and captopril respectively for 6months.The changes of systemic bloood pressure(SBP). Diastolic blood pressure(DBP),heart rate (HR), mean pulmonary artery pressure (Mpap) and pulmonary vascular resistance (PVR) in 3 groups were observed before and after administration,and adverse drug reactions were recorded.Results: After administration,,SBP,DBP,HR were decreased in 3 group, and SBP and HR in group C were decreased significatly. Mpap and PVR in group A and C were dropped (P<0.05),and Mpap and PVR in group C were dropped obviously(P<0.01).Compared with group A and B, decreasing of Mpap and PVR in group C had statistical significance (P<0.05). Severe adverse drug reaction was not found in each group Conclusion:Combined therapy of diltiazem and captopril is more efective and safe in the treatment of children' s PAH.%目的:观察地尔硫(卓)联合卡托普利治疗小儿肺动脉高压(PAH)的疗效及安全性.方法:将60例符合条件的患儿随机分成A、B、C组,每组各20例,分别给予地尔硫(卓)、卡托普利、地尔硫(卓)联合卡托普利,每组服药时间均为6个月.观察3组用药前、后体循环收缩压(SBP)、舒张压(DBP)和心率(HR),肺循环平均肺动脉压(mPAP)以及肺血管阻力(PVR)等指标变化,记录用药期间的不良反应.结果:用药后,三组SBP、DBP、HR均下降,C组SBP、HR下降明显(P<0.05);A、B组mPAP、PVR较用药前下降(P<0.05),且C组下降更明显(P<0.01),与A、B组相比,C组下降有统计学意义(P<0.05);各组均未见严重不良反应.结论:地尔硫(卓)联合卡托普利治疗小儿PAH更有效,且安全.

  5. 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

  6. 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

  7. Effects of captopril on experimental inhibitting of atherosclerosis in rabbit model%卡托普利对家兔实验性动脉粥样硬化的抑制作用

    Institute of Scientific and Technical Information of China (English)

    陈宇; 姜亦忠; 令孤志宏; 王志武; 于振香; 王春燕; 朴晓玲

    2001-01-01

    Objective To study the effects of captopril in atherosclerosis.Methods The models were developed by feeding high triglyc eride,high cholesterol diet.Serial measurement of blood cholesterol,triglyce rides,HDL,LDL of the rabbits were performed through out this period.At the end o f the experiment,the rabbits were killed and pathologic examinations were perfor med and the atherosclerosis lesion areas were measured.Results Increase of TG and LDL levels of the rabbits were inhibitted in captopril pretreatment group and selenium+Vitamine E treatment gr oup,but there were no significant differences in HDL and cholesterol levels in t hese groups.The area of atherosclerosis lesions of the rabbits was the smallest in p retreatment group compared with the other groups(P<0.01).Electron micros c opic pathologic examination showed that in atherosclerosis group,there were endo thelium necrosis,lipid deposits and SMC were mainly synthesized type,whereas in s elenium+Vitamine E treated group the changes of endotheium were insignifcant and SMC were mainly contracted type.Conclusions The study show captopril can delay the progre ss of the formation and development of athersoclerosis from various pathways.%目的 探讨卡托普利对平滑肌细胞增生、移行、动脉硬化形成和发展的影响,并进一步研究动脉粥样硬化(AS)的发病机制和AS家兔模型的制作方法。方法 选择日本大耳白兔利用高脂、高胆固醇膳食法建立AS模型,制作过程中动态观察血胆固醇(TC)、甘油三酯(TG)、低密度脂蛋白(LDL)、高密度脂蛋白( HDL)水平。实验结束后处死动物做病理学检查(光镜和电子显微镜),并做AS面积的测定。结果 卡托普利和硒维尔+VE联合用药可抑制TG及LDL 的升高,而对HDL和TC影响不大。AS斑块面积的测定以预防组最小。病理电镜片可见动脉硬化组内皮细胞坏死、脂质沉积,SMC以合成表型为主,硒维尔+VE联合用药内皮

  8. 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.

  9. The effects of captopril on serum uric acid in the elderly hypertensi on%卡托普利对老年高血压患者血尿酸的影响

    Institute of Scientific and Technical Information of China (English)

    邓学科; 杨柏松; 魏丽萍

    2001-01-01

    Objective To expl ore the effects of captopril on serum ur ic acid in aged patients with hypertensi on. Methods Fifty-five aged patients were treated with captopril,and their s erum acid,renal function,serum electrolytes and the clinical symptoms were examined b efore and after treatment respectively. Results Before treatment and after treatment of 2 weeks,4 weeks and 6 weeks,serum uric acid was(277.23±6 4.48)μmol.L-1,(375.63±114.01)μmol.L - 1,(394.71±98.72)μmol.L-1 and (352.44 ±138.81)μmol.L-1 respectively.After t reatment serum uric acid was markedly in creased(P<0.05)and no significant vari an ce was found in their renal function and serum electrolytes(P>0.05).There were 40 age d patients with high serum uric acid aft er treatment,including 8 cases temporari ly and 32 cases continuously(5 cases wit h arthritic symptoms:joint pain,red-edem a,etc.). Conclusions When th e elderly hypertension treated with capo pril,serum uric acid could elevate and a rthritic symptoms could develop as a res ult of serious high serum uric acid.The elderly who are treated with captopril s h ould have their serum uric acid examined regularly.%目的 探讨卡托普利对老年高 血压患者血尿酸的影响。 方法 观察55例老年高血压患者服 药前后血尿酸、尿素氮(BUN)、肌酐(Cr)、血钾(K+)、血钠(Na+)、血氯化物(Cl- )的变化及临床症状。 结果 服药后血尿酸升高〔2、4周和6 周 分别为(375.63±114.01)μmol.L-1、(394.71±98.72)μmol.L -1和(352.44±138.81)μmol.L-1〕,与服药前〔(277.23±64.48)μ mol.L-1〕相比有显著性差异(P<0.05)。BUN、Cr、K+、Na+ 、Cl无明显变化。服药后有40例患者血尿酸升高。其中,8例(14. 55%)血尿酸呈暂时性升高;32例(58.18%)血尿酸呈持续性升高,5例(9.08%)出现关节疼痛 、红肿等症状。 结论 老年高血压患

  10. Effect of captopril on the expression of tumor necrosis factor-alpha and matrix metalloproteinases-2in rats with myocardial infarction%卡托普利对大鼠心肌梗死后肿瘤坏死因子-α和基质金属蛋白酶-2表达的影响

    Institute of Scientific and Technical Information of China (English)

    上官海娟; 官洪山; 赵艳锋

    2011-01-01

    Objective To investigate the effect of captopnl on ventncular remadeling and cardiac function and the expres sion tumor necrosis factor-alpha( TNF-α ) and matrix metalloproteinase-2 ( MMP-2 ) in rats with myocardial infarction. Methods Myocardial infarction model was established by ligation of the anterior descending coronary artery in rats. After 24 hours of opera tion, survival rats were randomly divided into model group, model + captopril group ( rats were treated with 500 mg · kg -1 · d - 1 cap topril in their drinking water),twelve rats in each group. Six rats were selected randomly without ligation as sham operation group. The sham operation group and model group were treated with water. Six weeks after operation , TNF-α and type Ⅰ and Ⅲ collagen were detected with immunohistochemistry; MMP-2 protein were detected by westem-blot; Collagen volume fraction ( CVF) was assessed with Van Gieson. Left ventricular haemodynamics changes were recorded with baroceptor. Results Com pared with sham operation group, the left ventricular function of rats in model group and model + captopril group were obvi ously degraded( P < 0. 05 ) ; Captopril could significantly improve ventricular function after myocardial infarction ( P < 0. 05 ) . CVF and type Ⅰ /Ⅲ collagen ratio of non-infarct zone in model group and model + captopril group were significantly higher than those in sham operation group( P < 0. 01 ) ;Total hean weight/ body weight ( THW/BW) and left ventricular weight / body weight ( LVW/BW) obviously increased ( P <0. 01) . But the CVF, type Ⅰ/Ⅲ collagen ratio, THW/BW and LVW/BW in model + captopril group were significantly lower than those in the model group( P < 0. 05 ) . The expression of TNF-α and MMP 2 in the non-infarcted zone of model group were significantly higher than those in sham operation group ( P <0. 01) ; But in model + captopril group, the expression of TNF-α and MMP-2 were decresed compared with model group (P <0. 01

  11. 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

  12. Alteration of Gaq/11-Mediated Signal Transduction Pathway in Heart and Aorta of 2K1C rat after Captopril Treatment%卡托普利治疗后2K1C肾性高血压大鼠心脏和主动脉Gαq/11介导的信号转导通路的变化

    Institute of Scientific and Technical Information of China (English)

    白桦; 邢东琦; 吴立玲

    2002-01-01

    Objective To investigate the alteration of Gαq/11-mediated signal transduction pathway in heart and aorta of 2K1C renal hypertensive rats and the effect of captopril treatment. Methods Renal hypertension was performed by placing a sliver clip around the left renal artery. Captopril (150 mg/kg) was given from 4 to 8 weeks after operation. Systolic blood pressure was recorded by the tail-cuff method each week after surgery, the ratio of left ventricular weight to body weight (LV/BW) and morphologic changes in aorta were measured at 4 and 8 weeks after operation. The levels of Gαq/11 in heart and aorta were detected by Western Blot analysis, and phospholipase C (PLC) activities were determined by using [3H] PIP2 as substrate. Results 2K1C renal hypertensive rats had significant hypertension, cardiac hypertrophy and aorta thickening 4 and 8 weeks after operation. Systolic blood pressure and the LV/BW decreased to the level of sham group 4 weeks after captopril treatment while the morphologic change in aorta was not significant. For 2K1C group, Gαq/11 levels and PLC activities increased dramatically both in heart and in aorta at 4 weeks that remained at high levels until 8 weeks after the operation. After captopril treatment, the Gαq/11 level and PLC activity in heart decreased by 15.8% and 30.9% respectively with no changes in aorta. Conclusion Gαq/11-mediated signal transduction pathway participated in the development and maintain of 2K1C renal hypertension. Captopril reversed cardiac hypertrophy and this effect may be attributed by inhibiting the formation of angiotensin Ⅱ and, therefore, abolishing the activation of Gαq/11-mediated signal transduction pathway induced by angiotensin Ⅱ.%目的研究Gαq/11介导的信号转导通路在2K1C肾性高血压大鼠心脏和主动脉中的变化以及卡托普利治疗对其的影响. 方法制备2K1C肾性高血压大鼠模型, 于术后4~8周给予卡托普利(150 mg/kg),观察尾动脉收缩压、左室重

  13. 雷公藤多甙并卡托普利治疗小儿肾病型紫癜性肾炎疗效分析%Efficacy of tripterygium wilfordii polyglycoside and captopril in the treatment of children with kidney-type purpura nephritis

    Institute of Scientific and Technical Information of China (English)

    周嘉云; 张爱莉

    2010-01-01

    Objective To observed the efficacy of tripterygium wilfordii polyglycoside and captopril in the treatment of children with Henoch-Schonlein purpura nephritis kidney disease model. Methods One hundred and one children diagnosed with kidney-type purpura nephritis from May 1996 to June 2009 in our hospital, were respectively, randomly divided into treatment group (58 cases,oral tripterygium wilfordii polyglycoside and captopril) and the control group (43 patients, single-dose oral prednisone), observation of therapeutic effects of drugs in the two groups of children with edema, hypertension, hematuria, proteinuria efficacy, using SPSS10.0 software for statistical analysis. Results Fifty-one patients were cured (88%), effective in 7 patients (12%) in the treatment group, the control group cured 26 cases (61%), effective in 17 cases (39%), there was significant difference between the two groups (P<0.01). Pairs of edema, hematuria, hypertension were significantly different between the two groups(P<0.05 or P<0.01), and the efficacy of proteinuria was also significantly different (P<0.01). Conclusions Tripterygium wilfordii polyglycoside and captopril treatment of children with Henoch-Schonlein purpura nephritis kidney disease model is superior to single-dose prednisone, it is worth clinical application.%目的 观察雷公藤多甙并卡托普利对小儿肾病型紫癜性肾炎的治疗效果.方法 将101例诊断为肾病型紫癜性肾炎的患儿随机分为治疗组58例(口服雷公藤多甙和卡托普利)和对照组43例(口服单剂强的松),观察药物对两组患儿水肿、高血压、血尿、蛋白尿的疗效,采用SPSS10.0软件进行统计学分析.结果 治疗组治愈51例(88%),有效7例(12%);对照组治愈26例(61%),有效17例(39%),两组治愈率比较差异有统计学意义(P<0.01),对水肿、血尿、高血压的疗效比较差异有统计学意义(P<0.05或P<0.01),对蛋白尿的疗效比较差异亦有统计学意义(P<0.01).结论 雷

  14. 胺碘酮协同卡托普利对老年高血压伴阵发性心房颤动疗效观察%The clinical research of the treatment of Captopril and Amiodarone to elderly hypertensive patients with paroxysmal atrial fibrillation

    Institute of Scientific and Technical Information of China (English)

    谢基连; 林小青; 李仕宁

    2009-01-01

    Objective: To evaluate the treatment of Captopril and Amiodarone to cure the elder hypertension and paroxysmal atrial fibrillation. Methods: 70 cases of elderly hypertensive patients with paroxysmal atrial fibrillation were randomly divided into Amiodarone group and combination group (Captopril combined Amiodarone), they were treated of 12 months, the rhythm control of the two groups after treatment 3, 6, 9,12 months and the left atrial diameter after treatment 6, 12 months were calculated. Results: There were significant changes of the blood pressure after treatment in each group, but no significant difference between two groups. The rate of rhythm control of the combination group was significant higher than that of the Amiodarone group after 9 and 12 months treatment. The change of the left atrial diameter was significant between the two groups after 12 months treatment. Conclusion: Captopfil combined with Amiodarone can decrease the blood pressure, inhibit left atrial enlargement and effective in preventing recurrence of atrial fibrillation in elderly hypertensive paroxysmal atrial fibrillation.%目的:观察卡托普利联合胺碘酮治疗老年高血压伴阵发性心房颤动(房颤)患者的疗效.方法:将70例老年高血压伴阵发性房颤患者随机分为胺碘酮组和联合用药组(卡托普利联合胺碘酮),治疗12个月,计算两组治疗后第3、6、9、12个月的窦性心律维持率和治疗前及治疗后第6、12个月的左心房内径.结果:研究期结束后各组内治疗前后血压变化比较具有显著性,但两组间治疗后血压无显著性差异.治疗后9、12个月,联合用药组的窦性心律维持率显著高于胺碘酮组.两组间左心房内径在治疗后12个月时胺碘酮组显著高于联合用药组.结论:卡托普利联合胺碘酮治疗老年高血压伴阵发性房颤,可抑制左房扩大,并有效预防房颤复发.

  15. 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

  16. Improvement effect of captopril on insulin resistance mediated by PPARγin vascular endothelial cells%PPARγ介导卡托普利改善高糖诱导血管内皮细胞胰岛素抵抗的作用

    Institute of Scientific and Technical Information of China (English)

    严国强; 陈春香; 陈芳辉; 高艳; 储佳佳; 李腾; 黄起壬

    2015-01-01

    Aim To investigate the role of captopril in insulin resistance of endothelial cells induced by high glucose.Methods 1 .Improvement effect of captopril on insulin resistance in HUVECs was observed.The HUVECs were seeded in a 6-well plate and were ran-domly divided into 5 groups,namely,control group, IR group,IR together with different Cap concentrations (low,medium and high concentration),respectively. 2.Improvement effect of Cap on insulin resistance was mediated by PPARγin HUVECs.HUVECs were ran-domly divided into 6 groups,namely,control group, control +PPARγinhibitor (PI)(1 .0 μmol · L -1 ) group,IR group,IR +PI(1 .0 μmol·L -1 )group,IR +Cap(1 ×1 0 -5 mol·L -1 ) group,and IR +Cap +PI (1 .0 μmol·L -1 )group.All indicators were detected. Results After HUVECs were incubated with media containing 33 mmol·L -1 of glucose for 48 h,the NO levels were significantly decreased while ET-1 levels were significantly elevated,showing a significant differ-ence between IR group and control group (P 0.05).When the HUVECs in IR group were treated with DMEM containing glucose (33 mmol·L -1 )for 48 h and insulin for 30 min,the expression levels of PPARγmRNA and its protein in Cap groups were simi-lar to those in the IR group,and there was no signifi-cant difference between the two groups (P >0.05 );however, the expression levels of phosphorylated PPARγprotein in Cap groups were increased compared with IR group (P <0.05).The levels of NO were sig-nificantly increased whereas the levels of ET-1 were decreased in Cap groups,which had significant differ-ences compared with IR group (P <0.05).Nonethe-less,pre-treating with GW9662,a PPARγinhibitor, the improvement effects of Cap were markedly abol-ished.Conclusions Captopril could improve high glucose-induced insulin resistance of endothelial cells mediated by PPARγ,and the underlying mechanisms are related to the activation of PPARγ,rather than its expression.%目的:研究卡托

  17. 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.

  18. 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

  19. Efficacy of atenolol and captopril in reducing risk of macrovascular and microvascular complications in type 2 diabetes: UKPDS 39

    OpenAIRE

    1998-01-01

    Objective: To determine whether tight control of blood pressure with either a β blocker or an angiotensin converting enzyme inhibitor has a specific advantage or disadvantage in preventing the macrovascular and microvascular complications of type 2 diabetes.

  20. Scintigraphic diagnosis of early signs of heart failure and their correction with captopril in patients with myocardial infarction

    International Nuclear Information System (INIS)

    Potentialities of the radionuclide methods for diagnosis as applied to identification of the early signs of cardiac insufficiency (CI) in patients having had a myocardial infarction (MI) were studied as well as capoten effect on the character of revealed hemodynamics alterations. It was shown that the dynamic assessment of scintigraphic parameters of pulmonary circulation in patients permitted to identify the preclinical CI signs opportunely. Use of capoten low doses (up to 25 mg/d) in patients with MI from the acute period serves as the efficient method for correcting revealed hemodynamics failures

  1. Evaluation of Keishi-bukuryo-gan in a diabetic nephropathy model by comparison with aminoguanidine, butylated hydroxytoluene and captopril

    OpenAIRE

    Nakagawa, Takako; Oya, Takeshi; Sasahara, Masakiyo; Terasawa, Katsutoshi; Yokozawa, Takako

    2002-01-01

    桂枝茯苓丸の糖尿病性腎症に対する作用を,モデルラットを用い検討した。腎機能パラメーター,病理組織学的検討に加え,advanced glycation end products(AGEs)の蓄積,酸化ストレスに及ぼす影響を,アミノグアニジン(AGEs阻害薬),カプトプリル(アンジオテンシン変換酵素阻害薬),buthylated hydroxytoluene(BHT)(抗酸化剤)とで比較検討した。桂枝茯苓丸では腎機能(血清Cr,尿蛋白排泄量)と病理所見の有意な改善作用が認められ,糖尿病性腎症の進展を抑制することが実験的に明らかとなったが,このような腎保護作用はカプトプリルよりは弱く,アミノグアニジンと同程度であった。BHTには腎保護作用は認められなかった。腎組織中のAGEsの蓄積に対しては,桂枝茯苓丸,カプトプリル,BHTがいずれも有意に低下していたが,アミノグアニジンの作用よりは弱かった。腎組織中の脂質過酸化量はBHTで最も低下し,桂枝茯苓丸,カプトプリルでも有意に低下していた。一方,血中脂質過酸化に対しては,すべてにおいて有意な低下作用が認められたが,カプトプリルで最も強かった。...

  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 ... ...hiazide [DR:D00340] Antihypertensive ATC code: C09BA01 Anatomical Therapeutic Chemi

  3. Preparation of a Matrix Type Multiple-Unit Gastro Retentive Floating Drug Delivery System for Captopril Based on Gas Formation Technique: In Vitro Evaluation

    OpenAIRE

    Meka, Lingam; Kesavan, Bhaskar; Chinnala, Krishna Mohan; Vobalaboina, Venkateswarlu; YAMSANI, MADHUSUDAN RAO

    2008-01-01

    A gastro retentive floating drug delivery system with multiple-unit minitab’s based on gas formation technique was developed in order to prolong the gastric residence time and to increase the overall bioavailability of the drug. The system consists of the drug-containing core units prepared by direct compression process, which are coated with three successive layers of an inner seal coat, effervescent layer (sodium bicarbonate) and an outer gas-entrapped polymeric membrane of an polymethacryl...

  4. Preparation of a matrix type multiple-unit gastro retentive floating drug delivery system for captopril based on gas formation technique: in vitro evaluation.

    Science.gov (United States)

    Meka, Lingam; Kesavan, Bhaskar; Chinnala, Krishna Mohan; Vobalaboina, Venkateswarlu; Yamsani, Madhusudan Rao

    2008-01-01

    A gastro retentive floating drug delivery system with multiple-unit minitab's based on gas formation technique was developed in order to prolong the gastric residence time and to increase the overall bioavailability of the drug. The system consists of the drug-containing core units prepared by direct compression process, which are coated with three successive layers of an inner seal coat, effervescent layer (sodium bicarbonate) and an outer gas-entrapped polymeric membrane of an polymethacrylates (Eudragit RL30D, RS30D, and combinations of them). Only the system using Eudragit RL30D and combination of them as a gas-entrapped polymeric membrane could float. The time to float decreased as amount of the effervescent agent increased and coating level of gas-entrapped polymeric membrane decreased. The optimum system floated completely within 3 min and maintained the buoyancy over a period of 12 h. The drug release was controlled and linear with the square root of time. Increasing coating level of gas-entrapped polymeric membrane decreased the drug release. Both the rapid floating and the controlled release properties were achieved in the multiple-unit floating drug delivery system developed in this present study. The analysis of the parameter dissolution data after storage at 40 degrees C and 75% RH for 3 months showed, no significant change indicating the two dissolution profiles were considered to be similar (f2 value is more than 50). PMID:18459051

  5. 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...

  6. Early pharmacologic intervention may prevent the deterioration in endothelial function after experimental myocardial infarction in rats: effects of ibopamine and captopril.

    NARCIS (Netherlands)

    Buikema, H.; van Veldhuisen, D.J.; Hegeman, H.; van Gilst, W.H.

    1997-01-01

    BACKGROUND: Endothelial function is progressively disturbed after myocardial infarction (MI), which may be related to both neurohumoral activation and hemodynamic alterations. Consequently, it may be suggested that drugs that favorably affect these factors may also have a positive effect on endothel

  7. Effect of Captopril, An Angiotensin-Converting Enzyme Inhibitor, on Experimental Pulmonary Fibrosis%卡托普利对实验性肺间质纤维化的干预作用

    Institute of Scientific and Technical Information of China (English)

    夏蕾; 徐启勇; 叶燕青

    2003-01-01

    目的:观察血管紧张素转换酶(ACE)活性在博莱霉素(BLM)所致大鼠肺间质纤维化过程中的动态变化,了解ACE抑制剂卡托普利(CPT)对大鼠肺纤维化模型的影响.方法:45只SD大鼠随机分为3组:对照组、模型组和用药组.模型组和用药组经气管内注入BLM诱导肺纤维化,随即分别每日胃管内灌注生理盐水和CPT(60 mg*kg-1*d-1)进行干预;对照组气管和胃管内灌注均以生理盐水代替.各组动物均于气管内灌药后7,14,28 d 分别处死5只,测动物体重及肺湿重,取肺组织做HE染色,Ⅰ、Ⅲ型胶原的免疫组化,并行图像分析;心腔内取血测ACE的活性.结果:血清ACE活性在气管内灌注BLM后迅速上升,第7 d 达到高峰(与对照组比P<0.01),随后下降,到第28 d 基本恢复正常.CPT能显著降低血清中ACE的活性,减少肺内胶原的表达,减轻肺泡炎和肺纤维化的程度.结论:CPT能减轻BLM诱导的大鼠肺泡炎和肺纤维化.

  8. Mortality and morbidity remain high despite captopril and/or valsartan therapy in elderly patients with left ventricular systolic dysfunction, heart failure, or both after acute myocardial infarction - Results from the Valsartan in Acute Myocardial Infarction Trial (VALIANT)

    NARCIS (Netherlands)

    White, HD; Aylward, PEG; Huang, Z; Dalby, AJ; Weaver, WD; Barvik, S; Marin-Neto, JA; Murin, J; Nordlander, RO; van Gilst, WH; Zannad, F; McMurray, JJV; Califf, RM; Pfeffer, MA

    2005-01-01

    Background - The elderly constitute an increasing proportion of acute myocardial infarction patients and have disproportionately high mortality and morbidity. Those with heart failure or impaired left ventricular left ventricular function after acute myocardial infarction have high complication and

  9. Effectiveness of Captopril in Combination with Low-Dose Hydro-chlorothiazide for Systemic Hypertension%卡托普利与小剂量氢氯噻嗪合用治疗高血压疗效观察

    Institute of Scientific and Technical Information of China (English)

    龚铭; 叶向阳; 陈锡刚

    2000-01-01

    目的:研究卡托普利与小剂量氢氯噻嗪合用对高血压患者的疗效及对代谢的影响.方法:50例原发性高血压患者随机分为两组,第1组:单用卡托普利12.5 mg~7 5 mg,每日2~3次.第2组:卡托普利12.5 mg,每日2次,加服氢氯噻嗪12.5 mg,每日1次,两组治疗时间均为8周,测定治疗前后的基础血压,空腹血糖、血脂、血钾、血尿酸、尿素氮、肌酐, 以及治疗前后的24小时动态血压.结果:卡托普利加小剂量氢氯噻嗪组的总有效率及24小时动态血压结果均明显优于单用卡托普利组,而且两组治疗前后的代谢指标均无明显改变.结论:卡托普利与小剂量氢氯噻嗪合用治疗高血压较单用卡托普利更有效,而且对代谢无明显影响.

  10. Lupus induced by medicaments

    International Nuclear Information System (INIS)

    We describe a 55 years old female patient who consulted by fever syndrome, artralgias and the presence of high tittles positives antinuclear antibodies. She had arterial hypertension in treatment with captopril. We suspected the clinical diagnoses of drug-induced lupus; the withdraw of captopril was associated with the remission of the clinical and laboratory manifestations

  11. Ramipril

    Science.gov (United States)

    ... a class of medications called angiotensin-converting enzyme (ACE) inhibitors. It works by decreasing certain chemicals that tighten ... pharmacist if you are allergic to ramipril; other ACE inhibitors such as benazepril (Lotensin, in Lotrel), captopril (Capoten), ...

  12. Benazepril

    Science.gov (United States)

    ... a class of medications called angiotensin-converting enzyme (ACE) inhibitors. It works by decreasing certain chemicals that tighten ... pharmacist if you are allergic to benazepril; other ACE inhibitors such as captopril (Capoten), enalapril (Vasotec, in Vaseretic), ...

  13. Trandolapril

    Science.gov (United States)

    ... a class of medications called angiotensin-converting enzyme (ACE) inhibitors. It works by decreasing certain chemicals that tighten ... pharmacist if you are allergic to trandolapril; other ACE inhibitors such as benazepril (Lotensin, in Lotrel), captopril (Capoten), ...

  14. Fosinopril

    Science.gov (United States)

    ... a class of medications called angiotensin-converting enzyme (ACE) inhibitors. It works by decreasing certain chemicals that tighten ... pharmacist if you are allergic to fosinopril; other ACE inhibitors such as benazepril (Lotensin, in Lotrel), captopril (Capoten), ...

  15. Enalapril

    Science.gov (United States)

    ... a class of medications called angiotensin-converting enzyme (ACE) inhibitors. It works by decreasing certain chemicals that tighten ... pharmacist if you are allergic to enalapril; other ACE inhibitors such as benazepril (Lotensin, in Lotrel), captopril (Capoten), ...

  16. ABNORMAL LEFT VENTRICULAR SYSTOLIC AND DIASTOLIC FUNCTIONAL RESPONSE TO ISOMETRIC EXERCISE IN IDIOPATHIC DILATED CARDIOMY-OPATHY:BENEFICIAL EFFECT OF CAPTOPRIE

    Institute of Scientific and Technical Information of China (English)

    沈卫峰; 张宪; 胡厚达; 龚兰生

    1995-01-01

    In 19 patients with idiopathic dilated cardiomyopathy and symptoms of congetive haert failure,left ventricular (LV) systolic performance and diastolic velocity profiles were assessed by two-dimensional e-chocardiography and pulsed wave Doppler at rest and during handgrip exercise before and ninety minutes after administration of captopril (mean dose 25±12mg);range 12.5-50mg).Although heart rate and blood pressure increased similarly during handgrip exercise before and after captopril treatment,both were lower with handgrip exercise during captopril treatment.The results from this study indicated that acute angiotensin converting enzyme inhibition with captopril reduces preload and afterload and ameliorates hand-grip exercise-induced LV systolic and diastolic filling dysfunction in patients with congestive bheart failure secondary to idiopathic dilated cardiomyopathy.

  17. Pustulosis palmoplantaris udløst af angiotensinkonverterende enzymhaemmere

    DEFF Research Database (Denmark)

    Eriksen, Jesper Grau; Christiansen, J J; Asmussen, I

    1995-01-01

    demonstrated that the arachidonic acid system may play a role in the pathogenesis of psoriasis/volar pustulosis. Our patient was treated with Captopril and developed a rash identical to volar pustulosis within six weeks. Captopril was substituted with Perindopril, and the eruptions had almost disappeared five...... months later after a short systemic treatment with steroids. One month later the patient developed the same rash. Perindopril was withdrawn and the eruptions had disappeared two months later....

  18. 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

  19. 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.

  20. 卡托普利对大鼠心肌组织丝裂素活化蛋白激酶表达的影响%Affects of captopril on expression of mitogen-activated proten kinase in myocardium of renal hypertension rats

    Institute of Scientific and Technical Information of China (English)

    孙银平; 白桦; 邢东琦; 吴立玲

    2001-01-01

    目的探讨卡托普利对肾性高血压大鼠心肌组织丝裂素活化蛋白激酶(MAPK)表达的影响.方法复制二肾一夹高血压动物模型作为实验组,术后4周开始给予卡托普利者作为治疗组,以未进行二肾一夹者为对照组.术后8周测定动脉血压、心肌肥大指数及心肌组织MAPK的表达.结果与对照组相比,实验组动脉血压及心肌肥大指数显著升高,MAPK表达显著增强(P<0.01);卡托普利显著降低心肌MAPK的表达.结论心肌MAPK表达增强可能是血管紧张素II介导的心肌肥大信号转导通路中的重要环节.

  1. 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.

  2. 氯沙坦与卡托普利对冠心病患者胰岛素抵抗作用的临床研究%Comparison of effects of losartan and captopril on insulin resistance in coronary heart desease

    Institute of Scientific and Technical Information of China (English)

    穆叶赛; 刘金岩; 米热古力; 许力舒

    2003-01-01

    目的观察氯沙坦(科素亚)与卡托普利(开搏通)对冠心病患者胰岛素抵抗(ISR)的影响.方法将70例伴有胰岛素抵抗的冠心病患者在原扩冠,抗凝(消心痛+aspirin)等治疗基础上,随机分为2组,35例为氯沙坦治疗组(A组):每日服氯沙坦1次,50~100mg;35例为卡托普利治疗组(B组):每日服卡托普利3次,每次12.5~25mg;同时选择健康人25例为正常对照组(C组).疗程为3个月.治疗前后用放射免疫法检测胰岛素(IS),氧化酶法检测糖耐量(OGTT),测定血糖,计算胰岛素敏感性指数(CNL IS)及胰岛素抵抗指数(HOMA IR),治疗前后比较,并与正常对照组进行组间比较.结果两组治疗前空腹血糖,空腹及餐后2h胰岛素、HOMA IR、CNL IS与对照组比较差异有统计学意义(P<0.01),治疗后这些指标均有不同程度改善(P<0.05).两组体重指数(BMI)、腰围、空腹血糖、甘油三酯、血压等指标变化与对照组比较差异有统计学意义(P<0.01).这些指标在治疗后与治疗前比较变化有统计学意义(P<0.05).结论冠心病患者存在胰岛素抵抗.氯沙坦和卡托普利都能提高冠心病患者胰岛素敏感性,改善胰岛素抵抗.

  3. Effect of Captopril on Cardiomyocyte Apoptosis and Expression of Apoptosis-associated Genes in Rats with Heart Failure Post-infarction%卡托普利对心力衰竭大鼠心肌细胞凋亡和凋亡相关基因表达的影响

    Institute of Scientific and Technical Information of China (English)

    官洪山; 王虹; 哈黛文

    2005-01-01

    目的:研究心肌细胞凋亡和凋亡相关基因在心力衰竭发展中的变化及卡托普利的干预作用,从细胞凋亡角度探讨血管紧张转化酶抑制剂治疗心力衰竭的机制.方法:选用雄性SD大鼠,随机分为假手术组(sham组)、心梗组(MI组)和心梗后卡托普利干预组(MI+Cap组),经冠脉前降支结扎术建立心肌梗死模型,术后24小时的MI+Cap组大鼠给予Cap 400mg.kg-1.d-1,饮水给药,sham组和MI组大鼠饲普通饮用水.术后4周、6周检测大鼠非心梗区心肌细胞凋亡指数;western蛋白印迹检测心肌细胞凋亡加速基因Bax和凋亡抑制基础Bcl-2的蛋白表达水平,并计算Bax/Bcl-2蛋白比;压力传感器记录左室血流动力学改变.结果:①术后6周非心梗区心肌细胞凋亡指数,MI组及MI+Cap组均显著高于sham组(P<0.01),但MI+Cap组显著低于MI组(P<0.01);②与sham 组相比,MI组和MI+Cap组术后6周时的Bax蛋白表达量均显著增高(P<0.01),但MI+Cap组显著低于MI组(P<0.01);MI组和MI+Cap组的Bcl-2蛋白表达量均低于sham组(P<0.01),而MI+Cap组显著高于MI组(P<0.01);③MI组和MI+Cap组大鼠的心功能明显降低(与sham组比,P<0.01),而MI+Cap组大鼠的心功能显著改善(与MI组比,P<0.01).结果:血管紧张素转化酶抑制剂可通过调节凋亡相关基因Bax和Bcl-2的蛋白表达,减少心肌细胞凋亡,改善心功能.

  4. 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.

  5. 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

  6. 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.

  7. 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.

  8. 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.

  9. 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. PMID:26917399

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

    OpenAIRE

    David Chaupis-Meza; Juan Rojas; Manuel Gasco; Gustavo F. Gonzales

    2014-01-01

    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 ar...

  11. 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.

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

    International Nuclear Information System (INIS)

    Highlights: ► Thermodynamic and kinetic parameters of weak interactions in binary systems by DSC. ► Energy-barrier decrease for lactose dehydration induced by clobazam. ► Recrystallisation of metastable liquid clobazam induced by anhydrous alpha lactose. ► Decrease of lactose dehydration temperature in binary mixtures with captopril. ► 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 α-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.

  13. 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

  14. Influence of converting enzyme inhibition on the hormonal and renal adaptation to hyper- and hyponatraemic dehydration.

    Science.gov (United States)

    Gardes, J; Gonzalez, M F; Corvol, P; Ménard, J

    1986-04-01

    The present study was designed to investigate in rats the influence of converting enzyme inhibition with captopril on blood pressure, plasma urea, plasma renin concentration (PRC), plasma aldosterone and plasma vasopressin, and to define the interrelationships between PRC and these variables during equal degrees of either hyponatraemic (furosemide, 40 mg/kg for 2 days) or hypernatraemic (48-h water deprivation) dehydration. Chronic treatment with captopril (40 mg/kg daily) decreased blood pressure by 19% in normally hydrated treated rats, by 27% in water-deprived treated rats and by 40% in furosemide-treated rats. Plasma renin concentration, plasma aldosterone and plasma vasopressin were increased during both hypo- and hypernatraemic dehydration. Captopril decreased plasma aldosterone in water-deprived and furosemide-treated rats, whereas plasma vasopressin was unchanged. The significant correlation observed between plasma aldosterone and PRC in non-treated rats persisted in treated rats, the same level of plasma aldosterone being observed at values of PRC 10 times higher. On the other hand, the correlation between plasma vasopressin and PRC did not persist in captopril-treated rats. An increase in plasma urea was observed in both water-deprived treated rats and furosemide-treated rats. These data indicate that during hypo- and hypernatraemic dehydration, the renin-angiotensin system plays a role in regulating blood pressure, urea elimination and plasma aldosterone, but vasopressin regulation is not modified by its inhibition.

  15. 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.

  16. 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 l...

  17. 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 patien...

  18. 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...

  19. Drug hypersensitivity syndrome

    OpenAIRE

    Rashmi Kumari; Dependra K Timshina; Devinder Mohan Thappa

    2011-01-01

    Drug hypersensitivity syndrome (DHS) is an adverse drug reaction commonly associated with the aromatic antiepileptic drugs (AEDs), viz., phenytoin (PHT), carbamazepine (CBZ), phenobarbital (PB), lamotrigine, primidone, etc. It can also be caused by other drugs, such as sulfonamides, dapsone, minocycline, gold derivatives, cyclosporine, captopril, diltiazem, terbinafine, azathioprine and allopurinol. Diagnosis of DHS may be difficult because of the variety of clinical and laboratory abnormalit...

  20. 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.

  1. 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...

  2. Nyrearteriestenose--diagnostik og behandling

    DEFF Research Database (Denmark)

    Pedersen, Erling Bjerregaard; Andersen, Ulrik Bjørn

    2009-01-01

    Screening for renal artery stenosis (RAS) should be restricted to patients with a high RAS risk. Captopril renography, computed tomography (CT)-angiography, magnetic resonance (MR)-angiography and ultrasound (US) Doppler can be used. Most patients should receive medical treatment. If predictive...

  3. 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. PMID:27212217

  4. The role and rationale of nuclear medicine procedures in the differential diagnosis of renovascular hypertension

    International Nuclear Information System (INIS)

    The use of radionuclides in the differential diagnosis of renovascular hypertension has gone through many periods of enthusiasm and of disappointment. Regardless of the problems with the routine renogram, the availability of gamma camera renal evaluation makes possible meaningful preintervention of screening. The use of the test as a follow-up procedure is an extremely important but often overlooked application of radionuclides in the evaluation of renovascular hypertension. The radionuclide technique is a sensitive and accurate method of evaluating the results of percutaneous angioplasty or surgery or renal function in the affected kidney of patients with renovascular disease. A major change in our approach to the nuclear medicine diagnosis of renovascular hypertension has been the introduction of captopril renography. Although there is still a great deal of work to be done and many investigators are actively studying captopril renography, the potential of the test is clear. Captopril renography should include a baseline renogram, followed by the administration of 25 mg of captopril and a repeat study. Specificity and sensitivity data on this test probably will not be available for several years, but preliminary results are encouraging enough to justify routine use at this time in clinics in which screening for renovascular hypertension is carried out. (author)

  5. 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

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

    Directory of Open Access Journals (Sweden)

    Sandeep Kumar

    2016-02-01

    Full Text Available 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

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

    International Nuclear Information System (INIS)

    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

  8. 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.

  9. 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.

  10. 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

  11. 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.

  12. 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 of 60 Wistar rats were randomly divided into control group without modeling operation,and another 4 groups using subcutaneous injections of isopropyl adrenaline for 10 d to set up the MF model:model group with saline lavage treatment after modeling,captopril group with captopril lavage,ginseng mixture group A and group B with low and high dose mixture treatment respectively.After treatment for 14 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 group B were significantly lower than that of model group and group A(P<0.05);Model group and group A showed a higher hydroxyproline(Hyp)content in myocardial tissue than the control group and lower catalase(CAT)activity than Gontrol group(P<0.05);captopril group and group B showed a lower Hyp content and higher CAT activity compared with group A and model group(P<0.05),a significantly lower level of serum glutathione peroxidase(GSH-PX)and CAT and a higher level of serum creatine kinase,lactate dehydrogenase and H2O2 in model group and group A were observed compared with the control group(P<0.05).A higher level of GSH-PX and CAT and a lower level of creatine kinase,lactate dehydrogenase and H2O2 in captopril group and group B were observed compared with group A and model group(P<0.05);and histopathological examination showed that in captopril group and group B,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 of MF.

  13. 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

  14. Different angiotensin-converting enzyme inhibitors have similar clinical efficacy after myocardial infarction

    DEFF Research Database (Denmark)

    Hansen, Morten L; Gislason, Gunnar H; Køber, Lars;

    2008-01-01

    efficacy. Risk of all-cause mortality: trandolapril (reference) 1.00, ramipril 0.97 (0.89, 1.05), enalapril 1.04 (0.95, 1.150), captopril 0.95 (0.83, 1.08), perindopril 0.98 (0.84, 1.15) and other ACE inhibitors or angiotensin II receptor blockers (ARB) 1.06 (0.94, 1.19). Reinfarction: trandolapril...... (reference) 1.00, ramipril 0.98 (0.89, 1.08), enalapril 1.04 (0.92, 1.17), captopril 1.05 (0.89, 1.25), perindopril 0.96 (0.81, 1.14) and other ACE inhibitors or ARB 0.99 (0.86, 1.14). Furthermore, the association between ARBs and clinical events was similar to ACE inhibitors (trandolapril reference): all...

  15. Reversible diminished renal sup(99m)Tc-DMSA uptake during converting-enzyme inhibition in a patient with renal artery stenosis

    Energy Technology Data Exchange (ETDEWEB)

    Kremer Hovinga, T.K.; Beukhof, J.R.; Donker, A.J.M.; Luyk, W.H.J. van; Piers, D.A.

    1984-03-01

    A patient is described who had accelerated hypertension and unilateral renal artery stenosis, and who developed further deterioration in renal function during treatment with captopril, an angiotension-I (AI) converting-enzyme inhibitor. sup(99m)Tc-DMSA uptake was greatly diminished in the stenotic kidney, although renal blood flow and handling of /sup 131/I hippurate was preserved. Uptake of sup(99m)Tc-DMSA in the affected kidney returned after substitution of captopril by the vasodilator minoxidil, while a comparable degree of blood pressure control was maintained. This, caution must be taken when interpreting results of sup(99m)Tc-DMSA scintigraphy in patients with proven or suspected renal artery stenosis treated with an AI converting-enzyme inhibiting drug. Moreover, our finding points to the importance of glomerular filtration in the renal handling of /sup 99/Tc-DMSA.

  16. Renal autoregulation in medical therapy of renovascular hypertension

    OpenAIRE

    Lubas, Arkadiusz; Żelichowski, Grzegorz; Próchnicka, Agnieszka; Wiśniewska, Magdalena; Wańkowicz, Zofia

    2010-01-01

    Introduction Renovascular hypertension (RVH) is caused by renal ischaemia associated with haemodynamically significant renal artery stenosis (RAS). The choice of optimal treatment of atherosclerotic RAS is still controversial. Increase in the renal resistive index (RI) value after captopril administration is considered to indicate preserved renal autoregulation. The objective of the study was to assess the effect of medical therapy of RVH on renal autoregulation efficiency in patients with at...

  17. Role of the endogenous kallikrein-kinin system in modulating vasopressin-stimulated water flow and urea permeability in the toad urinary bladder.

    OpenAIRE

    Carvounis, C P; Carvounis, G; Arbeit, L A

    1981-01-01

    This study investigates the endogenous kallikrein-kinin system's role as a modulator of vasopressin action in the toad urinary bladder. Kalli-krein inhibition by aprotinin, which results in decreased kinin production, significantly increased both vasopressin and 8-Br-cyclic (c) AMP-stimulated water flow. Kinin potentiation by the kininase II inhibitor captopril (SQ 14225) significantly decreased vasopressin and 8-Br-cAMP-stimulated water flow. In contrast to water flow, vasopressin-stimulated...

  18. Nuove ipotesi patogenetiche nel pemfigo indotto da farmaci: ruolo dell'acetilcolinesterasi e meccanismi di autofagia

    OpenAIRE

    Petrazzuolo, Marcella

    2009-01-01

    Il pemfigo è una malattia autoimmune potenzialmente letale, che interessa la cute e le mucose, caratterizzata dal distacco delle cellule dell’epitelio stratificato (acantolisi). Il pemfigo si sviluppa in seguito ad un’ interazione tra fattori endogeni (genetici) ed esogeni. Infatti, in letteratura sono riportati differenti casi di sviluppo o esacerbazione della malattia in pazienti direttamente esposti a pesticidi, o sottoposti al trattamento con farmaci come il captopril o l'enalapril per pe...

  19. 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.

  20. [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.

  1. [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. PMID:8529571

  2. Relationship between insulin resistance and plasma endothelin in hypertension patients

    International Nuclear Information System (INIS)

    To explore the relationship between plasma endothelin and hypertension insulin resistance, and the improvement of insulin resistance in hypertension patients treated with captopril and l-amlodipine, 25 patients with primary hypertension and impaired glucose tolerance were selected and treated by captopril and l-amlodipine. Systolic pressure, diastolic pressure, fasting blood glucose, insulin and insulin antibody were measured before and after treatment and compared with healthy controls. The results showed that the plasma ET-1 level in hypertension group was significantly higher than that of healthy controls (P<0.01), and he plasma ET-1 level was positively correlated with FPG, FINS, Anti-INS, HOMA-IR. The systolic pressure, diastolic pressure, fasting blood glucose, insulin, insulin antibody and insulin resistance index in hypertension patients were decreased significantly after treatment (P<0.05). There is a good correlation between endothelin and insulin resistance index in hypertension patients. Captopril and l-amlodipine had obvious improvement effect on insulin resistance in hypertension patients. (authors)

  3. 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.

  4. Long-Term Effect of an Aqueous Fraxinus excelsior L. Seed Extract in Spontaneously Hypertensive Rats

    Directory of Open Access Journals (Sweden)

    Noemi López-Carreras

    2014-01-01

    Full Text Available The effect of long-term intake of different doses (20, 40, and 60 mg/kg/day of a Fraxinus excelsior L. seed extract (FESE on spontaneously hypertensive rats (SHR was evaluated. Water was used as control and captopril (50 mg/kg/day was used as positive control. Systolic blood pressure, body weight, and food and liquid intake were registered weekly in SHR. The antioxidant and vascular relaxing properties of FESE were also studied in these animals. The development of hypertension was attenuated in the groups treated with captopril or FESE. The antihypertensive effect was more accentuated in the captopril group than in the FESE groups, and it was paradoxically more accentuated in the groups treated with 20 mg/kg/day or 40 mg/kg/day of FESE than in the group treated with the highest dose of this extract. Body weight gain and food intake increased in the FESE groups. After removing the corresponding antihypertensive treatment, the arterial blood pressure and the body weight of the FESE treated animals returned to control values. In addition, FESE increased plasma antioxidant capacity and decreased plasma and liver malondialdehyde levels. Moreover, acetylcholine relaxation improved in the aorta rings from the FESE treated rats.

  5. 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

  6. Reversal of cardiac fibrosis in deoxycorticosterone acetate-salt hypertensive rats by inhibition of the renin-angiotensin system.

    Science.gov (United States)

    Brown, L; Duce, B; Miric, G; Sernia, C

    1999-01-01

    Fibrosis impairs cardiac function. This project has determined the expression and deposition of collagens and fibronectin and cardiac function in the deoxycorticosterone acetate (DOCA)-salt hypertensive rat after inhibition of the renin-angiotensin system. DOCA-salt hypertension was induced in 8-wk-old male Wistar rats by uninephrectomy and administration of DOCA (25 mg every fourth day, subcutaneously) and 1% NaCl in the drinking water for 4 wk. Starting 2 wk after surgery, rats were given either oral captopril (100 mg/kg), oral candesartan cilexetil (2 mg/kg), or subcutaneous spironolactone (50 mg/kg) daily for 2 wk (reversal protocol). DOCA-salt rats failed to gain weight with markedly increased water intake and decreased food intake; drug treatment did not alter these parameters. Systolic BP increased from 116+/-5 mmHg in uninephrectomized rats to 179+/-7 mmHg in DOCA-salt rats and was not decreased by treatment (captopril 172+/-1 mmHg; candesartan 187+/-2 mmHg; spironolactone 178+/-3 mmHg). Captopril, candesartan, and spironolactone reversed the increased collagen I mRNA in DOCA-salt rats; only candesartan reversed the increased collagen III mRNA. Collagen IV mRNA was unchanged in DOCA-salt rats and following treatment. Total fibronectin mRNA increased without changing the proportion of fibronectin mRNA as the fetal isoforms EIIIA and EIIIB. Captopril, candesartan, and spironolactone reversed the increased deposition of perivascular and interstitial collagen in DOCA-salt rats; the increased cardiac fibronectin deposition was reversed by candesartan and spironolactone. Captopril, candesartan, and spironolactone also attenuated or reversed the increased diastolic stiffness and the increased dP/dt but not the increased rate-pressure products in DOCA-salt rat hearts. Thus, inhibition of the renin-angiotensin system reverses cardiac fibrosis in DOCA-salt rats and returns some indices of myocardial function to normal. PMID:9892155

  7. 脂多糖对大鼠肺微血管内皮细胞ACE和ACE2表达的影响及血管紧张素转换酶抑制剂的干预作用%Effects of lipolysaccharide on expression of ACE and ACE2 in rat pulmonary microvascular endothelial cells and intervention effects of angiotensinconverting enzyme inhibitor

    Institute of Scientific and Technical Information of China (English)

    李亚春; 李颖川; 周明; 江伟

    2012-01-01

    目的 观察脂多糖(LPS)对大鼠肺微血管内皮细胞(PMVECs)血管紧张素转换酶(ACE)和血管紧张素转换酶2(ACE2)表达的影响及血管紧张素转换酶抑制剂( ACEI) Captopril的干预作用.方法 组织块法体外培养大鼠PMVECs,观察LPS对PMVECs作用的时间和浓度相关毒性以及Captopril的干预作用;再将PMVECs随机分为4组:对照组(n=6),不加干预措施;Captopril组(n=6),10-5mol/L Captopril孵育细胞8 h;LPS组(n=6),1 mg/mL LPS孵育细胞8 h;Captoril+ LPS组(n=6),10-5 moL/L Captopril孵育细胞30 min后再加入1 mg/mL LPS孵育8h.CCK8检测细胞活性;Western blotting法检测各组细胞ACE和ACE2的表达.结果 LPS可对大鼠PMECs产生明显的毒性作用,并可使细胞ACE表达上调及ACE2表达下降;经Captopril干预后,可明显抑制LPS的细胞毒性作用,并逆转LPS对PMVECs中ACE及ACE2表达的影响,使ACE和ACE2表达水平回调至对照组水平.结论ACEI能减轻LPS所致的PMVECs毒性作用,而ACE及ACE2表达的变化可能在这一过程中起重要作用.%Objective To investigate the effects of lipolysaccharide (LPS) on expression of angiotensin-converting enzyme (ACE) and angiotensin-converting enzyme 2 (ACE2) in rat pulmonary microvaeculai endothelial cells (PMVECs) and the intervention effects of angiotensin-converting enzyme inhibitor (ACEI) Captopril. Methods Rat PMVECs were cultured in vitro with tissue explants adherant method, the toxic effects of LPS on PMVECs were investigated by treatment of PMVECs with different concentrations of LPS for different time, and the intervention effects of Captopril were observed. PMVECs were randomly divided into control group (without intervention, n = 6), Captopril group (treatment with 10 -5 mol/L Captopril for 8 h, n =6), LPS group (treatment with 1 mg/mL LPS for 8 h, n =6) and Captoril + LPS group (treatment with 10 -5 mol/L Captopril for 30 min and 1 mg/mL LPS for 8 h, n =6) . Cell viability was determined by CCK8, and the

  8. 穴位埋线对慢性心力衰竭大鼠血压与心功能的影响%Influence of Acupoint-catgut-implantation on Blood Pressure and Cardiac Function in Chronic Congestive Heart Failure Rats

    Institute of Scientific and Technical Information of China (English)

    邓元江; 梁伟雄; 程淑意

    2011-01-01

    Objective To observe the effect of acupoint-catgut-implantation on blood pressure and cardiac function in chronic heart failure (CHF) rats. Methods A total of 60 SD female rats were randomly divided into shem-operation group (sham), CHF model group, catgut-implantation group, Captopril group. CHF model was established by suprarenal abdominal artery constriction. Surgical catgut (No. 3-0, 2-3 mm length piece) was implanted into bilateral “Neiguan” (PC 6), “Xinshu” (BL 15) and “Zusanli” (ST 36) twice for 7 weeks. Rats of the Captopril group were treated with intragastric infusion of Captopril from the 50th day on after the operation, once daily for 7 weeks. Blood pressure (BP) including the systolic blood pressure (SBP), diastolic blood pressure (DBP) and mean blood pressure (MBP), heart rate (HR) and the left ventricular ejection fraction (LVEF)were detected respectively by cardiac sonography. Results On the 14th week after modeling, in comparison with the sham group, the SBP, DBP, MBP and HR in rats of the model group were increased significantly (P<0.01, P<0.05), while LVEF of the model group was decreased considerably (P<0.01). Compared with the model group, the SBP, DBP, MBP and HR after 7 weeks' treatment in rats of the catgut-implantation and Captopril groups were decreased considerably (P<0.01), while the LVEF of the catgut-implantation group was increased evidently (P<0.05). No significant differences were found between the catgut-implantation and Captopril groups in the SBP, DBP, MBP and HR levels, and between the model and Captopril groups in LVEF values (P>0.05). Conclusion Acupoint-catgut-implantation can down-regulate BP and HR, and increase LVEF in chronic congestive heart failure rats, which may contribute to its effect in ameliorating the cardiac function.%目的:探讨穴位理线对慢性心力衰竭大鼠血压与心功能的干预作用.方法:将雌性SD大鼠随机分为假手术组、心衰模型组、穴位埋线组

  9. 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.

  10. 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

    2014-09-01

    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

  11. 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.

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

    Directory of Open Access Journals (Sweden)

    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.

  13. Angiotensin II and vasopressin are involved in the defense system against anaphylactic hypotension in anesthetized rats.

    Science.gov (United States)

    Wang, Mofei; Shibamoto, Toshishige; Kuda, Yuhichi; Sun, Lingling; Tanida, Mamoru; Kurata, Yasutaka

    2014-05-15

    Anaphylactic shock is sometimes life-threatening, but the defense system against this circulatory failure was not fully understood. Ameliorating roles of angiotensin (ANG) II and vasopressin in anaphylactic hypotension were investigated in anesthetized ovalbumin-sensitized Sprague-Dawley rats. The sensitized rats were randomly allocated to the following pretreatment groups (n=7/group): (1) control (non-pretreatment), (2) ANG II synthesis inhibitor captopril, (3) ANG II receptor antagonist losartan, and (4) V1a vasopressin receptor antagonist. Anaphylactic shock was induced by an intravenous injection of the antigen. The systemic arterial pressure (SAP), central venous pressure (CVP), portal venous pressure (PVP) and portal venous blood flow (PBF) were measured, and splanchnic vascular resistance (Rspl: (SAP-PVP)/PBF) was determined. In the control group, SAP markedly decreased, followed by a gradual recovery toward baseline. Rspl transiently decreased immediately after antigen, and then increased 1.5-fold at 15 min and thereafter. The pretreatment with either losartan, captopril or V1a receptor antagonist augmented the initial fall of SAP and attenuated the SAP recovery along with augmentation of the late increase in Rspl. The 2-h survival rate was significantly smaller in either pretreatment group than in the control group (100%). Plasma levels of ANG II and vasopressin increased to 3.8- and 9.8-fold, respectively, at 30 min after antigen in the control group, whereas captopril pretreatment inhibited the increase in ANG II. In conclusion, inhibition of ANG II or vasopressin exacerbates anaphylaxis-induced hypotension in anesthetized rats. PMID:24650734

  14. 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

  15. Metformin Exhibits Radiation Countermeasures Efficacy When Used Alone or in Combination with Sulfhydryl Containing Drugs

    OpenAIRE

    Miller, Richard C.; Murley, Jeffrey S.; David J Grdina

    2014-01-01

    Metformin, a biguanide drug used in the treatment of type II diabetes, was evaluated alone and in combination with amifostine, captopril, MESNA or N-acetyl-cysteine (NAC) for its ability to protect when administered 24 h after irradiation. Mouse embryo fibroblasts (MEF), human microvascular endothelial cells (HMEC) and SA-NH mouse sarcoma cells were exposed to 4 Gy in vitro. C3H mice were exposed to 7 Gy and evaluated utilizing an endogenous spleen colony assay system. Amifostine and WR1065, ...

  16. 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.

  17. Protection of Angiotensin converting enzyme Inhibitor and receptor antagonist in cardiovascular system%血管紧张素转换酶抑制剂及受体拮抗剂的心血管系统保护作用

    Institute of Scientific and Technical Information of China (English)

    黄元伟

    2002-01-01

    @@ 1血管紧张素转换酶抑制剂(ACEI)作用广泛,主要用于心血管疾病的防治 目前在我国上市的已有卡托普利(Captopril)、依那普利(enalapril)、西拉普利(Cilazapril)、培哚普利(Perindopril)、赖诺普利(Lisinopril)、苯那普利(benazepril)、福辛普利(Fosinopril)、雷米普利(rimipri).

  18. 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.

  19. 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. PMID:27287157

  20. Peganum Harmala L. Extract Reduces Oxidative Stress and Improves Symptoms in 6-Hydroxydopamine-Induced Parkinson's Disease in Rats.

    Science.gov (United States)

    Rezaei, Maryam; Nasri, Sima; Roughani, Mehrdad; Niknami, Zeinab; Ziai, Seyed Ali

    2016-01-01

    Parkinson's disease is one of the most common neurodegenerative disorders. There are many documents about the effects of oxidative stress in Parkinson's disease etiology. Angiotensin II activates NADPH dependent oxidases and causes superoxides formation. Peganum harmala L. extract, which has angiotensin converting enzyme (ACE) inhibitory effect, is considered to evaluate oxidative stress inhibition and Parkinson's disease improvement. Male rats weighting 200-250 g were divided into 5 groups: Control, Neurotoxin (injection of 6-hydroxydopamine into left hemisphere substantia nigra), Peganum harmala's seeds aqueous extract (10 mg/kg) and captopril (5 mg/kg). Peganum harmala and captopril were injected intraperitonealy -144, -120, -96, -72, -48, -24, -2, 4 and 24 h relative to 6-hydroxydopamine injection time. Muscle stiffness, apomorphine induced unilateral rotation, amount of brain's protein oxidation and lipid peroxidation, ACE activity and histology of substantia nigra were assayed in all groups. Peganum harmala improved Muscle stiffness and one-direction rotation behavior significantly. It also reduced brain's lipid and protein oxidation levels in neurotoxin-injected rats significantly. In Peganum harmala group compared to control group, brain's ACE activity was significantly inhibited. In histological study, Peganum harmala prevented degeneration of dopaminergic neurons, too. In conclusion, aqueous extract of Peganum harmala could prevent symptoms and reduced oxidative stress markers in rats with Parkinson's disease induced by 6-hydroxydopamine. PMID:27610168

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

    Science.gov (United States)

    Kopaliani, Irakli; Martin, Melanie; Zatschler, Birgit; Müller, Bianca; Deussen, Andreas

    2016-09-01

    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. PMID:27508250

  3. Cardiovascular-Active Venom Toxins: An Overview.

    Science.gov (United States)

    Rebello Horta, Carolina Campolina; Chatzaki, Maria; Rezende, Bruno Almeida; Magalhães, Bárbara de Freitas; Duarte, Clara Guerra; Felicori, Liza Figueiredo; Ribeiro Oliveira-Mendes, Bárbara Bruna; do Carmo, Anderson Oliveira; Chávez-Olórtegui, Carlos; Kalapothakis, Evanguedes

    2016-01-01

    Animal venoms are a mixture of bioactive compounds produced as weapons and used primarily to immobilize and kill preys. As a result of the high potency and specificity for various physiological targets, many toxins from animal venoms have emerged as possible drugs for the medication of diverse disorders, including cardiovascular diseases. Captopril, which inhibits the angiotensin-converting enzyme (ACE), was the first successful venom-based drug and a notable example of rational drug design. Since captopril was developed, many studies have discovered novel bradykinin-potentiating peptides (BPPs) with actions on the cardiovascular system. Natriuretic peptides (NPs) have also been found in animal venoms and used as template to design new drugs with applications in cardiovascular diseases. Among the anti-arrhythmic peptides, GsMTx-4 was discovered to be a toxin that selectively inhibits the stretch-activated cation channels (SACs), which are involved in atrial fibrillation. The present review describes the main components isolated from animal venoms that act on the cardiovascular system and presents a brief summary of venomous animals and their venom apparatuses. PMID:26812904

  4. 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.

  5. Proopiomelanocortin but not vasopressin or renin-angiotensin system induces resuscitative effects of central 5-HT1A activation in haemorrhagic shock in rats.

    Science.gov (United States)

    Sowa, P; Adamczyk-Sowa, M; Zwirska-Korczala, K; Pierzchala, K; Adamczyk, D; Paluch, Z; Misiolek, M

    2014-10-01

    The aim of this study was to determine the effectory mechanisms: vasopressin, renin-angiotensin system and proopiomelanocortin-derived peptides (POMC), partaking in the effects of serotonin through central serotonin 1A receptor (5-HT1A) receptors in haemorrhagic shock in rats. The study was conducted on male Wistar rats. All experimental procedures were carried out under full anaesthesia. The principal experiment included a 2 hour observation period in haemorrhagic shock. Drugs used - a selective 5-HT1A agonist 8-OH-DPAT (5 μg/5 μl); V1a receptor antagonist [β-mercapto-β, β-cyclo-pentamethylenepropionyl(1),O-me-Tyr(2),Arg(8)]AVP (10 μg/kg); angiotensin type I receptor antagonist (AT1) ZD7155 (0.5 mg/kg, i.v.); angiotensin-converting-enzyme inhibitor captopril (30 mg/kg, i.v.); melanocortin type 4 (MC4) receptor antagonist HS014 (5 μg, i.c.v.). There was no influence of ZD715, captopril or blocking of the V1a receptors on changes in the heart rate (HR), mean arterial pressure (MAP), peripheral blood flow or resistance caused by the central stimulation of 5-HT1A receptors (P≥0.05). However, selective blocking of central MC4 receptors caused a slight, but significant decrease in HR and MAP (Pvasopressin systems do not participate in these actions. PMID:25371525

  6. 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.

  7. 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.

  8. The renogram in renovascular hypertension

    International Nuclear Information System (INIS)

    This thesis comprises five reports on studies with renograms, radionuclide investigations of individual renal function in patients suspected of renovascular hypertension. The main question was to determine whether the renogram could trace functional changes in a kidney with a stenosed artery, before and after percutaneous transluminal angioplasty (PTA) treatment. In a given patient these functional changes could provide information on the significance of the artery stenosis as a cause of that patients' hypertension, and to some extent predict the blood pressure response after PTA treatment. An important issue in these studies is the registration of the renal effects created by captopril on the renogram. This drug with its specific inhibition of the conversion of angiotensine I to angiotensine II, amplifies the impairment of the glomerular filtration rate (GFR) in a kidney behind a stenosis. Captopril-induced deterioration of the GFR can be shown by renography, especially when it occurs in only one of two kidneys and for that reason does escape detection by overall renal function studies. 157 refs.; 16 figs.; 12 tabs

  9. The impact of four different classes of anesthetics on the mechanisms of blood pressure regulation in normotensive and spontaneously hypertensive rats.

    Science.gov (United States)

    Bencze, M; Behuliak, M; Zicha, J

    2013-01-01

    Most anesthetics induce characteristic hemodynamic changes leading to blood pressure (BP) reduction but the role of renin-angiotensin system (RAS), sympathetic nervous system (SNS) and nitric oxide (NO) synthesis in this BP reduction is unknown. We therefore studied the influence of four widely used anesthetics - pentobarbital (P), isoflurane (ISO), ketamine-xylazine (KX) and chloralose-urethane (CU) - on the participation of these vasoactive systems in BP maintenance. BP effects elicited by the acute sequential blockade of RAS (captopril), SNS (pentolinium) and NO synthase (L-NAME) were compared in conscious and anesthetized Wistar or spontaneously hypertensive rats (SHR). Except for pentobarbital all studied anesthetics evidenced by diminished BP responses to pentolinium. The absolute pentolinium-induced BP changes were always greater in SHR than Wistar rats. KX anesthesia eliminated BP response to pentolinium and considerably enhanced BP response to NO synthase inhibition in SHR. In both rat strains the anesthesia with ISO or CU augmented BP response to captopril, decreased BP response to pentolinium and attenuated BP response to NO synthase inhibition. In conclusion, pentobarbital anesthesia had a modest influence on BP level and its maintenance by the above vasoactive systems. Isoflurane and chloralose-urethane anesthesia may be used in cardiovascular experiments if substantial BP decrease due to altered contribution of RAS, SNS and NO to BP regulation does not interfere with the respective research aim. Major BP reduction (namely in SHR) due to a complete SNS absence is a major drawback of ketamine-xylazine anesthesia. PMID:24020816

  10. 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.

  11. Renin-angiotensin system blockers regulate the metabolism of isolated fat cells in vitro.

    Science.gov (United States)

    Caminhotto, R de O; Sertié, R A L; Andreotti, S; Campaãa, A B; Lima, F B

    2016-07-28

    Due to the presence of the renin-angiotensin system (RAS) in tissues and its specific influence on white adipose tissue, fat cells are possible targets of pharmacological RAS blockers commonly used as anti-hypertensive drugs. In the present study, we investigated the effects of different RAS blockers on fat cell metabolism, more specifically on lipolysis, lipogenesis and oxidation of energy substrates. Isolated primary adipocytes were incubated with different RAS blockers (aliskiren, captopril and losartan) in vitro for 24 h and lipolysis, lipogenesis and glucose oxidation capacities were determined in dose-response assays to a β-adrenergic agonist and to insulin. Although no change was found in lipolytic capacity, the RAS blockers modulated lipogenesis and glucose oxidation in a different way. While captopril decreased insulin-stimulated lipogenesis (-19% of maximal response and -60% of insulin responsiveness) due to reduced glucose derived glycerol synthesis (-19% of maximal response and 64% of insulin responsiveness), aliskiren increased insulin-stimulated glucose oxidation (+49% of maximal response and +292% of insulin responsiveness) in fat cells. Our experiments demonstrate that RAS blockers can differentially induce metabolic alterations in adipocyte metabolism, characterized by a reduction in lipogenic responsiveness or an increase in glucose oxidation. The impact of RAS blockers on adipocyte metabolism may have beneficial implications on metabolic disorders during their therapeutic use in hypertensive patients. PMID:27487419

  12. 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.

  13. 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.

  14. Synthesis, Characterization and Application of Water-soluble Gold and Silver Nanoclusters

    Science.gov (United States)

    Kumar, Santosh

    The term `nanotechnology' has emerged as a buzzword since the last few decades. It has found widespread applications across disciplines, from medicine to energy. The synthesis of gold and silver nanoclusters has found much excitement, due to their novel material properties. Seminal work by various groups, including ours, has shown that the size of these clusters can be controlled with atomic precision. This control gives access to tuning the optical and electronic properties. The majority of nanoclusters reported thus far are not water soluble, which limit their applications in biology that requires water-solubility. Going from organic to aqueous phase is by no means a simple task, as it is associated with many challenges. Their stability in the presence of oxygen, difficulty in characterization, and separation of pure nanoclusters are some of the major bottlenecks associated with the synthesis of water-soluble gold nanoclusters. Water-soluble gold nanoclusters hold great potential in biological labeling, bio-catalysis and nano-bioconjugates. To overcome this problem, a new ligand with structural rigidity is needed. After considering various possibilities, we chose Captopril as a candidate ligand. In my thesis research, the synthesis of Au25 nanocluster capped with captopril has been reported. Captopril-protected Au25 nanocluster showed significantly higher thermal stability and enhanced chiroptical properties than the Glutathione-capped cluster, which confirms our initial rationale, that the ligand is critical in protecting the nanocluster. The optical absorption properties of these Au25 nanoclusters are studied and compared to the plasmonic nanoparticles. The high thermal stability and solubility of Au25 cluster capped with Captopril motivated us to explore this ligand for the synthesis of other gold clusters. Captopril is a chiral molecule with two chiral centers. The chiral ligand can induce chirality to the overall cluster, even if the core is achiral

  15. 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.

  16. Toxins and drug discovery.

    Science.gov (United States)

    Harvey, Alan L

    2014-12-15

    Components from venoms have stimulated many drug discovery projects, with some notable successes. These are briefly reviewed, from captopril to ziconotide. However, there have been many more disappointments on the road from toxin discovery to approval of a new medicine. Drug discovery and development is an inherently risky business, and the main causes of failure during development programmes are outlined in order to highlight steps that might be taken to increase the chances of success with toxin-based drug discovery. These include having a clear focus on unmet therapeutic needs, concentrating on targets that are well-validated in terms of their relevance to the disease in question, making use of phenotypic screening rather than molecular-based assays, and working with development partners with the resources required for the long and expensive development process. PMID:25448391

  17. 全科医生处方集——血管紧张素转换酶抑制剂

    Institute of Scientific and Technical Information of China (English)

    方玉婷

    2011-01-01

    @@ 血管紧张素酶抑制剂ACE Inhibitors 1 贝那普利benazepril(洛丁新):高血压:起始剂量10 mg PO qd,通常维持剂量20-40 mg PO qd 最多80 mg/d [洛丁新10 mg]肝肾孕-?2 卡托普利captopril(开博通、凯宝压苧):高血压:起始剂量12.5 mg PO bid-tid,通常维持剂量25-150 mg PO bid-tid,最多450 mg/d.

  18. [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.

  19. Angiotensin processing activities in the venom of Thalassophryne nattereri.

    Science.gov (United States)

    Tenório, Humberto de Araújo; Marques, Maria Elizabeth da Costa; Machado, Sonia Salgueiro; Pereira, Hugo Juarez Vieira

    2015-05-01

    The venom of marine animals is a rich source of compounds with remarkable functional specificity and diversity. Thalassophryne nattereri is a small venomous fish inhabiting the northern and northeastern coast of Brazil, and represents a relatively frequent cause of injuries. Its venom causes severe inflammatory response followed frequently by the necrosis of the affected area. This venom presents characterized components such as proteases (Natterins 1-4) and a lectin (Nattectin) with complex effects on the human organism. A specific inhibitor of tissue kallikrein (TKI) reduces the nociception and the edema caused by the venom in mice. Our study sought to investigate the proteolytic activities against vasopeptides Angiotensin I, Angiotensin II, Angiotensin 1-9 and Bradykinin. The venom indicated angiotensin conversion against angiotensin I, as well as kininase against bradykinin. Captopril conducted the total inhibition of the converting activity, featuring the first report of ACE activity in fish venoms. PMID:25702959

  20. 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.

  1. 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

  2. 血管紧张素转换酶抑制剂的心血管系统保护作用

    Institute of Scientific and Technical Information of China (English)

    杜金山

    2001-01-01

    @@ 血管紧张素转换酶抑制剂(ACEI)作用广泛,疗效显著,主要用于心血管疾病.近年来在高血压、心力衰竭、心肌缺血、左室肥厚、左室重塑、动脉粥样硬化、肾病等疾病的防治中发挥着越来越重要的作用.除卡托普利(captopril)、依那普利(enalapril)外,西拉普利(cilazapril,商品名:一平苏)、培哚普利(perindopril,商品名:雅施达)、赖诺普利(lisinopril,商品名:捷赐瑞)、苯那普利(benazepril,商品名:洛丁新)等也已相继进入我国市场.

  3. Hypersomnolence with beta-adrenergic blockers.

    Science.gov (United States)

    Thachil, J; Zeller, J R; Kochar, M S

    1987-11-01

    An elderly, mildly demented, hypertensive male patient developed hypersomnolence on administration of propranolol for treatment of hypertension; no other cause for hypersomnolence was detected. Upon replacement of propranolol with atenolol, he felt better but continued to be quite somnolent. When atenolol was discontinued, he reported to have lack of sleep. On readministration of subtherapeutic doses of the same beta-adrenergic blocking agents, he once again experienced excessive sleepiness. By discontinuing beta-blocking agents and introducing captopril, he felt much better, became pleasant and talkative, and blood pressure was well controlled. Beta antagonists are important drugs in the management of many cardiovascular problems. Propranolol, a lipophilic beta-blocking agent, and atenolol, a hydrophilic beta-blocking agent, are two of the major agents currently used clinically in the United States. Numerous neuropsychiatric side-effects of the beta-adrenergic blocking drugs have been reported, but hypersomnolence is not readily recognized as one of them. PMID:3665616

  4. Hyponatremic Hypertensive Syndrome in an Obese man with Renal Ischemia

    International Nuclear Information System (INIS)

    Renovascular hypertension occasionally manifests as an electrolyte disorder. The combination of hyponetrimia and 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 renal function. Color Doppler renal ultrasound, and magnetic resonance angiography confirmed the diagnosis of renal artery stenosis. (author)

  5. 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.

  6. Possible involvement of ATP-dependent K-channel related mechanisms in the antihypertensive and cough suppressant effects of the novel ACE inhibitor (2S, 3aS, 7aS)-1-(N2-nicotinoyl-L-lysyl-gamma-D-glutamyl)octahydro-1H- indole-2-carboxylic acid.

    Science.gov (United States)

    Nagata, S; Takeyama, K; Hosoki, K; Karasawa, T

    1997-06-01

    The antihypertensive and cough suppressant mechanisms of DU-1777 ((2S,3aS,7aS)-1-(N2-nicotinoyl-L-lsyl-gamma-D-glutamyl )octahydro-1H-indole-2 -carboxylic acid, CAS 116662-73-8), a new long-acting angiotensin-1-converting enzyme (ACE) inhibitor, were investigated in vivo and in vitro. The antihypertensive effects of DU-1777 at 10 mg/kg p.o. and cromakalim at 0.3 mg/kg p.o. were partially (about 60%) or fully antagonized by glibenclamide at 10 mg/kg i.v. in 2-kidney, 1-clip renal hypertensive rats (2K-1C RHR). The antihypertensive effects of a Ca blocker (nifedipine) and other ACE inhibitors (captopril, alacepril, enalapril, lisinopril, imidapril and quanapril) were not antagonized by glibenclamide. In deoxycorticosterone acetate-salt hypertensive rats (DOCA-HR), the antihypertensive effects of DU-1777 at 3-30 mg/kg p.o. were fully antagonized by glibenclamide. However, in vitro, DU-1777 (10(-6)-10(-3) mol/l) did not affect aortic ring contractions induced by high K (30 mmol/l). In guinea pig, citric acid induced cough was increased by ACE inhibitors, captopril, alacepril, enalapril and lisinopril (10 and 30 mg/kg p.o.). DU-1777 had a tendency to decrease citric acid induced cough and the effect was antagonized by glibenclamide. These results suggest that while DU-1777 itself does not open ATP-dependent K channel, it indirectly produces these effects through unknown mechanisms in vivo. Moreover, these effects contributed to the antihypertensive effect in DOCA-HR and cough suppressant effect in guinea pigs. PMID:9239450

  7. A continuous fluorescent assay for the determination of plasma and tissue angiotensin I-converting enzyme activity

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    M.F. Alves

    2005-06-01

    Full Text Available A continuous assay using internally quenched fluorescent peptides with the general sequence Abz-peptidyl-(DnpP-OH (Abz = ortho-aminobenzoic acid; Dnp = 2,4-dinitrophenyl was optimized for the measurement of angiotensin I-converting enzyme (ACE in human plasma and rat tissues. Abz-FRK(DnpP-OH, which was cleaved at the Arg-Lys bond by ACE, was used for the enzyme evaluation in human plasma. Enzymatic activity was monitored by continuous recording of the fluorescence (lambdaex = 320 nm and lambdaem = 420 nm at 37ºC, in 0.1 M Tris-HCl buffer, pH 7.0, with 50 mM NaCl and 10 µM ZnCl2. The assays can be performed directly in the cuvette of the fluorimeter and the hydrolysis followed for 5 to 10 min. ACE measurements in the plasma of 80 healthy patients with Hip-His-Leu and with Abz-FRK(DnpP-OH correlated closely (r = 0.90, P < 0.001. The specificity of the assay was demonstrated by the complete inhibition of hydrolysis by 0.5 µM lisinopril or captopril. Abz-FRK(DnpP-OH cleavage by ACE was monitored in rat lung, kidney, heart, and liver homogenates in the presence of a cocktail of inhibitors containing trans-epoxy-succinyl-L-leucylamido-(4-guanido-butene, pepstatin, phenyl-methylsulfonyl fluoride, N-tosyl-L-phenylalanyl-chloromethyl ketone, and N-tosyl-lysyl-chloromethyl ketone to prevent undesirable hydrolysis. ACE activity in lung, heart and kidney homogenates, but not in liver homogenates, was completely abolished by 0.5 µM lisinopril or captopril. The advantages of the method are the procedural simplicity and the high sensitivity providing a rapid assay for ACE determinations.

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

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    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.

  9. Long-term antihypertensive effect of a soluble cocoa fiber product in spontaneously hypertensive rats

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    Sandra Fernández-Vallinas

    2016-05-01

    Full Text Available Background and Methods: This study evaluates the antihypertensive effect of long-term intake of a soluble cocoa fiber product (SCFP. Different doses of SCFP were evaluated (200, 400, and 800 mg/kg/day and a dose of 800 mg/kg/day of beta-glucan 0.75 (BETA-G was used as a standard fiber. Water, a neutral vehicle, was used as negative control, and 50 mg/kg/day captopril was used as positive control. Systolic blood pressure (SBP was measured weekly by the tail cuff method. Body weight, food, and liquid intake were also registered weekly in the rats from 10 to 24 weeks of life. Glucose, total cholesterol, and triglyceride levels; redox status; and the angiotensin-converting enzyme activity were also studied in the plasma samples of these animals. Results: Throughout the 10 weeks of treatment, captopril and SCFP (400 mg/kg/day demonstrated blood pressure lowering effects in the spontaneously hypertensive rats (p0.05; n=8. When the corresponding antihypertensive treatment, was disrupted the SBP values of the 400 mg/kg/day SCFP treated animals returned to control values (p>0.05; n=8. In addition, the SCFP significantly decreased (p<0.05; n=4 the glucose, cholesterol, and triglyceride levels and also the liver and plasma malondaldehyde levels. Moreover, the SCFP slightly increased the reduced glutathione levels in the liver. Conclusion: The SCFP could be used to control the blood pressure of hypertensive subjects for a long period of time and could improve metabolic complications associated to cardiovascular diseases.

  10. 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.

  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. PMID:25280267

  12. 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.

  13. 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.

  14. Effect of angiotensin-converting enzyme inhibitor, captoprol on proliferation, differentiation and migration of human epidermal stem cells%血管紧张素转化酶抑制剂对表皮干细胞增殖、分化、迁移的影响

    Institute of Scientific and Technical Information of China (English)

    廖选; 肖静; 刘宏伟; 程飚; 肖丽玲; 徐媛; 李升红

    2013-01-01

    目的 观察血管紧张素转化酶(ACE)抑制剂卡托普利对表皮干细胞(ESCs)增殖、迁移、分化的影响,探讨ACE在维持ESCs生物学功能中的作用.方法 利用差速贴壁法获得10例儿童的ESCs,进行离体培养,检测ACE在ESCs的表达.用XTT法检测不同浓度(1 ×l0-5、1×10-6、l×10-7、1×10-8mol/L) ACEI卡托普利对ESCs增殖的影响;体外创伤模型观察1×10-6mol/L的卡托普利对ESCs 6、12、18、24h各时间段的迁移能力;流式细胞仪检测K10的表达观察1×10-6mol/L的卡托普利对ESCs分化的影响.结果 培养的细胞经β1-整合素和K19免疫荧光双重标记染色,83.55%细胞为双标记阳性细胞,即ESCs.免疫荧光染色和逆转录-聚合酶链反应(RT-PCR)结果显示ESCs表达ACE.流式细胞仪定量检测培养的细胞ACE阳性率为74.2%.1×10-6mol/L的卡托普利可明显抑制ESCs的增殖(P<0.05),且在第5天达到峰值.1×10-6 mol/L的卡托普利可明显抑制细胞的迁移能力(P<0.05)和克隆能力(P<0.05).流式细胞仪检测结果表明,l×10-6 mol/L的卡托普利并不影响K10的表达(P>0.05).结论 ACE通过影响ESCs的增殖,迁移从而影响皮肤的损伤修复和自我更新.%Objective To observe the effect of angiotensin-converting enzyme (ACE) inhibitor,captoprol on the proliferation,differentiation and migration of human epidermal stem cells (ESCs),and explore the role of ACE in maintaining ESCs biological function.Methods Human ESCs were isolated by differential adhesion method from human skin and cultured in vitro,and the expression of ACE,β1-integrin K19 and K10 in human ESCs was examined by using immunostaining and flow cytometry.XTT cell proliferation assay was used to detect the impact of the different concentrations of ACE inhibitor,captopril on the proliferation of ESCs,and the scratch assay was done to evaluate the effect of 1 × 10-6 mol/L captopril on the migration of ESCs.Flow cytometry was used to detect K10

  15. 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

  16. 血管紧张素转化酶中药抑制剂的筛选模型研究%Establishment of three screening models of angiotensin converting enzyme inhibitors

    Institute of Scientific and Technical Information of China (English)

    巩颖; 王灵芝; 史新元; 乔延江

    2011-01-01

    Objective: To establish and compare three in vitro screening models of angiotensin converting enzyme inhibitors (ACEI), and provide methodological basis for screening ACEI drugs from Chinese herbal medicine.Method: Three screening models were established using rat serum, pure angiotensin converting enzyme (ACE) and crude extract enzyme from rabbit lung as enzyme sources, respectively, with corresponding testing methods, and captopril as the positive drug.Result: The IC50 of captopril was 2.30 nmol · L-1 using rat serum as the enzyme;and 1.04 nmol · L-1 for ACE pure enzyme; and 1.40 nmol · L-1 for crude extract enzyme from rabbit lung.Conclusion: Results from the three screening models were all in accordance with literature reports.These models can be applied to in vitro pharmaceutical screening.The selection of suitable screening model depend on the experimental situation and the inherent characters of models.%目的:研究比较不同的血管紧张素转化酶抑制剂(ACEI)筛选模型,提供从中草药中快速筛选ACEI药物的方法.方法:以卡托普利为阳性药,分别以大鼠血清、血管紧张素转化酶(ACE)纯酶、兔肺ACE粗提物作为酶源,采用不同的检测方法,建立3种ACEI筛选模型,考察多种中药有效成分ACEI活性.结果:大鼠血清粗提酶液模型检测卡托普利IC50值为2.30 nmol·L-1:ACE纯酶模型检测卡托普利IC50值为1.04 nmol·L-1;兔肺ACE粗提物模型检测卡托普利IC50值为1.40nmol.L-1,3种ACE筛选模型线性关系均良好,模型建立成功.结论:3种模型均町用于中草药的体外活性筛选,但各有利弊,可根据中草药组分和筛选模型的特点选择快速有效的模型.

  17. Comparison of the Efficacy and Safety of Different ACE Inhibitors in Patients With Chronic Heart Failure: A PRISMA-Compliant Network Meta-Analysis.

    Science.gov (United States)

    Sun, WeiPing; Zhang, HaiBin; Guo, JinCheng; Zhang, XueKun; Zhang, LiXin; Li, ChunLei; Zhang, Ling

    2016-02-01

    Heart failure is a public health problem and a great economic burden for patients and healthcare systems. Suppression of the renin-angiotensin system (RAS) by angiotensin-converting enzyme (ACE)-inhibitors remains the mainstay of treatment for heart failure. However, the abundance of ACE inhibitors makes it difficult for doctors to choose.We performed this network meta-analysis of ACEIs in patients with heart failure in order to address this area of uncertainty.We searched PubMed, Embase, CENTRAL, and Medline.Any randomized controlled trial evaluating the efficacy and safety of captopril, enalapril, lisinopril, ramipril, or trandolapril or combined interventions of 2 or more of these drugs.Two reviewers extracted the data and made the quality assessment. At first, we used Stata software (version 12.0, StataCorp, College Station, TX) to make traditional pairwise meta-analyses for studies that directly compared different interventions. Then, network meta-analysis was performed using WinBUGS (version 1.4.3, MRC Biostatistics Unit, Cambridge, UK).A total of 29 studies were included. Lisinopril was associated with a higher rate of all-cause mortality compared with placebo (odds ratio 65.9, 95% credible interval 1.91 to 239.6) or ramipril (14.65, 1.23 to 49.5). Enalapril significantly reduced systolic blood pressure when compared with placebo (standardized mean differences -0.6, 95% credible interval -1.03 to -0.18). Both captopril (odds ratio 76.2, 95% credible interval 1.56 to 149.3) and enalapril (274.4, 2.4 to 512.9) were associated with a higher incidence of cough compared to placebo.Some important outcomes such as rehospitalization and cardiac death were not included. The sample size and the number of studies were limited, especially for ramipril.Our results suggest that enalapril might be the best option when considering factors such as increased ejection fraction, stroke volume, and decreased mean arterial pressure. However, enalapril was associated with the

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

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    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.

  19. COMPARATIVE ASSESSMENT OF EFFECT OF COMBINED DRUGS OF ACE INHIBITOR AND DIURETIC (“NOLIPREL FORTE” AND “CAPOZIDE” ON CARDIOVASCULAR REMODELING IN HYPERTENSIVE PATIENTS

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    T. D. Kaplanov

    2005-01-01

    Full Text Available Aim. To assess antihypertensive efficacy and effect on cardio-vascular remodeling of combined drugs of ACE inhibitor and diuretic, “Noliprel forte” (NF and “Capozide” (CA, in hypertensive high risk patients.Material and methods. 50 hypertensive (II grade patients (25 men and 25 women, 19-65 years old with high cardio-vascular risk took part in comparative opened randomized study. No one of patients received antihypertensive therapy before study. All patients were randomized for therapy with one of combined drug of ACE inhibitors and diuretic. 25 patients took NF (perindopril 4 mg and indapamide 1,25 mg, and 25 patients -CA (captopril 50 mg and hydrochlorothiazide 25 mg. Duration of observation period was 6 months. Before study, after 3 and 6 months of therapy ambulatory blood pressure monitoring (ABPM, echocardiography, cardiac and vessel Dopplerography, ultrasound scanning of general carotid arteries with detection of intima-media thickness (IMT, pulse wave speed (PWS were held in all patients. Blood bio-chemical analysis was done also.Results. After 3 months 2 patients in NF group and 4 ones in CA group were required to reinforce of ther-apy with additional administration of perindoprile 4 mg and captopril 50 mg respectively. As a result of 6-month of therapy in NF group systolic dlood pressure (BP decreased in 14,0% (р<0,001 and diastolic BP – на 12,9% (р<0,001. CA reduced systolic BP by 17,9% (р<0,0001 and diastolic BP – by 17,5% (р<0,001. 76% and 70% of patients in NF and CA groups, respectively, reached target BP level. Positive dynamic of daily profile of BP was observed according to ABPM data. Cerebral blood flow did not worsen despite of BP decrease. Both drugs decreased in thickness of inter-ventricular septum and left ventricular mass. Besides, NF decreased in thickness of left ventricular posterior wall. Both drugs reduced in IMT and decreased in PWS. NF therapy did not change of blood biochemical parameters. CA

  20. COMPARATIVE ASSESSMENT OF EFFECT OF COMBINED DRUGS OF ACE INHIBITOR AND DIURETIC (“NOLIPREL FORTE” AND “CAPOZIDE” ON CARDIOVASCULAR REMODELING IN HYPERTENSIVE PATIENTS

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    T. D. Kaplanov

    2015-12-01

    Full Text Available Aim. To assess antihypertensive efficacy and effect on cardio-vascular remodeling of combined drugs of ACE inhibitor and diuretic, “Noliprel forte” (NF and “Capozide” (CA, in hypertensive high risk patients.Material and methods. 50 hypertensive (II grade patients (25 men and 25 women, 19-65 years old with high cardio-vascular risk took part in comparative opened randomized study. No one of patients received antihypertensive therapy before study. All patients were randomized for therapy with one of combined drug of ACE inhibitors and diuretic. 25 patients took NF (perindopril 4 mg and indapamide 1,25 mg, and 25 patients -CA (captopril 50 mg and hydrochlorothiazide 25 mg. Duration of observation period was 6 months. Before study, after 3 and 6 months of therapy ambulatory blood pressure monitoring (ABPM, echocardiography, cardiac and vessel Dopplerography, ultrasound scanning of general carotid arteries with detection of intima-media thickness (IMT, pulse wave speed (PWS were held in all patients. Blood bio-chemical analysis was done also.Results. After 3 months 2 patients in NF group and 4 ones in CA group were required to reinforce of ther-apy with additional administration of perindoprile 4 mg and captopril 50 mg respectively. As a result of 6-month of therapy in NF group systolic dlood pressure (BP decreased in 14,0% (р<0,001 and diastolic BP – на 12,9% (р<0,001. CA reduced systolic BP by 17,9% (р<0,0001 and diastolic BP – by 17,5% (р<0,001. 76% and 70% of patients in NF and CA groups, respectively, reached target BP level. Positive dynamic of daily profile of BP was observed according to ABPM data. Cerebral blood flow did not worsen despite of BP decrease. Both drugs decreased in thickness of inter-ventricular septum and left ventricular mass. Besides, NF decreased in thickness of left ventricular posterior wall. Both drugs reduced in IMT and decreased in PWS. NF therapy did not change of blood biochemical parameters. CA

  1. 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

  2. Acute and chronic antihypertensive effects of Cinnamomum zeylanicum stem bark methanol extract in L-NAME-induced hypertensive rats

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    Nyadjeu Paulin

    2013-01-01

    Full Text Available Abstract Background Previous study showed that the aqueous extract of the stem bark of Cinnamomum zeylanicum possesses antihypertensive and vasodilatory properties. The present work investigates the acute and chronic antihypertensive effects of the methanol extract of Cinnamomum zeylanicum stem bark (MECZ in L-NAME-induced hypertensive rats. Methods The acute antihypertensive effects of MECZ (5, 10 and 20 mg/kg administered intravenously were evaluated in rats in which acute arterial hypertension has been induced by intravenous administration of L-NAME (20 mg/kg. For chronic antihypertensive effects, animals were treated with L-NAME (40 mg/kg/day plus the vehicle or L-NAME (40 mg/kg/day in combination with captopril (20 mg/kg/day or MECZ (300 mg/kg/day and compared with control group receiving only distilled water. All drugs were administered per os and at the end of the experiment that lasted for four consecutive weeks, blood pressure was measured by invasive method and blood samples were collected for the determination of the lipid profile. The heart and aorta were collected, weighed and used for both histological analysis and determination of NO tissue content. Results Acute intravenous administration of C. zeylanicum extract (5, 10 and 20 mg/kg to L-NAME-induced hypertensive rats provoked a long-lasting decrease in blood pressure. Mean arterial blood pressure decreased by 12.5%, 26.6% and 30.6% at the doses of 5, 10 and 20 mg/kg, respectively. In chronic administration, MECZ and captopril significantly prevented the increase in blood pressure and organs’ weights, as well as tissue histological damages and were able to reverse the depletion in NO tissue’s concentration. The MECZ also significantly lower the plasma level of triglycerides (38.1%, total cholesterol (32.1% and LDL-cholesterol (75.3% while increasing that of HDL-cholesterol (58.4% with a significant low atherogenic index (1.4 versus 5.3 for L-NAME group. Conclusion MECZ

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

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    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.

  4. 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

  5. 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

  6. 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

  7. 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

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    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

  8. 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

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    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

  9. Uncaria Alkaloids' Intervention on the Aged Endothelial Cell Induced by D-Galactose%钩藤总生物碱对D-半乳糖诱导的内皮细胞衰老的干预

    Institute of Scientific and Technical Information of China (English)

    姜月华; 李运伦; 赵婧; 霍青

    2011-01-01

    目的 探讨钩藤总生物碱保护血管内皮细胞、抑制血管内皮细胞衰老的作用.方法 采用D-半乳糖诱导的大鼠主动脉内皮细胞建立衰老模型,扫描电镜技术观察衰老血管内皮细胞的形态,β-半乳糖苷酶染色法测定衰老血管内皮细胞发生率以间接反映β-半乳糖苷酶表达,PCR-ELISA法测定衰老血管内皮细胞端粒酶活性.结果 钩藤总生物碱可以改善血管内皮细胞形态、降低内皮细胞中β-半乳糖苷酶表达和端粒酶活性相对表达量(P<0.05).结论 钩藤总生物碱具有抑制内皮细胞衰老、保护血管内皮的效用.%Aim To investigate the effect of Uncaria alkaloids on protecting rat vascular endothelial cells and inhibiting cell senescence. Methods Aging model of rat aortic endothelial cells (REAC) was established by D-galactose. Treated with Uncaria alkaloids and Captopril, separately, then, the aging vascular endothelial cell morphology were observated by scanning electron microscopy, vascular endothelial cell senescence rate was determinated by β-galactosidase staining method, and telomerase activity was determinated by PCR-ELISA method. Results REAC cell morphology treated with Uncaria alkaloids or captopril was significantly improved, β-galactosidase expression and telomerase activity were significantly decreased (P < 0.05). The effects of each dose group of Uncaria alkaloids were: medium dose > low dose > high dose, suggesting that high dose of Uncaria alkaloids ( > 400 mg/L) may have a certain degree of cytotoxicity,and the best dose of Uncaria alkaloids dose was 200 mg/L. Conclusion Uncaria alkaloids can inhibit rat aortic endothelial cell senescence, and protect vascular endothelium.

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

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    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

  11. 1-(3-巯基-2-甲基丙酰基)吡咯-2-羧酸的合成%Synthesis of 1-(3-Mercapto-2-Methylpropionyl)-Pyrrolidine-2-Carboxylic Acid

    Institute of Scientific and Technical Information of China (English)

    娄凤文; 刘晴晴; 花荣; 朱成章; 卞谋旺; 刘清

    2013-01-01

    A novel protocol for the Michael addition of thiolacetic acid to methacrylic acid vinyl ester was devel-oped using a basic ionic liquid [bmim ]OH as catalyst and solvent ,the reaction was carried out at room temperature and could obtain good yields in 30 min .A new synthesis of active pharmaceutical ingredients named captopril ,the was achieved by Michael addition and N-acylation ,in high purity from methacrylic acid vinyl ester .%碱性离子液体[bmim ]OH能有效地促进硫代乙酸和甲基丙烯酸乙烯酯的迈克尔加成反应,反应在室温条件下进行,在30 min内可以取得定量收益率的2-甲基-3-乙酰硫基丙酸乙烯酯。以甲基丙烯酸乙烯酯为起始原料,提出了一种合成卡托普利的新方法。

  12. 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.

  13. 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.

  14. 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.

  15. One-pot synthesis, biological evaluation, and docking study of new chromeno-annulated thiopyrano[2,3-c]pyrazoles.

    Science.gov (United States)

    Parmar, Bhagyashri D; Sutariya, Tushar R; Brahmbhatt, Gaurangkumar C; Parmar, Narsidas J; Kant, Rajni; Gupta, Vivek K; Murumkar, Prashant R; Sharma, Mayank Kumar; Yadav, Mange Ram

    2016-08-01

    A one-pot synthesis of new chromeno-annulated thiopyrano[2,3-c]pyrazoles has been achieved through a domino-Knoevenagel-hetero-Diels-Alder reaction after combining various pyrazol-5-thiones with O-alkenyloxy/alkynyloxy-salicylaldehydes/naphthaldehydes in a Brønsted acidic ionic liquid, [Hmim]HSO[Formula: see text], methylimidazolium hydrogen sulphate, under microwave irradiation. The method is simple and in many cases the isolated products did not require further purification. The central pyranothiopyranyl cis-fusion was confirmed by 2D NMR NOESY and single-crystal X-ray analysis suggesting that the endo-E-Syn transition state would be the most favored pathway of the reaction. Many heterocycles of this new series were found active against six bacterial and two fungal strains. In addition, all the compounds possess good anti-oxidant activity with the ferric reducing anti-oxidant power value [Formula: see text]. All new structures were docked into active site of angiotensin I converting enzyme (ACE), assuming that the compounds possessed the anti-hypertensive activity potential on the basis of prediction of activity spectra of substances prediction results. Pyranyl ring oxygen in compound 9a forms two hydrogen bonds with HIS353 and HIS513 residues in the active site of the ACE having good G score ([Formula: see text]) of this compound, comparable to that of the reference drug captopril ([Formula: see text]). PMID:27017351

  16. CATETERES EM TERAPIA INTENSIVA

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    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.

  17. 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. PMID:27562708

  18. Inhibition and active-site modelling of prolidase.

    Science.gov (United States)

    King, G F; Crossley, M J; Kuchel, P W

    1989-03-15

    Consideration of the active-site model of prolidase led us to examine azetidine, pyrrolidine and piperidine substrate analogs as potential in vivo inhibitors of the enzyme. One of these, N-benzyloxycarbonyl-L-proline, was shown to be a potent competitive inhibitor of porcine kidney prolidase (Ki = 90 microM); its rapid protein-mediated permeation of human and sheep erythrocytes suggests that it may be effective in vivo. The higher homolog, N-benzyloxycarbonyl-L-pipecolic acid, was also a potent inhibitor of the enzyme while the antihypertensive drugs, captopril and enalaprilat, were shown to have mild and no inhibitory effects, respectively. Analysis of inhibitor action and consideration of X-ray crystallographic data of relevant Mn2+ complexes allowed the active-site model of prolidase to be further refined; a new model is presented in which the substrate acts as a bidentate ligand towards the active-site manganous ion. Various aspects of the new model help to explain why Mn2+ has been 'chosen' by the enzyme in preference to other biologically available metal ions. PMID:2924773

  19. 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.

  20. Drug Related Problems in the Management of Chronic Kidney Disease with Coronary Artery Disease

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    Winda H. Furqani

    2015-06-01

    Full Text Available Drug related problems were defined as conditions on patient’s therapy management that caused, or potentially caused unsuccessful therapy. This study was conducted at a hospital in Cimahi City in May 2014. In this study, DRPs were identified on a 59 years old woman who was diagnosed with chronic kidney disease and coronary artery disease with gangrene on the left hand (the third finger. The patient also had a diabetes mellitus for two until three years ago. Drug related problems (DRPs were found in this patient. Unnecessary drug therapy (administration of calsium polystirene sulfonate, inappropriate choosen antibiotic, inappropriate dosing (administration of amoxicillin and captopril, and risks drug interactions (captopril–furosemide, captopril–isosorbide dinitrate, and captopril–sodium bicarbonate. Patients with chronic kidney disease and coronary artery disease received complex drug therapy. These condition lead to higer risk of DRPs. The involvement of clinical pharmacist in interdisciplinary team for management of complex diseases was needed to monitor drug therapy to optimizing the therapy, minimalizing the risk of DRPs, and improving patient’s quality of life.

  1. Effects of oral enalapril and verapamil on dialysis adequacy and solute clearance in chronic ambulatory peritoneal dialysis

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    Shahnaz Atabak

    2013-01-01

    Full Text Available Peritoneal dialysis offers several advantages such as better clearance of intermediate/large molecules and better preservation of renal residual function when compared with hemodialysis. However, dialysis adequacy is one of the subjects of concern of this modality. There are some drugs that are capable of influencing solute transport in the peritoneum, such as acetyle co-enzyme inhibitors (ACE-I medications and calcium channel blockers. Captopril and Verapamil are often mentioned, but their use has shown varying conclusions and initial studies were performed with the intra-peritoneal administration of these drugs and there are only a few studies on the effect of the oral administration of these drugs. This study was undertaken with the aim to evaluate the effects of oral administration of Verapamil and Enalapril among continuous ambulatory peritoneal dialysis (CAPD patients. The results of this study showed that Verapamil and Enalapril do not have any effects on glucose, creatinine, sodium, potassium and urea clearance (during the 4-h peritoneal equilibration test (PET test. However, it was shown that Enalapril significantly increased the peritoneal urea Kt/V and caused a meaningful decrease in the diastolic and mean blood pressures. Therefore, we feel that Enalapril may be administered as an anti-hypertensive medication of choice in CAPD patients, which can also result in better dialysis adequacy. However, further studies with larger sample sizes are needed in the future.

  2. Effects of nine antihypertensive drugs on blood pressure variability in sinoaortic-denervated rats

    Institute of Scientific and Technical Information of China (English)

    Jin Wang; Fu-ming SHEN; Min-wei WANG; Ding-feng SU

    2006-01-01

    Aim: The present work was designed to investigate the effects of nine commonly used antihypertensive drugs on blood pressure (BP) and blood pressure variability (BPV) in conscious sinoaortic-denervated (SAD) rats. Methods: Seventy-two SAD rats were randomly divided into nine groups. They were respectively given nifedipine 3 mg/kg, nitrendipine 5 mg/kg, amlodipine 1 mg/kg, clonidine 10 μg/kg, prazosin 0.5 mg/kg, atenolol 20 mg/kg, telmisartan 20 mg/kg, hydrochlorothiazide 40 mg/kg or captopril 50 mg/kg. The drugs were given via a catheter previously implanted into the stomach. BP was recorded for 5 h from 1 h before drug administration to 4 h after drug administration in conscious, freely moving rats. Results: It was found that all these nine drugs significantly decreased BP in SAD rats. Six of these drugs (nifedipine, nitrendipine, amlodipine, clonidine, prazosin and atenolol) significantly decreased BPV in SAD rats, but the remaining three drugs did not. Clonidine and atenolol increased the heart period and the others did not. No drugs affected the heart period variability. Conclusion: Among nine antihypertensive drugs from different classes, calcium antagonists and sympathetic inhibitors decreased BPV in SAD rats.

  3. 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.

  4. Variantes alélicas de CYP2D6: *4, *6 y *10 en una muestra de residentes del estado Aragua, Venezuela

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    Carlos Flores-Angulo

    2015-12-01

    Full Text Available El objetivo del estudio fue determinar la frecuencia de las variantes del gen CYP2D6: *4, *6 y *10 y predecir el fenotipo metabolizador en una muestra de 145 individuos no consanguíneos, aparentemente sanos, residentes del estado Aragua, Venezuela. Los genotipos fueron determinados mediante ensayos de reacción en cadena de la polimerasa seguidos de digestión con endonucleasas de restricción. La predicción del fenotipo metabolizador se realizó con base al sistema Activity score. Las frecuencias de CYP2D6 *4, *6 y *10 fueron de 14,5%, 0,3% y 1%, respectivamente; un porcentaje significativo de individuos fueron categorizados como metabolizador rápido heterocigoto/metabolizador intermedio (23,5% y metabolizador lento (4,1%. Esta información tiene impacto clínico potencial, porque CYP2D6 interviene en el metabolismo de fármacos de prescripción frecuente como: carvedilol, captopril, cloroquina, codeína, fluoxetina, fluvastatina, haloperidol, idarrubicina, indinavir, imatinib, loperamida, nifedipina, ondansetrón y tamoxifeno

  5. Variantes alélicas de CYP2D6: *4, *6 y *10 en una muestra de residentes del estado Aragua, Venezuela

    Directory of Open Access Journals (Sweden)

    Carlos Flores-Angulo

    2015-10-01

    Full Text Available El objetivo del estudio fue determinar la frecuencia de las variantes del gen CYP2D6: *4, *6 y *10 y predecir el fenotipo metabolizador en una muestra de 145 individuos no consanguíneos, aparentemente sanos, residentes del estado Aragua, Venezuela. Los genotipos fueron determinados mediante ensayos de reacción en cadena de la polimerasa seguidos de digestión con endonucleasas de restricción. La predicción del fenotipo metabolizador se realizó con base al sistema Activity score. Las frecuencias de CYP2D6 *4, *6 y *10 fueron de 14,5%, 0,3% y 1%, respectivamente; un porcentaje significativo de individuos fueron categorizados como metabolizador rápido heterocigoto/metabolizador intermedio (23,5% y metabolizador lento (4,1%. Esta información tiene impacto clínico potencial, porque CYP2D6 interviene en el metabolismo de fármacos de prescripción frecuente como: carvedilol, captopril, cloroquina, codeína, fluoxetina, fluvastatina, haloperidol, idarrubicina, indinavir, imatinib, loperamida, nifedipina, ondansetrón y tamoxifeno

  6. Rapid recovery following fulminant meningococcemia complicated by myocarditis in a 15-year-old Nepalese girl: a case report

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    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

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

    Science.gov (United States)

    Benter, Ibrahim F.; Babiker, Fawzi; Al-Rashdan, Ibrahim; Yousif, Mariam; Akhtar, Saghir

    2013-01-01

    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. PMID:24066305

  8. Cardiovascular activity of 14-deoxy-11,12-didehydroandrographolide in the anaesthetised rat and isolated right atria.

    Science.gov (United States)

    Zhang, C; Kuroyangi, M; Tan, B K

    1998-12-01

    The cardiovascular activity of 14-deoxy-11,12-didehydroandrographolide (DDA) from Andrographis paniculata (Burm.f.) Nees (Acanthaceae) was elucidated in anaesthetised Sprague-Dawley (SD) rats and isolated rat right atria. In anaesthetised rats, DDA produced significant falls in mean arterial blood pressure (MAP) and heart rate in a dose-dependent manner with the maximum decrease of 37.6 +/- 2.6% and 18.1 +/- 4.8%, respectively. The ED50 value for MAP was 3.43 mmol kg-1. Pharmacological antagonist studies were done using this dose. The hypotensive action of DDA was not mediated through effects on the alpha-adrenoceptor, muscarinic cholinergic and histaminergic receptors, for it was not affected by phentolamine, atropine as well as pyrilamine and cimetidine. However, it seems to work via adrenoceptors, autonomic ganglia receptor and angiotensin-converting enzyme, since the hypotensive effect of DDA was negated or attenuated in the presence of propranolol, hexamethonium and captopril. In the isolated right atria, DDA caused negative chronotropic action and antagonised isoproterenol-induced positive chronotropic actions in a non-competitive and dose-dependent manner. These results further supported the bradycardia-inducing and beta-adrenoceptor antagonistic properties of DDA in vivo. PMID:9990649

  9. 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.

  10. 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.

  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. 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.

  13. Effect of Yuxingeng Fluid(愈心梗液)on Myocardial Energy Metabolism in Wistar Rats with Acute Myocardial Infarction

    Institute of Scientific and Technical Information of China (English)

    董国菊; 刘剑刚; 史大卓

    2004-01-01

    Objective: To examine the effect of Yuxingeng fluid (愈心梗液, YXGF) on myocardial energy metabolism in Wistar rats with acute myocardial infarction (AMI) by observing the ultrastructure of mitochondria and the enzyme activities of rat myocardial adenosine triphosphate (ATP), succinate dehydrogenase (SDH), acid phosphatase (ACP), alkaline phosphatase (ALP) and the content of glycogen. Methods: AMI models were established by ligature of left anterior descending coronary artery and then the rats with AMI were randomly divided into 7 groups: namely, blank group, model group, sham-operated group, captopil group, high-dose YXGF group, middle-dose YXGF group and Iow-dose YXGF group. From the next day after modeling, the rats were given YXGF through gastrogavage which lasted for 4 weeks. And then, the ultrastructure of mitochondria was observed by electronic microscope and the enzyme activities of ATP, SDH,ACP, ALP and the content of glycogen were determined. Results: Compared with model group, the other three groups of high-dose YXGF, middle-dose YXGF, Iow-dose YXGF and captopril group could protect the ultrastructure of mitochondria and significantly increase enzyme activities of ATP, SDH, ACP, ALP and the content of glycogen (P<0.01). Conclusion: YXGF can protect mitochondria and increase myocardial enzyme activities and the content of glycogen, which may be one of the mechanisms intervening in the pathological course of the early ventricular remodeling in rats with AMI.

  14. 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).

  15. The blood pressure effect and related plasma levels of flavan-3-ols in spontaneously hypertensive rats.

    Science.gov (United States)

    Quiñones, Mar; Margalef, Maria; Arola-Arnal, Anna; Muguerza, Begoña; Miguel, Marta; Aleixandre, Amaya

    2015-11-01

    We studied the short-term antihypertensive effect of flavan-3-ols (-)-epicatechin, (+)-catechin and (-)-catechin, in spontaneously hypertensive rats (SHR). Plasma metabolites and the corresponding plasma antioxidant capacity were determined. All the assayed flavan-3-ols decreased systolic blood pressure (SBP) in SHR. Their antihypertensive effects were less pronounced than that of Captopril (50 mg kg(-1)) and were not shown in normotensive Wistar-Kyoto rats. 6 mg kg(-1) (-)-epicatechin caused the maximum decrease in SBP. The maximum effects of the catechin monomers were observed post-administration of 0.5 mg kg(-1) of flavan-3-ols, (-)-catechin being the least effective among the three assayed compounds. Glucuronide and methyl glucuronide metabolites were obtained in the flavan-3-ol treated SHR, but it was not possible to relate the antihypertensive effect of the assayed flavan-3-ols with a concrete plasma metabolite or with their antioxidant effect. In conclusion, the studied flavan-3-ols could be responsible for the antihypertensive effect of cocoa products. PMID:26294331

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

    Directory of Open Access Journals (Sweden)

    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.

  17. Blocked of renin-angiotensin system effects on liver regeneration and liver function in mice%肾素-血管紧张素系统的阻断对小鼠肝脏再生及肝功能的影响

    Institute of Scientific and Technical Information of China (English)

    李斌; 梁艳; 谢经武; 李云

    2015-01-01

    目的:探讨应用卡托普利阻断肾素-血管紧张素系统(RAS)后对肝切除术小鼠肝脏再生及肝功能的影响。方法制备肝部分切除术后小鼠模型,实验组予以卡托普利腹腔内注射,分别于术后第1、3、5、7、9天测定肝脏再生情况及肝功能变化,并应用免疫组化方法检测肝组织中IL-6的表达,与对照组比较,应用统计学方法分析RAS阻断对其肝脏再生及肝功能的影响。结果术后第3天开始,RAS阻断可明显增加肝脏体重比(t=7.006,P=0.000),而至第7天,卡托普利反而可以降低肝脏体重比;术后第3天开始,应用卡托普利阻断RAS能够明显降低谷丙转氨酶(ALT)及谷草转氨酶(AST)及胆红素(BIL)的水平,而白蛋白实验组却明显高于对照组(P=0.013),然而血清碱性磷酸酶(ALP)的水平却没有变化,而自第7天开始,ALP表现为降低趋势,而ALT及AST未再出现显著差异。而IL-6在小鼠肝组织中表达,实验组明显低于对照组,二者具有统计学差异(χ2=7.500,P=0.006)。结论 RAS阻断可促进肝切除早期小鼠肝脏再生,并促进肝部分切除术后小鼠早期肝功能的恢复。%Objective To probe into the effect of the application of captopril blocking rennin-renin angiotensin system (RAS) on liver regeneration and liver function of mouse that has undergone partial hepatectomy. Methods Prepared model of postoperative partial hepatectomy mouse. The experimental group was administered captopril by intraperitoneal injection and conditions on liver regeneration and liver function change were measured respectively at the 1st, 3 rd, 5 th, 7 th and 9th day following the operation. The results were compared with that of the control group. Statistical methods were used to analyze the effect of RAS blockade on liver regeneration and liver function. Results Since the 3rd day following the operation, RAS blockade had significantly

  18. 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. )

  19. 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.

  20. 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.

  1. 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.

  2. Drug hypersensitivity syndrome.

    Science.gov (United States)

    Kumari, Rashmi; Timshina, Dependra K; Thappa, Devinder Mohan

    2011-01-01

    Drug hypersensitivity syndrome (DHS) is an adverse drug reaction commonly associated with the aromatic antiepileptic drugs (AEDs), viz., phenytoin (PHT), carbamazepine (CBZ), phenobarbital (PB), lamotrigine, primidone, etc. It can also be caused by other drugs, such as sulfonamides, dapsone, minocycline, gold derivatives, cyclosporine, captopril, diltiazem, terbinafine, azathioprine and allopurinol. Diagnosis of DHS may be difficult because of the variety of clinical and laboratory abnormalities and manifestations and because the syndrome may mimic infectious, neoplastic or collagen vascular disorders. The risk for developing hypersensitivity within 60 days of the first or second prescription in new users of PHT or CBZ was estimated to be 2.3-4.5 per 10,000 and 1-4.1 per 10,000, respectively. The syndrome is defined by the fever, skin rash, lymphadenopathy and internal organ involvement within the first 2-8 weeks after initiation of therapy. Internal manifestations include, among others, agranulocytosis, hepatitis, nephritis and myositis. Insufficient detoxification may lead to cell death or contribute to the formation of antigen that triggers an immune reaction. Cross-reactivity among PHT, CBZ and PB is as high as 70%-80%. Management mainly includes immediate withdrawal of the culprit drug, symptomatic treatment and systemic steroids or immunoglobulins. PMID:21220873

  3. Drug hypersensitivity syndrome

    Directory of Open Access Journals (Sweden)

    Rashmi Kumari

    2011-01-01

    Full Text Available Drug hypersensitivity syndrome (DHS is an adverse drug reaction commonly associated with the aromatic antiepileptic drugs (AEDs, viz., phenytoin (PHT, carbamazepine (CBZ, phenobarbital (PB, lamotrigine, primidone, etc. It can also be caused by other drugs, such as sulfonamides, dapsone, minocycline, gold derivatives, cyclosporine, captopril, diltiazem, terbinafine, azathioprine and allopurinol. Diagnosis of DHS may be difficult because of the variety of clinical and laboratory abnormalities and manifestations and because the syndrome may mimic infectious, neoplastic or collagen vascular disorders. The risk for developing hypersensitivity within 60 days of the first or second prescription in new users of PHT or CBZ was estimated to be 2.3-4.5 per 10,000 and 1-4.1 per 10,000, respectively. The syndrome is defined by the fever, skin rash, lymphadenopathy and internal organ involvement within the first 2-8 weeks after initiation of therapy. Internal manifestations include, among others, agranulocytosis, hepatitis, nephritis and myositis. Insufficient detoxification may lead to cell death or contribute to the formation of antigen that triggers an immune reaction. Cross-reactivity among PHT, CBZ and PB is as high as 70%-80%. Management mainly includes immediate withdrawal of the culprit drug, symptomatic treatment and systemic steroids or immunoglobulins.

  4. 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.

  5. 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. PMID:18608548

  6. Hyperaldosteronism: Screening and Diagnostic Tests.

    Science.gov (United States)

    Sabbadin, Chiara; Fallo, Francesco

    2016-06-01

    Primary aldosteronism (PA) is the most common secondary cause of hypertension, accounting for 10 % of hypertensives and 20 % of those with drug-resistant hypertension. Aldosterone excess is associated with the development of adverse cardiovascular, renal and metabolic effects that are partly independent of its effect on blood pressure. Guidelines recommended wider screening for PA in an effort to maximize detection of patients who may benefit from optimal, specific management. All patient groups with increased prevalence of PA, including hypertensive patients with type 2 diabetes mellitus and those with obstructive sleep apnea, should be carefully screened for PA. Screening with aldosterone-to-renin ratio (ARR) is the most practical and informative initial test. Subsequent confirmatory tests are: (1) oral salt loading; (2) saline infusion; (3) captopril challenge and (4) fludrocortisone suppression test. Confirmation of PA can avoid that patients with a false positive ARR would inappropriately undergo costly and harmful lateralization procedures. If confirmatory testing is positive, further investigations are directed toward determining the subtype of PA, as the treatment differs for each subtype. PMID:26971505

  7. Angiotensins processing activities in the venom and epidermic mucus of Scorpaena plumieri.

    Science.gov (United States)

    Tenório, Humberto de Araújo; Costa, Ricardo Bezerra; Costa Marques, Maria Elizabeth; Victor Dos Santos, Claudio Wilian; Gomes, Francis Soares; Vieira Pereira, Hugo Juarez

    2016-09-01

    The venom of marine animals is a rich source of compounds with remarkable selectivity and functional diversity. Scorpaena plumieri is the most venomous fish in the Brazilian fauna and is responsible for relatively frequent accidents involving anglers and bathers. In humans, its venom causes edema, erythema, ecchymoses, anxiety, nausea, vomiting, and syncope. The venom is chemically characterized by Sp-CTx, a enzyme able to generate an initial endothelium-dependent relaxation response, followed by a contraction response. This study sought to investigate the proteolytic activities regarding vasopeptides angiotensin I and II. Both the venom and the epidermal mucus presented angiotensin conversion activity for angiotensin I, as well as a capacity to form Ang 1-7 directly via Ang I and II. Captopril (10 μM) and EDTA (1 mM) were able to abolish the converting activity of the venom and the epidermal mucus, representing the first description of a converting activity in S. plumieri venom and epidermal mucus. PMID:27215174

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

    Science.gov (United States)

    Kato, Shingo; Itoh, Kyoko; Yaoi, Takeshi; Tozawa, Takenori; Yoshikawa, Yutaka; Yasui, Hiroyuki; Kanamura, Narisato; Hoshino, Akiyoshi; Manabe, Noriyoshi; Yamamoto, Kenji; Fushiki, Shinji

    2010-08-01

    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.

  9. 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.

  10. Posterior reversible encephalopathy syndrome in eclamptic patients: Neuroradiological manifestation, pathogenesis and management

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    Kutlešić Marija S.

    2015-01-01

    Full Text Available Introduction. Eclampsia is one of the most serious complications of hypertensive disorders of pregnancy, defined as the occurrence of one or more convulsions superimposed on preeclampsia. Besides the ordinary course of the disease, ranging from a mild to a severe form, with culmination in eclamptic seizures, there is a significant percent of cases where eclampsia starts unexpectedly, without typical premonitory symptoms and signs, which makes it difficult to prevent. Neuroradiological Characteristics and Pathogenesis of Eclampsia. Neuroradiological signs of eclampsia are described as posterior reversible encephalopathy syndrome, and are manifested by nausea, vomiting, headache, visual disturbances, altered mental status, convulsions and coma, together with characteristic findings on computed tomography or magnetic resonance imaging scan of the head, indicating the presence of vasogenic brain edema. The topic of this article are possible mechanisms of the development of posterior reversible encephalopathy syndrome in pregnancy and modalities of acute treatment of this emergency state. Management of Eclampsia. Magnesium sulphate is nowadays the drug of choice for the treatment and prevention of eclamptic seizures. Labetalol is considered to be the agent of choice in the treatment of hypertensive emergencies of pregnancy, followed by hydralazine, nifedipine, nicardipine, urapidil, nitroglycerin and sodium nitroprusside (in most refractory cases. Angiotensin converting enzyme inhibitors and angiotensin blocking drugs are contraindicated in pregnancy. Captopril and enalapril are allowed during lactation. Conclusion. Posterior reversible encephalopathy syndrome in eclamptic patients is completely reversible if adequate diagnosis is promptly made and intensive treatment immediately administered.

  11. Refined models of New Delhi metallo-beta-lactamase-1 with inhibitors: an QM/MM modeling study.

    Science.gov (United States)

    Wang, Yeng-Tseng; Cheng, Tian-Lu

    2016-10-01

    New Delhi metallo-beta-lactamase 1 (NDM-1) has been identified as a potential target for the treatment of multi-drug resistance bacterial infections. We used molecular docking, normal MD, SIE, QM/MM MD simulations, QM/MM GBSA binding free energy, and QM/MM GBSA alanine-scanning mutagenesis techniques to investigate interactions of the NDM-1 with 11 inhibitors (Tigecycline, BAL30072, D-captopril, Penicillin G, Ampicillin, Carbenicillin, Cephalexin, Cefaclor, Nitrocefin, Meropenem, and Imipenem). From our normal MD and QM/MM simulations, the correlation coefficients between the predicted binding free energies and experimental values are .88 and .93, respectively. Then simulations, which combined QM/MM/GBSA and alanine-scanning mutagenesis techniques, were performed and our results show that two residues (Lys211 and His250) have the strongest impact on the binding affinities of the 11 NDM-1/inhibitors. Therefore, our approach theoretically suggests that the two residues (Lys211 and His250) are responsible for the selectivity of NDM-1 associated inhibitors. PMID:26488313

  12. Clinical nuclear medicine applications in Turkey and specific renal studies

    International Nuclear Information System (INIS)

    Full text: Nuclear cardiology, nuclear oncology, pediatric nuclear medicine and nuclear endocrinology are the main application areas of clinical nuclear medicine in Turkey. Not only imaging studies, but also therapeutic application of radiopharmaceuticals is also performed at many institutes, such as hyperthyroidism treatment with radioiodine, thyroid cancer ablation and metastases treatment with radioiodine, radio synovectomy, metastatic pain therapy, and recently radioimmunotherapy of lymphomas. Almost all radionuclides and radiopharmaceuticals are obtained commercially from European countries, except 18-FDG which is obtained from two cyclotrons in Turkey. More than 30.000 renal procedures are performed at the University hospitals in a year. Pediatric age groups is approximately % 55 of patients. 99mTc-DTPA (%44), 99mTc-DMSA (%37), 99mTc-MAG3 (%17) and 99mTc-EC (%2) are the most commonly used radiopharmaceuticals for renal imaging. More than 6.000 vials of several pharmaceuticals are used for renal cortical scintigraphy (%35), dynamic renal imaging (%34), renal scintigraphy with diuretic (%27) and captopril scintigraphy (%4). Most common indication for renal cortical scintigraphy is detection of cortical scarring (%53). In addition, using single plasma sample method or gamma-camera method renal clearance measurements with 99mTc-MAG3 99mTc-DTPA have been used at some institutions

  13. 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. PMID:24206124

  14. 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

  15. 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.

  16. 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.

  17. Management of Cyclosporine and Nifedipine-Induced Gingival Hyperplasia.

    Science.gov (United States)

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

    2015-12-01

    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.

  18. 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

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

    Science.gov (United States)

    Kato, Shingo; Itoh, Kyoko; Yaoi, Takeshi; Tozawa, Takenori; Yoshikawa, Yutaka; Yasui, Hiroyuki; Kanamura, Narisato; Hoshino, Akiyoshi; Manabe, Noriyoshi; Yamamoto, Kenji; Fushiki, Shinji

    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. PMID:20660952

  20. 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.

  1. Gateways to clinical trials.

    Science.gov (United States)

    Bayes, M; Rabasseda, X; Prous, J R

    2002-01-01

    Gateways to Clinical Trials is a guide to the most recent clinical trials in current literature and congresses, which has been retrieved from the Clinical Studies knowledge area of Prous Science Integrity, the world's first drug discovery and development portal, providing information on study design, treatments, conclusions and references. This issue focuses on the following selection of drugs: Abacavir sulfate; abciximab; abetimus sodium; adalimumab; aldesleukin; almotriptan; alteplase; amisulpride; amitriptyline hydrochloride; amoxicillin trihydrate; atenolol; atorvastatin calcium; atrasentan; Beclometasone dipropionate; bosentan; Captopril; ceftriaxone sodium; cerivastatin sodium; cetirizine hydrochloride; cisplatin; citalopram hydrobromide; Dalteparin sodium; darusentan; desirudin; digoxin; Efalizumab; enoxaparin sodium; ertapenem sodium; esomeprazole magnesium; estradiol; ezetimibe; Famotidine; farglitazar; fluorouracil; fluticasone propionate; fosamprenavir sodium; Glibenclamide; glucosamine sulfate; Heparin sodium; HSPPC-96; hydrochlorothiazide; Imatinib mesilate; implitapide; Lamivudine; lansoprazole; lisinopril; losartan potassium; l-Propionylcarnitine; Melagatran; metformin hydrochloride; methotrexate; methylsulfinylwarfarin; Nateglinide; norethisterone; Olmesartan medoxomil; omalizumab; omapatrilat; omeprazole; oseltamivir phosphate; oxatomide; Pantoprazole; piperacillin sodium; pravastatin sodium; Quetiapine hydrochloride; Rabeprazole sodium; raloxifene hydrochloride; ramosetron hydrochloride; ranolazine; rasburicase; reboxetine mesilate; recombinant somatropin; repaglinide; reteplase; rosiglitazone; rosiglitazone maleate; rosuvastatin calcium; Sertraline; simvastatin; sumatriptan succinate; Tazobactam sodium; tenecteplase; tibolone; tinidazole; tolterodine tartrate; troglitazone; Uniprost; Warfarin sodium; Ximelagatran. PMID:11980386

  2. 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.

  3. 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.

  4. 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.

  5. 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.

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

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    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.

  7. 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

  8. COMPORTAMIENTO DEL USO DE HIPOTENSORES EN EL POLICLÍNICO CAPITÁN ROBERTO FLEITES / Use of hypotensive medications at Capitán Roberto Fleites Polyclinic

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    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

  9. Indomethacin-Induced Pancreatitis. A Second Case Report

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    Wassim Mahjoub

    2006-05-01

    Full Text Available A 71-year-old woman presented to the Emergency Unit with a one-day history of severe epigastric pain of sudden onset with nausea and vomiting. Her medical history was significant for hypertension which had been treated by captopril for one year and rheumatoid arthritis treated by indomethacin for one month. There was neither history of alcohol consumption nor trauma. No family history of pancreatitis was noted. Her physical examination revealed a mildly distended abdomen with epigastric tenderness. Laboratory data showed elevated blood amylase (918 IU/L; reference range: 40-84 IU/L and urine amylase levels (8,080 IU/L; reference range: 60-240 IU/L, an elevated white cell count (17,000 mL-1; reference range: 4,000-10,000 mL-1 and hypocalcemia (1.8 mmol/L; reference range: 2-2.25 mmol/L. Serum values of urea and creatinine were within normal reference levels. Bilirubinemia was 106 mmol/L (reference range: 5-17 mmol/L and direct bilirubinemia was 5 mmol/L (reference range: 0-5 mmol/L. Alanine aminotransferase (27 IU/L reference range: 0-35 IU/L, lactate-dehydrogenase (320 IU/L reference range: 160-320 IU/L, gamma-glutamyltransferase (40 IU/L; reference range: 8-40 IU/L, and alkaline phosphatase (128 IU/L; reference range: 40- 130 IU/L were within the normal range. Cholesterol (4.20 mmol/L; reference range: 3.78-6.32 mmol/L and triglycerides (0.86 mmol/L; reference range: 0.57-1.97 mmol/L were normal. A diagnosis of pancreatitis was made. The Ranson score was equal to three. Abdominal ultrasound revealed a normal biliary tree without any choledocholithiasis. The Wirsung duct was dilated with hypertrophy of the pancreas. Abdominal computed tomography (CT showed diffuse pancreatic necrosis with fluid collections in the anterior lateral space of both kidneys and in the lower omental sac. The course was uneventful with progressive clinical improvement; the patient started to eat one week after admission with no vomiting or pain. CT of the abdomen

  10. ACESSO A MEDICAMENTOS ESSENCIAIS EM FARMÁCIAS E DROGARIAS DO MUNICÍPIO DE ARARAQUARA.

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    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

  11. 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。

  12. Inhibition of Uncaria alkaloids on collagen deposition of SHR thoracic aorta and effects on matrix metalloproteinase%钩藤生物碱抑制高血压大鼠主动脉胶原沉积及对基质金属蛋白酶的影响

    Institute of Scientific and Technical Information of China (English)

    姜月华; 孙敬昌; 周洪雷; 王永瑞; 李运伦

    2012-01-01

    目的 探讨钩藤碱、异钩藤碱和钩藤总生物碱抑制SHR(自发性高血压大鼠(spontaneous hypertension rats,SHR)胸主动脉胶原沉积的实验效应及相关机制.方法 40只SHR随机分为5组:模型组、卡托普利组、异钩藤碱组、钩藤碱组和钩藤总生物碱组;Wistar大鼠8只作为正常对照组.卡托普利组给药量为每天17.5 mg·kg-1,异钩藤碱组、钩藤碱组和钩藤总生物碱组的给药量分别为每天5、5、50 mg·kg-1,模型组和正常组给予等容量生理盐水.灌胃给药8周.取胸主动脉,通过Masson染色法、免疫组织化学染色法、原位杂交法并结合图像分析技术,观察钩藤碱、异钩藤碱和钩藤总生物碱对SHR胸主动脉胶原、ColⅠ、ColⅢ、MMP-9、MMP-2、TIMP-2表达的影响.结果 钩藤碱、异钩藤碱和钩藤总生物碱能够降低SHR胸主动脉胶原含量,下调ColⅠ、ColⅢ的蛋白和mRNA表达水平,上调MMP-9和MMP-2蛋白表达水平,上调MMP-9 mRNA表达水平,下调TIMP-2蛋白和mRNA表达水平.结论 钩藤碱、异钩藤碱和钩藤总生物碱具有抑制SHR胸主动脉胶原重塑的效应,部分机制与上调MMP-9和MMP-2、下调TIMP-2的表达有关.%Aim To study the inhibition of rhyncho-phylline, isorhynchophylline and Uncaria alkaloids on collagen deposition in SHR ( spontaneous hypertensionrats )thoracic aorta and the related mechanisms. Methods 40 SHR were randomly divided into five groups: model group , captopril group , rhynchophylline group ,isorhynchophylline group and total Uncaria alkaloids group,with the 8 Wistar rats as normal control group. Intragastric administrated for 8 weeks, dose: captopril group, 17.5 mg "kg"1 body weight per day; isorhynchophylline group and rhynchophylline group, 5 mg ? Kg'1 body weight per day; total Uncaria alkaloids group, 50 mg ? Kg'1 body weight per day; model group and normal control group were given same volume of saline. Thoracic aorta was taken by surgery. Collagen deposition

  13. 异叶青兰总黄酮对高血压大鼠心肌肥厚的影响%Effects of Dracocephalum heterophyllum Benth flavonoid on cardiac hypertrophy of hypertension rats

    Institute of Scientific and Technical Information of China (English)

    何雯; 邬利娅·伊明; 司丽君; 苗娜; 阿吉艾克拜尔·艾萨; 帕尔哈提·克热木

    2013-01-01

    目的 观察异叶青兰总黄酮对肾性高血压大鼠心肌肥厚的影响.方法 左肾动脉狭窄(2K1C)法建立高血压大鼠模型,术后第6周随机分为5组:假手术组(Sham);模型组(Model);异叶青兰总黄酮高剂量组(DHBFH)、低剂量组(DHBFL);卡托普利组(Captopril).灌胃给药6周后进行超声心动图、心肌病理学检测,白介素-1β(IL-1β)、肿瘤坏死因子-α(TNF-α)、基质金属蛋白酶-9(MMP-9)和基质金属蛋白酶抑制剂-1(TIMP-1)mRNA的测定.结果 给药6周后,模型组大鼠左心室室壁厚度、心肌细胞大小及左心室心肌间质纤维化程度较假手术组明显升高,IL-1β、TNF-α明显升高(P<0.01),MMP-9、TIMP-1 mRNA的相对表达量明显升高(P<0.01),给予DHBFH后,左心室肥厚及心肌纤维化较模型组明显降低,IL-1β、TNF-α明显降低,MMP-9、TIMP-1 mRNA的相对表达量明显降低(P<0.01).结论 异叶青兰总黄酮能改善高血压大鼠心肌肥厚及心肌纤维化程度,可能与其能够降低血压,降低IL-1β、TNF-α水平,调节MMP-9/TIMP-1的表达有关.%Aim To study the effect of Dracocephalum heterophyllum Benth flavonoid ( DHBF ) on cardiac hypertrophy of hypertension rats. Methods Hypertension rats model was established by renal artery stenosis surgery ( two kidneys one clip ). Six weeks after the surgery, the rats were randomly divided into 5 groups Sham group; Model group; DHBF high dose group ( DHBFH ); DHBF low dose group( DHBFL ) and Cap-topril group. After treated for 6 weeks, the echocardio-graphy, histological examination of the heart were performed. The levels of IL-1 β , TNF-α, the relative expression of MMP-9 mRNA and TIMP-1 mRNA were detected by real-time PCR . Results After 6 weeks treatment, the wall thickness of left ventricle, myocar-dial cell size and interstitial fibrosis of the myocardial cells in the left ventricl in Model group were significantly increased compared with those in sham group( P <0. 01 ). Treatment with

  14. Protective effect of Dracocephalum heterophyllum Benth.on blood vessel endothelium of hypertensive rats%异叶青兰总黄酮对高血压大鼠血管内皮的保护作用

    Institute of Scientific and Technical Information of China (English)

    何雯; 邬利娅·伊明; 司丽君; 闫冬; 王雪飞; 萨迪克·诺莫诺夫; 帕尔哈提·克热木

    2013-01-01

    目的:研究异叶青兰总黄酮(Dracocephalumheterophyllum Benth flavonoid,DHBF)对高血压大鼠血管内皮的保护作用.方法:左肾动脉狭窄法建立“两肾一夹”高血压大鼠模型,设假手术组(Sham),模型组(Model),异叶青兰总黄酮低剂量组(DHBF-L)300 mg·kg 1·d-1、高剂量组(DHBF-H)600 mg·kg-1·d-1,卡托普利组(Captopril)20 mg·kg-1·d-1.灌胃给药6周,每周无创尾套法测量大鼠尾动脉收缩压.硝酸还原酶法测定血清中一氧化氮(NO)水平,放射免疫法测定心肌中ET-1含量,血浆中TXB2、6-keto-PGF1.含量,计算其比值.结果:异叶青兰总黄酮两剂量组能明显降低肾性高血压大鼠尾动脉收缩压(P<0.05,P<0.01),升高NO水平(P<0.05,P<0.01),降低ET水平(P<0.01),降低TXB2与6-keto-PGF1α比值(P<0.05).结论:异叶青兰总黄酮对高血压大鼠的血管内皮具有一定的保护作用.%OBJECTIVE To study the protective effect of Dracocephalum heterophyllum Benth flavonoid(DHBF) on blood vessel endothelium of hypertensive rats.METHODS Two-kidney-one-clip hypertensive rats were obtained by narrowing left kidney arteries.5 groups were divided as sham; model; DHBF low dose group (DHBF-L,300 mg·kg-1 ·d-1); DHBF high dose group (DHBF-H,600 mg· kg-1· d-1) and captopril (20 mg· kg-1) group.The drugs were given by intragastric administration for 6 weeks.Systolic blood pressure (SBP) was measured by tail cuff approach every week.After the sixth week,,the levels of NO in serum were measured by nitrate reductase method,The levels of ET in heart,TXB2,6-keto-PGF1α in plasma were all measured by radioimmunoassay and the ratio of TXB2 and 6-keto-PGF1α were calculated.RESULTS DHBF significantly reduced hypertensive rats' blood pressure(P<0.05,P<0.01),increased the concentration of NO (P<0.05,P<0.01)while decreased the content of ET(P<0.01) ; reduced the ratio of TXB2and 6-keto-PGF10 (P<0.05).CONCLUSION The re sults suggest that DHBF could be used to

  15. 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

  16. 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

  17. 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.

    Directory of Open Access Journals (Sweden)

    Maira Quirós Enríquez.

    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

  18. 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

  19. 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.

  20. 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

  1. 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.

  2. Investigation of interaction studies of cefpirome with ACE-inhibitors in various buffers

    Science.gov (United States)

    Nawaz, Muhammad; Arayne, Muhammad Saeed; Sultana, Najma; Abbas, Hira Fatima

    2015-02-01

    This work describes a RP-HPLC method for the determination and interaction studies of cefpirome with ACE-inhibitors (captopril, enalapril and lisinopril) in various buffers. The separation and interaction of cefpirome with ACE-inhibitors was achieved on a Purospher Star, C18 (5 μm, 250 × 4.6 mm) column. Mobile phase consisted of methanol: water (80:20, v/v, pH 3.3); however, for the separation of lisinopril, it was modified to methanol-water (40:60, v/v, pH 3.3) and pumped at a flow rate of 1 mL min-1. In all cases, UV detection was performed at 225 nm. Interactions were carried out in physiological pH i.e., pH 1 (simulated gastric juice), 4 (simulated full stomach), 7.4 (blood pH) and 9 (simulated GI), drug contents were analyzed by reverse phase high performance liquid chromatography. Method was found linear in the concentration range of 1.0-50.0 μg mL-1 with correlation coefficient (r2) of 0.999. Precision (RSD%) was less than 2.0%, indicating good precision of the method and accuracy was 98.0-100.0%. Furthermore, cefpirome-ACE-inhibitors' complexes were also synthesized and results were elucidated on the basis of FT-IR, and 1H NMR. The interaction results show that these interactions are pH dependent and for the co-administration of cefpirome and ACE-inhibitors, a proper interval should be given.

  3. Biology of infantile hemangioma.

    Science.gov (United States)

    Itinteang, Tinte; Withers, Aaron H J; Davis, Paul F; Tan, Swee T

    2014-01-01

    Infantile hemangioma (IH), the most common tumor of infancy, is characterized by an initial proliferation during infancy followed by spontaneous involution over the next 5-10 years, often leaving a fibro-fatty residuum. IH is traditionally considered a tumor of the microvasculature. However, recent data show the critical role of stem cells in the biology of IH with emerging evidence suggesting an embryonic developmental anomaly due to aberrant proliferation and differentiation of a hemogenic endothelium with a neural crest phenotype that possesses the capacity for endothelial, hematopoietic, mesenchymal, and neuronal differentiation. Current evidence suggests a putative placental chorionic mesenchymal core cell embolic origin of IH during the first trimester. This review outlines the emerging role of stem cells and their interplay with the cytokine niche that promotes a post-natal environment conducive for vasculogenesis involving VEGFR-2 and its ligand VEGF-A and the IGF-2 ligand in promoting cellular proliferation, and the TRAIL-OPG anti-apoptotic pathway in preventing cellular apoptosis in IH. The discovery of the role of the renin-angiotensin system in the biology of IH provides a plausible explanation for the programed biologic behavior and the β-blocker-induced accelerated involution of this enigmatic condition. This crucially involves the vasoactive peptide, angiotensin II, that promotes cellular proliferation in IH predominantly via its action on the ATIIR2 isoform. The role of the RAS in the biology of IH is further supported by the effect of captopril, an ACE inhibitor, in inducing accelerated involution of IH. The discovery of the critical role of RAS in IH represents a novel and fascinating paradigm shift in the understanding of human development, IH, and other tumors in general. PMID:25593962

  4. 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.

  5. Valsartan in the treatment of heart failure or left ventricular dysfunction after myocardial infarction

    Directory of Open Access Journals (Sweden)

    Naylin Bissessor

    2007-09-01

    Full Text Available Naylin Bissessor1, Harvey White21Cardiology Research Fellow, 2Director of Coronary Care and Green Lane, Cardiovascular Research Unit, Green Lane Cardiovascular Research Unit, Auckland City Hospital, Auckland, New ZealandAbstract: The physiological role of the renin angiotensin aldosterone system (RAAS is to maintain the integrity of the cardiovascular system. The effect of angiotensin II is mediated via the angiotensin type I receptor (AT1 resulting in vasoconstriction, sodium retention and myocyte growth changes. This causes myocardial remodeling which eventually leads to left ventricular hypertrophy, dilation and dysfunction. Inhibition of the RAAS with angiotensin converting enzyme (ACE inhibitors after acute myocardial infarction has been shown to reduce cardiovascular morbidity and mortality. Angiotensin receptor blockers (ARBs specifically inhibit the AT1 receptor. It has not been known until the performance of the VALIANT (valsartan in acute myocardial infarction trial whether blockade of the angiotensin receptor with an ARB or combination of an ACE inhibitor and ARB leads to similar outcomes as an ACE inhibitor. The VALIANT trial demonstrated equal efficacy and non-inferiority of the ARB valsartan 160 mg bid compared with captopril 50 mg tds, when administered to high risk patients with left ventricular dysfunction or heart failure in the immediate post myocardial infarction period. The combination therapy showed no incremental benefit over ACE inhibition or an ARB alone and resulted in increased adverse effects. This review examines the role of valsartan in left ventricular dysfunction post myocardial infarction. We also discuss pharmacokinetics, dosing, side effects, and usage in the elderly.Keywords: valsartan, heart failure, left ventricular dysfunction, myocardial infarction

  6. 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.

  7. A structural view of the antibiotic degradation enzyme NDM-1 from a superbug.

    Science.gov (United States)

    Guo, Yu; Wang, Jing; Niu, Guojun; Shui, Wenqing; Sun, Yuna; Zhou, Honggang; Zhang, Yaozhou; Yang, Cheng; Lou, Zhiyong; Rao, Zihe

    2011-05-01

    Gram-negative Enterobacteriaceae with resistance to carbapenem conferred by New Delhi metallo-β-lactamase 1 (NDM-1) are a type of newly discovered antibioticresistant bacteria. The rapid pandemic spread of NDM-1 bacteria worldwide (spreading to India, Pakistan, Europe, America, and Chinese Taiwan) in less than 2 months characterizes these microbes as a potentially major global health problem. The drug resistance of NDM-1 bacteria is largely due to plasmids containing the blaNDM-1 gene shuttling through bacterial populations. The NDM-1 enzyme encoded by the blaNDM-1 gene hydrolyzes β-lactam antibiotics, allowing the bacteria to escape the action of antibiotics. Although the biological functions and structural features of NDM-1 have been proposed according to results from functional and structural investigation of its homologues, the precise molecular characteristics and mechanism of action of NDM-1 have not been clarified. Here, we report the three-dimensional structure of NDM-1 with two catalytic zinc ions in its active site. Biological and mass spectroscopy results revealed that D-captopril can effectively inhibit the enzymatic activity of NDM-1 by binding to its active site with high binding affinity. The unique features concerning the primary sequence and structural conformation of the active site distinguish NDM-1 from other reported metallo-β-lactamases (MBLs) and implicate its role in wide spectrum drug resistance. We also discuss the molecular mechanism of NDM-1 action and its essential role in the pandemic of drug-resistant NDM-1 bacteria. Our results will provide helpful information for future drug discovery targeting drug resistance caused by NDM-1 and related metallo-β-lactamases. PMID:21637961

  8. A case of bilateral aldosterone-producing adenomas differentiated by segmental adrenal venous sampling for bilateral adrenal sparing surgery.

    Science.gov (United States)

    Morimoto, R; Satani, N; Iwakura, Y; Ono, Y; Kudo, M; Nezu, M; Omata, K; Tezuka, Y; Seiji, K; Ota, H; Kawasaki, Y; Ishidoya, S; Nakamura, Y; Arai, Y; Takase, K; Sasano, H; Ito, S; Satoh, F

    2016-06-01

    Primary aldosteronism due to unilateral aldosterone-producing adenoma (APA) is a surgically curable form of hypertension. Bilateral APA can also be surgically curable in theory but few successful cases can be found in the literature. It has been reported that even using successful adrenal venous sampling (AVS) via bilateral adrenal central veins, it is extremely difficult to differentiate bilateral APA from bilateral idiopathic hyperaldosteronism (IHA) harbouring computed tomography (CT)-detectable bilateral adrenocortical nodules. We report a case of bilateral APA diagnosed by segmental AVS (S-AVS) and blood sampling via intra-adrenal first-degree tributary veins to localize the sites of intra-adrenal hormone production. A 36-year-old man with marked long-standing hypertension was referred to us with a clinical diagnosis of bilateral APA. He had typical clinical and laboratory profiles of marked hypertension, hypokalaemia, elevated plasma aldosterone concentration (PAC) of 45.1 ng dl(-1) and aldosterone renin activity ratio of 90.2 (ng dl(-1) per ng ml(-1 )h(-1)), which was still high after 50 mg-captopril loading. CT revealed bilateral adrenocortical tumours of 10 and 12 mm in diameter on the right and left sides, respectively. S-AVS confirmed excess aldosterone secretion from a tumour segment vein and suppressed secretion from a non-tumour segment vein bilaterally, leading to the diagnosis of bilateral APA. The patient underwent simultaneous bilateral sparing adrenalectomy. Histopathological analysis of the resected adrenals together with decreased blood pressure and PAC of 5.2 ng dl(-1) confirmed the removal of bilateral APA. S-AVS was reliable to differentiate bilateral APA from IHA by direct evaluation of intra-adrenal hormone production. PMID:26538381

  9. Maitake Mushroom Extracts Ameliorate Progressive Hypertension and Other Chronic Metabolic Perturbations in Aging Female Rats

    Directory of Open Access Journals (Sweden)

    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.

  10. Synthesis and characterization of retrograded starch nanoparticles through homogenization and miniemulsion cross-linking.

    Science.gov (United States)

    Ding, Yongbo; Zheng, Jiong; Zhang, Fusheng; Kan, Jianquan

    2016-10-20

    A new and convenient route to synthesizing retrograded starch nanoparticles (RS3NPs) through homogenization combined with a water-in-oil miniemulsion cross-linking technique was developed. The RS3NPs were optimized using Box-Behnken experimental design. Homogenization pressure (X1), oil/water ratio (X2), and surfactant (X3) were selected as independent variables, whereas particle size was considered as a dependent variable. Results indicated that homogenization pressure was the main contributing variable for particle size. The optimum values for homogenization pressure, oil/water ratio, and surfactant were 30MPa, 9.34:1, and 2.54g, respectively, whereas the particle size was predicted to be 288.2 nm. Morphological, physical, chemical, and functional properties of the RS3NPs were the assessed. Scanning electron microscopy and dynamic light scattering images showed that RS3NP granules were broken down to size of about 222.2nm. X-ray diffraction results revealed a disruption in crystallinity. The RS3NPs exhibited a slight decrease in To, but Tp and Tc increased and narrowest Tc-To. The solubility and swelling power were also increased. New peaks at 1594.84 and 1403.65cm(-1) were observed in the FTIR graph. However, homogenization minimally influenced the antidigestibility of RS3NPs. The absorption properties improved, and the adsorption kinetic described the contact time on the adsorption of captopril onto RS3NPs. In vitro release experiment indicated that the drug was released as follows: 21% after 2h in SGF, 42.78% at the end of 8h (2h in SGF and 6h in SIF), and 92.55% after 12h in SCF. These findings may help better utilize RS3NP in biomedical applications as a drug delivery material. PMID:27474611

  11. Angiotensin II receptors in the gonads

    Energy Technology Data Exchange (ETDEWEB)

    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. Prevalence of cough among patients treated with angiotensin converting enzyme inhibitors

    Directory of Open Access Journals (Sweden)

    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.

  13. 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.

  14. In vivo hypotensive effect and in vitro inhibitory activity of some Cyperaceae species

    Directory of Open Access Journals (Sweden)

    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.

  15. Effect of lercanidipine on myocardial remodeling induced by myocardial infarction in rats%乐卡地平对心肌梗死大鼠心肌重构的影响

    Institute of Scientific and Technical Information of China (English)

    罗永鑫; 姚明辉; 鲁映青; 贡沁燕

    2003-01-01

    目的:观察乐卡地平对心肌梗死大鼠心肌重构的影响.方法:雄性Wistar大鼠,结扎冠状动脉左前降支,造成心肌梗死.实验分为4组:假手术组、心肌梗死模型组、卡托普利组、乐卡地平组.在结扎冠状动脉后3 h开始,分别灌胃给予生理盐水、生理盐水、卡托普利50 mg*kg-1和乐卡地平2.5 mg*kg-1,qd,共35 d.给药容积均为10 mL*kg-1.最后一次给药后24 h,处死大鼠取心脏,测定全心重量和体重比(THW/ BW)、梗死范围(IS)、左心室内径(LVD)、室间隔厚度(ST),用天狼猩红染色,在图像分析系统下测量心肌间质胶原容积系数(ICVF)和血管周围胶原容积系数(PCVF).结果:心肌梗死模型组大鼠的THW/ BW[(0.38±s 0.03) %] 和LVD[(8.8±1.4)mm]均显著比假手术组[(0.325±0.016) %;(6.5±0.3)mm]大(P<0.05,P<0.01),ST[(1.71±0.22)mm]则明显比假手术组[(2.75±0.18)mm]小(P<0.01),IS为(26±3)%.与模型组比较,卡托普利和乐卡地平组大鼠的IS[(18±6) %,(19±7) %]和LVD[(7.5±0.8)mm,(7.7±0.9)mm]显著变小(P<0.05 ,P<0.01);ST[(2.4±0.4)mm, ( 2.4±0.5)mm]显著变大(P<0.05, P<0.01).心肌梗死模型组大鼠心肌ICVF和PCVF分别为(6.7±1.0) %和(67.41±0.11) %,明显比假手术组[(4.0±0.5) %, (43.40±0.11) %]大(P<0.05, P<0.01).卡托普利组和乐卡地平组大鼠心肌的ICVF分别是(5.0±1.0) %,(4.913±0.012) %; PCVF分别是(47.54±0.15) %,(46.18±0.18) %,均比心肌梗死模型组明显减小(P<0.01).结论:乐卡地平能够改善心肌梗死大鼠的心肌重构.%AIM: To observe the effect of lercanidipine on myocardial remodeling induced by myocardial infarction (MI). METHODS: MI was induced by permanent ligation of the left anterior descending coronary artery (LAD) in male Wistar rats. Rats were randomly divided into four groups: sham operation group, MI model group, captopril 50 mg*kg-1 group and lercanidipine 2.5 mg*kg-1 group. Three hours after the operation, the drugs or normal saline were administrated ig qd

  16. A Novel Vasoactive Proline-Rich Oligopeptide from the Skin Secretion of the Frog Brachycephalus ephippium.

    Directory of Open Access Journals (Sweden)

    Daniel Dias Rufino Arcanjo

    Full Text Available Proline-rich oligopeptides (PROs are a large family which comprises the bradykinin-potentiating peptides (BPPs. They inhibit the activity of the angiotensin I-converting enzyme (ACE and have a typical pyroglutamyl (Pyr/proline-rich structure at the N- and C-terminus, respectively. Furthermore, PROs decrease blood pressure in animals. In the present study, the isolation and biological characterization of a novel vasoactive BPP isolated from the skin secretion of the frog Brachycephalus ephippium is described. This new PRO, termed BPP-Brachy, has the primary structure WPPPKVSP and the amidated form termed BPP-BrachyNH2 inhibits efficiently ACE in rat serum. In silico molecular modeling and docking studies suggest that BPP-BrachyNH2 is capable of forming a hydrogen bond network as well as multiple van der Waals interactions with the rat ACE, which blocks the access of the substrate to the C-domain active site. Moreover, in rat thoracic aorta BPP-BrachyNH2 induces potent endothelium-dependent vasodilatation with similar magnitude as captopril. In DAF-FM DA-loaded aortic cross sections examined by confocal microscopy, BPP-BrachyNH2 was found to increase the release of nitric oxide (NO. Moreover, BPP-BrachyNH2 was devoid of toxicity in endothelial and smooth muscle cell cultures. In conclusion, the peptide BPP-BrachyNH2 has a novel sequence being the first BPP isolated from the skin secretion of the Brachycephalidae family. This opens for exploring amphibians as a source of new biomolecules. The BPP-BrachyNH2 is devoid of cytotoxicity and elicits endothelium-dependent vasodilatation mediated by NO. These findings open for the possibility of potential application of these peptides in the treatment of endothelial dysfunction and cardiovascular diseases.

  17. 中枢移行性アンジオテンシン変換酵素阻害剤投与によるラット脳内ペプチド性物質のプロファイリング

    OpenAIRE

    金澤, 佐知子; 細井, 一広; 照井, 一史; 下山, 律子; 中川, 潤一; 板垣, 史郎; 早狩, 誠

    2014-01-01

    本研究は,中枢移行性ACE 阻害剤(ACEI)による記憶保持亢進の機序を解明することである.中枢移行性ACEI(captopril),非中枢移行性ACEI (imidapril)およびARB(losartan)投与ラットでの脳内ペプチドの発現変化をHPLC 法およびTOF-MS 法を用いて検索した.その結果,TOF-MS 法では,captopril 投与群で特異的に発現が亢進するペプチドを多数検出できたが, その多くは質量数3,000以下であった.なお,これらの質量数はすべて一価イオンとして検出されたことから,すべて物質固有の質量数を反映していた.検出した質量数は,ACE が分解する脳内ペプチド(LH-RH,substance P, β-neoendorphin, neuromedin B, LVV-hemorphin-7, amyloid β-protein)やinsulin-regulated aminopeptidase(IRAP)の基質と考えられているvasopressin とは異なる値を示した.脳内にはACE やIRAP 以外にも活性中心にZn2+を有するメタロプロテア...

  18. 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).

  19. 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

  20. Role of α2-adrenoceptors in the lateral parabrachial nucleus in the control of body fluid homeostasis

    International Nuclear Information System (INIS)

    Central α2-adrenoceptors and the pontine lateral parabrachial nucleus (LPBN) are involved in the control of sodium and water intake. Bilateral injections of moxonidine (α2-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 α2-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 α2-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 α2-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 α2-adrenoceptors in the LPBN may affect palatability and, consequently, ingestion of sodium as well as renal sodium excretion

  1. 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.

  2. 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.

  3. Pharmacological characterization of the rat paw edema induced by Bothrops lanceolatus (Fer de lance) venom.

    Science.gov (United States)

    de Faria L; Antunes, E; Bon, C; de Araújo, A L

    2001-06-01

    The inflammatory response induced by Bothrops lanceolatus venom (BLV) in the rat hind-paw was studied measuring paw edema. Non-heated BLV (75microg/paw) caused a marked paw edema accompanied by intense haemorrhage whereas heated venom (97 degrees C, 30s; 12.5-100microg/paw) produced a dose- and time-dependent non-haemorrhagic edema. The response with heated BLV was maximal within 15min disappearing over 24h. Heated venom was then routinely used at the dose of 75microg/paw. The prostacyclin analogue iloprost (0.1microg/paw) potentiated by 125% the venom-induced edema. The histamine H(1) receptor antagonist mepyramine (6mg/kg) or the serotonin/histamine receptor antagonist cyproheptadine (6mg/kg) partially inhibited BLV-induced edema whereas the combination of both compounds virtually abolished the edema. The lipoxygenase inhibitor BWA4C (10mg/kg), but not the cyclooxygenase inhibitor indomethacin (10mg/kg), significantly inhibited the edema (35% reduction; P<0.05). Dexamethasone (1mg/kg) also markedly (P<0.001) reduced venom-induced edema. The bradykinin B(2) receptor antagonist Hoe 140 (0.6mg/kg) reduced by 30% (P<0.05) the venom induced edema, whereas the angiotensin-converting enzyme inhibitor captopril (300microg/paw) potentiated by 42% (P<0.05) the edema. Bothrops lanceolatus antivenon (anti-BLV) reduced by 28% (P<0.05) the venom-induced edema while intravenous administration of antivenom failed to affect the edema. In conclusion, BLV-induced rat paw edema involves mast cell degranulation causing local release of histamine and serotonin, a phenomenon mediated mainly by kinins and lipoxygenase metabolites. Additionally, the use of a specific Bothrops lanceolatus antivenom, given subplantarily or intravenously, revealed to be little effective to prevent BLV-induced edema. PMID:11137542

  4. 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.

  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. Analysis of the Application of Antihypertensive Oral Drugs in Our Hospital in 2010-2012%2010~2012年我院口服抗高血压药应用分析

    Institute of Scientific and Technical Information of China (English)

    陈春荣; 刘爽

    2013-01-01

    Objective:To investigate the application of oral antihypertensive drugs in our hospital, and provide evidence for clinical rational drug use. Methods: to col ect oral pharmacy store management system of antihypertensive drugs in our hospital sales data, by who (WHO) by defined daily dose (DDD) method, the 2010-2012 of oral antihypertensive drugs in our hospital drug consumption sum, DDDs of drugs daily cost (DDDs), (DDC), drug utilization index (DUI) statistical analysis. Results: the oral antihypertensive drug sales amount is increasing year by year, calcium antagonists (CCB), angiotensin II receptor antagonist (ARB) and angiotensin converting enzyme inhibitor (ACEI) ranks among the top 3. Valsartan Antihypertensive sales amount of the largest. Captopril is used in our hospital, the highest frequency of antihypertensive drugs most widely used. Conclusion:the application of antihypertensive drugs in our hospital basical y conforms to the principle of medication safety, ef ective, economy.%目的:了解我院口服抗高血压药物的应用情况,为临床合理用药提供依据。方法收集我院药库管理系统口服抗高血压药销售数据,采用世界卫生组织(WHO)推荐的限定日剂量(DDD)方法,对我院2010~2012年口服抗高血压药的用药金额、用药频度(DDDs)、药品日均费用(DDC)、药物利用指数(DUI)进行统计分析。结果我院口服抗高血压药销售金额呈逐年上升趋势,钙离子拮抗剂(CCB)、血管紧张素Ⅱ受体拮抗剂(ARB)和血管紧张素转换酶抑制剂(ACEI)位居前3位。缬沙坦是我院销售金额最大的抗高血压药。卡托普利是我院使用频率最高、应用最广泛的抗高血压药。结论我院抗高血压药物应用基本符合安全、有效、经济的用药原则。

  7. Potential prescription patterns and errors in elderly adult patients attending public primary health care centers in Mexico City

    Directory of Open Access Journals (Sweden)

    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

  8. The right choice of antihypertensives protects primary human hepatocytes from ethanol- and recombinant human TGF-β1-induced cellular damage

    Directory of Open Access Journals (Sweden)

    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

  9. 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.

  10. 持续泵入硝普钠﹑多巴胺治疗顽固性心力衰竭19例疗效观察

    Institute of Scientific and Technical Information of China (English)

    范希廷

    2014-01-01

    Objective Observe trace pump continuous pump into the denitration prachanda sodium, dopamine in chronic heart failure of treatment effect. Methods Select our May 2012until 2013 November in our hospitalization 19cases intractable hf patients in routine to oxygen, the radix rehmanniae, diuretics, captopril, times his joy grams and remove incentive, correct electrolyte disorders such as treatment on the basis of, be trace pump continuous pump into the denitration prachanda sodium and dopamine. The patients were observed before and after the treatment to improve cardiac function and heart rate, blood pressure, respiratory changes. Results Trace pump continuous pump into the denitration prachanda sodium and dopamine total effective treatment resistant heart failure, heart rate, respiration 94.7% have satisfactory cosmetic were markedly improved (P<0.05). Conclusion Trace pump continuous pump into the denitration prachanda sodium and dopamine intractable hf treatment results were satisfactory, popularization.%目的:观察微量泵持续泵入硝普钠、多巴胺在顽固性心衰治疗中的效果。方法选取我院2012年5月至2013年11月于我院住院治疗的19例顽固性心衰患者,在常规予以吸氧、洋地黄、利尿剂、卡托普利、倍他乐克及去除诱因、纠正电解质紊乱等治疗基础上,予以微量泵持续泵入硝普钠及多巴胺。结果微量泵持续泵入硝普钠及多巴胺治疗顽固性心衰总有效率94.7%,心率、呼吸均明显改善(P<0.05)。结论微量泵持续泵入硝普钠及多巴胺治疗顽固性心衰疗效满意,值得推广应用。

  11. 1例多囊肝多囊肾合并脑出血患者的药学监护%Pharmaceutical care on a patient with cerebral hemorrhage with polycystic liver and polycystic kidney disease

    Institute of Scientific and Technical Information of China (English)

    石秀锦; 魏国义

    2012-01-01

    One 76-year-old male patient with cerebral hemorrhage, polycystic liver and polycystic kidney, pulmonary infection and hypertension was hospitalized. The patient was given empirical anti-infection treatment with cefepime for pulmonary infection. Considering the renal insufficiency and susceptibility culture results of the patient, clinical pharmacists proposed to treat with fusidic sodium, vancomycin and cefoperazone/sulbactam. Fat overload syndrome induced by intralipid was analyzed, and clinical pharmacist recommended to withdraw the intralipid intravenous infusion and switch to glucose injection to supply of energy. In addition, the elderly patient with renal hypertension, the selection of antihypertensive drugs was discussed, and captopril, telmisartan and sodium nitroprusside should be changed to fosinopril sodium, amlodipine besylate and furosemide. After the rational optimization of the treatment, the pulmonary infection was controlled timely and effectively and the blood pressure was controlled stably. The symptoms of this patient improved markedly.%1例76岁男性患者,因多囊肝多囊肾合并脑出血、肺部感染及高血压入院.针对患者肺部感染,医生经验性给予头孢吡肟,结合患者肾功能不全及药敏培养结果,临床药师建议采用夫西地酸钠、万古霉素及头孢哌酮钠/舒巴坦钠联合抗感染;同时,对脂肪乳引起的脂肪超载综合征进行分析,建议停用脂肪乳静脉滴注,改用葡萄糖注射液供给能量;并对患者降压药物的选择进行讨论,建议将卡托普利、替米沙坦、硝普钠改为福辛普利钠、苯磺酸氨氯地平、呋塞米.经合理优化治疗方案后,患者感染得到及时、有效的治疗,血压控制较平稳,病情明显好转.

  12. Therapeutic possibilities of Bothrops jararaca in high dilution

    Directory of Open Access Journals (Sweden)

    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

  13. Utility of a transdermal delivery system for antihypertensive therapy. Part 1.

    Science.gov (United States)

    Sclar, D A; Skaer, T L; Chin, A; Okamoto, M P; Gill, M A

    1991-07-18

    A retrospective evaluation of patient-level Medicaid claims data from two states was undertaken to discern the fiscal utility of transdermally delivered clonidine versus both the oral formulation of clonidine and oral formulations of eight other antihypertensive agents. In the first phase of our two-part study, we compared paid claims data (n = 1,135) from Florida for transdermal and oral clonidine. Multivariate regression analysis was used to evaluate the incremental impact of six variables on health-care expenditures in the first year after patients were given a diagnosis of hypertension. These variables were: age, gender, prior utilization of medical services, regimen complexity, and dosage formulation. Patients prescribed transdermal clonidine experienced a significant (p less than or equal to 0.001) increase in prescription expenditures and significant reductions in the use of physician (p less than or equal to 0.05), laboratory (p less than or equal to 0.10), and hospital (p less than or equal to 0.05) services. Moreover, savings were maximized (p less than or equal to 0.001) where multi-drug regimens incorporated the transdermal delivery system. In the second phase of our study we compared paid claims data (n = 8,894) from South Carolina for transdermal clonidine and for nine oral antihypertensive agents: atenolol, captopril, clonidine, diltiazem, enalapril, metoprolol, prazosin, terazosin, and verapamil-SR. Once again, regression analysis was used, this time to evaluate the incremental impact of five variables on health-care expenditures in the first year post diagnosis: age, gender, prior utilization of medical services, regimen complexity, and Medication Possession Ratio (MPR), an index of compliance. The data from part 2 of our study revealed that patients assigned a b.i.d. oral antihypertensive agent experienced a significant reduction (p less than or equal to 0.05) in MPR and a significant (p less than 0.05) increase in health-care expenditures when

  14. 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.

  15. [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

  16. Identification of retinoic acid in a high content screen for agents that overcome the anti-myogenic effect of TGF-beta-1.

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    Chateen Krueger

    Full Text Available BACKGROUND: Transforming growth factor beta 1 (TGF-β1 is an inhibitor of muscle cell differentiation that is associated with fibrosis, poor regeneration and poor function in some diseases of muscle. When neutralizing antibodies to TGF-β1 or the angiotensin II inhibitor losartan were used to reduce TGF-β1 signaling, muscle morphology and function were restored in mouse models of Marfan Syndrome and muscular dystrophy. The goal of our studies was to identify additional agents that overcome the anti-myogenic effect of TGF-β1. METHODOLOGY/PRINCIPAL FINDINGS: A high-content cell-based assay was developed in a 96-well plate format that detects the expression of myosin heavy chain (MHC in C2C12 cells. The assay was used to quantify the dose-dependent responses of C2C12 cell differentiation to TGF-β1 and to the TGF-β1 Type 1 receptor kinase inhibitor, SB431542. Thirteen agents previously described as promoting C2C12 differentiation in the absence of TGF-β1 were screened in the presence of TGF-β1. Only all-trans retinoic acid and 9-cis retinoic acid allowed a maximal level of C2C12 cell differentiation in the presence of TGF-β1; the angiotensin-converting enzyme inhibitor captopril and 10 nM estrogen provided partial rescue. Vitamin D was a potent inhibitor of retinoic acid-induced myogenesis in the presence of TGF-β1. TGF-β1 inhibits myoblast differentiation through activation of Smad3; however, retinoic acid did not inhibit TGF-β1-induced activation of a Smad3-dependent reporter gene in C2C12 cells. CONCLUSIONS/SIGNIFICANCE: Retinoic acid alleviated the anti-myogenic effect of TGF-β1 by a Smad3-independent mechanism. With regard to the goal of improving muscle regeneration and function in individuals with muscle disease, the identification of retinoic acid is intriguing in that some retinoids are already approved for human therapy. However, retinoids also have well-described adverse effects. The quantitative, high-content assay will be

  17. Perindopril: first-line treatment for hypertension.

    Science.gov (United States)

    Zanchetti, A; Desche, P

    1989-01-01

    The antihypertensive efficacy and acceptability of perindopril (P) were compared to those of captopril (C), atenolol (A) and a diuretic, hydrochlorothiazide + amiloride (D), in 3 double-blind parallel multicenter studies involving 165, 173, and 165 patients, respectively. Patients with essential hypertension and a supine DBP between 95 and 125 mmHg (mean 103.9, 106.2, and 105.2 mmHg, respectively) after a 1-month placebo period were randomized to P 4 mg once daily (o.d.) and either C 25 mg twice daily, or A 50 mg o.d. or D (hydrochlorothiazide 50 mg + amiloride 5 mg o.d.) and treated for 3 months, with visits at monthly intervals. If necessary, treatment was adjusted at each visit to control BP (supine DBP less than or equal to 90 mm Hg): firstly by doubling the dose and secondly, one month later, by the addition of a second drug, a diuretic in the studies versus C or A, a beta-blocker in the study versus D. At 3 months, BP control on monotherapy in the three studies was achieved in the following proportion of patients: 49% with P vs 49% with C; 55% with P vs 48% with A; 72% with P vs 72% with D. Most of the patients controlled by P received 4 mg, about 15% were controlled with 8 mg. A further percentage of patients was controlled with combination therapy, the combination with a diuretic being more effective with P than with C (26 vs 8%) or A (23 vs 10%) and the combination with a beta-blocker being less effective with P than with D (5 vs 13%). The total percentage of patients controlled was greater with P than with C (75 vs 57%, p = 0.016) or A (78 vs 58%, p = 0.006) and there was no significant difference between P and D (78 vs 84%). The drop-out rate due to side-effects was up to 6% with P, similar to that observed with C (4%), A (5%) and D (5%). Most of the complaints reported with P were minor and non-specific, their incidence being similar to that observed with the other drugs. Cough was reported with both P (1%) and C (2%) as well as with A (1%) and D (1

  18. 培哚普利片治疗原发性高血压的疗效研究%Curative Effect of Perindopril Tablets Treating Essential Hypertension

    Institute of Scientific and Technical Information of China (English)

    马昌勇

    2014-01-01

    Objective ToexplorethecurativeeffectofPerindoprilTabletstreatingessentialhypertension.Methods 120patientswithprimaryhypertensioninourhospitalfromOctober2012toOctober2013,whichweredividedintotwo groups,60 cases in treatment group were treated with Perindopril Tablets;60 cases in control group were treated with capto-pril. After two months of treatment,curative effect and changes of observation index before and after the treatment of two groups werecompared.Results Aftertreatment,thetotaleffectiverateoftreatmentgroupwashigherthancontrolgroup,thediffer-ence was statistically significant( P<0. 05);Diastolic blood pressure,systolic blood pressure and heart rate of treatment group were lower than control group,the incidence of adverse reaction was lower than control group,the differences were statistically significant(P<0.05).Conclusion ThecurativeeffectofPerindoprilTabletstreatinghypertensionsignificantlyisremarka-ble,has less adverse reaction.%目的:探讨培哚普利片治疗原发性高血压的临床疗效。方法将2012年10月-2013年10月在本院进行治疗的120例原发性高血压患者分为两组,治疗组60例,应用培哚普利片治疗;对照组60例,应用卡托普利治疗。治疗两个月后,比较两组患者的治疗效果和治疗前后的观察指标的变化。结果治疗后,治疗组总有效率高于对照组,差异有统计学意义( P<0.05);治疗组的舒张压、收缩压以及心率均低于对照组,不良反应发生率也低于对照组,差异均有统计学意义( P<0.05)。结论培哚普利片治疗原发性高血压的临床疗效显著,不良反应少。

  19. Efficacy of Carvedilol in Patients with Dilated Cardiomyopathy due to Beta-Thalassemia Major; a Double-Blind Randomized Controlled Trial

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    Afsaneh Ashrafi

    2010-09-01

    Full Text Available Objective: Dilated cardiomyopathy is the end result of chronic iron overload in patients with beta thalassemia major. The objective of the present study was to evaluate the safety and efficacy of Carvedilol in patients with beta thalassemia major and dilated cardiomyopathy.Methods: During a six-month period, fourteen patients with beta-thalassemia major and heart failure without diabetes mellitus referred to pediatric cardiology clinic enrolled in this double blind, randomly assigned study. All patients were on anti failure therapy with Digoxin, Captopril and Furosemide. Carvedilol was started at a dosage of 3.12 mg bid and for patients who had a systolic blood pressure >100 mmHg, heart rate >60/min and no signs of low cardiac output the dosage was increased every two weeks to a maximum of 25 mg bid. Clinical signs and symptoms, systolic and diastolic echocardiographic indexes and Tissue Doppler Imaging (TDI data were collected from each patient.Findings: Eight patients received Carvedilol (Group 1 and six received placebo (Group 2. The mean age of patients in Group1 and 2 were 16±0.7 years and 17±3 years respectively. Only one patent in Group 1 tolerated increasing Carvedilol dosage to more than 6.25 mg bid. Changes in New York Heart Association (NYHA classification, Ejection fraction, End diastolic dimension changes, TDI systolic(S, early (Ea and late (Aa diastolic waves were not statistically significant in these two Groups (P>0.05. Pulse Doppler E/A wave ratio of mitral valve in Group1 and Group 2 changed from 1.1±0.37 m/s to 1.8±0.40 m/s and from 1.34±0.30 m/s to 2.6±0.23m/s respectively (P=0.04.Conclusion: Patients with thalassemia and dilated cardiomyopathy have poor tolerance to increasing Carvedilol dosage and develop decreased systolic blood pressure during advancement of the drug dosage. Carvedilol can be effective in prevention of progression of diastolic dysfunction in these patients.

  20. 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。

  1. Analysis of Clinical Effect of Valsartan Combined with Perindopril in Treatment of Diabetic Nephropathy%缬沙坦联合培哚普利治疗糖尿病肾病的临床效果分析

    Institute of Scientific and Technical Information of China (English)

    王艳华

    2015-01-01

    Objective To investigate the joint without perindopril valsartan split clinical curative effect for the treatment of diabetic nephropathy.Methods Our hospital in March 2013 ~May 2014 were treated 96 cases of diabetic nephropathy were randomly divided into experimental and control groups, the control group were treated with the use of valsartan alone method for treatment,patients in the experimental group Valerian sand Tan and perindopril treatment.Results The experimental group of valsartan and perindopril combination therapy, with a total effective rate of the experimental group were 93.7%, significantly better than the control group of patients with total efficiency of 68.9%, the difference was significant (P0.05.Conclusion Valsartan combined without perindopril captopril treatment of diabetic nephropathy effect is remarkable, for renal tissue took place, worthy of promotion.%目的:探讨缬沙坦联合培哚普利治疗糖尿病肾病的临床疗效。方法选取我院2013年3月~2014年5月收治的96例糖尿病肾病患者,将其随机分为实验组和对照组,对照组患者采用单独使用缬沙坦方法进行治疗,实验组患者在对照组方法的基础上加入培哚普利进行治疗。结果实验组采用缬沙坦和培哚普利联合治疗,实验组患者的总有效率为93.7%,明显优于对照组患者的总有效率68.9%,差异显著(P0.05。结论采用缬沙坦联合培哚普利治疗糖尿病肾病效果显著,对肾组织无毒害作用,值得推广。

  2. 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

  3. 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.

  4. 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

  5. Measuring access to medicines: a survey of prices, availability and affordability in Shaanxi province of China.

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    Minghuan Jiang

    Full Text Available OBJECTIVE: To measure the prices and availability of selected medicines in Shaanxi Province after the implementation of new healthcare reform in 2009. METHODS: Data on the prices and availability of 47 medicines were collected from 50 public and 36 private sector medicine outlets in six regions of Shaanxi Province, Western China using a standardized methodology developed by the World Health Organization and Health Action International from September to October 2010. Medicine prices were compared with international reference prices to obtain a median price ratio. Affordability was measured as the number of days' wages required for the lowest-paid unskilled government worker to purchase standard treatments for common conditions. FINDINGS: The mean availabilities of originator brands and lowest-priced generics were 8.9% and 26.5% in the public sector, and 18.1% and 43.6% in the private sector, respectively. The public sector procured generics and originator brands at median price ratios of 0.75 and 8.49, respectively, while patients paid 0.97 and 10.16. Final patient prices for lowest-priced generics and originator brands in the private sector were about 1.53 and 8.36 times their international retail prices, respectively. Public sector vendors applied high markups of 30.4% to generics, and 19.6% to originator brands. In the private sector, originator brands cost 390.7% more, on average, than their generic equivalents. Generic medicines were priced 17.3% higher in the private sector than the public sector. The lowest-paid government worker would need 0.1 day's wages to purchase captopril for lowest-priced generics from private sector, while 6.6 days' wages for losartan. For originator brands, the costs rise to 1.2 days' wages for salbutamol inhaler and 15.6 days' wages for omeprazole. CONCLUSIONS: The prices, availability and affordability of medicines in China should be improved to ensure equitable access to basic medical treatments, especially for

  6. Clinical pharmacokinetics of vasodilators. Part II.

    Science.gov (United States)

    Kirsten, R; Nelson, K; Kirsten, D; Heintz, B

    1998-07-01

    -fed infants, combined with more women delaying pregnancy until their fourth decade, has entailed an increase in the need for hypertension management during lactation. Low dose hydrochlorothiazide, propranolol, nifedipine and enalapril or captopril do not pose enough of a risk of preclude breastfeeding in this group. The most frequently used antihypertensive agents during pregnancy are methyldopa, labetalol and calcium channel antagonists. Methyldopa and beta-blockers are the drugs of choice for treating mild to moderate hypertension. Prazosin and hydralazine are used to treat moderate to severe hypertension and hydralazine, urapidil or labetalol are used to treat hypertensive emergencies. The use of overly aggressive antihypertensive therapy during pregnancy should be avoided so that adequate uteroplacental blood flow is maintained. Methyldopa is the only drug accepted for use during the first trimester of pregnancy. PMID:9673832

  7. 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.

  8. Altered efficacy of AT1R-targeted treatment after spontaneous cancer cell-AT1R upregulation

    International Nuclear Information System (INIS)

    Targeting of the renin angiotensin system (RAS) reduces tumour growth in experimental models of cancer. We aimed to establish if combined targeting of the 'classical' and 'alternative' arms of the RAS could result in synergistic inhibition of colorectal cancer (CRC) liver metastases. Immediately following induction of CRC liver metastases through intrasplenic injection of murine CRC cells, treatment with irbesartan (AT1R blocker; 50 mg/kg/day s.c.), captopril (ACE inhibitor; 750 mg/kg/day i.p.), CGP42112A (AT2R agonist; 0.6 μg/kg/hr i.p.), and/or ANG-(1-7) (24 μg/kg/hr i.p.) began and continued for 21 days. Liver to body weight ratio and/or stereology were used as a measure of tumour burden. Immunohistochemistry was used to determine AT1R and VEGF expression as well as proliferation (Ki67), apoptosis (active caspase 3) and angiogenesis (CD34). Combined RAS therapies failed to improve upon single arm therapies. However, while irbesartan previously inhibited tumour growth in this model, in the current experiments irbesartan failed to affect tumour burden. Subsequent analysis showed a cancer-cell specific upregulation of the angiotensin II type I receptor (AT1R) in irbesartan-insensitive compared to irbesartan-sensitive tumours. The upregulation of AT1R was associated with an increase in proliferation and VEGF expression by cancer cells. While animals bearing irbesartan-sensitive tumours showed a marked decrease in the number of proliferating cells in the liver and VEGF-expressing infiltrating cells in the tumour following AT1R treatment, these were unchanged by treatment in animals bearing irbesartan-insensitive (high AT1R expressing) tumours. Although the results do not support increased efficacy of combined treatment, they provide intriguing evidence of the importance of RAS expression in determining patient response and tumour growth potential and suggest that components of the RAS could be used as biomarkers to aid in patient selection

  9. A Comparative Effectiveness Meta-Analysis of Drugs for the Prophylaxis of Migraine Headache.

    Directory of Open Access Journals (Sweden)

    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

  10. Evaluation of the assistance to diabetics and or hypertenses at a Primary Health Care Unit

    Directory of Open Access Journals (Sweden)

    Claudio Oliveira Souto

    2010-11-01

    Full Text Available This paper bas the general objective to perform an evaluation of the assistance to hypertenses and/or diabetics at a health care unit of Primary Health Care, taking into account the importance of nontransmissible chronic diseases, being the cardiovascular diseases the first cause of mortality in Brazil - systemic arterial hypertension and diabetes mellitus are the main risk factors of the population, which are potentially controllable. A descriptive cross-sectional study was held, with a quantitative approach on a population of 462 hypertensive and diabetic patients, registered al the health unit of Planalto, Santa Rosa (RS; the pieces of information gathered refer to the period from September 2006 to September 2007. We noticed that, in general, structure toward care, as recommended by the Ministry of Health, is adequate. We found 431 hypertensive patients registered at the health unit, corresponding to a coverage rate of 59.6%, and 83 diabetic patients, corresponding to a coverage rate of 64.8%. The highest concentration of the registered individuals is between the age range of 50 to 69 years (56.9%. We confirmed that 87.4% of the registered patients presented one visit or more with the family and community physician (MFC; 75.5% attended on time to the date of return visit; 52.2% adhered to the treatment; 16.7% were smokers; 39.6% led a sedentary life and 49.8% were obese. The increase of the left ventricle was the most frequent complication. Metformin, hydrochlorothiazide and captopril are not being distributed to the registered patients on a regular basis. There is a lot of glibenclamide in stock. The cardiovascular high risk stratification found in this study corresponds to 23.1% by means of the British strategy and 37.3% of the American strategy, bringing to the surface the cost-benefit discussion in the treatment with the use of statins. The cardiovascular high-risk patients showing LDL cholesterol below 100mg/dl correspond to 16.3% by the

  11. The Clinical Observation on the Effect of WeenXin Granules to Pulse Pressure of P atients with Coron ary Heart Disease%稳心颗粒对冠心病脉压影响的临床观察

    Institute of Scientific and Technical Information of China (English)

    高博

    2011-01-01

    Objective:To observe the impact of WenXin granules on pulse pressure of patients with coronary heart disease.Methods:The 143 patients with coronary heart disease were randomly divided into two groups:the treat group(73) and the control group(70), tested the resting blood pressure with cuff bag mercury sphygmomanometer consistent with measurement standard, calculated the pulse pressure.The treat group was treated with WenXin granules(27 g/d,3/d,per os) and the control gronp was treated with captopril(37.5 mg/d,3/d)the basis medication of the two groups were same,l month was 1 course oftrcatment. Results: WenXin granules decrease elevated pulse pressure duc to coronary heart disease 9.06 mmHg(1 mmHg 0.133 kPa),P<0.005, the difference was significant. Conclusion:WenXin granules has significant effect of reducing the pnlse pressnre,can reduce the incidence of coronary heart disease.%目的:观察稳心颗粒对冠心病脉压的影响.方法:将143例冠心病患者随机分为治疗组(73例)与对照组(70例),治疗组用稳心颗粒27 g/d,3次/d,口服;对照组用卡托普利37.5 mg/d,3次/d;2组均以1个月为1个疗程,用符合计量标准的袖袋式水银柱血压计测静息血压,计算脉压.结果:稳心颗粒对因冠心病增高的脉压平均可降低9.06 mmHg(1 mmHg=0.133 kPa),与对照组比较有统计学意义(P<0.05).结论:稳心颗粒有较明显地降低脉压作用,可降低冠心病的发病率.

  12. 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.

  13. 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?

    Directory of Open Access Journals (Sweden)

    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

  14. 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

    Directory of Open Access Journals (Sweden)

    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

  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. 96孔板法用于高通量血管紧张素转化酶抑制剂体外检测%Establishment of in Vitro High-throughput Activity Detection Method for Angiotensin Converting Enzyme Inhibitors Based on 96 Well Plates

    Institute of Scientific and Technical Information of China (English)

    骆琳; 丁青芝; 马海乐

    2012-01-01

    A high throughput method for the determination of angiotensin converting enzyme (ACE) inhibitory activity, using 96-well plate technology, has been developed. Hydrolysis of N-[3-(2-furyl) acryloyl[L-phenylalanyl-glycyl-glycine (FAPGG) to N-[3-(2-furyl)acryloyl]-L-phenylalanine (FAP) and glycyl-glycine(GG) by ACE was quantified by measuring the decrease in absorbance at 340 nm to evaluate the activity of ACE. The percentage inhibition of angiotensin converting enzyme inhibitory (ACEI) was determined by comparing the results of control and test samples. The effects of different buffer systems, chloride ion concentration, ACE activity (ACE enzyme concentration), pH value of buffer system on the test of the activity of angiotensin converting enzyme inhibitors in vitro model reaction system of detection were investigated. The new method can detect ACE inhibitory activity of no more than 96 ACEI samples in 10 s or so on microplate-reader for ELISA. For different batches of sample, the RSD was less than 0. 001%, p = 0. 667(>0. 05), which shows no significant difference between the results measured. The method is simple, accurate, stable, and reliable in antihyperten-sive peptide in vitro inhibitory activity of ACE measured. The method was used to detect a famous angiotensin converting enzyme inhibitors product named Captopril and a IC50 value ( Half inhibitory concentration) of 16.19 nmol/L was obtained, which is consistent with the results have been reported in extensive literature.%为在体外迅速检测血管紧张素转化酶抑制剂( ACEI)的抑制活性,选用96孔板,以呋喃丙烯酰三肽(FAPGG)为模拟底物,通过检测血管紧张素转化酶(ACE)酶解FAPGG生成N-[3-(呋喃)丙稀醇酰-2-苯丙氨酸( FAP)和双甘氨肽(GG)后340 nm处吸光值的下降衡量ACE的活性,采用加入ACEI前后ACE的活性变化衡量ACEI的活性.考察了不同缓冲体系、Cl-浓度、ACE酶活性(ACE酶浓度)、缓冲体系的pH值等对上述检测模型反应

  17. Relationship between ACEI/D gene polymorphism and curative effects of angiotensinconverting enzyme inhibitor in elderlyhypertension patients%老年高血压患者 ACEI/D基因多态性与 ACE 抑制剂疗效的相关性

    Institute of Scientific and Technical Information of China (English)

    梁冰; 胡丙清; 刘绪和

    2014-01-01

    Objective To explore the relationship between the ACE geneinsertion /deletion ( I/D ) polymorphism and the curative effects of angiotensin-converting enzyme inhibitor ( ACEI ) in elderly patients with hypertension.Methods Polymerase chain reaction(PCR) technique was used to detect ACE I/D polymorphism in 108 subjects of elderly hypertensionpatients who received no therapy ever , and the patients were classified as II, ID and DD genotype .Meanwhile captopril was administered for 6 weeks to all patients .Measure the blood pressure of all patients during the treatment and post treatment .Results The frequency of II genotype was 27%, the ID genotype was 33%and the DD genotype was 40%.4 patients in II group were markedly effective and 14 patients were effective , the effective rate was 61%.In ID group, 8 patients were markedly effective and 18 patients were effective , effective rate was 73%.In DD group 29 patients were markedly effective , 11 patients were effective , effective rate was 93%.Curative effect of captoprilwas significantly higher in DD group than in ID and II group(P<0.05).Conclusions ACE I/D gene polymorphism can be use as one of adjunctive indicators for predicting the effect of using ACEI inelderly patients with hypertension .%目的:探讨老年高血压患者ACE I/D基因多态性与血管紧张素转换酶抑制剂( ACEI )疗效的相关性。方法选取108例老年高血压未经降压治疗的患者;应用聚合酶链反应( PCR )方法检测其ACE I/D基因多态性,有三种表现形式:II型、DD型和ID型,根据其基因多态性分为三组,对所有高血压患者均给予卡托普利口服6周。治疗前后及治疗过程中对患者的血压进行监测。结果(1)108例高血压患者中II基因型频率为27%;ID型为33%;DD型为40%;(2)II组显著有效4例,有效14例,总有效率61%;ID组显著有效8例,有效18例,总有效率73%;DD组显著有效29例,有效11

  18. Optimal antagonism of the Renin-Angiotensin-aldosterone system: do we need dual or triple therapy?

    Science.gov (United States)

    Werner, Christian; Pöss, Janine; Böhm, Michael

    2010-07-01

    The cardiovascular and cardiorenal disease continuum comprises the transition from cardiovascular risk factors to endothelial dysfunction and atherosclerosis, to clinical complications such as myocardial infarction (MI) and stroke, to the development of persistent target-organ damage and, ultimately, to chronic congestive heart failure (CHF), end-stage renal disease or premature death. The renin-angiotensin-aldosterone system (RAAS) is involved in all steps along this pathway, and RAAS blockade with ACE inhibitors or angiotensin AT(1)-receptor antagonists (angiotensin receptor blockers; ARBs) has turned out to be beneficial for patient outcomes throughout the disease continuum. Both ACE inhibitors and ARBs can prevent or reverse endothelial dysfunction and atherosclerosis, thereby reducing the risk of cardiovascular events. These drugs have further been shown to reduce end-organ damage in the heart, kidneys and brain. Aldosterone antagonists such as spironolactone and eplerenone are increasingly recognized as a third class of RAAS inhibitor with potent risk-reducing properties, especially but not solely with respect to the inhibition of cardiac remodelling and the possible prevention of heart failure. In secondary prevention, head-to-head comparisons of ACE inhibitors and ARBs, such as the recent ONTARGET study, provided evidence that, in addition to better tolerability, ARBs are non-inferior to ACE inhibitors in the prevention of clinical endpoints such as MI and stroke in cardiovascular high-risk patients. However, the combination of both ramipril and telmisartan at the maximally tolerated dosage achieved no further benefits and was associated with more adverse events such as symptomatic hypotension and renal dysfunction. In acute MI complicated by heart failure, the VALIANT trial has shown similar effects of ACE inhibition with captopril and ARB treatment with valsartan, but dual RAAS blockade did not further reduce events. In CHF, meta-analyses of RESOLVD, Val

  19. Diuréticos melhoram a capacidade funcional em pacientes com insuficiência cardíaca congestiva Diuretics improve functional capacity in patients with congestive heart failure

    Directory of Open Access Journals (Sweden)

    Francesca Tadeu Eterno

    1998-05-01

    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 (pPURPOSE: The 6-9 minute walking test was used in this study to evaluate the impact of these drugs on functional capacity of patients admitted to the Hospital because of Heart Failure (CHF. METHODS: Ten patients (5 males and 5 females with mean age of 47 years and NYHA CHF functional class III or IV underwent a 6-9 minute walking test at admission and on the day of discharge from the Hospital. The following parameters were evaluated both at admission and discharge: body weight, echocardiography-derived LV dimensions and function, plasmatic levels of sodium, potassium, BUN, creatinine, hemoglobin and hematocrit. Treatment consisted of increasing outpatient dose of furosemide (IV and/or PO plus the association of thiazide if necessary. The previous dose regimen of digitalis, ACE inhibitors or the association nitrate and hydralazine was kept unchanged. RESULTS: Time to

  20. 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

  1. 前列地尔治疗糖尿病肾病的临床研究%Clinical research of Alprostadil in the treatment of diabetic nephropathy

    Institute of Scientific and Technical Information of China (English)

    叶海燕; 杨昆; 周径; 张彦中

    2012-01-01

    目的 探讨联合应用前列地尔对糖尿病肾病患者的临床疗效.方法 将2010年1~12月我院收治的66例患者随机分为研究组和对照组各33例.两组患者均常规行降糖、饮食控制、蛋白摄入限量等基础性治疗,并给予卡托普利口服治疗,研究组患者在此基础上加用前列地尔.结果 研究组患者治疗后总有效率为93.94%,明显高于对照组(63.64%),差异有统计学意义(P < 0.05);两组患者治疗前各指标比较差异无统计学意义(P > 0.05);治疗后两组患者各指标均有明显下降(P < 0.05),但研究组血尿素氮(BUN)、空腹血糖(FPG)、白蛋白排泄率(UAER)明显低于对照组,差异有统计学意义(P < 0.05).结论前列地尔对于治疗糖尿病肾病具有较好的临床效果,能够有效提高对肾功能的修复和保护作用.%Objective To investigate the clinical curative effects of combined Alprostadil in the treatment of patients with diabetic nephropathy. Methods 66 cases admitted to our hospital from January 2010 to December 2010 were randomly divided into study group and control group, with 33 cases in each group. Both groups of patients received routine blood glucose reduction, diet control, protein intake limit and other basic treatment as well as oral administration of Captopril. Patients of the study group received additional Alprostadil on the basis. Results The total effective rate of the study group was 93.94%, which was significantly higher than 63.64% of the control group, with statistically significant difference (P 0.05); after the treatment, all the indicators of the two groups decreased significantly (P < 0.05), but blood urea nitrogen (BUN), fasting plasma glucose (FPG), urinary albumin excretion rate (UAER) of the study group were significantly lower than those of the control group, with statistically significant differences (P < 0.05). Conclusion Alprostadil shows good clinical curative effects in the treatment of diabetic

  2. The clinical curative effect of combiningdiuretics in the treatment of refractory cirrhotic ascitesand its influence on electrolyte%利尿剂联合应用治疗难治性肝硬化腹水临床疗效及对电解质的影响

    Institute of Scientific and Technical Information of China (English)

    叶应春

    2015-01-01

    Objective This paper was to investigate the clinical effect of combining multiple diuretics in the treatment of refractory cirrhotic ascites and to analyze the effect on electrolyte.Methods 100 patients with refractory cirrhotic ascites in our hospital during June 2013 and June 2014 were selected as the research object. They were randomly divided into observation group and control group.The former were treated with spironolactone and captopril at the first 7 days.Then depending on the actual situation, some of them got furosemide combined with dopamine as a combination.Finally, patients whose curative effects were not reached expect got mannitol therapy as a combination.While the control group got only albumin and furosemide.The treatment lasted for 28 days.Then we compared their treatment effect and the change of Na +and K +levels in blood and urine. Results The total efficiency rate of the observation group was 96.0%, which was significantly higher than 84. 0%of the control group (P0.05).But the 24h urine Na+and K+of both groups were significantly increased, and the two indexes of the observation group were obviously higher than that of control group, the difference has statistically significant (P<0.05).Conclusions The combination of multiple diuretics helps to increase the curative effect of refractory ascites due to cirrhosis, it is worth promoting.%目的:探讨多种利尿剂联合应用治疗难治性肝硬化腹水的临床疗效,并分析该疗法对电解质的影响。方法纳入2013年6月至2014年6月我院收治的100例难治性肝硬化腹水患者为研究对象,随机均分为观察组及对照组。前者首7d予安体舒通联合巯甲丙脯酸治疗,次7d视实际情况,酌情加用速尿联合多巴胺治疗,最后对未达预期疗效者予甘露醇治疗;后者应用白蛋白及速尿。均持续治疗28 d。对比两组疗效及治疗前后血及尿钠钾水平变化。结果观察组总有效率96.0

  3. 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

  4. 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

  5. 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

  6. 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,

  7. 维药异叶青兰醇提物对肾性高血压大鼠的影响及机制研究%Effect and mechanisms investigation of Dracocephalum heterophyllum Benth from Uighur Medicine in the renal hypertensive rats

    Institute of Scientific and Technical Information of China (English)

    司丽君; 马晓玲; 何雯; 王雪飞; 萨迪克·诺莫诺夫; 帕尔哈提·克力木

    2014-01-01

    目的:探讨异叶青兰醇提物对肾性高血压大鼠血压的影响及其降压机制。方法利用肾动脉狭窄法建立两肾一夹高血压大鼠模型;将成模的高血压大鼠随机分为假手术组、模型组、异叶青兰高剂量组(D HBE-H)、异叶青兰低剂量组(DHBE-L)、卡托普利组;灌胃给药5 w ,每周无创尾套法测量大鼠尾动脉血压;5 w 后用颈总动脉插管测血流动力学指标,采用硝酸还原酶法测定心肌组织中一氧化氮(N O )水平,化学比色法测定心肌组织中一氧化氮合成酶(NOS)水平,酶联免疫吸附法(ELISA)测定心肌组织中内皮素(ET)和血管紧张素Ⅱ(AngII)水平。结果与模型组相比,异叶青兰醇提物能使肾性高血压大鼠尾动脉收缩压明显降低;颈动脉收缩压(SBP)、舒张压(DBP)、左室收缩压(LVSP)、降低左室舒张末期压(LVEDP)均显著降低,室内压对数值最大变化速率(± dp/dtmax)/LVSP和收缩指数(CI)升高,NO水平升高,ET水平降低;AngII水平降低。结论异叶青兰醇提物能降低肾性高血压大鼠血压,增强心脏舒缩功能。%Objective To observe the effects of Dracocephalum heterophyllum Benth (DHBE) on blood pressure in renovascular hypertensive rats (RHR) and explore its mechanisms .Methods Two-kidney-one-clip RHRs were obtained by narrowing left kidney arteries .6 groups were divided as control ,model ,DH-BE high dose group (DHBE-H) ,DHBE low dose group (DHBE-L) and captopril groups .The drugs were given by intragastric administration for 5 weeks .Systolic blood pressure (SBP) were measured by tail cuff approach every week .After the fifth week ,we utilized left ventricular incubation to measure hemodynamic parameters .The levels of nitric oxide (NO) ,nitric oxide synthase (NOS) in heart were respectively meas-ured by nitrate reductase method and chemical colorimetry .The levels of endothelin (ET ) and

  8. 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

  9. 青钱柳叶水提物对Nω-硝基左旋精氨酸甲酯盐酸盐诱导的高血压大鼠的影响%Effect of the Aqueous Extract from Cyclocarya paliurus on Hypertensive Rats Induced by Nω-nitro-L-arginine Methyl Ester Hydrochloride

    Institute of Scientific and Technical Information of China (English)

    刘晓霞; 席加喜; 王硕; 张春花; 刘华钢; 缪剑华

    2012-01-01

    目的:探讨青钱柳叶水提物对Nω-硝基左旋精氨酸甲酯盐酸盐(L-NAME,Nω-nitro-L-arginine methyl ester hydrochloride)诱导的高血压大鼠的影响.方法:用L-NAME ig给药4周复制高血压大鼠模型.将40只高血压大鼠随机分为模型组、青钱柳叶水提物低、中、高剂量组(3.0,6.0,12.0 g·kg-1·d-1)和卡托普利组(0.010 g·kg-1·d-1),每组8只.另外正常8只SD大鼠作为空白组.采用无创尾动脉测压法,每周测定大鼠血压1次,共6周.计算大鼠左心室质量指数和肾脏质量指数,观察胸主动脉形态学变化.结果:给予青钱柳叶水提物6周后,高血压大鼠的收缩压和舒张压明显降低(P <0.01或P<0.05),其中低、中、高剂量组的收缩压下降率分别为16.18%,16.92%,16.92%;舒张压下降率分别为15.98%,15.73%,16.64%.同时治疗组左心室质量指数和肾脏质量指数下降(P<0.01或P<0.05),能够缓和胸主动脉中膜增厚现象.结论:青钱柳叶水提物对L-NAME诱导的高血压大鼠血压有降低作用.%Objective; To observe the effect of the aqueous extract from Cyclocarya paliurus on hypertensive rats induced by Z.-NAME ( Nω -nitro-L-arginine methyl ester hydrochloride). Method; Hypertensive rats were given by L-NAME for 4 weeks to produce hypertensive model. The 40 hypertensive rats were randomly divided into model group, C. paliurus extract low, medium and high dose group (3.0, 6.0, 12. 0 g · kg ') , captopril group (0.010 g - kg-1') , additional 8 rats were choose as control group. Non-invasive blood pressure measurement was used to detect the arterial blood pressure of rat tail once a week for 6 weeks. The left ventricular weight index and kidney weight index were calculated, and morphological changes of the thoracic aorta were observed. Result; After 6 weeks of administration, the systolic and diastolic blood pressure of hypertensive rats significantly decreased ( P < 0. 01 , P < 0. 05 ) , in low, medium and high

  10. Influence of Tiangou Jiangya capsule on blood pressure in renovascular hypertension rats%天钩降压胶囊对肾血管性高血压大鼠血压的影响

    Institute of Scientific and Technical Information of China (English)

    杨庆; 李玉洁; 刘晓霓; 翁小刚; 陈颖; 朱晓新; 韩晓; 邹丽娟; 李丹

    2011-01-01

    目的:观察天钩降压胶囊对肾血管性高血压大鼠的血压的影响并初步探讨其作用机制.方法:将72只Wistar大鼠随机分为正常对照组、模型组、卡托普利组(0.03 g·kg-1)、天钩降压胶囊低、中、高剂量组(5.4,10.8,21.6g· kg-1).采用无创血压仪测量鼠尾动脉血压;采用放射免疫法测定大鼠血中PRA,AngⅡ,ALD,6-酮-前列腺F1α,ET和TXB2的含量;采用硝酸还原酶法测定大鼠血中NO的含量.结果:模型组收缩压、舒张压和平均压明显升高,大鼠血中PRA,AngⅡ,ALD明显降低,ET水平明显增高;天钩降压胶囊能明显降低模型大鼠的血压,提高大鼠血中肾素活性,降低大鼠血中ET含量,升高NO含量.结论:天钩降压胶囊具有降低肾性高血压模型大鼠血压的作用,其降低血压的机制可能与其调控模型大鼠RAAS系统的分泌以及改善血管内皮的功能有关.%Objective: To observe the effect of Tiangou Jiangya capsule(TJC) on blood pressure in renovascular hypertension rats and explore its possible mechanism. Method; Seventy-two Wistar rats were randomly divided into normal control group, model group, captopril group, TJC small, medium and high dose groups. Non-invasive blood pressure measurement was used to detect the arterial blood pressure of rat tails. PRA, Ang Ⅱ , ALD, 6-Keto-PGF1α, ET and TXB2 content in blood was measured by radioimmunoas-say. NO content in blood was determined by method of nitrate reductase. Result; The systolic, diastolic and mean pressure significantly increased, serum PRA, Ang Ⅱ , ALD decreased, ET levels significantly increased in model group rats. TJC significantly reduced blood pressure, improved the plasma renin activity, decreased ET levels and increased NO content of model rats. Conclusion; TJC can reduce blood pressure of renovascular hypertention rats, and the mechanism may be related to its regulating lower blood pressure regulation of the secretion of RAAS system and

  11. 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

  12. 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,vigorous exercises should be avoided to decrease adverse cardiac events.

  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. Effect of Wenxin Granule on the Related Indexes of Senile Patients with Primary Hypertension and Acute Left Cardiac Failure%稳心颗粒对老年原发性高血压合并急性左心衰竭患者相关指标的影响

    Institute of Scientific and Technical Information of China (English)

    郑慧玲; 林明英; 吴玉琼

    2016-01-01

    目的:探讨稳心颗粒对老年原发性高血压合并急性左心衰竭患者相关指标的影响。方法:160例老年原发性高血压合并急性左心衰竭患者随机分为对照组(80例)和观察组(80例)。对照组患者给予卡托普利片初始剂量12.5 mg,口服,每日2~3次,按需要1~2周内增加至50 mg,每日2~3次(如患者近期服用大量利尿药,处于低钠和/或低血容量,血压正常或偏低患者,初始剂量为6.25 mg,每日3次);观察组患者在对照组治疗的基础上给予稳心颗粒9 g,口服,每日3次。两组疗程均为4周。观察两组患者治疗前后的收缩压(SBP)、舒张压(DBP)、脉压(PP)、正常R-R间期标准差(SDNN)、正常R-R间期平均标准差(SDANN)、全程每5 min R-R间期标准差的平均值(SDNN-Index)、相邻正常R-R间期差值的均方根(RMSSD)、相邻两个R-R间期>50 ms的个数占一定时间内R-R期间总个数的百分比(PNN50)及不良反应发生情况。结果:治疗后,两组患者SBP、DBP、PP均显著低于同组治疗前,且观察组低于对照组;SDNN、SDANN、SDNN-Index、RMSSD、PNN50均显著高于同组治疗前,且观察组高于对照组,差异均有统计学意义(P<0.05)。两组患者不良反应发生率比较,差异无统计学意义(P>0.05)。结论:在常规治疗的基础上,稳心颗粒可显著降低老年原发性高血压合并左心衰竭患者的血压,改善心功能,且安全性较好。%OBJECTIVE:To investigate the effects of Wenxin granule on the related indexes of senile patients with primary hy-pertension and acute left cardiac failure. METHODS:160 senile patients with primary hypertension and acute left cardiac failure were randomly divided into control group(80 cases)and observation group(80 cases). Control group received 12.5 mg captopril, orally,twice to 3 times a day (if patients had taken plenty of diuretic

  15. 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,

  16. Clinical Characteristics of Primary Renal Tubular Hypokalemic Alkalosis%原发肾小管性低钾碱中毒的临床特点

    Institute of Scientific and Technical Information of China (English)

    范树颖; 张碧丽; 王文红; 张碹; 李莉; 杜悦新

    2011-01-01

    Objective To explore the clinical characteristics of primary renal tubular hypokalemic alkalosis. Methods Eight patients with primary renal tubular hypokalemic alkalosis were selected in the Children's Hospital of Tianjin. There were 4 patients with Bartter syndrome(BS) and 4 patients with Gitelman syndrome(GS). Clinical data,biochemical tests,therapy and outcome were retrospectively analyzed.Results The onset age of BS were at infancy stage. The main symptoms included diarrhea, vomiting, dehydration and growth retardation. And the onset age of GS ranged from 10 to 15 years old with the main symptoms of weakness,paralysis and tetany. They had normal blood pressure.The biochemical tests showed hypokalemic, metabolic alkalosis, increase of urine potassium and urine chlorine in all patients. Four patients with BS had hyperreninemia and hyperaldosteronism. Angiotonin was elevated in all 4 patients with GS ,while rennin was elevated in 3 patients of them and aldosterone was obviously elevated in 2 patients. The urine Ca/Cr ratio in BS was elevated(>0.2) ,while patients with GS had hyponagnesaemia and low level of urine Ca/Ct ratio(<0.2). B - type ultrasonic wave showed that both kidneys's resonance had even reinforce in 2 patients with BS, and one of them had left pyelectasis. All symptoms resolved after treatment with potassium or combined magnesium supplementation,indomethacin,spironolactone and captopril. Conclusions Prinary renal tubular hypokalemic alkalosis is characterized by hypokalemic, metabolic alkalosis, hyperreninemic, hyperaldosteronism and normal blood pressure. Measured level of serum magnesium, urine potassium and chlorine and Ca/Ct ratio, rennin angiotonin and aldosterone can help make diagnosis. There are differences in onset mechanism,clinical manifestation,treatment and prognosis between BS and GS.%目的 探讨原发肾小管性低钾碱中毒的临床特点.方法 收集在天津市儿童医院住院治疗的原发肾

  17. 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

  18. 小剂量药物联合治疗高血压的可行性研究%Feasibility Study of Small Doses of Combined Drug Therapy in Treating Hypertension

    Institute of Scientific and Technical Information of China (English)

    丁绍祥

    2011-01-01

    Objective To analyze the present situation of individual treatment plan in treating hypertension with small doses of combined drugs including nifedipine ( N ), atenolol ( A ), hydrochlorothiazide ( H ) and captopril ( C ) after four years of its spread in grass roots, Xining. To evaluate the feasibility of the plan and the existing problems. Methods Select all the medical records of hypertension patients treated by NAHC individual treatment therapy in Xining from January 1, 2006 to December 31, 2009 to summarize and analyze this method from the aspects of its technical training, drugs selection, joins procedure, method of taking drugs, treatment costs and blood pressure of the patients before treatment, the blood pressure after treatment, the situation of continual medicine - taking, the reason of withdrawal from the therapeutic schedule and so on. Results A total of 801 patients were included with average age ( 57. 3 ± 10. 3 ), 340 males and 433 females. Before treatment, the average systolic blood pressure ( SBP ): ( 147. 9 ± 19. 4 ) mm Hg, the average diastolic blood pressure ( DBP ): ( 91. 4 ± 14. 1 ) mm Hg; After treatment, 368 subjects have records of blood pressure, the male are 160 cases and female 280 cases. The average SBP: ( 128. 5 ± 12. 4 ) mm Hg, the average DBP: ( 80. 05 ±8. 7 ) mm Hg. 351 patients' hypertension were recovered; the total effective rate was 95. 4% ; 85 cases had kept on taking medicine for 2 years or more, accounting for 10. 6% . Because the medical records are not complete, the numbers of no sex record, no contact phone number, no blood pressure record before treatment, no age record, no previous highest blood pressure record or family history were respectively 28, 29, 33, 34, 365 and 392. The average expense of daily use on drugs was 0. 09 yuan, and annual cost was 33 yuan. Conclusion The cost of NAHC indi-viduation therapeutic schedule is inexpensive with sound therapeutic effects and is fit to be popularized in the grass roots

  19. 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

  20. 槲皮素对大鼠实验性高血压、高血糖合并高脂血症作用的研究%Effects of quercetin on hypertension,hyperglycemia and hypercholesterolemia in rats

    Institute of Scientific and Technical Information of China (English)

    翟云鹏; 汪建云; 刘耀武; 羊倩倩; 张明珠; 王涛; 尹家乐; 鲁茜

    2012-01-01

    Objective To observe the preventive and therapeutic effects of quercetin on hypertension , hyperglycemia and hypercholesterolemia in rats. Methods Adult spontaneously hypertensive male rats were fed high - fat and high — sugar diet for four weeks , and then received intraperitoneal injection of streptozotocin once in a dose of 35 mg/kg to induce the model of hypertension , hyperglycemia and hypercholesterolemia. Meanwhile, Wistar rats fed normal diet were set as control group. The model rats were randomly divided into 3 groups; model group, captopril group (CAP) , quercetin group (QE). Every group was fed high -fat and high - sugar diet and treated for 8 weeks. After treatment, blood samples were collected. Blood pressure, blood glucose, total cholesterol ( TC) , triglyeride ( TG) , low density lipoprotein cholesterol (LDL — C ) , high density lipoprotein cholesterol ( HDL — C) , kidney index ( RI) , blood urea nitrogen (BUN), creatinine (Cr) were measured. Results Compared with normal control groups , blood pressure, blood glucose , total cholesterol, triglyeride, LDL — C were significantly increased and HDL — C were decreased in three groups of model rats (P <0. 01). Compared with the model group , blood pressure, Cr in CAP rats were significantly lower (P < 0.05 or P < 0.01) ; blood pressure, blood glucose, TC, TG, LDL - C, RI, BUN and Cr in QE rats were significantly reduced (P <0.05 or P <0.01) ; HDL - C level in QE rats was significantly higher (P <0.05). Conclusion The results suggest that effects of quercetin are better on hypertension , hyperglycemia and hypercholesterolemia in rats than cap -topril.%目的 探讨槲皮素对大鼠高血压、高血糖合并高脂血症的治疗作用.方法 成年雄性自发性高血压大鼠(SHR)高糖高脂饲料喂养4周后,给予小剂量链脲霉素(streptozotocin,STZ) 35 mg/kg腹腔注射诱导高血压、高血糖合并高脂血症大鼠模型,以基础饲料喂养的Wistar大鼠作为正常对照.将

  1. Metabolismo de fármacos y lesión hepática

    Directory of Open Access Journals (Sweden)

    Elso Manuel Cruz Cruz

    2015-03-01

    el menor porcentaje. Los fármacos que ocasionan lesión hepática de forma intrínseca pueden actuar directamente sobre el hepatocito, o a través de algún compuesto tóxico generado durante su metabolismo; ejemplos de ello son el paracetamol, ácido acetilsalicílico y muchos de sus derivados. Por otra parte, la hepatotoxicidad idiosincrática es aquella que ocurre de forma impredecible y no depende de la dosis del fármaco, ésta tiene mayor incidencia. Ejemplos de medicamentos que provocan esta hepatotoxicidad son: ácido valproico, alopurinol, amiodarona, bupropión, captopril, carbamazepina, ciclofosfamida, ciproheptadina, clindamicina, clotrimazol, diclofenaco, enalapril, estatinas, fenitoína, fenobarbital, fluoxetina, flutamida, glibenclamida, ibuprofeno, isoniazida, ketoconazol, lisinopril, losartán, metotrexate, nefazodona, nevirapina, nitrofurantoína, paroxetina, pirazinamida, quinolonas, rifampicina, risperidona, ritonavir, sertralina, sulfonamidas, tetraciclina, trazodona, troglitazona, verapamil, entre muchos otros. (1, 3 Se proponen diferentes mecanismos causantes de lesión hepatocelular: la alteración de la homeostasis del calcio intracelular, que conduce al desarreglo de las fibrillas de actina existentes en la superficie del hepatocito, modificando la membrana celular, con posterior rotura y lisis; interrupción de los filamentos cerca de los canalículos, con la rotura de éstos y reducción en la excreción biliar, fenómeno que también puede estar asociado a la interrupción del transporte de bilis por las bombas proteicas; reacciones que involucran al sistema del citocromo P-450, al generar reacciones de alta energía que producen enlaces covalentes fármaco-enzima, creando complejos proteicos no funcionales que migran hacia la superficie de la célula y son inmunogénicos, convirtiéndose en blanco de las células T citolíticas y de las citosinas; algunos fármacos inhiben la función mitocondrial por efecto en la beta-oxidación de los