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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. Compound list: captopril [Open TG-GATEs

    Lifescience Database Archive (English)

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

  3. Development studies of captopril certified reference material

    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.

  4. 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...

  5. Captopril

    Science.gov (United States)

    ... angiotensin-converting enzyme (ACE) inhibitors. It decreases certain chemicals that tighten the blood vessels, so blood flows ... metallic taste, or decreased ability to taste cough fast heartbeat ... the Food and Drug Administration's (FDA) MedWatch Adverse Event Reporting ...

  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. 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

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

    OpenAIRE

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

    2015-01-01

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

  10. 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

  11. 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.

  12. 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

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

    Energy Technology Data Exchange (ETDEWEB)

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

    1990-04-01

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

  14. 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

  15. 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

  16. 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

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

    Science.gov (United States)

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

    2015-01-01

    We describe a 39-year-old woman with an apparent captopril-induced, contact mucosal-dominant pemphigus vulgaris and angioedema, who took captopril during a bout of arterial hypertension. This exposure suggests that captopril and pathophysiology of angioedema stimulated the development of pemphigus vulgaris, which was diagnosed using the novel, indirect immunofluorescence BIOCHIP mosaic, with the modification to detect serum IgG4 autoantibodies. We discuss the patient, who experienced a chain of events leading to the active stage of pemphigus vulgaris, and review concepts of pemphigus vulgaris inducible by drugs and pathological immunity. PMID:26560224

  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; Rouleau, Jean-Lucien; Køber, Lars; Maggioni, Aldo P; Solomon, Scott D; Swedberg, Karl; Van de Werf, Frans; White, Harvey; Leimberger, Jeffrey D; Henis, Marc; Edwards, Susan; Zelenkofske, Steven; Sellers, Mary Ann; Califf, Robert M

    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...... angiotensin-receptor blocker valsartan, the ACE inhibitor captopril, and the combination of the two on mortality in this population of patients. METHODS: Patients receiving conventional therapy were randomly assigned, 0.5 to 10 days after acute myocardial infarction, to additional therapy with valsartan (4909...... (P<0.001). The valsartan-and-captopril group had the most drug-related adverse events. With monotherapy, hypotension and renal dysfunction were more common in the valsartan group, and cough, rash, and taste disturbance were more common in the captopril group. CONCLUSIONS: Valsartan is as effective as...

  19. 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

  20. [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

  1. Renal artery stenosis detection by combined Gates' technique and captopril test in hypertensive patients

    International Nuclear Information System (INIS)

    We studied 11 hypertensive patients by a radionuclide technique using Gates' method with [/sup 99m/Tc]DTPA to investigate the acute effects of captopril on glomerular filtration rate (GFR). Five patients had hypertension with unilateral renal artery stenosis (RAS) angiographically documented and six patients had essential hypertension (EH). Total and split GFR were determined under control conditions and after oral administration of captopril (50 mg). In the patients with RAS, captopril induced a significant decrease of GFR in the stenotic kidneys (from 42.4 +/- 4 to 29.6 +/- 3 ml/min, p less than 0.01), while no changes were observed in the nonstenotic kidneys (from 61.2 +/- 3 to 61.6 +/- 5 ml/min, NS). Total GFR was 103.6 +/- 5 ml/min under control conditions and decreased to 91.8 +/- 6 ml/min after captopril (p less than 0.05). No significant changes of GFR were detected after captopril administration in patients with EH. In a separate group of ten patients with EH, good correlation between 24-hr creatinine clearance and fractional uptake of [/sup 99m/Tc]DTPA was obtained. Good reproducibility of this radionuclide technique was also shown. This study demonstrates that the computed radionuclide GFR determination coupled with the captopril test allows one to unmask angiotensin II-dependent renal function and hemodynamic changes. This technique can be useful in clinical practice for identifying patients with renovascular hypertension

  2. Comparative Study of Captopril Derivatization Reaction by LC-UV, LC-MS and CE-UV Methods

    OpenAIRE

    Donáth-Nagy, Gabriella; Vancea, Szende; Imre, Silvia

    2011-01-01

    The LC-UV, LC-MS and CE-UV study of chemical reaction between captopril and p-bromophenacyl bromide as derivatizing reagent is reported. During transformation of captopril, its thiol group is involved and the reaction is irreversible. Neutral or alkaline environments favor derivatization. The yield of reaction increases linear with the concentration of the reagent, while changes in temperature do not influence it significantly. Kinetic studies show that derivatization of captopril...

  3. Protective behavior of captopril on Hg(++)-induced toxicity on kidney mitochondria. In vivo and in vitro experiments.

    Science.gov (United States)

    Chávez, E; Zazueta, C; Osornio, A; Holguín, J A; Miranda, M E

    1991-01-01

    Mercurials are known to induce morphological and functional modifications in kidney mitochondria. In this work we studied in vitro and in vivo the protective effect of captopril on the deleterious effect of Hg(++)-induced nonspecific membrane permeability changes to Ca++ and membrane de-energization. In vivo the administration of captopril prevented the toxic effects of mercury poisoning on membrane permeability, oxidative phosphorylation and Ca++ homeostasis. Moreover, captopril preserves kidney tissue morphology from Hg(++)-induced damage. The protective effect of captopril is most likely related to the existence of a sulfhydryl group in the drug. PMID:1988667

  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. Protective Effects of Captopril against Aflatoxin B1-Induced Hepatotoxicity in Isolated Perfused Rat Liver

    Directory of Open Access Journals (Sweden)

    Amir Moghadam- Jafari

    2014-02-01

    Full Text Available 8TBackground: The liver is the major target organ for aflatoxin B1 (AFB1. Ingestion of aflatoxin causes hepatotoxicty. In this study, captopril as new agent to help the hepatotoxicity induced by aflatoxin was suggested. 8TMaterials and Methods: The isolated perfused rat liver (IPRL was chosen for evaluating hepatic function. Sixteen rats were divided randomly into four experimental groups: control, captopril, AFB1 and AFB1 + captopril. The level of glutathione content and lipid peroxidation, as marker of oxidative stress and lactate dehydrogenase (LDH, alanine transaminase (ALT and aspartate transaminase (AST activities and pH of the perfusate medium were measured. 8TResults: There was a significant decrease in lipid peroxidation and same increase was observed in glutathione level. Treatment with captopril also modulated the enzymes activity and pH of perfusate. 8TConclusion: This study showed that captopril protects the hepatotoxicty induced by AFB1. Therefore, this drug may provide an effective new strategy to reduce of aflatoxins toxicity.

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

    International Nuclear Information System (INIS)

    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. 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.

  10. 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.

  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. 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).

  16. The radioprotective effect and mechanism of captopril on radiation induced-heart damage in rats

    Energy Technology Data Exchange (ETDEWEB)

    Chang, Seung Hee; Lee, Kyung Ja; Koo, Hea Soo [Ewha Womans University, Seoul (Korea, Republic of)

    2004-03-15

    Captopril (angiotension converting enzyme inhibitor) is known to have a radioprotective effect in the lungs, intestines and skin, but its effect in the heart is unclear. To investigate the radioprotective effect and mechanism of captopril in the heart, the histopathological changes and immunohistochemical stains were compared with radiation alone, and radiation combined with captopril, in the rats. The histopathological changes and immunohistochemical stains (TNF {alpha} , TGF {beta} 1, PDGF and FGF2) were examined in the radiation alone and the combined captopril and radiation groups, 2 and 8 weeks after irradiation. Each group consisted of 8 to 10 rats (Sprague-Dawley). Irradiation (12.5 Gy) was given to the left hemithorax in a single fraction. Captopril (50 mg/Kg/d) mixed with water, was given orally and continuously from the first week prior to, up to the 8th week of the experiment. In the radiation alone group, the ventricle at 2 weeks after irradiation showed prominent edema ({rho} = 0.082) and fibrin deposit ({rho} = 0.018) compared to the control group. At 8 weeks, the edema was decreased and fibrosis increased compared to those at 2 weeks. The histopathological changes of the combined group were similar to those of the control group, due to the reduced radiation toxicity at 2 and 8 weeks. The endocardial fibrin deposit ({rho} = 0.047) in the atrium, and the interstitial fibrin deposit ({rho} = 0.019) and edema ({rho} = 0.042) of the ventricle were reduced significantly in the combined group compared to those in the radiation alone group at 2 weeks. The expressions of TNF- {alpha} , TGF- {beta} 1, PDGF and FGF-2 in the radiation alone group were more increased than in the control group, especially in the pericardium and endocardium of the atrium at 2 weeks. At 8 weeks, the pericardial TNF- {alpha} and TGF- {beta} 1, in the radiation alone group continuously increased. The expressions of TNF- {alpha} , TGF- {beta} 1, and PDGF were decreased in the combined

  17. 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.

  18. Captopril for prevention of Contrast Induced Nephropathy in patients undergoing Coronary Angioplasty: A double blind placebo controlled clinical trial

    Directory of Open Access Journals (Sweden)

    M Hashemi

    2005-09-01

    Full Text Available Background: Contrast induced nephropathy is a potential cause of mortality and morbidity in patients undergoing angiography–angioplasty. Except for hydrating and probably low – isoosmolar contrast agents in high risk groups, other modalities have not provided benefit. We investigated preventive effects of captopril for contrast induced nephropathy during angiography–angioplasty. Methods: In a double blind placebo controlled clinical trial, 88 patients were randomized to two groups: 42 patients received captopril (12.5 mg every 8 hours from 2 hours before the procedure until 48 hours thereafter, and 46 patients received placebo in the same manner. Serum creatinine was measured before and 48 hours after angioplasty. The data were analyzed by SPSS software, using unpaired student t-test for comparing mean creatinine rise in both groups and paired student t-test for the changes in serum creatinine in each group. Results: The mean creatinine rise in captopril group (0.214 mg/dl and placebo group (0.226 mg/dl were not significantly different. The incidence of acute renal failure (creatinine rise more than 0.5 mg/dl in the captopril (11.9 % and placebo group (10.8 % were not significantly different. Conclusion: Captopril does not effectively prevent contrast nephropathy, but it is not harmful for renal function and can be administered safely during angiography – angioplasty in patients with normal renal function. However, the effect of captopril in patients with high- risk characteristics remains to be clarified. Of note, we found a trend for less creatinine rise in diabetics who received captopril during the procedure in comparison to diabetics who received placebo. Keywords: Angiography, Angioplasty, Contrast induced Nephropathy, Captopril, Angiotension Converting Enzyme Inhibitor, Creatinine

  19. The effect of captopril on the superior mesenteric artery and portal venous blood flow in normal man.

    OpenAIRE

    Ray-Chaudhuri, K; Thomaides, T; Maule, S; Watson, L.; Lowe, S; Mathias, C J

    1993-01-01

    1. Measurements of superior mesenteric artery and portal venous blood flow were made non-invasively along with systemic and other regional (cardiac index, forearm and cutaneous blood flow) vascular responses to acute ingestion of the ACE inhibitor captopril (50 mg) or placebo (50 mg vitamin C), in 12 healthy subjects while supine and during head-up tilt. 2. After captopril, superior mesenteric artery and portal blood flow rose markedly with a reduction in superior mesenteric artery vascular r...

  20. 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...

  1. 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)

    Soares de Moura R.

    1997-01-01

    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 (P<0.05 reduction in arterial blood pressure (D 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

  2. 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.

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

    OpenAIRE

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

    2012-01-01

    Background/Aim: Portal hypertension is an important and potentially fatal complication of liver disease whereby cellular and fibrotic alterations manifest to increase portal venous pressure. The aim of this study is to investigate the effect of captopril, pentoxifylline (PTX), and cordyceps sinensis in pre-hepatic portal hypertensive rats. Settings and Design: Wister male rats were divided at random into 3 main groups: the first group: control rats. The second group: sham-operated rats and th...

  4. 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...

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

    Directory of Open Access Journals (Sweden)

    Ahmed F Ahmed

    2012-01-01

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

  6. Late blood pressure reduction in shr subjected to transient captopril treatment in youth: possible mechanisms

    Czech Academy of Sciences Publication Activity Database

    Zicha, Josef; Dobešová, Zdenka; Kuneš, Jaroslav

    2008-01-01

    Roč. 57, č. 3 (2008), s. 495-498. ISSN 0862-8408 R&D Projects: GA MŠk(CZ) 1M0510; GA ČR(CZ) GA305/08/0139 Institutional research plan: CEZ:AV0Z50110509 Keywords : captopril * nifedipine * late effects of early treatment Subject RIV: FA - Cardiovascular Diseases incl. Cardiotharic Surgery Impact factor: 1.653, year: 2008

  7. 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)

  8. 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.

  9. 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

  10. Determination of free captopril in human plasma by liquid chromatography with mass spectrometry detection.

    Science.gov (United States)

    Vancea, Szende; Imre, Silvia; Donáth-Nagy, Gabriella; Béla, Tokés; Nyulas, Mária; Muntean, Teofil; Borka-Balás, Réka

    2009-07-15

    A new simple, sensitive and selective liquid chromatography coupled with mass spectrometry (LC/MS) method for quantification of captopril after precolumn derivatization with p-bromo-phenacyl-bromide in human plasma was validated. Plasma samples were analysed on a monolithic column (Cromolith Performance-RP 18e, 100 mm x 4.6 mm I.D., 3 microm) under isocratic conditions using a mobile phase of a 40:60 (v/v) mixture of acetonitrile and 0.1% (v/v) formic acid in water. The flow rate was 1 mL/min at the column temperature of 30 degrees C. In these chromatographic conditions, the retention time was 4.4 min for captopril derivative. The detection of the analyte was in MRM mode using an ion trap mass spectrometer with electrospray positive ionisation. The monitored ions were 216, 253, 255, 268, 270 m/z derived from 415 m/z for derivatized captopril. The sample preparation was very simple and consisted in plasma protein precipitation from 0.2 mL plasma using 0.3 mL methanol after the derivatization reaction was completed. Calibration curves were generated over the range of 10-3000 ng/mL with values for coefficient of correlation greater than 0.993 and by using a weighted (1/y(2)) quadratic regression. The values for precision (CV %) and accuracy (relative error %) at quantification limit were less than 9.9% and 3.9%, for within- and between-run, respectively. The mean recovery of the analyte was 99%. Derivatized samples demonstrated good short-term, long-term, post-preparative and freeze-thaw stability. This is the first reported LC-MS/MS method for analysis of captopril in human plasma that uses protein precipitation as sample processing procedure. The method is very simple and allows obtaining a very good recovery of the analyte. The validated LC-MS/MS method has been applied to a pharmacokinetic study of 50mg captopril tablets on healthy volunteers. PMID:19559901

  11. 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.

  12. 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

    in Acute Myocardial Infarction Trial (VALIANT). RESULTS: The number of individuals adjudicated as having a fatal or non-fatal MI in the captopril group was 559 (total investigator reported events 798), 587 (796) in the valsartan group, and 554 (756) in the combination group; valsartan versus captopril, p...

  13. 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...

  14. 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.

  15. 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

  16. 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.)

  17. 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.

  18. 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 ...

  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. Sensitive detection of mercury (II) ion using water-soluble captopril-stabilized fluorescent gold nanoparticles

    Energy Technology Data Exchange (ETDEWEB)

    Feng, Jiu-Ju; Huang, Hong; Chen, Wei-Jie; Chen, Jian-Rong; Lin, Hong-Jun; Wang, Ai-Jun, E-mail: ajwang@zjnu.cn

    2013-07-01

    In our work, a simple, facile, and green method was developed for the synthesis of water-soluble and well-dispersed fluorescent gold nanoparticles (Au NPs) within 5 min, using captopril as a capping agent. The as-prepared Au NPs showed strong emission at 414 nm, with a quantum yield of 5.5%. The fluorescence of the Au NPs can be strongly quenched by mercury (II) ion (Hg{sup 2+}) due to the stronger interactions between thiolates (RS{sup −}) and Hg{sup 2+}. It was applied to the detection of Hg{sup 2+} in water samples in the linear ranges of 0.033–0.133 μM and 0.167–2.500 μM, with a detection limit of 0.017 μM. Therefore, the as-prepared Au NPs can meet the requirement for monitoring Hg{sup 2+} in environmental samples. - Graphical abstract: In this work, we developed a simple, fast and facile method for the preparation of water-soluble and fluorescent gold nanoparticles (Au NPs). The trace existence of Hg{sup 2+} could strongly quench the fluorescence of the Au NPs. The Au NPs were used to detect highly toxic Hg{sup 2+} in water samples with high sensitivity and selectivity. Highlights: ► Water-soluble fluorescent Au NPs stabilized by captopril ► The synthesis procedure was simple, fast and facile. ► The fluorescence of the Au NPs can be strongly quenched by Hg{sup 2+}. ► The Au NPs were used to the assay of Hg{sup 2+} in water samples with high sensitivity and selectivity.

  1. 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

  2. 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.

  3. [sup 99m]TC-MAG[sub 3] renal function scintigraphy and captopril in the diagnosis of renovascular hypertension. [sup 99m]Tc-MAG[sub 3]-Nierenfunktionsszintigraphie ohne und mit Captopril zur Diagnostik der renovaskulaeren Hypertonie

    Energy Technology Data Exchange (ETDEWEB)

    Piepenburg, R. (Mainz Univ. (Germany). Klinik mit Poliklinik fuer Nuklearmedizin); Bockisch, A. (Mainz Univ. (Germany). Klinik mit Poliklinik fuer Nuklearmedizin); Andreas, J. (Mainz Univ. (Germany). Klinik mit Poliklinik fuer Nuklearmedizin); Dueber, C. (Mainz Univ. (Germany). Klinik fuer Roentgendiagnostik); Kann, P. (Mainz Univ. (Germany). 3. Medizinische Klinik und Poliklinik, Innere Medizin und Endokrinologie); Maier, G. (Mainz Univ. (Germany). Klinik mit Poliklinik fuer Nuklearmedizin); Hahn, K. (Mainz Univ. (Germany). Klinik mit Poliklinik fuer Nuklearmedizin)

    1993-08-01

    In this study, the diagnostic value of renal function scintigraphy performed both without and with ACE inhibition has been evaluated using the new radiopharmaceutical [sup 99m]Tc-MAG[sub 3]. In cases of decompensated renal artery stenoses, the typical scan finding with this tubular excreted agent was shown to be a distinct parenchymal nuclide retention in combination with a delayed appearance of the radiotracer in the pelvic system. Using this criterion in 43 patients with suspected renovascular hypertension, sensitivity and specificity were 89 and 88%, respectively. Bilateral positive findings were non-specific; excluding them from the study, specificity increased to 100%. In renal insufficiency, captopril scans seem to be of reduced diagnostic value. Summarising our experiences, renal function scintigraphy using [sup 99m]Tc-MAG[sub 3] without and with captopril was proved to be a reliable non-invasive method to detect or exclude haemodynamically relevant renal artery stenosis. (orig.)

  4. 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

  5. Captopril for prevention of Contrast Induced Nephropathy in patients undergoing Coronary Angioplasty: A double blind placebo controlled clinical trial

    OpenAIRE

    Hashemi, M.; Kharazi, A; Shahidi, S.

    2005-01-01

    Background: Contrast induced nephropathy is a potential cause of mortality and morbidity in patients undergoing angiography–angioplasty. Except for hydrating and probably low – isoosmolar contrast agents in high risk groups, other modalities have not provided benefit. We investigated preventive effects of captopril for contrast induced nephropathy during angiography–angioplasty. Methods: In a double blind placebo controlled clinical trial, 88 patients were randomized to two groups: 42 pa...

  6. Influence of chronic captopril treatment on norepinephrine-induced vasoconstriction in SHR and WKY : In vitro study

    Czech Academy of Sciences Publication Activity Database

    Líšková, Silvia; Kuneš, Jaroslav; Zicha, Josef

    2008-01-01

    Roč. 26, Suppl.1 (2008), S168-S168. ISSN 0263-6352. [Scientific Meeting International Society of Hypertension /22./ , Scientific Meeting European Society of Hypertension /18./. 14.06.2008-19.06.2008, Berlin] Institutional research plan: CEZ:AV0Z50110509 Keywords : cpo1 * captopril teratment * norepinephrine-induced vasoconstriction * SHR and WKY Subject RIV: FA - Cardiovascular Diseases incl. Cardiotharic Surgery

  7. Influence of chronic captopril treatment on norepinephrine-induced vasoconstriction in SHR and WKY : In vivo study

    Czech Academy of Sciences Publication Activity Database

    Pintérová, Mária; Kuneš, Jaroslav; Dobešová, Zdenka; Zicha, Josef

    2008-01-01

    Roč. 26, Suppl.1 (2008), S174-S174. ISSN 0263-6352. [Scientific Meeting International Society of Hypertension /22./ , Scientific Meeting European Society of Hypertension /18./. 14.06.2008-19.06.2008, Berlin] Institutional research plan: CEZ:AV0Z50110509 Keywords : cpo1 * captopril teratment * norepinephrine-induced vasoconstriction * SHR and WKY Subject RIV: FA - Cardiovascular Diseases incl. Cardiotharic Surgery

  8. 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

  9. 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

  10. 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.

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

    International Nuclear Information System (INIS)

    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 (λmax 407 nm). Beer's law is obeyed in a concentration range of 4.60 x 10-4 - 1.84 x 10-3 mol l-1 of CPT with an excellent correlation coefficient (r = 0.9995). The limit of detection and limit of quantification were 7.31 x 10-6 and 2.43 x 10-5 mol l-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. 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.

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

    Directory of Open Access Journals (Sweden)

    Brandy Viera Valdés

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

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

  14. Assay of free captopril in human plasma as monobromobimane derivative, using RPLC/(+)ESI/MS/MS: validation aspects and bioequivalence evaluation.

    Science.gov (United States)

    Medvedovici, Andrei; Albu, Florin; Sora, Iuliana Daniela; Udrescu, Stefan; Galaon, Toma; David, Victor

    2009-10-01

    A sensitive method for determination of free captopril as monobromobimane derivative in plasma samples is discussed. The internal standard (IS) was 5-methoxy-1H-benzimidazole-2-thiol. Derivatization with monobromobimane immediately after blood collection and plasma preparation prevents oxidation of captopril to the corresponding disulfide compound and enhances the ionization yield. Consequently, derivatization enhances sample stability and detection sensitivity. Addition of the internal standard was made immediately after plasma preparation. The internal standard was also derivatized by monobromobimane, as it contains a thiol functional group. Preparation of plasma samples containing captopril and IS derivatives was based upon protein precipitation through addition of acetonitrile, in a volumetric ratio 1:2. The reversed-phase liquid chromatographic separation was achieved on a rapid resolution cartridge Zorbax SB-C(18), monitored through positive electrospray ionization and tandem MS detection using the multiple-reaction monitoring mode. Transitions were 408-362 amu for the captopril derivative and 371-260 amu for the internal standard derivative. The kinetics of captopril oxidation to the corresponding disulfide compound in plasma matrix was also studied using the proposed method. A linear log-log calibration was obtained over the concentration interval 2.5-750 ng/mL. A low limit of quantitation in the 2.5 ng/mL range was obtained. The analytical method was fully validated and successfully applied in a three-way, three-period, single-dose (50 mg), block-randomized bioequivalence study for two pharmaceutical formulations (captopril LPH 25 and 50 mg) against the comparator Capoten 50 mg. PMID:19402182

  15. 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

  16. 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...

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

    OpenAIRE

    Santana Téllez, Tomás Noel

    2012-01-01

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

  18. 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

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

    Directory of Open Access Journals (Sweden)

    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.

  20. 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.

  1. 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)

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

    Directory of Open Access Journals (Sweden)

    Anna Alice Rolim Chaves

    2010-01-01

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

  3. 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

  4. 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

  5. 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

  6. 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

  7. 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

  8. 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

  9. 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.

  10. 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

  11. 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

  12. Study on the dynamic change of endothelin and the effect of treatment by captopril in the development of stenosis of aorta after balloon injury in rabbits

    International Nuclear Information System (INIS)

    Objective: To study the dynamic change of endothelin (ET) in the blood, the pathological change, and the ET-IR (ET-immunoreaction, ET-IR) in the development of stenosis after balloon injury of rabbit aorta, and to investigate the effect of captopril on the prevention of restenosis after transluminal angioplasty. Methods: According to the different time of being killed after micro-balloon angioplasty, 48 rabbits were divided randomly into 6 groups such as 6-hour group, 1-day group, 3-day group, 7-day group, 15-day group, and 22-day group. 6 out of 8 rabbits of each group were created models of aortic endothelium injury by micro-balloon angioplasty, and 3 of them were given captopril (2 mg·kg-1·d-1 p. o.) from 1 day before balloon injury to the day being killed. The rest 2 rabbits in each group were controls. ET level in the plasma was measured by ELISA before, as well as after micro-balloon angioplasty, and pathomorphological examination of local aorta was carried out to observe the intimal thickness and the extent of lumen stenosis, and ET-IR was assessed by immunohistochemical technique in the aortic wall. Results: (1) The major change of vascular stenosis was the proliferation of vascular smooth muscle cell (VSMC) and endothelium. (2) ET levels in the plasma and ET-IR in the local aortic wall were significantly increased after micro-balloon angioplasty. (3) The intimal thickness and extent of lumen stenosis in the group of medical treatment by captopril were significantly lower than those in injury group. Conclusions: The experimental results show that the major pathologic change of vascular stenosis is the significant proliferation of VSMC and endothelium. Further more, ET is a key factor in the development of vascular stenosis, and captopril can prevent restenosis after angioplasty. (author)

  13. 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...

  14. Practical issues when initiating captopril therapy in chronic heart failure. What is the appropriate dose and how long should patients be observed?

    Science.gov (United States)

    McLay, J S; McMurray, J; Bridges, A; Struthers, A D

    1992-11-01

    To assess the feasibility of introducing captopril in patients with chronic heart failure on an outpatient rather than an inpatient basis a double-blind placebo-controlled study was carried out to compare either 6.25 mg or 25.0 mg of captopril as a starting dose; followed by either incremental doses of 6.25, 12.5, and 25.0 mg (low dose group), or 25.0 mg 8 hourly (high dose group) respectively. Forty-one patients in a general medical ward within a large teaching hospital with moderate to severe, stable, diuretic-controlled chronic heart failure, who were not hyponatraemic, hypokalaemic or on a dose of diuretic greater than 120 mg of frusemide took part. No patient experienced symptomatic hypotension. Both doses of captopril produced a significant drop in blood pressure (BP), the magnitude of which was similar in both groups. The first dose-induced fall correlated significantly with subsequent dose-related reductions in BP. Therefore if a patient did not have a hypotensive response to the first dose of captopril he/she would be unlikely to have one with subsequent doses. In the group as a whole, the magnitude of the fall in BP after the first dose correlated significantly with starting plasma levels of angiotensin II, atrial natriuretic peptide (ANP), aldosterone, and renin. However, on an individual basis, the two patients with the greatest fall in blood pressure did not have the most activated renin-angiotensin-aldosterone (RAA) system. This serves to emphasise the unpredictability of this response and the need to initiate therapy under clinical observation.(ABSTRACT TRUNCATED AT 250 WORDS) PMID:1464341

  15. 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

  16. The role of chronic captopril (CPT) and N-acetyl-cysteine (NAC) treatment in L-NAME hypertension in the rat

    Czech Academy of Sciences Publication Activity Database

    Dobešová, Zdenka; Kuneš, Jaroslav; Zicha, Josef

    Fyziologický ústav AV ČR, v. v. i.. Roč. 55, č. 3 (2006), 5P-6P ISSN 0862-8408. [Nitric Oxide: Basic Regulations and Pharmacological Interventions. 21.09.2005-24.09.2005, Tucepi] R&D Projects: GA MZd(CZ) NR7786 Keywords : captopril * N- Acetyl cysteine * L-NAME hypertension * rat Subject RIV: FA - Cardiovascular Diseases incl. Cardiotharic Surgery

  17. 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

  18. 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.

  19. 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

  20. 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

  1. Fabrication of Ru–Pd bimetallic monolayer on nanoporous gold film electrode with excellent electrocatalytic performance towards captopril oxidation

    International Nuclear Information System (INIS)

    This paper describes a simple and novel method to construct ruthenium–palladium (RuPd) bimetallic thin films by coating thin layer of RuPd metals on the nanoporous gold film (NPGF) electrode. The codeposition of Ru and Pd was done through oxidation of copper underpotential deposition (UPD) layer by Ru and Pd ions. This low RuPd-loading electrode (RuPdNPGF) behaved as the nanostructured bimetallic RuPd for the detection of captopril (CAP). Whereas at the surface of the bare electrode an electrochemical activity for CAP cannot be observed, a very sharp anodic peak of the potential of −0.295 V (vs. Ag/AgCl) in pH = 7.0 is obtained using the prepared RuPdNPGF electrode. RuPdNPGF exhibited an excellent performance toward electrochemical oxidation of CAP without any additional mediator showing a significant decrease in the anodic over potential, a high sensitivity and a low detection limit (1.25 × 10−9 M) for CAP. Under the optimized conditions, the amperometric of CAP showed two linear ranges for determination of CAP: 2.50 × 10−9 to 4.75 × 10−7 M CAP and 2.5 × 10−6 to 3.25 × 10−5 M CAP. The results show that the RuPdNPGF electrode exhibited a selective, rapid response, good stability with excellent precision (RSD = 2.19%)

  2. Electropolymerization of taurine on gold surface and its sensory application for determination of captopril in undiluted human serum.

    Science.gov (United States)

    Hasanzadeh, Mohammad; Pournaghi-Azar, Mohammad Hossein; Shadjou, Nasrin; Jouyban, Abolghasem

    2014-05-01

    Polytaurine film was electrodeposited on gold (Au) electrode through cyclic voltammetry from taurine and phosphate buffer solution. The electrocatalytic effect of polytaurine modified Au (PT/Au) electrode was investigated for electro-oxidation of captopril (CAP). Electrocatalytical activity of PT/Au electrode was studied using cyclic voltammetry (CV), chronoamperometry and differential pulse voltammetry (DPV). DPV was used to evaluate the analytical performance of CAP in the presence of phosphate buffer solution and good limit of detection was obtained by this sensor. The experimental conditions influencing the determination of CAP were optimized and under optimal conditions, the oxidation peak current was proportional to CAP concentration in the range of 0.06-0.2 μM, while the detection limit was 0.03 μM (S/N=3). The results revealed that PT promotes the rate of oxidation by increasing the peak current. Finally, the applicability of the method to direct assay of human serum is described. The proposed sensor was successfully applied to determine cadaverine in fish samples, yielding satisfactory results. The spiked recoveries were in the range of 96.0-105.0%. PMID:24656369

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

    Science.gov (United States)

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

    2015-05-01

    In this work, near-infrared spectroscopy (NIRS) method was used to evaluate the uniformity of dosage units of three captopril 25 mg tablets commercial batches. The performance of the calibration method was assessed by determination of Q value (0.9986), standard error of estimation (C-set SEE = 1.956), standard error of prediction (V-set SEP = 2.076) as well as the consistency (106.1%). These results indicated the adequacy of the selected model. The method validation revealed the agreement of the reference high pressure liquid chromatography (HPLC) and NIRS methods. The process evaluation using the NIRS method showed that the variability was due to common causes and delivered predictable results consistently. Cp and Cpk values were, respectively, 2.05 and 1.80. These results revealed a non-centered process in relation to the average target (100% w/w), in the specified range (85-115%). The probability of failure was 21:100 million tablets of captopril. The NIRS in combination with the method of multivariate calibration, partial least squares (PLS) regression, allowed the development of methodology for the uniformity of dosage units evaluation of captopril tablets 25 mg. The statistical process control strategy associated with NIRS method as PAT played a critical role in understanding of the sources and degree of variation and its impact on the process. This approach led towards a better process understanding and provided the sound scientific basis for its continuous improvement. PMID:24344991

  4. 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

  5. Captopril and Hydrochlorothiazide

    Science.gov (United States)

    ... a class of medications called angiotensin-converting enzyme (ACE) inhibitors. It works by decreasing certain chemicals that tighten ... Capoten); hydrochlorothiazide (HCTZ; Microzide, Oretic); angiotensin-converting enzyme (ACE) inhibitors such as benazepril (Lotensin, in Lotrel), enalapril (Vasotec, ...

  6. 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

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

    Directory of Open Access Journals (Sweden)

    Graciette Matioli

    2004-04-01

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

  8. 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。

  9. 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.

  10. 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

  11. 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.

  12. 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

  13. 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。...

  14. 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.

  15. Effect of melatonin, captopril, spironolactone and simvastatin on blood pressure and left ventricular remodelling in spontaneously hypertensive rats

    Czech Academy of Sciences Publication Activity Database

    Šimko, F.; Pecháňová, Olga; Pelouch, Václav; Krajčírovičová, K.; Müllerová, M.; Bednárová, K.; Adamcová, M.; Paulis, L.

    2009-01-01

    Roč. 27, Suppl.6 (2009), S5-S10. ISSN 0263-6352 R&D Projects: GA ČR GA305/09/0336 Institutional research plan: CEZ:AV0Z50110509 Keywords : cardiac hypertrophy * fibrosis * ventricular remodeling Subject RIV: FA - Cardiovascular Diseases incl. Cardiotharic Surgery Impact factor: 4.988, year: 2009

  16. 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

  17. 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...

  18. 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

  19. Hemodynamic and radionuclide ventriculography changes in response to intravenous captopril and digoxin and their combinations in patients with severe heart failure

    International Nuclear Information System (INIS)

    It is shown that radionuclide ventriculography is not a reliable indicator of treatment response in patients with hearth failure and a severely depressed left ventricular ejection fraction. (author). 12 refs.; 14 figs

  20. 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

  1. The effect of captopril on nitric oxide formation and on generation of radical forms of mitochondrial respiratory chain compounds in ischemic rat heart

    Czech Academy of Sciences Publication Activity Database

    Vavřínková, H.; Tutterová, M.; Stopka, Pavel; Divišová, J.; Kazdová, L.; Drahota, Zdeněk

    2001-01-01

    Roč. 50, č. 5 (2001), s. 481-489. ISSN 0862-8408 R&D Projects: GA ČR GA203/97/0642; GA MZd NB5299 Keywords : ACE inhibitors * L-arginine * mitochondrial radicals Subject RIV: BO - Biophysics Impact factor: 1.027, year: 2001

  2. 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.

  3. 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

  4. Selectivity of Inhibition of N-Succinyl- l , l -Diaminopimelic Acid Desuccinylase in Bacteria: The product of dapE-gene Is Not the Target of l -Captopril Antimicrobial Activity

    OpenAIRE

    Narasimha Rao Uda; Marc Creus

    2011-01-01

    The emergence of bacterial strains that are resistant to virtually all currently available antibiotics underscores the importance of developing new antimicrobial compounds. N-succinyl-l,l-diaminopimelic acid desuccinylase (DapE) is a metallohydrolase involved in the meso-diaminopimelate (mDAP)/lysine biosynthetic pathway necessary for lysine biosynthesis and for building the peptidoglycan cell wall. Because DapE is essential for Gram-negative and some Gram-positive bacteria, DapE has been pro...

  5. Dynamic kidney scan and radionuclide angiography of kidneys with capitulator for diagnosis of preclinical forms of diabetic nephropathy

    International Nuclear Information System (INIS)

    Twelve healthy subjects and 24 patients with type 1 diabetes were investigated before and after administration of 25 mg captopril. Dynamic kidney scan and radionuclide angiography was performed. The induces improved at increase and reduction of glomerular filtration minute volume after captopril

  6. 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

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

    Energy Technology Data Exchange (ETDEWEB)

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

    2002-03-01

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

  8. Lisinopril and Hydrochlorothiazide

    Science.gov (United States)

    ... a class of medications called angiotensin-converting enzyme (ACE) inhibitors. It works by decreasing certain chemicals that tighten ... lisinopril; hydrochlorothiazide (HCTZ, Microzide, Oretic); angiotensin-converting ... such as benazepril (Lotensin), captopril (Capoten), enalapril (Vasotec , ...

  9. Benazepril and Hydrochlorothiazide

    Science.gov (United States)

    ... a class of medications called angiotensin-converting enzyme (ACE) inhibitors. It works by decreasing certain chemicals that tighten ... Lotensin); hydrochlorothiazide (HCTZ, Microzide, Oretic); angiotensin-converting enzyme (ACE) inhibitors such as captopril (Capoten), enalapril (Vasotec, in Vaseretic), ...

  10. 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), ...

  11. Perindopril

    Science.gov (United States)

    ... a class of medications called angiotensin-converting enzyme (ACE) inhibitors. It makes blood flow more smoothly by preventing ... you are allergic to perindopril, angiotensin-converting enzyme (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. Enalapril and Hydrochlorothiazide

    Science.gov (United States)

    ... a class of medications called angiotensin-converting enzyme (ACE) inhibitors. It works by decreasing certain chemicals that tighten ... Vaseretic); hydrochlorothiazide (HCTZ, Microzide, Oretic); angiotensin-converting enzyme (ACE) inhibitors such as benazepril (Lotensin, in Lotrel), captopril (Capoten), ...

  15. 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), ...

  16. 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), ...

  17. Quinapril

    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 quinapril; other ACE inhibitors such as benazepril (Lotensin, in Lotrel), captopril (Capoten), ...

  18. 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.

  19. Demonstration of extrapulmonary activity of angiotensin converting enzyme in intact tissue preparations.

    OpenAIRE

    Lembeck, F.; Griesbacher, T; Eckhardt, M.

    1990-01-01

    1. The activity of angiotensin converting enzyme (ACE) has been studied on functional parameters of intact isolated preparations of extrapulmonary tissues. The conversion of angiotensin I (A I) to angiotensin II (A II) and the cleavage of bradykinin (BK) were used as indicators of ACE activity. Captopril was employed as a specific inhibitor of ACE. 2. Captopril augmented the BK-induced contractions of the rat isolated uterus, the BK- and substance P-induced contractions of the guinea-pig ileu...

  20. Heart failure

    Institute of Scientific and Technical Information of China (English)

    1992-01-01

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

  1. 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....

  2. Effect of drug properties on formulation properties of eudragit non effervescent floating microparticulates

    OpenAIRE

    S L Harikumar; Singh, Satish

    2011-01-01

    The objective of the present investigation was to investigate the effects of selected drugs (captopril and celecoxib) properties on different parameters drug entrapment, in vitro drug release, release pattern, in vitro drug permeation and buoyancy in the formulation of Eudragit S100 non effervescent floating microparticulates. Microparticulates were in size ranges 268.36-352.27 μm (captopril) and 271.36- 365.54 μm (celecoxib). Encapsulation efficiency of celecoxib was good as compar...

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

    OpenAIRE

    Galina A. Alyamovskaya; Elena S. Keshishian; Elena G. Verchenko; Vera V. Bereznitskaya

    2015-01-01

    We report the use of oral sildenafil in a 7-month-old preterm newborn with severe bronchopulmonary dysplasia and pulmonary arterial hypertension refractory to captopril and inhaled budesonide, and need of consistent oxygenation. Sildenafil was prepared as a powder for oral administration. Oral sildenafil treatment was continued for 11 months. Oxygen supplement was suspended after 4 months and captopril administration was finished after 7 months of sildenafil treatment. There were no adverse e...

  4. 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.

  5. 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.

  6. Radiation-induced pulmonary endothelial dysfunction in rats: modification by an inhibitor of angiotensin converting enzyme

    International Nuclear Information System (INIS)

    The ability of the angiotensin converting enzyme (ACE) inhibitor Captopril to modify radiation-induced pulmonary endothelial dysfunction was determined in male rats sacrificed 2 months after a single dose of 10-30 Gy of 60Co gamma rays to the right hemithorax. Half of each dose group consumed feed containing 0.12% w/w Captopril (60 mg/kg/day) continuously after irradiation, and half consumed control feed. Four markers of endothelial function were monitored: ACE activity, plasminogen activator (PLA) activity, and prostacyclin (PGI2) and thromboxane (TXA2) production. All data were plotted as dose-response curves, and subjected to linear regression analysis. The Captopril modifying effect was expressed as the ratio of isoeffective doses at a common intermediate response (DRF), or as the ratio of the response curve slopes. Right lung ACE and PLA activity decreased linearly, and PGI2 and TXA2 production increased linearly with increasing radiation dose. Captopril exhibited DRF values of 1.4-2.1, and slope ratios of 1.4-5.1 for all four functional markers (p less than 0.05). Thus, the ACE inhibitor Captopril ameliorates radiation-induced pulmonary endothelial dysfunction in rats sacrificed 2 months postirradiation. Although the mechanism of Captopril action is not clear at present, these data suggest a novel application for this class of compounds as injury-modifying agents in irradiated lung

  7. 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.

  8. Circulating endothelin-1 levels in lean non-insulin-dependent diabetic patients. Influence of ACE inhibition.

    Science.gov (United States)

    Ferri, C; Laurenti, O; Bellini, C; Faldetta, M R; Properzi, G; Santucci, A; De Mattia, G

    1995-01-01

    To evaluate the effect of captopril on plasma endothelin-1 (ET-1) levels and insulin sensitivity, 15 lean normotensive men (51.6 +/- 3.8 years) affected by non-insulin-dependent diabetes mellitus (NIDDM) underwent 2-h euglycemic hyperinsulinemic clamp. Each patient was then assigned to receive either captopril (25 mg twice daily for 1 week) or placebo, in a double-blind randomized fashion, before repeating clamp. At baseline, plasma ET-1 levels were 0.77 +/- 0.25 pg/mL in captopril (n = 10) and 0.83 +/- 0.3 pg/mL in placebo patients (n = 5). A twofold increase in plasma ET-1 levels occurred during the 2-h insulin infusion in both groups (P < .05 after 60 and 120 min), with a rapid return to baseline after 30 min from insulin withdrawal. After 1 week of therapy, total glucose uptake significantly increased in captopril (from 3.71 +/- 1.70 mg/kg/min to 4.24 +/- 1.72 mg/kg/min, P < .03) but not in placebo patients. Plasma ET-1 levels significantly decreased after captopril therapy (0.48 +/- 0.25 pg/mL at time 0, P < .03 v pretreatment levels), but were unaffected by placebo. Moreover, captopril slightly reduced the magnitude of ET-1 increment during insulin infusion (0.65 +/- 0.28 pg/mL and 0.88 +/- 0.48 pg/mL at 60 and 120 min, respectively, P < .05 v time 0). As a consequence, during the second insulin infusion circulating ET-1 levels were significantly lower in captopril- than in placebo-treated patients at time 0 (P < .02), 60 (P < .002), 120 (P < .004), and 150 min (P < .001).(ABSTRACT TRUNCATED AT 250 WORDS) PMID:7734095

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

    International Nuclear Information System (INIS)

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

  10. 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.

  11. Structure-function analysis of angiotensin-converting enzyme inhibitors as modifiers of radiation-induced pulmonary endothelial dysfunction in rats

    International Nuclear Information System (INIS)

    It was concluded that the angiotensin-converting enzyme (ACE) inhibitor CGS13945 modifies radiation-induced pulmonary endothelial dysfunction in rats, indicating that presence of a thiol group is not essential for therapeutic efficacy in this class of compounds. On the other hand, CGS13945 exhibits a differential sparing of radiation-induced pulmonary endothelial dysfunction, as does penicillamine. A structure-function analysis of the present and previous data indicates all of the ACE inhibitors tested (Captopril, CL242817 and CGS13945) spare the radiation-induced suppression in lung ACE and PLA activity; all of the thiol compounds tested (penicillamine, Captopril and CL242817) spare the radiation-induced elevation in lung PGI2 and TXA2 production; and the thiol ACE inhibitors (Captopril and CL242817) spare all four endothelial responses. (author)

  12. 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

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

    Directory of Open Access Journals (Sweden)

    Hashimoto Mitsuo

    2002-01-01

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

  14. 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...

  15. Angiotensin converting enzyme and memory: preclinical and clinical data.

    Science.gov (United States)

    Sudilovsky, A; Turnbull, B; Croog, S H; Crook, T

    Results from both preclinical and clinical studies described here suggest that ACE may have a role in the modulation of cognitive memory processes in the rat and in humans. The finding of improved cognitive performance among patients treated with captopril relative to those treated with propranolol or methyldopa is consistent with other clinical and prec-clinical data. Clinical data derive primarily from quality of life measures based on interviews with patients in the same clinical trial from which our other cognitive data are drawn. For example, mental acuity in the workplace was reported to have improved significantly from baseline to week 24 in patients on captopril (p less than 0.05), although it did not change in patients treated with propranolol and worsened in those receiving methyldopa (Croog et al, 1987). The difference between captopril and methyldopa was significant (p less than 0.01). Pre-clinical data come primarily from studies demonstrating that inhibitors of ACE delay CAE in rats when compared not only with methyldopa, but also with saline (Sudilovsky et al, 1984, 1986). A fundamental question is how could inhibition of ACE improve cognitive functioning independent of blood pressure control. It is known that captopril exerts its antihypertensive effects primarily through inhibition of the ACE and that this is present in the brain as well as in non-neuronal tissues elsewhere (Ganten et al, 1982; Strittmatter et al, 1983, 1984). The activity of the enzyme has been found to be significantly increased in the caudate nucleus, the frontal cortex, parahyppocampal gyrus, and medial hippocampus of patients dying with Alzheimer's disease when compared to age-matched controls (Arregui et al, 1982). In addition, AII has been shown to impair performance on various learning and memory paradigms in animals (Melo and Graeff, 1975; Morgan and Routtenberg, 1977). Raising the level of endogenous AII by intravenous administration of its precursor renin has similar

  16. 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.

  17. 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...

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

    DEFF Research Database (Denmark)

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

    2008-01-01

    . The valiant trial identified 14,527 patients with acute myocardial infarction complicated by either clinical or radiologic signs of heart failure and/or left ventricular dysfunction for whom baseline creatinine was measured. Patients were randomly assigned to receive captopril, valsartan, or both. Glomerular...

  19. Udvikling af sklerodermisk krise hos patient med uerkendt sklerodermi

    DEFF Research Database (Denmark)

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

    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 the...

  20. 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)

  1. 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

  2. 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.

  3. 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

  4. 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

  5. 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

  6. 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

  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. 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.

  9. Changes in the renin angiotensin system during the development of colorectal cancer liver metastases

    International Nuclear Information System (INIS)

    Blockade of the renin angiotensin system (RAS) via angiotensin I converting enzyme (ACE) inhibition reduces growth of colorectal cancer (CRC) liver metastases in a mouse model. In this work we defined the expression of the various components of the RAS in both tumor and liver during the progression of this disease. Immunohistochemistry and quantitative RT-PCR was used to examine RAS expression in a mouse CRC liver metastases model. CRC metastases and liver tissue was assessed separately at key stages of CRC liver metastases development in untreated (control) mice and in mice treated with the ACE inhibitor captopril (750 mg/kg/day). Non-tumor induced (sham) mice indicated the effect of tumors on normal liver RAS. The statistical significance of multiple comparisons was determined using one-way analysis of variance followed by Bonferroni adjustment with SAS/STAT software. Reduced volume of CRC liver metastases with captopril treatment was evident. Local RAS of CRC metastases differed from the surrounding liver, with lower angiotensin II type 1 receptor (AT1R) expression but increased ANG-(1-7) receptor (MasR) compared to the liver. The AT1R localised to cancer and stromal infiltrating cells, while other RAS receptors were detected in cancer cells only. Tumor induction led to an initial increase in AT1R and ACE expression while captopril treatment significantly increased ACE expression in the final stages of tumor growth. Conversely, captopril treatment decreased expression of AT1R and angiotensinogen. These results demonstrate significant changes in RAS expression in the tumor-bearing captopril treated liver and in CRC metastases. The data suggests the existence of a tumor-specific RAS that can be independently targeted by RAS blockade

  10. 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.

  11. 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.

  12. Converting enzyme inhibition and blood pressure reactivity to psychological stressors.

    Science.gov (United States)

    Dimsdale, J E; Mills, P; Ziegler, M; Leitz, K; Nelesen, R

    1992-08-01

    There is considerable interest in blood pressure reactivity to psychological stressors. Because the sympathetic nervous system and the renin-angiotensin system are so responsive to stressors and are themselves the targets of many antihypertensive medications, many investigators have wondered if such medications decrease the blood pressure response to stressful stimuli. We studied 25 normotensive and 21 hypertensive men in a double-blind crossover study during which they received either placebo for 4 days or captopril (25 mg b.i.d.) for 4 days while they were hospitalized in a clinical research center. Patients were studied at resting baseline, while performing a mathematics task, and while reading out loud a disturbing newspaper article. Although captopril lowered the resting blood pressure levels, it had no effect on the amplitude of reactivity to stressors. PMID:1639462

  13. 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.

  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. Combinational chelation therapy abrogates lead-induced neurodegeneration in rats

    International Nuclear Information System (INIS)

    Lead, a ubiquitous and potent neurotoxicant causes oxidative stress which leads to numerous neurobehavioral and physiological alterations. The ability of lead to bind sulfhydryl groups or compete with calcium could be one of the reasons for its debilitating effects. In the present study, we addressed: i) if chelation therapy could circumvent the altered oxidative stress and prevent neuronal apoptosis in chronic lead-intoxicated rats, ii) whether chelation therapy could reverse biochemical and behavioral changes, and iii) if mono or combinational therapy with captopril (an antioxidant) and thiol chelating agents (DMSA/MiADMSA) is more effective than individual thiol chelator in lead-exposed rats. Results indicated that lead caused a significant increase in reactive oxygen species, nitric oxide, and intracellular free calcium levels along with altered behavioral abnormalities in locomotor activity, exploratory behavior, learning, and memory that were supported by changes in neurotransmitter levels. A fall in membrane potential, release of cytochrome c, and DNA damage indicated mitochondrial-dependent apoptosis. Most of these alterations showed significant recovery following combined therapy with captopril with MiADMSA and to a smaller extend with captopril + DMSA over monotherapy with these chelators. It could be concluded from our present results that co-administration of a potent antioxidant (like captopril) might be a better treatment protocol than monotherapy to counter lead-induced oxidative stress. The major highlight of the work is an interesting experimental evidence of the efficacy of combinational therapy using an antioxidant with a thiol chelator in reversing neurological dystrophy caused due to chronic lead exposure in rats.

  16. Influence of combined antihypertensive and antidepressant therapy on left ventricular remodeling in patients with arterial hypertension, anxiety and depression

    OpenAIRE

    Y. A. Vasyuk; T.V. Dovzenko; E.A. Nesterova; I.A. Sadulaeva; K.V. Tarasova

    2008-01-01

    Aim. To assess influence of combined antihypertensive (captopril or metoprolol) and antidepressant (thianeptin or sertralin) therapy on clinical status, blood pressure (BP) and myocardial function in patients with arterial hypertension (HT) and affective disorders (AD).Material and methods. 106 patients with HT were involved in the study. 64 patients (60,4%) had concomitant AD. All patients were divided into 3 groups. 46 patients with HT and AD were included in the 1-st group. They received m...

  17. Vasopressin reduces cardiac function and augments cardiopulmonary baroreflex resistance increases in man.

    OpenAIRE

    Ebert, T J; Cowley, A W; Skelton, M

    1986-01-01

    We examined the effects of physiologic infusions of arginine vasopressin (AVP) on cardiovascular hemodynamics and on reflex responses initiated by decreasing cardiopulmonary baroreceptor stimulation (with lower body negative pressure) in 10 healthy, captopril-pretreated young men (19-27 yr). Their responses were compared with those of four volunteers given isosmotic infusion. Heart rate, stroke volume, blood pressure, and forearm blood flow were measured by electrocardiography, impedance card...

  18. Medication errors in oral dosage form preparation for neonates: The importance of preparation technique

    OpenAIRE

    Valizadeh, Sousan; Rasekhi, Mehri; Hamishehkar, Hamed; Asadollahi, Malihe; Hamishehkar, Hadi

    2015-01-01

    Objective: Considering the inability of neonates to swallow oral drugs in the form of solid tablets, the lack of appropriate dosage forms for infants, and the necessity to prepare some pills for neonates, the current study investigated dosage accuracy in drugs for neonates prepared from tablets by analyzing the concentrations of final products. Methods: Captopril and spironolactone, oral dosage forms that are not suitable for infants, were chosen as the drug model for this study. Demographic ...

  19. 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...

  20. 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...

  1. 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...

  2. Investigating Generic and Brand Name Pharmaceutical’s Market Shares and Prices in Tunisia

    OpenAIRE

    Chebbi, Houssem Eddine; Boujelbene, Younes; Ayadi, Inès

    2008-01-01

    The purpose of this paper is to investigate how the brand name’s market shares in Tunisia are affected by generic competition during the pre-reform period of the Tunisian health insurance system following the methodological approach developed by Aronsson et al. (2001). In this study we use data for three molecules Captopril (antihypertensive) Glibenclamide (antidiabetic) and Carbamazepine (antiepileptic) from IMS Health database. The data span from the third quarter 2002 to second quarter 200...

  3. Direct proof for local generation and release of angiotensin II in peripheral human vascular tissue.

    Science.gov (United States)

    Mizuno, K; Niimura, S; Tani, M; Haga, H; Inagami, T; Fukuchii, S

    1991-01-01

    Previously we reported that immunoreactive angiotensin II (Ang II) release from isolated perfused human umbilical veins was inhibited by the angiotensin-converting enzyme inhibitor captopril. To further investigate the mechanism by which Ang II is generated in the blood vessels of humans, we examined the effects of various inhibitors of the renin-angiotensin system (captopril, delapril, N-acetyl-pepstatin, and human renin inhibitor KRI-1314) on Ang II release from perfused human umbilical cord veins in vitro. Isolated human umbilical veins were perfused with Krebs-Ringer solution, and immunoreactive Ang II released into the perfusate was measured directly by using a Sep-Pak C18 cartridge connected to the perfusion system. Both captopril and delapril diacid (10(-9) to 5 x 10(-6) mol/L), an active metabolite of delapril hydrochloride, suppressed the Ang II release in a dose-dependent fashion; the maximal percent suppression of Ang II release evoked by these inhibitors (5 x 10(-6) mol/L) was 56% and 64%, respectively, for captopril and delapril. Both N-acetyl-pepstatin (10(-9) to 10(-5) mol/L) and KRI-1314 (10(-9) to 10(-6) mol/L) suppressed Ang II release in a dose-related manner. At a 10(-6) mol/L concentration, KRI-1314 produced a 74% reduction in the basal rate of Ang II release, and a reduction threefold greater than the maximal reduction in basal Ang II release produced by N-acetyl-pepstatin.(ABSTRACT TRUNCATED AT 250 WORDS) PMID:2009152

  4. 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.

  5. 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.

  6. Soft-Template-Synthesized Mesoporous Carbon for Oral Drug Delivery

    Energy Technology Data Exchange (ETDEWEB)

    Saha, Dipendu [ORNL; Warren, Kaitlyn E [ORNL; Naskar, Amit K [ORNL

    2014-01-01

    Template-synthesized mesoporous carbons were successfully used in in vitro investigations of controlled delivery of three model drugs, captopril, furosemide, and ranitidine hydrochloride. Captopril and furosemide exhibited desorption kinetics over 30 40 h, and ranitidine HCl had a complete release time of 5 10 h. As evident from the slow release kinetics, we contend that our mesoporous carbon is an improved drug-delivery medium compared to state-of-the-art porous silica-based substrates. The mesoporous carbons, synthesized from phloroglucinol and lignin, a synthetic and a sustainable precursor, respectively, exhibit BET surface area of 200 400 m2 g-1 and pore volume of 0.2 0.6 cm3 g-1. The phloroglucinol-based carbon has narrower pore widths and higher pore volume than the lignin-derived counterpart and maintains a longer release time. Numerical modeling of the release kinetics data reveals that the diffusivities of all the drugs from lignin-based carbon media are of equivalent magnitude (10-22 to 10-24 m2 s-1). However, a tailored reduction of pore width in the sorbent reduces the diffusivity of smaller drug molecules (captopril) by an order of magnitude. Thus, engineered pore morphology in our synthesized carbon sorbent, along with its potential to tailor the chemistry of its interaction with sorbet, can be exploited for optimal delivery system of a preferred drug within its therapeutic level and below the level of toxicity.

  7. [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

  8. 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)

  9. 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

  10. 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

  11. 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

  12. 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

  13. 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 urinary Ac-SDKP after actinonin treatment. We conclude that release of Ac-SDKP from Tβ4 is mediated by successive hydrolysis involving meprin-α and POP. PMID:26962108

  14. 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.

  15. Effect of losartan on sodium appetite of hypothyroid rats subjected to water and sodium depletion and water, sodium and food deprivation.

    Science.gov (United States)

    Badauê-Passos, D; Ventura, R R; Silva, L F; Olivares, E L; Ramalho, M J; Antunes Rodrigues, J; Reis, L C

    2001-09-01

    The involvement of angiotensin AT1 receptors in sodium appetite was studied in hypothyroid rats treated with the angiotensin II antagonist losartan. Losartan was administered chronically by the oral route or acutely by the subcutaneous route after water and sodium depletion or water, sodium and food deprivation. Three days after addition of losartan to the food at the dose of 1.0 mg x g(-1), the rats significantly reduced (P < 0.02) their spontaneous intake of 1.8% NaCl. Increasing the dose of losartan to 2.0 and 4.0 mg x g(-1) did not reduce NaCl intake; in contrast, the intensity of the sodium appetite gradually returned to previous levels. The simultaneous administration of captopril, an angiotensin converting enzyme inhibitor, and losartan significantly increased (P < 0.05) NaCl intake and after captopril removal NaCl intake returned to the levels observed with losartan treatment alone. The administration of losartan 4 days after the beginning of captopril treatment significantly reduced (P < 0.0001) NaCl intake. Following acute administration of losartan, water- and sodium-depleted rats significantly reduced their NaCl and water intake (P < 0.001). The administration of losartan also induced a significant reduction in NaCl and water intake in water, NaCl and food-deprived rats (P < 0.0001 and P < 0.001, respectively). The present results show that chronic treatment with oral losartan inhibited spontaneous sodium appetite in hypothyroid rats. Continuation of treatment rendered rats resistant to the blockade of AT1 receptors. Water and sodium depletion and water, NaCl and food deprivation induced sodium appetite, which in the short term depends on cerebral angiotensinergic activity mediated by the activation of AT1 receptors. PMID:11571491

  16. Mitigation of radiation-induced lung fibrosis by angiotensin converting enzyme inhibitors

    International Nuclear Information System (INIS)

    The aim of this study was to test the mitigating potential of angiotensin converting enzyme inhibitors (ACEi) against radiation-induced pulmonary fibrosis, which could result from accidental exposure or radiological terrorism. Rats (WAG/RijCmcr) were exposed to a single dose of 13 Gy of X-irradiation to the whole thorax, at the dose rate of 1.43 Gy/min. Three structurally-different ACEi's, captopril (145-207 mg/m2/day), enalapril (19-28 mg/m2/day) and fosinopril (19-28 mg/m2/day) were administered in drinking water beginning 1 week after whole thoracic irradiation. Rats that survived acute pneumonitis (6-12 weeks) were accessed monthly after irradiation for the effects on lung structure and function. Endpoints included breathing rate, wet:dry weight ratio, collagen content and histolopathological studies. Treatment with captopril or enalapril, but not fosinopril, beginning 1 week after 13 Gy X-irradiation improved survival of rats. Mortality of 30-35% was observed with administration of captopril or enalapril compared to 70% for 13 Gy alone. All three ACEi's attenuated radiation-induced lung fibrosis at 7 months after irradiation based on histological indices and measurement of lung collagen. After whole-thoracic irradiation, ACEi's mitigate radiation induced pulmonary fibrosis based on histological and biochemical endpoints. These treatments were effective even when administration was not started until one week after irradiation. Our findings support the therapeutic potential of ACEi's against chronic radiation induced lung injury. (author)

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

    Directory of Open Access Journals (Sweden)

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

    2011-01-01

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

  18. 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

  19. 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

  20. Concurrent neutral endopeptidase and ACE inhibition in experimental heart failure: renal and hormonal effects

    DEFF Research Database (Denmark)

    Helin, K

    1993-01-01

    Neutral endopeptidase (NEP) inhibitors have been shown to strengthen the effects of endogenous atrial natriuretic peptide (ANP). It has been well documented that angiotensin I-converting enzyme (ACE) inhibitors act beneficially in chronic congestive heart failure (CHF). In the present study, renal...... and hormonal effects of SCH 34826, an orally active NEP inhibitor, were studied in a coronary-ligation model of experimental CHF in the rat. The effects were compared to those of captopril. The drugs were also administered in combination. In anaesthetized rats with CHF, SCH 34826 (90 mg kg-1 sc) elevated...

  1. 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, ...

  2. 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.

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

    DEFF Research Database (Denmark)

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

    2006-01-01

    BACKGROUND: The VALIANT trial compared the efficacy and safety of captopril, valsartan, and their combination in patients with left ventricular systolic dysfunction, heart failure, or both after acute myocardial infarction (MI). By examining this international trial population of high-risk patients......, we sought to determine geographic variations in the use of 3 key treatments for MI. METHODS: We analyzed data from 14,512 high-risk patients with MI in the VALIANT trial from the 20 countries that had enrolled >100 patients. International variation in the proportion of patients receiving (1...

  4. Vliv chronického podávání captoprilu na vasokonstrikci vyvolanou noradrenalinem (NA) u SHR a WKY : In vivo studie

    Czech Academy of Sciences Publication Activity Database

    Pintérová, Mária; Kuneš, Jaroslav; Dobešová, Zdenka; Zicha, Josef

    2008-01-01

    Roč. 50, č. 9 (2008), K168-K168. ISSN 0010-8650. [Konference ČSH /25./, Konference prac. skupiny preventivní kardiologie ČKS /17./, Konference prac. skupiny srdeční selhání ČKS /13./. 02.10.2008-04.10.2008, Český Krumlov] R&D Projects: GA MŠk(CZ) 1M0510; GA ČR(CZ) GA305/08/0139 Institutional research plan: CEZ:AV0Z50110509 Keywords : cpo1 * captopril * norepinephrine-induced vasoconstriction * SHR and WKY rat Subject RIV: FA - Cardiovascular Diseases incl. Cardiotharic Surgery

  5. Vliv chronického podávání captoprilu na noradrenalinem vyvolanou vasokonstrikci u potkanů SHR a WKY: studie in vitro

    Czech Academy of Sciences Publication Activity Database

    Líšková, Silvia; Kuneš, Jaroslav; Zicha, Josef

    2008-01-01

    Roč. 50, č. 9 (2008), K161-K161. ISSN 0010-8650. [Konference ČSH /25./, Konference prac. skupiny preventivní kardiologie ČKS /17./, Konference prac. skupiny srdeční selhání ČKS /13./. 02.10.2008-04.10.2008, Český Krumlov] R&D Projects: GA MŠk(CZ) 1M0510; GA ČR(CZ) GA305/08/0139 Institutional research plan: CEZ:AV0Z50110509 Keywords : cpr1 * norepinephrine-induced vasoconstriction * captopril * SHR and WKY Subject RIV: FA - Cardiovascular Diseases incl. Cardiotharic Surgery

  6. Effects of Chinese herbal medicines Shengmai injection and Xuesaitong injection on ventricular fibrillation threshold and connexin 43 expression in rats with myocardial infarction

    Directory of Open Access Journals (Sweden)

    Ai-ming Wu

    2011-07-01

    Full Text Available Objective: To explore the effects of Shengmai injection and Xuesaitong injection, compound Chinese herbal medicines for replenishing qi and activating blood, on ventricular fibrillation threshold, heart structure and connexin 43 (Cx43 expression in rats with myocardial infarction (MI.Methods: One hundred male SD rats were randomly divided into sham operation group, model group, Yiqi Huoxue (YQHX group (Shengmai injection plus Xuesaitong injection and captopril group. MI model of rats was established by ligating left anterior descending coronary artery, and rats in sham operation group were prepared in the same way except for the ligation of coronary artery. Rats were treated with corresponding drugs for 1 month from next day after modeling. After treatment ventricular fibrillation threshold was detected, and heart weight index, left ventricular internal diameter and percentage of myocardial infarction were measured. Expression of Cx43 mRNA in myocardium was detected by real-time fluorescent quantitative polymerase chain reaction, and expression of Cx43 protein was observed by immunohistochemical method.Results: Compared with the sham operation group, ventricular fibrillation threshold decreased significantly, heart weight index and left ventricular internal diameter increased, while expressions of Cx43 mRNA and protein decreased remarkably in the model group (P<0.01. Compared with the model group, ventricular fibrillation threshold was increased significantly, heart weight index, left ventricular internal diameter and percentage of myocardial infarction were decreased significantly in the YQHX group and captopril group (P<0.05 or P<0.01. When it comes to expression of Cx43, both Cx43 mRNA and protein expressions were increased remarkably in the YQHX group compared with the model group (P<0.05 or P<0.01, while only density mean and integral optical density of Cx43 protein expression were increased significantly in the captopril group

  7. 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).

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

    OpenAIRE

    Fernández-Vallinas, Sandra; Miguel, Marta; Aleixandre, Amaya

    2016-01-01

    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, ...

  9. B. Imaging in cases of renal transplantation, renovascular hypertension, renal obstruction, and vesicoureteral reflux

    International Nuclear Information System (INIS)

    This paper is designed for the radiology resident and practitioner with an interest in the role of nuclear medicine in urologic practice. The importance of functional imaging is emphasized. The techniques, criteria, and findings for the proper diagnosis of difficult genitourinary problems with radionuclide imaging are presented. Individual subject areas include the use of radionuclide renography to monitor renal transplantation, the evolving role of captopril renography in the diagnosis of renovascular hypertension, the use of diuresis renography for the initial diagnosis and management of renal obstruction, and the role of radionuclide cystography in the management of vesicoureteral reflux

  10. 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.

  11. 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

  12. Progress in renal nuclear medicine

    International Nuclear Information System (INIS)

    Progress in nuclear nephrology has come through an understanding of two specific pharmacological interventions: Frusemide and Captopril. Obstruction to outflow may be defined as an increased resistance to outflow above normal. This is usually associated with dilatation of the outflow tract. The obstructing uropathy cannot usually be distinguished from a dilated baggy unobstructive pelvis by examination of the renal images nor the renal activity time curve. In this situation a diuretic renography test with frusemid and calculation of outflow efficiency is very helpful. Captopril intervention was introduced as a form of stress test for the kidney and is able to improve the specificity of the distinction between Essential and Renovascular Hypertension. The typical features therefore are a delayed peak to the renogram, an impaired second phase, a series of images showing a delay in the time for activity to appear in the pelvis, and a prolongation of the mean parenchymal transit time. A study is also a good predictor of the presence of functionally significant restenosis if the patient is followed serially. In conclusion, intervention in renal nuclear medicine is becoming part of standard practice. The substitution of time based measurements for count based measurements should be the trend for the future. (author)

  13. 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

  14. 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

  15. Antihypertensive Properties of a Novel Morphologic Derivative (4-tert-buthyl-2,6-bis(thiomorpholine-4-ilmethyl)phenol).

    Science.gov (United States)

    Martínez-Aguilar, Luisa; Lezama-Martínez, Diego; Orozco-Cortés, Nancy V; González-Espinosa, Claudia; Flores-Monroy, Jazmin; Valencia-Hernández, Ignacio

    2016-03-01

    We evaluated the antihypertensive properties of 4-tert-buthyl-2,6-bis(thiomorpholine-4-ilmethyl)phenol (TBTIF). Spontaneously hypertensive rats were treated with TBTIF or captopril (both at 1 mg·kg·d intramuscularly for 4 days), and their blood pressure (BP) was assessed. In some experiments, concentration response curves to angiotensin I or angiotensin II were generated in rat aortic rings and in the absence or presence of Ang-(1-7), N-monomethyl L-arginine, or both; additionally, the angiotensin-converting enzyme (ACE) and ACE2 mRNA levels were quantified in the aortic rings using reverse transcription-polymerase chain reaction. TBTIF diminished BP and reduced angiotensin I- or angiotensin II-induced vasoconstriction. The presence of Ang-(1-7) induced a greater reduction in vasoconstriction, and this effect was reversed by L-N-monomethyl arginine. Moreover, TBTIF decreased the mRNA of ACE and increased the mRNA of ACE2. In conclusion, TBTIF diminished rat BP through nitric oxide-dependent and nitric oxide-independent mechanisms. In contrast to captopril, TBTIF exhibits better antihypertensive properties through mechanisms that involve ACE2. PMID:26566152

  16. 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

  17. 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.

  18. 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.

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

    Directory of Open Access Journals (Sweden)

    Y. A. Vasyuk

    2016-01-01

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

  20. 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

  1. 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

  2. 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. PMID:26235921

  3. 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

  4. 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.

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

    Directory of Open Access Journals (Sweden)

    Kamille Abdool

    2015-05-01

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

  6. 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

  7. 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.

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

    DEFF Research Database (Denmark)

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

    2003-01-01

    BACKGROUND: The VALsartan In Acute myocardial iNfarcTion (VALIANT) trial compared outcomes with: (1) angiotensin-converting enzyme inhibition (ACEI) with the reference agent captopril; (2) angiotensin-receptor blockade (ARB) with valsartan; or (3) both in patients with heart failure (HF) and....../or left ventricular systolic dysfunction (LVSD) after myocardial infarction (MI). AIMS: a goal of this active-control trial was to simulate conditions that would lead current practitioners to use ACEIs. Thus, we compared characteristics of VALIANT patients with those of patients in placebo...... at enrollment. Most (72%) had Killip class>/=II HF. Patients received evidence-based therapies at rates similar to those of contemporary MI trials and at an improved rate compared with prior placebo-controlled ACEI trials. CONCLUSION: VALIANT represents the largest globally representative cohort enrolled...

  9. 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

  10. Salt appetite of adrenalectomized rats after a lesion of the SFO.

    Science.gov (United States)

    Wilson, Wendy L; Starbuck, Elizabeth M; Fitts, Douglas A

    2002-11-15

    Circumventricular organs such as the subfornical organ (SFO) may mediate the effects of circulating angiotensin (ANG) II on salt appetite under conditions of sodium depletion in the rat. We studied the effects of an electrolytic lesion of SFO on salt appetite after adrenalectomy (ADX) in Long-Evans rats. The SFO lesion had no effect on saline intake, but it did abolish water intake after acute peripheral treatments with 2 mg/kg of captopril or a 10 mg/kg of furosemide. These findings contrast with other recent data from this laboratory demonstrating large reductions in salt appetite in adrenal-intact rats with lesions of either SFO or the organum vasculosum laminae terminalis during acute iv infusions of ANG II. Thus, the SFO may contribute to the salt appetite response to circulating ANG II, but it is not essential for the response to adrenalectomy. PMID:12429407

  11. Kidney-enquete 1992: State of the art of renal function scintigraphy in Germany

    International Nuclear Information System (INIS)

    The aim of the 'Nierenenquete 1992' was to evaluate the present importance, indications and methodological strategies of the renography (RG) in Germany. A questionnaire containing 11 issues was sent to a total of 158 nuclear medicine physicians. 103 of these are practicing at a hospital, 55 at a clinic. The questionnaire demonstrated, that RG today is carried out at a highly differentiated level. An important step toward this status today is the introduction of 99mTc-MAG-3, which has rapidly become the renal radiopharmaceutical agent of first choice for RG in Germany. The increasing use of RG in the pediatric field and for functional monitoring of the transplanted kidney is very likely due to the excellent acceptance of 99mTc-MAG-3. 84% of all nuclear medicine physicians have adopted interventional techniques (e.g. Furosemid, Captopril). These additional indications are responsible for the increase of RG's performed last year. (orig.)

  12. State-of-the-art renal diagnostics in nuclear medicine

    International Nuclear Information System (INIS)

    99mTc-MAG3 is one the mostly used radiopharmaceutical for the assessment of the renal function in nuclear medicine. This review presents the pharmacokinetics of the radiopharmaceutical, which substantiates its use for the assessment of the tubular secretion and renal function. It includes a table for the absorbed dose in critical organs for different renal function agents. The treatment techniques are presented in details. For the determination of the tubular extraction rate the Tauxe method is proposes, but it is outlined that this method is not applicable to patients with ascites, edema, hypoproteinaemia or proteinuria. The clearance values are presented for persons of age 4-17 years and after 18. Captopril scintigraphy using 99mTc-MAG is described in cases with renovascular hypertension. For the renal function assay the dynamic furosemide scintigraphy is presented. Examples for the application of each method are given

  13. Local generation and action of angiotensin II in dog iris sphincter muscle.

    Science.gov (United States)

    Okamura, T; Wang, Y; Toda, N

    1992-10-01

    Existence of the renin-angiotensin system was pharmacologically investigated in the dog isolated iris sphincter muscle. The sphincter muscle contracted in response to tetradecapeptide, a synthetic renin substrate, angiotensin (ANG) I and ANG II dose-dependently. The contractions induced by these peptides were suppressed by treatment with saralasin, indomethacin and aspirin. Contractile responses to tetradecapeptide and ANG I were also reduced by KRI-1314, a renin inhibitor, and captopril, respectively. ANG II stimulated the release of prostaglandin (PG) F2 alpha from the sphincter muscle. Angiotensin-converting enzyme activity was measurable in the sphincter muscle. Miosis was observed by intracameral injection of ANG I and ANG II into the anterior chamber. These results strongly suggest that angiotensin generating enzymes function in the sphincter muscle and ANG II produced by these enzymes contracts the sphincter muscle via the formation of PG (s), possibly PG F2 alpha. PMID:1336465

  14. A BRIEF VIEW ON ANTIHYPERTENSIVE DRUGS DELIVERY THROUGH TRANSDERMAL PATCHES

    Directory of Open Access Journals (Sweden)

    V. Rastogi*, Pragya, P. Upadhyay

    2012-07-01

    Full Text Available Transdermal Drug Delivery System (TDDS is one of the systems lying under the category of controlled drug delivery, in which the aim is to deliver the drug through skin in a predetermined and controlled rate. Hypertension is one of the common disorder for the mankind. It is not a disease in itself, but is an important risk factor for cardiovascular mortality and morbidity. The present article delivers a brief view on the work been done to increase the bioavailability of various antihypertensive drugs by formulated and delivered as transdermal patches. The different drugs includes carvedilol, metoprolol, atenolol, propranolol, labetolol, verapamil, indapamide, losartan, bisoprolol, timolol maleate, nicardipine hydrochloride, captopril, clonidine, pinacidil, nitrendipine, nicorandil, diltiazem hydrochloride, lisinopril, nifedipine, amlodipine, valsartan, enalapril maleate.

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

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    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

  16. 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.

  17. 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.

  18. 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)

  19. 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

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

    Science.gov (United States)

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

    2016-06-21

    Dystroglycan (DG) is widely expressed in various tissues, and throughout the cerebral microvasculature. It consists of two subunits, α-DG and β-DG, and the cleavage of the latter by matrix metalloproteinase (MMP)-2 and -9 underlies a number of physiological and pathological processes. However, the involvement of MMP-2/-9-mediated β-DG cleavage in cerebral ischemia remains uncertain. In astrocytes, DG is crucial for maintaining the polarization of aquaporin-4 (AQP4), which plays a role in the regulation of cytotoxic and vasogenic edema. The present study aimed to explore the effects of MMP-2/-9-mediated β-DG cleavage on AQP4 polarization and brain edema in acute cerebral ischemia. A model of cerebral ischemia was established via permanent middle cerebral artery occlusion (pMCAO) in male C57BL/6 mice. Western blotting, real-time polymerase chain reaction (PCR), immunohistochemical staining, immunofluorescent staining, electron microscopy, and light microscopy were used. Captopril was applied as a selective MMP-2/-9 inhibitor. Recombinant mouse MMP (rmMMP)-2 and -9 were used in an in vitro cleavage experiment. The present study demonstrated evidence of β-DG cleavage by MMP-2/-9 in pMCAO mouse brains; this cleavage was implicated in AQP4 redistribution and brain edema in cerebral ischemia. In addition, captopril exacerbated cytotoxic edema and ameliorated vasogenic edema at 24h after pMCAO, and alleviated brain edema and neurological deficit at 48h and 72h. In conclusion, this study provides novel insight into the effects of MMP-2/-9-mediated β-DG cleavage in acute cerebral ischemia. Such findings might facilitate the development of a therapeutic strategy for the optimization of MMP-2/-9 targeted treatment in cerebral ischemia. PMID:27038751

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

    Directory of Open Access Journals (Sweden)

    Cavalcante-Lima H.R.

    2005-01-01

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

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

    Directory of Open Access Journals (Sweden)

    Marwa Yousr

    2015-12-01

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

  3. A 1H nuclear magnetic resonance study of structural and organisational changes in the cell

    International Nuclear Information System (INIS)

    Increasing importance is being placed on understanding the role of membrane lipids in many different areas of biochemistry. It is of interest to determine what interactions may occur between membrane lipids and drug species. Furthermore, an increasing body of evidence suggests that membrane lipids are involved in the pathology of numerous diseases such as rheumatoid arthritis, cancer and HIV. Clearly, the more information available on the mechanisms involved in diseases, the greater the potential for identifying a cure or even a prevention. 1H nuclear magnetic resonance (NMR) spectroscopy was used to study the alterations in membrane lipid organisation and structure in intact, viable cultured cells. Changes in the 1H NMR spectra and the spin-lattice relaxation measurements of the human K562 and the rat FRTL-5 cell lines were observed on the addition of the fatty acid species: triolein, evening primrose oil, arachidonic acid and ITF 1779. Results indicate that the membrane lipids are reorganised to accommodate the interpolation of these molecules. The spatial arrangement adopted by each of these species appeared to dictate its effect on the lipids. Doxorubicin and menadione, both known to cause oxidative stress, were added to K562 cells. Although both agents are known to act by different mechanisms, the NMR data and scanning electron microscopy suggested that both caused similar alterations in the membrane organisation and lipid fluidity. Protrusions were formed indicating areas of weakness in the membrane. Spin-echo NMR was employed to investigate the action of the thiol-containing compounds, penicillamine, captopril and N-acetylcysteine in erythrocytes under conditions of oxidative stress. Results indicate that while captopril acts as a free radical scavenger, penicillamine may act as either oxidant or reductant. N-acetylcysteine was observed to act as a reducing agent. (author)

  4. 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.

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

    Energy Technology Data Exchange (ETDEWEB)

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

    1993-01-01

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

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

    Directory of Open Access Journals (Sweden)

    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.

  7. Diagnosis and treatment of primary aldosteronism. An analysis of 18 cases

    International Nuclear Information System (INIS)

    Early diagnosis of primary aldosteronism (PA) is important because the worldwide prevalence of PA among unselected hypertensive patients is 5% to 15%. We examined the records of 18 patients with PA who were evaluated at Toho University Medical Center Omori Hospital. We analyzed the results of confirmatory testing and subtype differentiation among 18 patients (7 men and 11 women, mean age (mean±standard deviation (SD), 55.1±14.7 years) who had received a diagnosis of PA within the previous 2.5 years. On confirmatory testing of PA, the ratios of positive results on the furosemide-upright test, captopril-loading test, and adrenocorticotropic hormone (ACTH) stimulation test were 88.9, 69.2 and 68.8%, respectively. On subtype differentiation, among 14 patients who underwent ACTH-stimulated adrenal venous sampling (ACTH-AVS), 6 were found to have bilateral hyperaldosteronism (BHA) and 8 were found to have aldosterone-producing adrenal adenoma (APA, 1 right and 7 left adenomas). In 2 of 4 patients who did not undergo ACTH-AVS, APA with right adenoma was diagnosed by abdominal CT scan and 131I-adosterol scintigraphy, however, determination of PA subtype was not possible in the remaining 2 patients. Patients with APA underwent adrenalectomy, and spironolactone was administered to patients with BHA. The therapeutic effectiveness of adrenalectomy and spironolactone did not differ. The furosemide-upright test should be the first choice for definitive diagnosis of PA; the captopril-loading test and ACTH stimulation test should be regarded as secondary examinations. It is necessary to use more than one confirmatory test, because these tests sometimes result in false negatives. Abdominal CT scan is not always useful for localizing adrenal tumors; therefore, we suggest a combination of CT scan, 131I-adosterol scintigraphy, and ACTH-AVS in determining the appropriate therapy. (author)

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

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    Macedo Cristiano Ricardo Bastos de

    2001-01-01

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

  9. Angiostatin generating capacity and anti-tumour effects of D-penicillamine and plasminogen activators

    International Nuclear Information System (INIS)

    Upregulation of endogenous angiostatin levels may constitute a novel anti-angiogenic, and therefore anti-tumor therapy. In vitro, angiostatin generation is a two-step process, starting with the conversion of plasminogen to plasmin by plasminogen activators (PAs). Next, plasmin excises angiostatin from other plasmin molecules, a process requiring a donor of a free sulfhydryl group. In previous studies, it has been demonstrated that administration of PA in combination with the free sulfhydryl donor (FSD) agents captopril or N-acetyl cysteine, resulted in angiostatin generation, and anti-angiogenic and anti-tumour activity in murine models. In this study we have investigated the angiostatin generating capacities of several FSDs. D-penicillamine proved to be most efficient in supporting the conversion of plasminogen to angiostatin in vitro. Next, from the optimal concentrations of tPA and D-penicillamine in vitro, equivalent dosages were administered to healthy Balb/c mice to explore upregulation of circulating angiostatin levels. Finally, anti-tumor effects of treatment with tPA and D-penicillamine were determined in a human melanoma xenograft model. Surprisingly, we found that despite the superior angiostatin generating capacity of D-penicillamine in vitro, both in vivo angiostatin generation and anti-tumour effects of tPA/D-penicillamine treatment were impaired compared to our previous studies with tPA and captopril. Our results indicate that selecting the most appropriate free sulfhydryl donor for anti-angiogenic therapy in a (pre)clinical setting should be performed by in vivo rather than by in vitro studies. We conclude that D-penicillamine is not suitable for this type of therapy

  10. Angiostatin generating capacity and anti-tumour effects of D-penicillamine and plasminogen activators

    Directory of Open Access Journals (Sweden)

    Maass Cathy N

    2006-06-01

    Full Text Available Abstract Background Upregulation of endogenous angiostatin levels may constitute a novel anti-angiogenic, and therefore anti-tumor therapy. In vitro, angiostatin generation is a two-step process, starting with the conversion of plasminogen to plasmin by plasminogen activators (PAs. Next, plasmin excises angiostatin from other plasmin molecules, a process requiring a donor of a free sulfhydryl group. In previous studies, it has been demonstrated that administration of PA in combination with the free sulfhydryl donor (FSD agents captopril or N-acetyl cysteine, resulted in angiostatin generation, and anti-angiogenic and anti-tumour activity in murine models. Methods In this study we have investigated the angiostatin generating capacities of several FSDs. D-penicillamine proved to be most efficient in supporting the conversion of plasminogen to angiostatin in vitro. Next, from the optimal concentrations of tPA and D-penicillamine in vitro, equivalent dosages were administered to healthy Balb/c mice to explore upregulation of circulating angiostatin levels. Finally, anti-tumor effects of treatment with tPA and D-penicillamine were determined in a human melanoma xenograft model. Results Surprisingly, we found that despite the superior angiostatin generating capacity of D-penicillamine in vitro, both in vivo angiostatin generation and anti-tumour effects of tPA/D-penicillamine treatment were impaired compared to our previous studies with tPA and captopril. Conclusion Our results indicate that selecting the most appropriate free sulfhydryl donor for anti-angiogenic therapy in a (preclinical setting should be performed by in vivo rather than by in vitro studies. We conclude that D-penicillamine is not suitable for this type of therapy.

  11. 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

  12. 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

  13. 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.

  14. 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

  15. 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

  16. 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

    Directory of Open Access Journals (Sweden)

    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

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

    Directory of Open Access Journals (Sweden)

    Ashley Chao Cardeso

    2009-01-01

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

  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. 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.

  20. 99mTc-DTPA candesartan renography in the diagnosis of renovascular hypertension

    International Nuclear Information System (INIS)

    Aim: Captopril renography (CPR) has been proved to be highly accurate in the diagnosis of patients with renovascular hypertension (RVH). However, a false-negative rate up to 20% has been described. Candesartan, a new angiotensin II AT1-receptor antagonist (ARA), has proved to be more effective to lower blood pressure in hypertensive patients than losartan, the most widely used drug of the group. The aim of this study was to evaluate the feasibility and the potential clinical value of candesartan renography (CSR) in the diagnosis of RVH and to compare on a head-to-head basis, the results of CPR and CSR. Material and Methods: A total of 39 studies were performed on 14 patients (9 female, 5 male, median age 45.5 yr, range: 35-74 yr) with moderate-to-high risk of RVH, using a three-day protocol (1: CPR, 2: CSR, 3: baseline). If the CPR and CSR studies were normal, no further studies were done. A dose of 296 MBq of 99mTc-DTPA was i.v. injected one hour after captopril (50 mg), and three hours after candesartan (8 mg) interventions. Patients were imaged supine with a LFOV camera equipped with a LEHR collimator. Renogram curves were generated and split kidney uptake was also calculated during tracer uptake interval (2 to 3 min), using the area method. A study was considered of high probability for RVH (positive) when an unilateral change ≥2 in the renogram grade and/or a reduction in the relative kidney uptake greater than 10% was seen in the CPR/CSR study compared with the baseline acquisition. Patients underwent angiography (n=10) or colour doppler (n=4) within 2 weeks of nuclear studies. Results: Six patients were diagnosed by correlative imaging with unilateral (n=5) or bilateral (n=1) renal artery stenosis (RAS). In this group CPR was positive in 2/7 (29%) renal units whereas CSR was positive in 6/7 (86%). No evidence of significant RAS was demonstrated in the remaining group of patients (n=8) in whom CPR and CSR studies were negative for RVH. Conclusion: These

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

    Directory of Open Access Journals (Sweden)

    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

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

    Directory of Open Access Journals (Sweden)

    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

  3. 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。

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

    Directory of Open Access Journals (Sweden)

    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.

  5. Involvement of Kallikrein-Kinin System on Cardiopulmonary Alterations and Inflammatory Response Induced by Purified Aah I Toxin from Scorpion Venom.

    Science.gov (United States)

    Medjadba, Wafa; Martin-Eauclaire, Marie-France; Laraba-Djebari, Fatima

    2016-02-01

    Bradykinins are released from kininogen by kallikrein. They increase capillary lung permeability after their binding to β1 and especially β2 receptors before being metabolized by kininase enzyme. This study was performed to evaluate cardiopulmonary damages and inflammatory response on injected rats with Aah I toxin of scorpion venom and the involvement of Kallikrein-Kinin system in this pathogenesis. Obtained results revealed that Aah I toxin induces inflammatory cell infiltration accompanied by cellular peroxidase activities, a release of cytokine levels, pulmonary and myocardial damage, with altered metabolic activities and imbalanced redox status. Administration of aprotinin (bradykinin inhibitor) and especially icatibant (bradykinin β2 receptor antagonist) seemed to be able to protect animals against the toxicity of Aah I; nevertheless, the use of captopril (kininase II inhibitor) reduced partially some cardiac disorders. These findings indicate that the kallikrein-kinin system may contribute to the physiopathological effect and lung edema formation induced by toxin, which suggests a potential use of drugs with significant anti-kinin properties. PMID:26361946

  6. 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.

  7. Right atrial stretch alters fore- and hind-brain expression of c-fos and inhibits the rapid onset of salt appetite.

    Science.gov (United States)

    De Gobbi, Juliana Irani Fratucci; Menani, Jose Vanderlei; Beltz, Terry G; Johnson, Ralph F; Thunhorst, Robert L; Johnson, Alan Kim

    2008-08-01

    The inflation of an intravascular balloon positioned at the superior vena cava and right atrial junction (SVC-RAJ) reduces sodium or water intake induced by various experimental procedures (e.g. sodium depletion; hypovolaemia). In the present study we investigated if the stretch induced by a balloon at this site inhibits a rapid onset salt appetite, and if this procedure modifies the pattern of immunohistochemical labelling for Fos protein (Fos-ir) in the brain. Male Sprague-Dawley rats with SVC-RAJ balloons received a combined treatment of furosemide (Furo; 10 mg (kg bw)(-1)) plus a low dose of the angiotensin-converting enzyme inhibitor captopril (Cap; 5 mg (kg bw)(-1)). Balloon inflation greatly decreased the intake of 0.3 m NaCl for as long as the balloon was inflated. Balloon inflation over a 3 h period following Furo-Cap treatment decreased Fos-ir in the organum vasculosum of the lamina terminalis and the subfornical organ and increased Fos-ir in the lateral parabrachial nucleus and caudal ventrolateral medulla. The effect of balloon inflation was specific for sodium intake because it did not affect the drinking of diluted sweetened condensed milk. Balloon inflation and deflation also did not acutely change mean arterial pressure. These results suggest that activity in forebrain circumventricular organs and in hindbrain putative body fluid/cardiovascular regulatory regions is affected by loading low pressure mechanoreceptors at the SVC-RAJ, a manipulation that also attenuates salt appetite. PMID:18556369

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

    Directory of Open Access Journals (Sweden)

    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.

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

    Directory of Open Access Journals (Sweden)

    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.

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

    Directory of Open Access Journals (Sweden)

    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.

  11. Severe Hypertension Secondary to Renal Artery Stenosis and Cushing's Syndrome

    International Nuclear Information System (INIS)

    We present an unusual patient who simultaneously had severe renal artery stenosis RAS and Cushings syndrome. The case highlights the difficulty of reaching a specific diagnosis of Cushings syndrome and the possible interaction between Cushings syndrome and some other concurrent illnesses that this patient had. A 37-year old man presented with severe hypertension HTN and uncontrolled diabetes mellitus DM without clear physical signs of Cushings syndrome. He was found to have severe osteoporosis, proximal myopathy, several cutaneous warts, tinea versicolor, and chronic viral hepatitis. Captopril-stimulated renal scan and renal artery angiogram revealed severe RAS. Partial balloon dilatation of RAS led to improvement in HTN. Unexpectedly, urine free cortisol 24 hour was found extremely high. Serum adrenocorticotropic hormone ACTH was also elevated and high dose dexamethasone suppression tests were inconclusive. Several imaging studies failed to localize the source of ACTH. Despite normal MRI of the pituitary gland, bilateral inferior petrosal sinus sampling IPSS localized the source of ACTH secretion to the right side of the pituitary gland and right anterior hemihypophysectomy resulted in cure of Cushings disease, HTN, DM, and tinea versicolor with significant improvement in cutaneous warts, osteoporosis, and chronic hepatitis. In conclusion, RAS and Cushings syndrome may occur together. Significant hypercortisolemia can occur without clear signs of Cushings syndrome. Controlling hypercortisolemia is of paramount importance when treating chronic infections in patients with Cushing's syndrome. (author)

  12. 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

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

    International Nuclear Information System (INIS)

    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. (author)

  14. 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.

  15. 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

    2015-12-01

    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

  16. 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

  17. 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

  18. 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.

  19. 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.

  20. Participation of neutral endopeptidase 24.11 (NEP;enkephalinase A) in kinin metabolism in vitro and in vivo

    International Nuclear Information System (INIS)

    Studies were done in 2 phases in rats. (1) Bradykinin was added catheter-collected urine, and its hydrolysis was determined by RIA. Three different kiniases were found by application of specific inhibitors. Kininase I-type carboxypeptidase was inhibited by 2-mercaptomethyl-3-guanidinoethyl-thiopropanoic acid, kiniase II by captopril and NEP by phosphoramidon (PA). Surprisingly, NEP was responsible for 68% of total kininase, while kininase I and II contributed only 9 and 23%. (2) To study the effects of inhibition of NEP on renal function, rats were infused with PA (330 μg/hr/kg, n=6). Urinary kinin level, kininase, GFR, RBF, U/sub Na/V, U/sub K/V and UV were measured. PA decreased total urinary kininase activity from 284 to 58 ng/min/kg (77%, p 125I-Tyr-bradykinin infused into the aorta did not appear in urine intact during PA administration. In conclusion, this is the first demonstration of NEP catabolizing kinins in vivo; its inhibition increased the excretion of intrarenally generated kinins. Changes in water and electrolyte excretion may be caused by kinins generated in the distal nephron

  1. 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

  2. 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.

  3. 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

  4. 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

  5. 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.

  6. 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

  7. Direct effect of alpha-human atrial natriuretic peptide on human vasculature in vivo and in vitro.

    Science.gov (United States)

    Hughes, A; Thom, S; Goldberg, P; Martin, G; Sever, P

    1988-02-01

    1. The effect of a alpha-human atrial natriuretic peptide (1-28) (ANP) on human vasculature was investigated in vivo and in vitro. Possible involvement of vascular dopamine receptors and the renin-angiotensin system in the response to ANP was also studied in vivo. 2. Forearm blood blow was measured by venous occlusion plethysmography. Isolated human blood vessels were studied using conventional organ bath techniques. 3. ANP (0.1-1 microgram/min, intra-arterially) produced a dose-dependent increase in forearm blood flow, corresponding to a 163% increase in net forearm blood flow in the study arm. This action of ANP was not antagonized by (R)-sulpiride (100 micrograms/min, intra-arterially), a selective vascular dopamine receptor antagonist, or 50 mg of oral captopril, an inhibitor of angiotensin-converting enzyme. 4. ANP (1 nmol/l-1 mumol/l) produced concentration-dependent relaxation of isolated human arteries, including brachial artery, but was without effect on isolated human saphenous vein. 5. ANP produces vasodilatation in vivo and relaxes isolated human arterial smooth muscle. This action of ANP may contribute to its reported hypotensive effects in vivo. PMID:2962803

  8. 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.

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

    Directory of Open Access Journals (Sweden)

    Shrestha P

    2013-08-01

    Full Text Available Pratyush Shrestha,1 Nabin K Shrestha,2 Smith Giri31Department of Surgery, College of Medical Sciences, Bharatpur, Nepal; 2Department of Internal Medicine, BP Koirala Institute of Health Sciences, Dharan, Nepal; 3Department of Internal Medicine, Tribhuvan University Teaching Hospital, Kathmandu, NepalIntroduction: Fulminant meningococcemia is a relatively rare life-threatening disease caused by Neisseria meningitidis. The clinical presentation is varied, but, when associated with myocarditis, it carries a particularly poor prognosis. We report a case of a patient with fulminant meningococcemia who subsequently developed severe myocardial dysfunction and successfully recovered within a period of 14 days of hospitalization.Case presentation: A 15-year-old girl presented with headache, fever, body ache, and diarrhea for 1 day, and ecchymotic rash over her body for 4 hours. Blood cultures confirmed infection with N. meningitidis. After 6 days in the hospital, the patient developed anasarca, elevated jugular venous pressure, and shock. The patient was managed with intravenous ceftriaxone and captopril. Over the next 3 days the patient rapidly improved and started walking.Conclusion: Meningococcemia complicated by myocarditis has an extremely poor prognosis with high mortality. Our case suggests that recovery from a severe myocardial dysfunction can occur rapidly within a few days. Prompt recognition and management in this case might have contributed to the patient's rapid recovery from myocarditis.Keywords: Neisseria meningitidis, Nepal, recovery, shock

  10. La bioinformática estructural o la realidad virtual de los medicamentos

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    Marcelo A. Martí

    2009-01-01

    Full Text Available La bioinformática estructural consiste, entre otras cosas, en realizar una simulación de del comportamiento de biomoléculas, principalmente proteínas y sus entornos, en diferentessituaciones. Al igual que un simulador de vuelo nos puede decir si un piloto se encuentra en condiciones de conducir con éxito un avión a su destino, la simulación con las biomoléculas puede establecer la capacidad de una droga para inhibir algunas enzimas o la posibilidad que dos proteínas puedan interactuar entre ellas. De este modo la bio informática contribuirá a un cambio en el paradigma del diseño de drogas permitiendo una mayor rapidez en su descubrimiento y en el proceso de optimización. Hay ejemplos exitosos de este nuevo paradigma como el caso de losinhibidores selectivos COX-2 como el Celecoxib usados en enfermedades inflamatorias crónicas, los inhibidores de la enzima convertidora de angiotensina (ECA como el Captopril, empleados en el tratamiento de la hipertensión y diversos compuestos para el tratamiento del HIV.

  11. 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

  12. 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.

  13. 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

  14. 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.

  15. 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

  16. 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.

  17. Physiological Activities of Thiacremonone Produced in High Temperature and High Pressure Treated Garlic

    Science.gov (United States)

    Woo, Koan Sik; Hwang, In Guk; Kim, Hyun Young; Lee, Sang Hoon; Jeong, Heon Sang

    2016-01-01

    To examine the possibility of using thiacremonone isolated from high-temperature-high-pressure treated garlic, this study investigated the physiological activities properties. The IC50 values of hydroxyl, superoxide, hydrogen peroxide, and nitric oxide radical scavenging activities of thiacremonone were 92.50, 65.05, 12.60, and 81.53 μg/mL, respectively. On the other hand, the activities of vitamin C were 104.93, 99.43, 42.42, and 122.64 μg/mL, and the activities of butylated hydroxyanisole were 37.22, 68.45, 22.47, and 40.54 μg/mL, respectively. The IC50 value of ACE inhibition activities of thiacremonone and captoprill were 0.265 and 0.036 μg/mL, respectively. The IC50 value of xanthine oxidase inhibition activities of thiacremonone and allopurinol were 39.430 and 9.346 μg/mL, respectively. The IC50 value of tyrosinase inhibition activities of thiacremonone and kojic acid were 101.931 and 65.648 μg/mL, respectively. PMID:27069909

  18. 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.

  19. Cystinuria in children in Bahrain

    International Nuclear Information System (INIS)

    Cystinuria is a rare autosomal recessive trait with a defect in transportof cystine and other dibasic amino acids in the kidney and intestine. Renalstone formation is the only clinical presentation of Cystinuria. We presentherewith three cases with Cystinuria. We present herewith three cases withcystinuria. Case 1 is a 13-year-old boy known to have Bernard Souliersyndrome who presented at the age of six years with staghorn stone of theleft kidney. He was treated with extracorporeal shock wave lithotripsy (ESWL)with little benefit, followed by percutaneous nephrolithotomy (PCNL). Hestill gets recurrent renal stones and is being treated with high fluidintake, low sodium diet, captopril, K-citrate and D-pencillamine. Case 2 is a10-year-old boy, brother of the first patient, who was diagnosed ascystinuria on family screening. He presented with bilateral tiny renalstones. Case 3 is a four-year-old girl who was presented at the age of 1.5years with urinary tract infection (UTI). Renal ultrasound showed lefthydronephrosis and intravenous pyelography (IVP) showed bilateral ureteralstones. She underwent cystoscopy and lithiotripsy twice; currently she is oncaptopril, K-citrate, high fluid intake and low sodium diet. We believe thisis the first report of cystinuria in children from Bahrain. (author)

  20. 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

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

    International Nuclear Information System (INIS)

    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.

  2. 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

  3. 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.

  4. Direct and indirect assessment of skeletal muscle blood flow in chronic congestive heart failure

    Energy Technology Data Exchange (ETDEWEB)

    LeJemtel, T.H.; Scortichini, D.; Katz, S.

    1988-09-09

    In patients with chronic congestive heart failure (CHF), skeletal muscle blood flow can be measured directly by the continuous thermodilution technique and by the xenon-133 clearance method. The continuous thermodilution technique requires retrograde catheterization of the femoral vein and, thus, cannot be repeated conveniently in patients during evaluation of pharmacologic interventions. The xenon-133 clearance, which requires only an intramuscular injection, allows repeated determination of skeletal muscle blood flow. In patients with severe CHF, a fixed capacity of the skeletal muscle vasculature to dilate appears to limit maximal exercise performance. Moreover, the changes in peak skeletal muscle blood flow noted during long-term administration of captopril, an angiotensin-converting enzyme inhibitor, appears to correlate with the changes in aerobic capacity. In patients with CHF, resting supine deep femoral vein oxygen content can be used as an indirect measurement of resting skeletal muscle blood flow. The absence of a steady state complicates the determination of peak skeletal muscle blood flow reached during graded bicycle or treadmill exercise in patients with chronic CHF. Indirect assessments of skeletal muscle blood flow and metabolism during exercise performed at submaximal work loads are currently developed in patients with chronic CHF.

  5. 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

  6. 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.

  7. 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

    Directory of Open Access Journals (Sweden)

    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

  8. Clinical laboratory in the biochemical evaluation of hypertension in Nigeria.

    Science.gov (United States)

    Oghagbon, E K; Okesina, A B; Oparinde, D P

    2007-03-01

    Hypertension is a worldwide problem. It is associated with severe complications that are worse in blacks! Effective management of hypertension requires that the pathophysiologic mechanism, underlining the condition be identified. The clinical laboratory can help in this regard by separating primary hypertension cases (high plasma rennin activity and low plasma rennin activity types) from those of secondary and mendelian types of hypertension. However most clinical laboratories in Nigeria do not provide some of the needed specialized tests-plasma renin activity level, urinary coritsol, plasma aldosterone and metanephrines, plasma natriuretic peptide and oral captopril tests, on routine bases. Importantly, clinicians in Nigeria should consider seriously, the role of the clinical laboratory in the management of hypertension, a condition that affects about 20% of the adult population. They should look beyond "basic or routine tests" in the management of patients with hypertension. Specific tests that will assist in the proper diagnoses of the type of hypertension in a patient should be carried out routinely on every case of hypertension. This will assist in justifying the addition of such investigations in laboratory tests repertoire, when laboratory budgets are prepared. PMID:17876918

  9. 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

  10. Medicamentos e sondas de nutrição Drugs and feeding tubes

    Directory of Open Access Journals (Sweden)

    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

  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. 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

  14. 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)

    Lidia Vázquez Montero

    2006-12-01

    Full Text Available Background: Arterial hypertension is a risk factor for many cardiovascular and cerebrovascular diseases. Objective: To evaluate the pharmacological treatment in patients with arterial hypertension, also suffering from heart failure. Methods: A descriptive-prospective study was carried out, this consisted in the use of prescription-indication drugs through a simple random sample study of 43 patients, representing the 35.2 % in six Family Clinical Units of the urban area of Camarones’ Communitarian Policlinic, Palmira, Cienfuegos, during the first semester of 2004. Results: the 51.2 % of the patients were included in the class II of the New York Heart Asociation’s classification, and the 55.8% were considered hypertense class II. The hypertensive drugs more used were the captopril and the clortalidone, and among the drugs associated to the hypertensive ones it was included the isosorbide dinitrate, the digoxin and the acetylsalicylic acid. The 87.3 % of the patients received a correct dose, and in the 88.9% it was followed an adequate administration interval. The prescription was considered adequate in the 65.1 % of the studied patients. Conclusions: the advances in the treatment of these diseases are due to different factors, even though the study shows that the treatment of the patient of the series is adecuate, it should be bettered as long as possible.
    Fundamento: La hipertensión arterial constituye un factor de riesgo para muchas enfermedades cardio y cerebrovasculares. Objetivo: Evaluar el tratamiento farmacológico en pacientes con hipertensión arterial que padecen además, de insuficiencia cardiaca. Métodos: Se realizó un estudio descriptivo retrospectivo, de utilización de medicamentos de tipo indicación prescripción, a través de un muestreo aleatorio simple, con una

  15. 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

  16. 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

  17. Therapeutic adherence in outpatients with heart failure registered with a community pharmacy

    Directory of Open Access Journals (Sweden)

    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

  18. 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

  19. 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.

  20. 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.

  1. 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

  2. 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

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

    Directory of Open Access Journals (Sweden)

    C.A.F. Andrade

    2014-01-01

    Full Text Available 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.

  4. Radiation-induced endothelial dysfunction and fibrosis in rat lung: modification by the angiotensin converting enzyme inhibitor CL242817

    International Nuclear Information System (INIS)

    The purpose of this study was to evaluate the angiotensin converting enzyme (ACE) inhibitor CL242817 as a modifier of radiation-induced pulmonary endothelial dysfunction and pulmonary fibrosis in rats sacrificed 2 months after a single dose of 60Co gamma rays (0-30 Gy) to the right hemithorax. CL242817 was administered in the feed continuously after irradiation at a regimen of 60 mg/kg/day. Pulmonary endothelial function was monitored by lung ACE activity, plasminogen activator (PLA) activity, and prostacyclin (PGI2) and thromboxane (TXA2) production. Pulmonary fibrosis was evaluated by lung hydroxyproline (HP) content. Lung ACE and PLA activities decreased with increasing radiation dose, and cotreatment with CL242817 significantly ameliorated both responses. CL242817 dose-reduction factors (DRF) were 1.3-1.5 for ACE and PLA activity. Lung PGI2 and TXA2 production increased with increasing radiation dose, and CL242817 almost completely prevented both radiation responses. The slope of the radiation dose-response curves in the CL242817-treated rats was essentially zero, precluding calculation of DRF values for PGI2 and TXA2 production. Lung HP content also increased with increasing radiation dose, and CL242817 significantly attenuated this response (DRF = 1.5). These data suggest that the ability of ACE inhibitors to ameliorate radiation-induced pulmonary endothelial dysfunction is not unique to captopril, rather it is a therapeutic action shared by other members of this class of compounds. These data also provide the first evidence that ACE inhibitors exhibit antifibrotic activity in irradiated rat lung

  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. 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.

  7. 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.

  8. AVALIAÇÃO DA ADESÃO AO TRATAMENTO MEDICAMENTOSO E NÃO MEDICAMENTOSO DE PACIENTES HIPERTENSOS ATENDIDOS NO PSF GUARITÁ, ITAPERUNA-RJ

    Directory of Open Access Journals (Sweden)

    Raphael Laiber BONADIMAN

    2015-12-01

    Full Text Available Foi realizada uma pesquisa durante os meses de agosto e setembro de 2010, com 108 pacientes hipertensos atendidos no PSF (Programa Saúde da Família Guaritá, localizado no bairro Vinhosa, no município de Itaperuna, estado do Rio de Janeiro. O objetivo do estudo foi verificar o grau de adesão ao tratamento medicamentoso e não medicamentoso nos quadros de hipertensão arterial bem como avaliar os níveis pressóricos dos pacientes. Os resultados indicaram que 63,9% dos pacientes não seguem dieta alimentar específica para hipertensão arterial e 75% dos pacientes não praticam exercícios físicos.  Em relação ao tratamento medicamentoso, o anti-hipertensivo mais utilizado foi a hidroclorotiazida, presente no tratamento de 63,9% dos pacientes avaliados, seguido do captopril (61,1% dos pacientes, propranolol (27,8%, dentre outros prescritos para menos de 25% dos pacientes.  A avaliação da adesão ao tratamento medicamentoso indicou que 69,4% dos pacientes apresentam adesão plena, 17,6% relataram omissão de doses e apenas 13% relataram não adesão ao tratamento. Um total de 87,9% dos pacientes apresentou níveis pressóricos acima dos limites de normalidade. De acordo com os resultados pode-se concluir que os pacientes possuem alta adesão ao tratamento farmacológico e baixa adesão ao tratamento não farmacológico, o que pode ser responsável pela dificuldade de controle dos níveis da pressão arterial.

  9. 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.

  10. 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...

  11. Cost-effectiveness analysis of treatments to reduce cholesterol levels, blood pressure and smoking for the prevention of coronary heart disease: evaluative study carried out in Spain.

    Science.gov (United States)

    Plans-Rubió, P

    1998-05-01

    This study assessed the cost effectiveness of treatments for the primary prevention of coronary heart disease in Spain, which included smoking cessation and reductions in blood cholesterol levels and BP. Cost-effectiveness ratios (measured in terms of US dollars per life-year gained) ranged from 2,608 US dollars to 8,058 US dollars per life-year gained for therapies aimed at smoking cessation, from 7,061 US dollars to 126,990 US dollars per life-year gained for antihypertensive drug treatment, from 15,487 US dollars to 1,689,022 US dollars per life-year gained for the drug treatment of hypercholesterolaemia and from 12,792 US dollars to 149,246 US dollars per life-year gained for cholesterol-lowering diets. In individuals with blood cholesterol levels of 7.7 mmol/L, cost-effectiveness ratios of drug treatment ranged from 33,850 US dollars to 302,088 US dollars. Cost-effectiveness ratios were lower in men than in women for all programmes evaluated. Cost-effectiveness analysis of cholesterol-lowering drugs indicated that lovastatin (HMG-CoA reductase inhibitor) was more cost effective than cholestyramine (bile acid sequestrant) and gemfibrozil (fibrate). Hydrochlorothiazide, propranolol and nifedipine were more cost effective antihypertensive treatments than prazosin and captopril. Cost-effectiveness ratios obtained in this study could be used to develop disease management strategies to facilitate the efficient use of healthcare resources and to reduce costs. When resources for coronary heart disease are limited, available treatments should be selected on the basis of their average and incremental cost-effectiveness ratios. PMID:17165328

  12. 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

  13. IRMPD spectroscopy of protonated S-nitrosocaptopril, a biologically active, synthetic amino acid.

    Science.gov (United States)

    Coletti, Cecilia; Re, Nazzareno; Scuderi, Debora; Maître, Philippe; Chiavarino, Barbara; Fornarini, Simonetta; Lanucara, Francesco; Sinha, Rajeev K; Crestoni, Maria Elisa

    2010-11-01

    S-Nitrosocaptopril, a biologically active S-nitrosothiol, is generated as protonated species and isolated in the gas phase by electrospray ionization coupled to Fourier Transform Ion Cyclotron Resonance (FT-ICR) or ion-trap mass spectrometry. The structural and IR spectroscopic characterization of protonated S-nitrosocaptopril (SNOcapH(+)) is aided by the comparative study of the parent species lacking the NO feature, namely protonated captopril. The study is accomplished by methodologies based on tandem mass spectrometry, namely by energy resolved collision-induced dissociation and infrared multiple-photon dissociation (IRMPD) spectroscopy, backed by density functional theory calculations. IRMPD spectra have been obtained both in the 1000-1900 cm(-1) fingerprint range, using a beamline of the infrared free electron laser (IR-FEL) at the Centre Laser Infrarouge d'Orsay (CLIO), and in the O-H and N-H stretching region (2900-3700 cm(-1)) using the tunable IR radiation of a tabletop parametric oscillator/amplifier (OPO/OPA) laser source. The structural features of the ion have been ascertained by comparison of the experimental IRMPD spectra with the IR transitions calculated for the lowest energy isomers. Evidence is obtained that protonation occurs at the amide carbonyl oxygen which is found to be the thermodynamically most basic site. However, SNOcapH(+) is present as a thermally equilibrated mixture of low-energy structures, with a major contribution of the most stable isomer characterized by a trans relationship of the positively charged OH group with respect to the carboxylic acid functionality on the adjacent proline ring and by an anti conformation at the S-N (partial) double bond, though the energy difference with the analogous trans-syn isomer is less than 1 kJ mol(-1). The highly diagnostic N-O stretching mode has been unambiguously identified, which may be regarded as an informative probe for S-nitrosation features in more complex, biologically active

  14. [Hypotensive action of human renin inhibitor KRI-1314 in the common marmoset].

    Science.gov (United States)

    Saitoh, H; Etoh, Y; Murakami, M; Kubota, T; Miyazaki, M

    1994-04-01

    The possibility of using KRI-1314, a new cyclohexylnorstatine derivative, as an antihypertensive drug was examined using common marmosets. KRI-1314 strongly inhibited plasma renin activity (PRA) in both humans and marmosets, with a 50% inhibitory concentration of 4.7 x 10(-9) and 6.9 x 10(-9) M, respectively. In anesthetized marmosets, the increase in both blood pressure and PRA induced by bolus intravenous injection of RH-renin (0.15 microgram/kg) was suppressed by constant intravenous infusion of KRI-1314 (0.01 and 0.1 mg/kg/min) in a dose-dependent manner. In the sustained hypertension induced by continuous intravenous infusion of RH-renin (0.1 microgram/kg/min), a dose-dependent hypotensive response was produced by bolus intravenous injection of KRI-1314 (0.03-3 mg/kg). In the sodium-depleted model, whose PRA was increased by a two-week low-sodium diet coupled with furosemide loading, both intravenous injection (0.1-3 mg/kg) and oral administration (10 and 30 mg/kg) of KRI-1314 to anesthetized and conscious animals, respectively, lowered blood pressure dose-dependently with PRA suppression. The hypotensive activity of orally administered KRI-1314 (30 mg/kg) was almost equal to that of orally administered captopril (1 mg/kg). KRI-1314 did not affect heart rate in any of the experiments. These results indicate that the potent human renin inhibitor KRI-1314 may become an orally effective drug for treating renin-dependent hypertension. PMID:8175079

  15. 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.

  16. 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

  17. 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

  18. 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

  19. Economic impact of an ultrasonographic contrast agent on the diagnosis and initial management of patients with suspected renal artery stenosis

    International Nuclear Information System (INIS)

    To determine resource use in the diagnosis and management of Canadian hypertensive patients with suspected renal artery stenosis and to estimate the impact of diagnosis with contrast-enhanced duplex Doppler ultrasonography (US) on resource use. Seventy-eight patients with suspected renal artery stenosis underwent usual diagnostic tests (captopril-enhanced renal scintigraphy or duplex Doppler US) and contrast-enhanced US. A management pathway ('planned') describing the medical resources required for further patient care was outlined on the basis of results from each test (separately), and a modified management pathway ('recommended'), which considered data from both diagnostic methods, was also outlined. Medical resources and productivity losses were assessed prospectively for a 3-month period after patients underwent both tests ('actual' management pathway). With usual diagnostic methods, 14 (18%) of the tests were inconclusive, whereas only 1 (1%) of the enhanced US examinations was inconclusive; the cost-efficacy ratio was $422 and $343 per successful diagnosis, respectively. Further management costs for patients with an inconclusive diagnosis were estimated at $6370 after the usual diagnostic tests, but only $1278 with enhanced US. Although the costs of the planned and recommended management pathways were similar ($227 and $294 per patient respectively), the proportion of patients requiring further resources was lower with enhanced US (56% v. 46%). Three-month actual management costs ranged from $121 to $1605 per patient (mean $360). Diagnostic tests and surgical procedures were the major cost drivers in all pathways, and costs wore highest for patients in whom stenosis was diagnosed. For patients with suspected renal artery stenosis, contrast-enhanced US had a higher diagnostic success rate than usual diagnostic methods and afforded savings through lower administrative costs and lower medical resource consumption for patients whose diagnosis was unclear after

  20. 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.

  1. [Duality of angiotensin II receptors and risk for stroke and cancer: what is the connection?].

    Science.gov (United States)

    Fournier, A; Ghitu, A; Darabont, R; Mazouz, H; Makdassi, R; Canaple, S; Rosa, A; Fernandez, L A

    Angiotensin II (AII) acts by 2 types of receptors: the ATI receptor which mediates its actions on vasoconstriction, renin (inhibition) and aldosterone (stimulation) secretions, cellular proliferation and angiogenesis and the non-AT1 (often called AT2) receptors. Mainly expressed in the embryon these latter may favor cellular differentiation and recruitment of collateral circulation. Angiotensin converting enzyme inhibitors (ACEI) decrease the synthesis of All and therefore the stimulation of both receptor types whereas AT1-receptor antagonists (AT1RA) block only the stimulation of these latter and increase the stimulation of AT2 receptor since they increase the production of All secondarily to the inhibition of the feedback of renin secretion by All. Experimentally ACEI and AT1RA decrease angiogenesis and cellular proliferation and favor cellular differentiation which could explain the protective effect of ACEI against cancer suggested recently in a Scotish study. Despite of their common suppressive effect on angiogenesis AT1RA may better than ACEI protect against ischemic events specially the cerebral ones because they favor the rapid recruitment of collateral circulation. This has been demonstrated for losartan in case of abrupt ligation of the carotid in the gerbil since its previous administration protects against fatal cerebral ischemia whereas its previous administration with enalapril abolishes this protection. These data may explain why, in the CAPP trial, captopril which has prevented more effectively diabetes occurrence could not be proved superior to diuretics and/or betablocker in the prevention of myocardial infarction and specially of strokes for which exist on the contrary a suspicion of a lower protection. Therefore a comparative trial between AT1RA and ACEI in the prevention of stroke recurrence should appear as a priority for Public Health and Pharmaceutical Industry Authorities. PMID:10360191

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

    Science.gov (United States)

    Arcanjo, Daniel Dias Rufino; Vasconcelos, Andreanne Gomes; Comerma-Steffensen, Simón Gabriel; Jesus, Joilson Ramos; Silva, Luciano Paulino; Pires, Osmindo Rodrigues; Costa-Neto, Claudio Miguel; Oliveira, Eduardo Brandt; Migliolo, Ludovico; Franco, Octávio Luiz; Restini, Carolina Baraldi Araújo; Paulo, Michele; Bendhack, Lusiane Maria; Bemquerer, Marcelo Porto; Oliveira, Aldeidia Pereira; Simonsen, Ulf; Leite, José Roberto de Souza de Almeida

    2015-01-01

    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. PMID:26661890

  3. 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.

  4. Fufang Xue Shuan Tong capsules inhibit renal oxidative stress markers and indices of nephropathy in diabetic rats

    Science.gov (United States)

    FANG, DONGHONG; WAN, XUESI; DENG, WANPING; GUAN, HONGYU; KE, WEIJIAN; XIAO, HAIPENG; LI, YANBING

    2012-01-01

    Fufang Xue Shuan Tong (FXST) capsules, a traditional Chinese medicine, have been used to treat diabetic nephropathy for many years. FXST has been shown to attenuate elevated levels of oxidative stress in the retina of diabetic rats. However, whether FXST protects kidneys through the same mechanism(s) remains unclear. In this study, diabetes was induced in rats by administration of a high-fat diet and low-dose streptozotocin. Rats were administered low (450 mg/kg/day), middle (900 mg/kg/day) or high (1800 mg/kg/day) doses of FXST orally for 3 months. Another group was administered 50 mg/kg/day orally for the same period. The results indicated that all doses of FXST reduced urinary protein excretion and creatinine clearance and ameliorated the diabetic nephropathy-related mesangial matrix expansion. However, only middle and high doses of FXST prevented glomerular hypertrophy in diabetic rats, and the high dose showed the greatest inhibitory effect with regard to mesangial matrix expansion. Furthermore, superoxide dismutase activities were significantly elevated, whereas malondialdehyde levels were significantly reduced in the renal cortex following FXST treatment. The kidney-protective role of FXST is not inferior to that of captopril, one of the most commonly used drugs for the treatment of diabetic nephropathy. In conclusion, FXST retards the progression of diabetic nephropathy, while high-dose FXST shows the most prominent effect in counteracting the pathological changes of diabetic nephropathy. The renoprotective action of FXST is induced by the reduction of oxidative stress in diabetic nephropathy. PMID:23226741

  5. 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

  6. 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。

  7. 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

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

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    José Antonio Corona-Rojo

    2009-08-01

    Full Text Available José Antonio Corona-Rojo1, Marina Altagracia-Martínez1, Jaime Kravzov-Jinich1, Laura Vázquez-Cervantes1, Edilberto Pérez-Montoya2, Consuelo Rubio-Poo31Division of Biological Sciences and Health, Metropolitan Autonomous University, Campus Xochimilco (UAM-X, Xochimilco, México; 2National Polytechnical Institute (IPN, México DF; 3Faculty of Higher Studies – Zaragoza (FES-Zaragoza, National Autonomous University of México (UNAM, México City, MéxicoIntroduction: Six out of every 10 elderly persons live in developing countries.Objective: To analyze and assess the drug prescription patterns and errors in elderly outpatients attending public health care centers in Mexico City, Mexico.Materials and methods: A descriptive and retrospective study was conducted in 2007. Fourteen hundred prescriptions were analyzed. Prescriptions of ambulatory adults aged >70 years who were residents of Mexico City for at least two years were included. Prescription errors were divided into two groups: (1 administrative and legal, and (2 pharmacotherapeutic. In group 2, we analyzed drug dose strength, administration route, frequency of drug administration, treatment length, potential drug–drug interactions, and contraindications. Variables were classified as correct or incorrect based on clinical literature. Variables for each drug were dichotomized as correct (0 or incorrect (1. A Prescription Index (PI was calculated by considering each drug on the prescription. SPSS statistical software was used to process the collected data (95% confidence interval; p < 0.05.Results: The drug prescription pattern in elderly outpatients shows that 12 drugs account for 70.72% (2880 of prescribed drugs. The most prescribed drugs presented potential pharmacotherapeutic errors (as defined in the present study. Acetylsalicylic acid–captopril was the most common potential interaction (not clinically assessed. Potential prescription error was high (53% of total prescriptions. Most

  9. 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

  10. 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。

  11. Fatores associados à adesão ao tratamento antihipertensivo por idosos na atenção primária

    Directory of Open Access Journals (Sweden)

    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.

  12. 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

  13. 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

  14. 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

  15. 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

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

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    Ehnert S

    2013-03-01

    Full Text Available Sabrina Ehnert,1 Teresa Lukoschek,2 Anastasia Bachmann,2 Juan J Martínez Sánchez,1 Georg Damm,3 Natascha C Nussler,4 Stefan Pscherer,5 Ulrich Stöckle,1 Steven Dooley,2 Sebastian Mueller,6 Andreas K Nussler11Eberhard Karls Universität Tübingen, BG Trauma Center, Tübingen, Germany; 2Mol Hepatology - Alcohol Associated Diseases, Department of Medicine II, Medical Faculty, Mannheim, Germany; 3Department of General, Visceral, and Transplantation Surgery, Charité University Medicine, Berlin, Germany; 4Clinic for General, Visceral, Endocrine Surgery and Coloproctology, Clinic Neuperlach, Städtisches Klinikum München GmbH, Munich, Germany; 5Department of Diabetology, Klinikum Traunstein, Kliniken Südostbayern AG, Traunstein, Germany; 6Department of Medicine, Salem Medical Center, Ruprecht-Karls-Universität, Heidelberg, GermanyBackground: Patients with alcoholic liver disease (ALD often suffer from high blood pressure and rely on antihypertensive treatment. Certain antihypertensives may influence progression of chronic liver disease. Therefore, the aim of this study is to investigate the impact of the commonly used antihypertensives amlodipine, captopril, furosemide, metoprolol, propranolol, and spironolactone on alcohol-induced damage toward human hepatocytes (hHeps.Methods: hHeps were isolated by collagenase perfusion. Reactive oxygen species (ROS were measured by fluorescence-based assays. Cellular damage was determined by lactate-dehydrogenase (LDH-leakage. Expression analysis was performed by reverse-transcription polymerase chain reaction and Western blot. Transforming growth factor (TGF-β signaling was investigated by a Smad3/4-responsive luciferase-reporter assay.Results: Ethanol and TGF-β1 rapidly increased ROS in hHeps, causing a release of 40%–60% of total LDH after 72 hours. All antihypertensives dose dependently reduced ethanol-mediated oxidative stress and cellular damage. Similar results were observed for TGF-β1-dependent

  17. 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.

  18. 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

  19. 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。

  20. 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。

  1. 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.

  2. 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

  3. 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

  4. A new experimental approach in endothelium-dependent pharmacological investigations on isolated porcine coronary arteries mounted for impedance planimetry

    Science.gov (United States)

    Tankó, László B; Mikkelsen, Erich O; Simonsen, Ulf

    1999-01-01

    The aim of this study was to investigate whether the balloon-based impedance planimetry technique could be a useful tool in endothelium-dependent investigations. Porcine large coronary arteries contracted with prostaglandin F2α (PGF2α, 10 μM) did not relax to bradykinin (0.1 nM–0.1 μM), but did relax to sodium nitroprusside (SNP, 10 μM). However, after eversion of the segments, bradykinin induced relaxations with pD2 values and maximal responses of 8.78±0.09 and 75±2% (n=6), respectively. Incubation with captopril (1 μM) did not reveal a relaxation to bradykinin in the normal vessel configuration and had no influence on the concentration-relaxation relationship in everted segments. Lowering the luminal pressure in contracted segments from 131±5 mmHg (isometric, n=5) to 60 mmHg (isobaric, n=5) did not facilitate the action of bradykinin. Eversion of segments did not influence the concentration-response relationship for K+ (4.7–125 mM), PGF2α (0.3–30 μM), and SNP (30 nM–30 μM), although the time-courses of responses were faster when the agents were added from the intimal compared to the adventitial side of the preparation. In the same everted segment contracted with PGF2α, the concentration-response relationship for bradykinin was not different under isometric and isobaric conditions. These results indicate that, (1) reduced endothelium-dependent relaxations to adventitially administered substances can be ascribed to a diffusion barrier in the vessel wall, while enzymatic degradation, luminal pressure and precontractile responses seem not to play a role, (2) impedance planimetry applied to everted cylindrical segments could be a useful experimental approach in pharmacological studies of endothelium-dependent responses under isobaric and isometric conditions. PMID:10498848

  5. Kininogenase activity of Thalassophryne nattereri fish venom.

    Science.gov (United States)

    Lopes-Ferreira, Mônica; Emim, José Artur da Silva; Oliveira, Vitor; Puzer, Luciano; Cezari, Maria Helena; Araújo, Mariana da Silva; Juliano, Luiz; Lapa, Antônio José; Souccar, Caden; Moura-da-Silva, Ana Maria

    2004-12-01

    Accidents caused by the venomous fish Thalassophryne nattereri are characterized by edema, intense pain and necrosis at the site of the sting. This study assessed the nociceptive and edematogenic activities of T. nattereri venom after injection into the mouse hindpaw and determination of the paw licking duration and weight. Subplantar injections of the venom (0.1-6 microg) induced a dose-related increase of the paw licking time and paw swelling with maximal values at 3 microg (209.5 +/- 57.5 s and 135.0 +/- 6.8 mg, respectively). Pretreatment of mice with either indomethacin (10 mg/kg, i.p.), a cyclooxygenase inhibitor, dexamethasone (1 mg/kg, s.c.), a steroid anti-inflammatory agent, cyproheptadine (1 mg/kg, i.p.), antagonist of serotonin receptors or L-NAME (100 mg/kg, s.c.), inhibitor of nitric oxide syntase, did not affect the venom-induced nociceptive and edematogenic responses. Injection of the opioid analgesic fentanyl (0.1 mg/kg, s.c.) reduced the paw licking time induced by 1 microg venom by 84% of control, without affecting the paw swelling. Both nociceptive and edematogenic responses were reduced after treatment with a specific tissue kallikrein inhibitor (TKI, 100 mg/kg, i.p.) by 78% and 24% from control values, respectively. Administration of a specific plasma kallikrein inhibitor (PKSI(527,) 100 mg/kg, s.c.) did not affect the venom-induced nociceptive response, but it decreased the paw edema by 15% from control. After injection of the angiotensin-converting enzyme inhibitor captopril (100 mg/kg, i.p.) the venom-induced nociceptive end edematogenic responses were increased by two-fold. The role of kallikreins possibly present in the venom was further assessed by hydrolysis of human kininogen and kininogen-derived synthetic peptides, showing the release of kallidin (Lys-bradykinin). The hydrolysis was inhibited by metal chelating agents but not by serino-, aspartyl- or cysteino-proteinase inhibitors. The data suggest that a protease with tissue

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

    Directory of Open Access Journals (Sweden)

    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.

  7. 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

  8. 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

  9. 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

  10. 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

  11. 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

  12. 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

  13. 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

  14. 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

  15. 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

  16. 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

  17. 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

  18. 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

  19. 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

  20. 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

  1. 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

  2. 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

  3. 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