MedWorm: Captopril

  S-Allyl-Mercapto-Captopril: A Novel Compound in the Treatment of Cohen-Rosenthal Diabetic Hypertensive Rats

J Clin Hypertens (Greenwich). S-allyl-mercapto-captopril (CPSSA) is a conjugate of captopril with allicin, an active principle in garlic with multiple beneficial actions on metabolic syndrome abnormalities, including weight preservation, observed by the authors in fructose-induced hypertensive hyperinsulinemic rats and in Koletsky rats. The aim of the study was to examine blood pressure (BP) and glucose levels in the Cohen-Rosenthal Diabetic Hypertensive (CRDH) model as well as to follow their weight preservation. CRDH rats (n=14) were fed the sugar-rich copper-free diet essential for the development of diabetes mellitus. Two months later BP and blood glucose levels were measured. CPSSA was diluted in drinking water and administered at a final dose of 53.5 mg/kg/d (n=8). Control rats (n=6)...

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  Captopril directly inhibits matrix metalloproteinase-2 activity in continuous ambulatory peritoneal dialysis therapy.

CONCLUSION: ACE inhibitors, such as captopril, may be applied as important compounds for MMP-2 inhibition in inflammation caused by CAPD. PMID: 20184869 [PubMed - as supplied by publisher] (Source: International Journal of Clinical Chemistry)

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  Resolving issues of content uniformity and low permeability using eutectic blend of camphor and menthol

Gohel M C, Nagori S AIndian Journal of Pharmaceutical Sciences 2009 71(6):622-629The aim of present study were to arrest the problem of content uniformity without the use of harmful organic solvent and to improve <i>ex vivo</i> permeability of captopril, a low dose class III drug as per biological classification system. Eutectic mixture of camphor and menthol was innovatively used in the work. Captopril solution in eutectic mixture was blended with Avicel PH 102 and then the mixture was blended with mannitol in different ratios. Formulated batches were characterized for angle of repose and Carr's index. A selected batch was filled in hard gelatin capsule. Tablet dosage form was also developed. Capsules and tablets were characterized for ...

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  Confirmatory Tests in the Diagnosis of Primary Aldosteronism

Horm Metab ResDOI: 10.1055/s-0029-1246186AbstractPrimary aldosteronism is the most common form of secondary hypertension and patients with hyperaldosteronism are more prone to premature cardiovascular complications compared to essential hypertensives. The diagnostic flow-chart for the diagnosis of PA is performed in three steps: a) screening; b) confirmation; and c) subtype differentiation. Instead of proceeding directly to subtype classification, the recently published Endocrine Society Guidelines recommend that patients with a positive ARR should undergo a confirmatory test, in order to definitively confirm or exclude the diagnosis of PA. The Guidelines recognize four testing procedures: oral sodium loading, saline infusion, fludrocortisone suppression, and captopril challenge. Herein we...

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  Comparative effects of captopril and L-carnitine on blood pressure and antioxidant enzyme gene expression in the heart of spontaneously hypertensive rats.

In conclusion, we have found that L-carnitine and captopril have a similar antioxidant effect in the hearts of hypertensive rats. The molecular regulation of antioxidant enzymes through an inhibition of the renin-angiotensin system and a modulation of the NF-kB/IkB system seems to be responsible for this antioxidant effect. PMID: 20123095 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology)

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  Diagnosis of primary aldosteronism: Comparison of post-captopril active renin concentration and plasma renin activity.

CONCLUSIONS: The correlation of individual PRA and ARC after administration of captopril was excellent; especially at the lower PRA levels. Post-captopril ARR(ARC) values used to diagnose PA are not different from post-captopril PRA-based (ARR(PRA)) values in patients without kidney, liver and heart failure. Primary aldosteronism can be diagnosed with a post-captopril cutoff value of ARR(ARC)>35.5 pmol/ ng. PMID: 20117105 [PubMed - as supplied by publisher] (Source: International Journal of Clinical Chemistry)

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  Prevalence of primary aldosteronism among Bulgarian hypertensive patients

Abstract  Primary aldosteronism (PA) has long been considered a rare disease, but a higher prevalence was suggested recently. The aim of this study was to evaluate the prevalence of PA in a group of Bulgarian hypertensive patients, including patients with adrenal incidentalomas (AI). The aldosterone to renin ratio (ARR)>750 was used as a positive screening test and the Captopril test was performed to confirm the diagnosis. Adrenal CT scan was used to differentiate between the main subtypes of PA-aldosterone-producing adenoma (APA) and idiopathic hyperaldosteronism (IHA). The diagnosis of APA was retrospectively confirmed after surgery. After excluding other forms of endocrine hypertension, except PA, we investigated a total of 472 consecutive hypertensive patients, among...

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  Endothelial Function Impairment in Chronic Venous Insufficiency: Effect of Some Cardiovascular Protectant Agents

In segments of human varicose veins, endothelial function was assessed by measuring relaxation induced by acetylcholine in noradrenaline-precontracted preparations. In addition, concentration-response curves to acetylcholine were obtained before and after incubation with the arterial endothelium protectant agents captopril, losartan, troglitazone, pravastatin, or simvastatin. The antivaricose agent escin was also tested. Mean acetylcholine-induced relaxation of varicose venous rings was about 13%, approximately one third of that reported for control saphenous veins. Concentration-response curves to acetylcholine were ‘‘u’’ shaped, the result of endothelium-mediated relaxation at low concentrations, superseded by subsequent smooth muscle contractile responses. Relaxa...

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  MMP-mediated cleavage of beta-dystroglycan in myelin sheath is involved in autoimmune neuritis.

Authors: Zhao XL, Li GZ, Sun B, Zhang ZL, Yin YH, Tian YS, Li H, Li HL, Wang DS, Zhong D alpha-/beta-Dystroglycans (DG) located at the outmost layer of myelin sheath play a critical role in its formation and stability in the peripheral nerve system. The demyelination of nerve fibers is present in autoimmune neuritis, however, it is not known about the molecular mechanisms underlying this pathological process. In an animal model of experimental autoimmune neuritis, we observed that beta-DG cleavage was associated with the demyelination of peripheral nerves. The neuritis and beta-DG cleavage were accompanied by matrix metalloproteinase (MMP)-2/-9 over-expressions and attenuated by captopril, a MMP inhibitor. The blockade of MMPs also improves clinical signs. Our results reveal a crucial ...

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  Myelopoiesis modulation by ACE hyperfunction in kinin B(1) receptor knockout mice: relationship with AcSDKP levels.

Authors: Oliveira CR, Paredes-Gamero E, Barbosa CM, Nascimento FD, Reis FC, Ferreira AT, Carmona AK, Pesquero JB, Tersariol IL, Araújo RC, Bincoletto C Angiotensin I-converting enzyme (ACE), a common element of renin-angiotensin system (RAS) and kallikrein-kinin system (KKS), is involved in myelopoiesis modulation, mainly by cleaving the tetrapeptide N-acetyl-seryl-aspartyl-lysyl-proline (AcSDKP). Based on this finding and in our results showing B1 and B2 kinin receptors expression in murine bone marrow (BM) cells, we evaluated the ACE influence on myelopoiesis of kinin B1 receptor knockout mice (B1KO) using long-term bone marrow cultures (LTBMCs). Captopril and AcSDKP were used as controls. Enhanced ACE activity, expressed by non-hematopoietic cells (Ter199(-) and CD45(-)), was o...

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

Authors: Albuquerque D, Nihei J, Cardillo F, Singh R Increasing evidence implies beneficial effects of angiotensin-converting enzyme (ACE) inhibitors beyond those of their original indications to control hypertension. One of the most attractive non-hemodynamic properties of ACE inhibitors is their ability to regulate cytokine production. The mechanism(s) underlying the role of ACE inhibitors on cytokine synthesis are not well understood but they have traditionally been attributed to the inhibition of angiotensin (Ang) II formation. In fact, it has been extensively demonstrated that ACE inhibitors decrease Ang II-induced production of proinflammatory cytokines and chemokines. However, it is not well described if inhibition of endogenous Ang II generation by ACE inhibitors modulates syst...

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  Exploiting iminoquinone free radical production for thiol based drugs determination in pharmaceutical formulations

A spectrophotometric flow analysis procedure to determine Captopril (CPT) and N-acetyl-L-cysteine (NAC) in pharmaceutical formulations was developed based on the reaction with iminoquinone radical produced from the N,N-dimethyl-p-phenilenediamene (DMPD) oxidation in acid medium. The reagents addition order was evaluated and analytical parameters were optimized. The linear concentrations ranges were 2.5-90 and 5.0-50 mg L-1 for CPT and NAC, respectively. Limits of detection (3σ) were calculated at 0.22 and 1.8 mg L-1 and the relative standard deviation (N = 10) were lower than 1.0 and 2.1% for CPT and NAC, respectively. The procedure was employed for CPT and NAC determination in diverse pharmaceutical formulations and by applying paired t-test the results were in agreement with those obtai...

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  Captopril: Angioedema in an elderly patient following sublingual administration: case report

(Source: Reactions)

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  CAPTOPRIL AND HYDROCHLOROTHIAZIDEtablet [TEVA Pharmaceuticals USA Inc]

Updated Date: Dec 29, 2009 EST (Source: DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST))

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  Angiotensin II stimulates trafficking of NHE3, NaPi2, and associated proteins into the proximal tubule microvilli

Angiotensin II (ANG II) stimulates proximal tubule (PT) sodium and water reabsorption. We showed that treating rats acutely with the angiotensin-converting enzyme inhibitor captopril decreases PT salt and water reabsorption and provokes rapid redistribution of the Na+/H+ exchanger isoform 3 (NHE3), Na+/Pi cotransporter 2 (NaPi2), and associated proteins out of the microvilli. The aim of the present study was to determine whether acute ANG II infusion increases the abundance of PT NHE3, NaPi2, and associated proteins in the microvilli available for reabsorbing NaCl. Male Sprague-Dawley rats were infused with a dose of captopril (12 µg/min for 20 min) that increased PT flow rate ~20% with no change in blood pressure (BP) or glomerular filtration rate (GFR). When ANG II (20 ng·kg...

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  Medicinal Chemistry of Drugs used in Diabetic Cardiomyopathy.

Authors: Adeghate E, Kalasz H, Veress G, Teke K Diabetes mellitus is a common disease and contributes to a high degree of morbidity and mortality. Cardiovascular complications, including diabetic cardiomyopathy are major causes of morbidity and mortality in diabetic patients. Diabetic cardiomyopathy is a condition that affects the myocardium, primarily. It is not necessarily associated with ischemic heart disease, high blood pressure, valvular or congenital anomalies. The pathology of diabetic cardiomyopathy includes interstitial fibrosis, apoptosis of cardiomyocytes, abnormal energy utilization, small vessel disease and cardiac neuropathy. These pathologies are induced by hyperglycemia and oxidative stress. Biochemical as well as electrolyte changes, especially reduced calcium availab...

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  Study of a lipophilic captopril analogue binding to angiotensin I converting enzyme

In this study, we present the biological activity of silacaptopril, a silylated analogue of captopril, and its binding affinity towards ACE. Based on the recently determined crystal structures of both the ACE domains, a series of docking calculations were carried out in order to study the structural characteristics and the binding properties of silacaptopril and its analogues with ACE. Copyright © 2009 European Peptide Society and John Wiley & Sons, Ltd. (Source: Journal of Peptide Science)

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  Effects of a protocol of ischemic postconditioning and/or captopril in hearts of normotensive and hypertensive rats

Abstract  Brief periods (a few seconds) of cyclic coronary occlusions applied early in reperfusion induce a cardioprotection against infarct size, called postconditioning (PostC) in which B2-bradykinin receptors play a pivotal role. Since angiotensin-converting enzyme (ACE) inhibitors reduce degradation of kinins, we studied the effects of PostC on infarct size and postischemic myocardial dysfunction in both normotensive (WKY) and spontaneously hypertensive rats (SHR) acutely or chronically treated with the ACE inhibitor Captopril. Isolated hearts from SHR and WKY rats were subjected to the following protocols: (a) ischemia for 30- and 120-min reperfusion (I/R); (b) I/R + PostC protocol (5-cycles 10-s I/R); (c) pretreatment with Captopril for 4-weeks before to subj...

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  ADAMTS-1 contributes to the antifibrotic effect of Captopril by accelerating the degradation of type I collagen in chronic viral myocarditis.

We examined the role of ADAMTS-1 in the antifibrotic activity of the ACE inhibitor Captopril in a chronic viral myocarditis (CVMC) model. Balb/c mice were assigned to five groups: normal control group1 (group 1) , normal control group2 (group 2), CVMC model group(group 3), CVMC control group (group 4) and Captopril therapy group (group 5) . Group 3, 4 and 5 received Coxsackievirus B(3) to induce CVMC and group 5 was treated with Captopril (100mg/kg )for 28days. Heart sections were stained with picrosirius red and collagen volume fraction calculated. ADAMTS-1 expression was determined by Western blot. Type I collagen and carboxyterminal telopeptide of type I collagen (ICTP) were measured by RT- PCR. Group 4 mice had significantly increased collagen volume fraction compared to groups 2 and 5...

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  Captopril: Contact dermatitis: case report

(Source: Reactions)

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  [Comment] Optimising management of chronic heart failure

When the ELITE II study was unable to show superiority of 50 mg per day of the angiotensin-receptor blocker (ARB) losartan in comparison with 150 mg per day of the angiotensin-converting-enzyme (ACE) inhibitor captopril in patients with systolic chronic heart failure, one explanation was that the dose of the ARB might have been too low compared with that of the ACE inhibitor. This possibility was supported by the non-superior result with this dose of losartan versus 150 mg per day of captopril in patients with left ventricular systolic dysfunction after myocardial infarction, in addition to beneficial outcomes with 100 mg per day of losartan in patients with diabetic nephropathy and left ventricular hypertrophy. However, the hypothesis that the losartan 50 mg per day dose was suboptimum se...

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  Effect of angiotensin converting enzyme inhibitor on matrix metalloproteinase-9 activity in patients with Kawasaki disease.

CONCLUSION: ACE inhibitor may be effective for preventing CAA formation in KD patients, especially IVIG non-responders. PMID: 19945447 [PubMed - as supplied by publisher] (Source: International Journal of Clinical Chemistry)

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  Successful Applications of Computer Aided Drug Discovery: Moving Drugs from Concept to the Clinic.

Authors: Talele TT, Khedkar SA, Rigby AC Drug discovery and development is an interdisciplinary, expensive and time-consuming process. Scientific advancements during the past two decades have changed the way pharmaceutical research generate novel bioactive molecules. Advances in computational techniques and in parallel hardware support have enabled in silico methods, and in particular structure-based drug design method, to speed up new target selection through the identification of hits to the optimization of lead compounds in the drug discovery process. This review is focused on the clinical status of experimental drugs that were discovered and/or optimized using computer-aided drug design. We have provided a historical account detailing the development of 12 small molecules (Captopri...

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  Angiotensin Converting Enzyme (ACE) Inhibitory Peptides: Production and Implementation of Functional Food.

Authors: De Leo F, Panarese S, Gallerani R, Ceci LR In recent decades, the most successful strategy for controlling blood pressure has been inhibition of the angiotensin-converting enzyme (ACE). ACE inhibitors of chemical synthesis (captopril, enalapril, ramipril and trandolapril) have been widely used clinically to reduce mortality in patients with heart failure, and in patients with recent myocardial infarction and heart failure or marked left ventricular dysfunction. In addition to preventive and therapeutic drugs, increased attention has been paid to identifying dietary compounds that may contribute to cardiovascular treatment and prevention. ACE inhibitory peptides, derived from a multitude of plant and animal proteins such as milk, soy or fish, represent sources of health-enhanci...

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  Renin-Angiotensin System Suppression Mitigates Experimental Radiation Pneumonitis

Purpose: To find the mitigators of pneumonitis induced by moderate doses of thoracic radiation (10–15 Gy).Methods and Materials: Unanesthetized WAG/RijCmcr female rats received a single dose of X-irradiation (10, 12, or 15 Gy at 1.615 Gy/min) to the thorax. Captopril (an angiotensin-converting enzyme inhibitor) or losartan (an angiotensin receptor blocker) was administered in the drinking water after irradiation. Pulmonary structure and function were assessed after 8 weeks in randomly selected rats by evaluating the breathing rate, ex vivo vascular reactivity, and histopathologic findings. Survival analysis was undertaken on all animals, except those scheduled for death.Results: Survival after a dose of 10 Gy to the thorax was not different from that of unirradiated rats for ≤1 year. S...

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  The Effect of Captopril on Progression of Retinopathy in Type 2 Diabetes

Diabetes Technology & Therapeutics Nov 2009, Vol. 11, No. 11: 711-715. (Source: Diabetes Technology)

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  Development and validation of an HPLC method for the simultaneous analysis of 23 selected drugs belonging to different therapeutic groups in human urine samples.

Authors: Baranowska I, Markowski P, Baranowski J We have developed and validated a new and reliable gradient reversed-phase high-performance liquid chromatography (RP-HPLC) method with a diode array detector (DAD) for the simultaneous separation and determination of 23 frequently prescribed selected drugs belonging to different therapeutic groups in human urine samples. For the drugs listed below, this method of analysis for human urine was also successfully applied to determine urine concentrations of these drugs in samples from treated patients: enalapril (ENA), paracetamol (PAR), sotalol (SOT), dipyrone (DIP), vancomycin (VAN), captopril (CAP), fluconazole (FLU), cefazolin (CEF), metoprolol (MET), aspirin (ASP), ticlopidine (TIC), prednisolone (PRE), propranolol (PRO), digoxin (DIG)...

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  ACE inhibition by astilbin isolated from Erythroxylum gonocladum (Mart.) O.E. Schulz

Abstract: Erythroxylum species have several traditional uses in different countries, including the treatment of hypertension. The ethanol extract from E. gonocladum aerial parts, a species endemic to the Brazilian cerrado, elicited a concentration-dependent inhibition of angiotensin converting enzyme (ACE) (pIC50=4.53±0.05). Extract fractionation led to the isolation of two compounds, whose structures were assigned by spectrometric data as astilbin and β-sitosterol, along with a mixture of palmitic, stearic and linolenic acids. This is the first report on the occurrence of these compounds on E. gonocladum. Astilbin promoted significant ACE inhibition in vitro (pIC50=5.86±0.33) and its activity did not differ from captopril, when both compounds were assayed at 10μM concentration. (Sourc...

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  Angiotensin II stimulates trafficking of NHE3, NaPi2 and associated proteins into the proximal tubule microvilli.

Authors: Riquier-Brison AD, Leong PK, Pihakaski-Maunsbach K, McDonough AA Angiotensin II (AngII) stimulates proximal tubule (PT) sodium and water reabsorption. We showed that treating rats acutely with the angiotensin converting enzyme inhibitor captopril decreases PT salt and water reabsorption and provokes rapid redistribution of the Na(+)/H(+) exchanger isoform 3 (NHE3), Na(+)/Pi co-transporter 2 (NaPi2) and associated proteins out of the microvilli. The aim of the present study was to determine whether acute AngII infusion increases the abundance of PT NHE3, NaPi2 and associated proteins in the microvilli available for reabsorbing NaCl. Male Sprague Dawley rats were infused with a dose of captopril (12mug/min for 20min) that increased PT flow rate ~20% with no change in blood press...

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  Solubility of Captopril in 2-Propanol, Acetone, Acetonitrile, Methyl Acetate, Ethyl Acetate, and Butyl Acetate

Journal of Chemical & Engineering Data, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable). (Source: Journal of Chemical and Engineering Data)

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  Clinical research Captopril and losartan modify mitogen-induced proliferative response and expression of some differentiation antigents on peripheral blood mononuclear cells in chronic uraemic patients

Conclusions: Our in vitro results seem to indicate that captopril and losartan interfere with immune cells and depress some functions of immune cells in chronic uremic patients and healthy subjects. It is very difficult at present to establish significance of these in vitro immunosuppresive effects of captopril and losartan reflects their in vivo action. Its significance for clinical implications necessitates further extensive studies. (Source: Articles of Archives of Medical Science - TERMEDIA publishing house)

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  CAPTOPRIL Tablet CAPTOPRIL (Captopril) Tablet [Apotex Corp.]

Updated Date: Oct 21, 2009 EST (Source: DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST))

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  Captopril-enhanced renal scintigraphy in the diagnosis of pediatric hypertension

Abstract  Hypertension in childhood is no longer a rare condition mainly secondary to renal, or renovascular diseases, as a growing proportion of children are obese and hypertensive, with the phenotype of metabolic syndrome. Thus, we need to reconsider our practice in the examination of the hypertensive child and redefine the place of non-invasive methods for screening of renovascular hypertension, and specifically, to evaluate the value of captopril-enhanced renal scintigraphy at the two ends of the palette: the obese child with hypertension and the severely hypertensive prepubertal child. Renal artery stenosis in children is mainly due to fibromuscular dysplasia and stenoses associated with syndromes involving single or multiple smaller branch vessels. This explains the l...

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  Med Sci Monit 2009; 15(11):BR334-338 "Influence of selected angiotensin-converting enzyme inhibitors on alloxan-induced diabetic cataract in rabbits"

Conclusions: ACEIs delay diabetic cataractogenesis in an experimental animal model. The ACEI functional groups have different influences on the pattern and rate of lens opacity. (Source: Medical Science Monitor)

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  Pharmacodynamic interaction of captopril with garlic in isoproterenol-induced myocardial damage in rat

It is known that various preparations of garlic and angiotensin-converting enzyme (ACE) inhibitor such as captopril (CAP) have beneficial effects on the left ventricular function and cardiovascular events after myocardial infarction (MI) when used individually. There is no reported interaction between garlic homogenate (GH) and CAP during and after acute MI. Thus the purpose of the current study was to evaluate the possible pharmacodynamic interaction of GH with CAP on isoproterenol (ISO)-induced myocardial damage in rat. Female Wistar albino rats were treated with GH at three different doses of 125; 250 and 500 mg/kg orally for 30 days and CAP (30 mg/kg, p.o.) was incorporated in the interactive groups during the last seven days of GH treatment. Myocardial damage was induced by administra...

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  Sardine Peptide with Angiotensin I-Converting Enzyme Inhibitory Activity Improves Glucose Tolerance in Stroke-Prone Spontaneously Hypertensive Rats.

Authors: Otani L, Ninomiya T, Murakami M, Osajima K, Kato H, Murakami T An enzymatic hydrolysate of sardine protein (sardine peptide, SP) derived from sardine muscle possesses angiotensin I-converting enzyme (ACE) inhibitory activity. In the present study, we investigated the effect of SP on the blood glucose levels in stroke-prone spontaneously hypertensive rats (SHRSPs). Ten-week-old SHRSPs were assigned to three groups. The control group was given tap water for 4 weeks, while the experimental groups were given water containing SP (1 g/kg/d) or an ACE inhibitor, captopril (8 g/kg/d). Treatment with SP and captopril decreased ACE activity in the kidney, aorta, and mesentery. There were no differences in fasting blood glucose levels among the three groups, whereas SP and captopril admi...

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  The effectiveness of Hibiscus sabdariffa in the treatment of hypertension: A systematic review

The objectives of this review were to examine the evidence of effectiveness and safety of hibiscus in the treatment of hypertension.Methods: We searched several medical databases (MEDLINE, EMBASE, CINAHL, Cochrane Central Register of Controlled Trials, and the specialized register of the Cochrane Hypertension Group and the general engine Google) to January 2009.We included randomized controlled trials that had examined Hibiscus's effectiveness and safety in the treatment of primary hypertension in adults. Two authors independently selected the trials for the review, extracted the data, and critically appraised the included studies.Results: Four trials, with a total of 390 patients, met our inclusion criteria. Two studies compared Hibiscus sabdariffa to black tea; one study compared it to c...

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  Chemiluminescence spectra for the oxidation of sulphite in the presence of fluorescent and non-fluorescent enhancers.

Authors: Adcock JL, Francis PS, Barnett NW The spectral distribution of chemiluminescence provides key evidence in the elucidation of the reaction mechanism and emitting species. We have collected chemiluminescence spectra for the oxidation of sodium sulphite and captopril in the presence of a range of fluorescent and non-fluorescent enhancers. This evidence was used to evaluate several previously proposed light-producing pathways, and revealed some new approaches to enhance the chemiluminescent oxidation of sulphite and thiol compounds. Chemiluminescence reactions between sulphite and permanganate produce two potential emitters: one derived from the oxidation of sulphite (in some cases via energy transfer to a more efficient luminophore) and another derived from the reduction of perma...

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  Differences between99mTc-DTPA and99mTc-MAG3 captopril renographies in renovascular hypertension

Abstract  Captopril renography (CRS) with99mTc-DTPA and99mTc-MAG3 was performed on a 21-year-old woman with renovascular hypertension due to right renal artery stenosis caused by fibromuscular dysplasia. In the affected kidney, the renogram pattern was substantially changed with99mTc-DTPA and99mTc-MAG3 following the administration of captopril, and the quantitated renal uptake indicating individual renal function was significantly decreased in99mTc-DTPA and slightly decreased in99mTc-MAG3. In the contralateral normal kidney, the renogram showed some minor changes with both radioagents, while the quantitated renal uptake was significantly decreased with99mTc-DTPA and substantially increased with99mTc-MAG3. The combined use of physiologically different renal agents99mTc-DTPA and...

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  Variable kidney position mimicking renal artery branch stenosis in a Tc-99m-DTPA captopril scintigraphy

Abstract  Tc-99m-DTPA captopril scintigraphy was performed in a patient with suspected renovascular hypertension. Markedly impaired right renal function (Glomerular filtration rate (GFR) values for the right kidney = 14 ml/min, left kidney = 79 ml/min) was detected in the initial captopril study. Only lower pole activity of the right kidney was observed during the whole study. Since prior ultrasonographic examinations have shown bilateral normal kidney parenchyma, branch stenosis of the right upper pole was suspected. Besides significant function improvement in the following baseline study (GFR values for the right kidney = 59 ml/min, left kidney = 79 ml/min), the right kidney, this time normally shaped, was visibly higher positioned. Because of the possibility of mobile ki...

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  Contact dermatitis to captopril

(Source: Contact Dermatitis)

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  Long-term stability of extemporaneously prepared captopril oral liquids in glass bottles.

CONCLUSION: Extemporaneously prepared oral liquid formulations of captopril 1 and 5 mg/mL were chemically stable when stored in glass bottles at room temperature for 12 months when stabilized with 0.1 mg/ mL disodium edetate at a low pH. PMID: 19767378 [PubMed - as supplied by publisher] (Source: American Journal of Health-System Pharmacy : AJHP)

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  Capozide (hydrochlorothiazide/ captopril) LS Tablets - Product discontinued

Source: eMC (electronic Medicines Compendium) Area: Other Library Updates > SPC Changes Capozide (hydrochlorothiazide/ captopril) LS tablets from ER Squibb have been discontinued. (Source: NeLM - Cardiovascular Medicine)

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  Synthesis, Synchrotron X-ray Diffraction, and Kinetic Studies on the Formation of a Novel Thiolatocobalamin of Captopril: Evidence for cis-trans Isomerization in the β-Axial Ligand

Inorganic Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable). (Source: Inorganic Chemistry)

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  Non-NMDA receptors in the lateral parabrachial nucleus modulate sodium appetite.

Authors: De Gobbi JI, Beltz TG, Johnson RF, Menani JV, Thunhorst RL, Johnson AK Glutamatergic mechanisms have been implicated in the control of fluid ingestion. In the present study, we investigated whether non-N-methyl-D-aspartate (NMDA) glutamatergic receptors in the lateral parabrachial nucleus (LPBN) are involved in the control of water and sodium intake. Male Sprague-Dawley rats had cannulas implanted bilaterally into the LPBN. They were acutely depleted of water and sodium by injections of the diuretic furosemide (Furo; 10 mg/kg, bw) and a low dose of the angiotensin-converting enzyme inhibitor, captopril (Cap; 5 mg/kg, bw). Bilateral LPBN injections of the non-NMDA receptor antagonist DNQX (2 and 5 nmol/0.2 mul) increased the ingestion of 0.3 M NaCl and water of Furo/Cap treated...

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  Secondary prevention of ischaemic cardiac events

New evidence; conclusions changed for: Anticoagulants in addition to antiplatelet treatments: Two systematic reviews added comparing intensive warfarin plus aspirin versus aspirin alone. Both reviews found that warfarin plus aspirin decreased the risk of non-fatal MI and stroke, but increased the risk of major bleeding compared with aspirin alone in people with acute coronary syndrome. The evidence supports the recategorisation from Likely to be ineffective or harmful to Trade-off between benefits and harms. Fish oil consumption (from oily fish or capsules): Two systematic reviews added comparing advice to increase fish oil consumption or fish oil consumption versus control. The reviews found that increased fish oil consumptio...

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  Production and Secretion of Adiponectin from 3T3-L1 Adipocytes: Comparison of Antihypertensive Drugs.

ConclusionIn this comparative model, telmisartan, and to a lesser extent, losartan, increased production and secretion of adiponectin from 3T3-L1 adipocytes compared to the other antihypertensive drugs.American Journal of Hypertension 2009; doi:10.1038/ajh.2009.171. PMID: 19730415 [PubMed - as supplied by publisher] (Source: American Journal of Hypertension)

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  Catalytic properties of recombinant dipeptidyl carboxypeptidase from Escherichia coli: a comparative study with angiotensin I-converting enzyme

Biological Chemistry 390 (9): 931-940 Abstract Dipeptidyl carboxypeptidase from Escherichia coli (EcDcp) is a zinc metallopeptidase with catalytic properties closely resembling those of angiotensin I-converting enzyme (ACE). However, EcDcp and ACE are classified in different enzyme families (M3 and M2, respectively) due to differences in their primary sequences. We cloned and expressed EcDcp and studied in detail the enzyme's S3 to S1′ substrate specificity using positional-scanning synthetic combinatorial (PS-SC) libraries of fluorescence resonance energy transfer (FRET) peptides. These peptides contain ortho-aminobenzoic acid (Abz) and 2,4-dinitrophenyl (Dnp) as donor/acceptor pair. In addition, using FRET substrates developed for ACE [Abz-FRK(Dnp)P-OH, Abz-SDK(Dnp)P-OH and Abz-LFK(Dnp...

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  Effects of microinjection of angiotensin II and captopril to VTA on morphine self-administration in rats.

This study suggests the probable interaction between Ang II and opioid system in the VTA. PMID: 19700383 [PubMed - in process] (Source: Acta Biologica Hungarica)

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  Captopril: Exacerbation of Parkinson's disease in an elderly patient: case report

(Source: Reactions)

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  Captopril: Lichenoid eruption in an elderly patient: case report

(Source: Reactions)

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  Inhibition of intracellular Angiotensin II formation blocks high glucose effect on mesangial matrix.

Authors: Singh R, Choubey D, Chen J, Leehey DJ High glucose causes increased matrix synthesis by glomerular mesangial cells and angiotensin II (Ang II) has been shown to mediate this effect of glucose. These studies investigate whether inhibition of Ang II formation can block high glucose-induced increase in mesangial matrix. Human mesangial cells were incubated with 25mM glucose (HG) along with captopril, an ACE inhibitor to block Ang II formation. In other experiments, cells were nucleofected with siRNA to knockdown angiotensinogen (Agt), the precursor of Ang II, and then exposed to high glucose. Captopril blocked high glucose-induced increase in Ang II levels in the cell media (extracellular) but failed to inhibit it in the cell lysate (intracellular). Moreover, captopril treatment ...

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  Evaluation of lipid profile in diabetic and hypertensive patients treated with captopryl

INTRODUÇÃO E JUSTIFICATIVA: Doença arterial coronariana (DAC) é a principal causa mundial de morte em indivíduos adultos, e como importantes fatores de risco tratáveis envolvidos estão o diabetes mellitus (DM), as dislipidemias e a hipertensão arterial sistêmica (HAS). O tratamento com anti-hipertensivos pode provocar alterações indesejáveis no perfil lipídico, atenuando seus efeitos benéficos antiaterogênicos na redução da pressão arterial (PA). OBJETIVO: Avaliar o perfil lipídico de indivíduos diabéticos tipo 2 com hipertensão essencial tratados somente com captopril ou em combinação com outros anti-hipertensivos, procurando evidenciar a melhora no padrão lipídico destes pacientes, levando a efeito protetor. MATERIAL E MÉTODOS: Foram avaliados níveis de colest...

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  Combination of Captopril and Allopurinol Retards Fructose-Induced Metabolic Syndrome.

Conclusion: A high fructose diet can induce metabolic syndrome even in the setting of caloric restriction. Captopril and allopurinol synergistically reduce features of the metabolic syndrome, especially hypertension, insulin resistance and dyslipidemia. Combination allopurinol and ACE inhibitor therapy might provide a superior means to prevent diabetes and cardiovascular disease. PMID: 19696478 [PubMed - as supplied by publisher] (Source: American Journal of Nephrology)

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  Effect of chronic pre-treatment with angiotensin converting enzyme inhibition on skeletal muscle mitochondrial recovery after ischemia/reperfusion

Impaired skeletal muscle energetic participates in peripheral arterial disease (PAD) patient's morbidity and mortality. Angiotensin converting enzyme inhibition (ACEi), cornerstone for pharmacologic risk factor management in PAD patients, might also be interesting by protecting skeletal muscle energetic. We therefore determined whether chronic ACEi might reduce ischemia-induced mitochondrial respiratory chain dysfunction in the frequent setting of hindlimb ischemia[ndash]reperfusion. Ischemic legs of rats submitted to 5 h ischemia induced by a rubber band tourniquet applied on the root of the hindlimb followed by reperfusion without (IR, n = 11) or after ACEi (n = 14; captopril 40 mg/kg per day during 28 days before surgery) were studied and compared to that of sham-operated animals (n = 1...

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  Combinational chelation therapy abrogates lead induced neurodegeneration in rats.

Authors: Pachauri V, Saxena G, Mehta A, Mishra D, Flora SJ 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, 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...

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  Implantation of a three-dimensional fibroblast matrix improves left ventricular function and blood flow after acute myocardial infarction.

This study was designed to determine if a viable biodegradable three-dimensional fibroblast construct (3DFC) patch implanted on the left ventricle after myocardial infarction (MI) improves left ventricular (LV) function and blood flow. We ligated the left coronary artery of adult male Sprague-Dawley rats and implanted the 3DFC at the time of the infarct. Three weeks after MI, the 3DFC improved LV systolic function by increasing (p < 0.05) ejection fraction (37 +/- 3% to 62 +/- 5%), increasing regional systolic displacement of the infarcted wall (0.04 +/- 0.02 to 0.11 +/- 0.03 cm), and shifting the passive LV diastolic pressure volume relationship toward the pressure axis. The 3FDC improved LV remodeling by decreasing (p < 0.05) LV end-systolic and end-diastolic diameters with no chan...

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  Effect of different vasodilators on NTPDase activity in healthy and hypertensive patients

Conclusion: It is postulated that there was an interaction between vasodilators, NO donors and inhibition of NTPDase. (Source: Thrombosis Research)

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

Authors: Vancea S, Imre S, Donáth-Nagy G, Béla T, Nyulas M, Muntean T, Borka-Balás R 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 tra...

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  Rapid analysis of captopril in human plasma and pharmaceutical preparations by headspace solid phase microextraction based on polypyrrole film coupled to ion mobility spectrometry.

Authors: Karimi A, Alizadeh N A rapid, simple, and sensitive headspace solid phase microextraction coupled to ion mobility spectrometry (HS-SPME-IMS) method is presented for analysis of the highly specific angiotensin-converting enzyme (ACE) inhibitor, captopril (CAP). Positive ion mobility spectra of CAP were acquired with an ion mobility spectrometer equipped with a corona discharge ionization source. Mass-to-mobility correlation equation was used to identify product ions. A dodecylsulfate-doped polypyrrole (PPy-DS) coating was used as a fiber for SPME. The results showed that PPy-DS based SPME fiber was suitable for successfully extracting CAP from human blood plasma and pharmaceutical samples. The HS-SPME-IMS method provided good repeatability (R.S.D.s<4%) for aqueous and spiked...

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  Captopril: Angioedema in an elderly patient: case report

(Source: Reactions)

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  Preservation and Modulation of Peritoneal Function. A Potential Role of Pyruvate and Betaine.

Conclusions: Efforts focused in improving the dialyzing capabilities of the peritoneal membrane by means of pharmacological manipulation, have not yet offered clinically relevant innovations. Conversely, interventions designed to preserve the peritoneum as a reusable dialyzing living membrane are more promising, especially those aimed at neutralizing oxidative and osmotic injury. PMID: 19494598 [PubMed - as supplied by publisher] (Source: Contributions to Nephrology)

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  Captopril: Angioedema in an elderly patient: case report.

Page: 9 (Source: Reactions Weekly)

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  Captopril/imipenem: Linear IgA bullous dermatosis in an elderly patient: case report

(Source: Reactions)

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  Captopril/imipenem: Linear IgA bullous dermatosis in an elderly patient: case report.

Page: 11 (Source: Reactions Weekly)

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  Inhibition of renin-angiotensin system in experimental acute pancreatitis in rats: A new therapeutic target?

CONCLUSIONS: This study not only demonstrated the differential effects of captopril, losartan and L-158809 in acute pancreatitis but also showed that there is still much to investigate about pancreatic renin-angiotensin system. Inhibition of angiotensin-converting enzyme should be evaluated carefully as a potential new therapeutic target in acute pancreatitis. PMID: 19525099 [PubMed - as supplied by publisher] (Source: Experimental and Toxicologic Pathology)

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  Usefulness of Beta Blockers in High-Risk Patients After Myocardial Infarction in Conjunction With Captopril and/or Valsartan (from the VALsartan In Acute Myocardial Infarction [VALIANT] Trial)

In conclusion, no evidence was found of adverse interactions between the angiotensin-receptor blocker valsartan and β blockers or of a negative effect of the combination of valsartan, captopril, and β blockers. (Source: The American Journal of Cardiology)

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  Synergistic decrease in blood pressure by captopril combined with losartan in spontaneous hypertensive rats.

This study was designed to examine the anti-hypertensive effect of the combination therapy of captopril with losartan by oral administration using both independent and cross-over experimental protocols. In independent experimental protocols, four different groups of spontaneous hypertensive rats (SHR) were treated for 1 or 2 weeks: control, captopril (20 mg/kg/day), losartan (20 mg/kg/day), and combination captopril (10 mg/kg/day) with losartan (10 mg/kg/day). In cross-over protocols, each SHR received all four treatments for 1 or 3 days with an interval of several days between each injection for washing-out and return to high blood pressure (BP) levels. BP and heart rate (HR) were measured in conscious telemetered SHR. According to the results from the independent protocol, regardless of ...

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  Involvement of central angiotensin II type 1 receptors in LPS-induced systemic vasopressin release and blood pressure regulation in rats

The purpose of this study was to evaluate the involvement of central angiotensin II (ANG II) and ANG II type 1 (AT1) receptors in systemic release of arginine vasopressin (AVP) and blood pressure regulation during endotoxemia. LPS (150 µg/kg) was injected intravenously 30 min after intracerebroventricular (icv) losartan (50 µg), an AT1 receptor antagonist, or subcutaneous (sc) captopril (50 mg/kg), an angiotensin-converting enzyme inhibitor. Rats with icv and sc saline injections served as control. LPS administration increased plasma AVP concentration from 2.1 ± 0.2 to 15.2 ± 2.5 pg/ml (60 min after LPS injection) without significant changes in plasma osmolality or hematocrit. LPS-induced AVP secretion was significantly attenuated by pretreatment with icv losartan...

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

Authors: Medvedovici A, Albu F, Sora ID, Udrescu S, Galaon T, David V 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 ...

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  Induction of apoptosis in leukemic cell lines treated with captopril, trandolapril and losartan: A new role in the treatment of leukaemia for these agents

Abstract: Renin–angiotensin system (RAS) in the bone marrow is related to proliferation and cellular differentiation. We investigated the effect of ACE inhibitors (ACEI) captopril (>1mM) and trandolapril (>0.05mM) and losartan (0.2mM) on K562 cell line and K562 transfected with c-myc, bcl-x and bcl-2 (KmycB, Kbclx and Kbcl2 respectively). RAS components, proliferation, apoptosis and c-myc expression were analyzed. ACEI and losartan inhibited cell growth, decreased c-myc expression and increased apoptosis. These effects seem to be associated to angiotensin II-induced Smad activation. This work offers a new possible line of treatment for some acute myeloid leukemias and a new area of clinical research. (Source: Leukemia Research)

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  Regulation of Oxygen Utilization by Angiotensin II in Chronic Kidney Disease

Angiotensin II blockade effects on renal oxygen consumption are measured with captopril and losartan on board to determine what underlies the angiotensin II blockade benefit - besides hemodynamics? Kidney International (Source: Medscape Urology Headlines)

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  Contrasting effects of steroids and angiotensin-converting-enzyme inhibitors in a mouse model of dystrophin-deficient cardiomyopathy

Conclusion In a mouse model of dystrophin-deficient cardiomyopathy, ACE-I produced haemodynamic benefit, whereas steroids accelerated progression of cardiomyopathy. Although mouse models may not entirely replicate the human condition, comprehensive monitoring of cardiac function with these therapies is essential. (Source: European Journal of Heart Failure)

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  Role of symmetric dimethylarginine in vascular damage by increasing ROS via store-operated calcium influx in monocytes

Conclusions. SDMA, a uraemic retention solute considered inert, stimulates ROS production of monocytes by acting on Ca2+ entry via SOCs. This pro-inflammatory effect may trigger vascular pathology and may be involved in altering the prevalence of cardiovascular disease in CKD. (Source: Nephrology Dialysis Transplantation)

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  Effects of three vasoactive peptides isolated from the plasma of the snake Bothrops jararaca.

Effects of three vasoactive peptides isolated from the plasma of the snake Bothrops jararaca. Comp Biochem Physiol C Toxicol Pharmacol. 2009 May;149(4):552-8 Authors: Barreto SA, Chaguri LC, Prezoto BC, Lebrun I Incubation of plasma from the snake Bothrops jararaca (BJP) with trypsin generated two hypotensive peptides. The primary structure of the peptides was established for three sequences as: Asn-Pro-Phe-Val-Asp-Ala (fraction 13), Ser-Lys-Pro-Asn-Met-Ser-Asp-Glu-Ser-Leu-Ala-Val-Ala-Ile (fraction 14), Asn-Pro-Phe- Val-Asp-Ala (fraction 15). These peptides display homology with fragments of albumin from Trimeresurus flavoviridis. A bolus intra-arterial injection of the purified or the synthetic peptide produced a strong and sustained vasopressor response in the anaesthetized s...

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  Implantation of a 3-dimensional fibroblast matrix improves left ventricular function and blood flow after acute myocardial infarction.

CONCLUSION: This biodegradable 3DFC patch improves LV function and myocardial blood flow 3 weeks after MI. This is a potentially new approach to cell-based therapy for heart failure after MI. PMID: 19500469 [PubMed - as supplied by publisher] (Source: Cell Transplantation)

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  FDA Safety Changes: Luvox/Luvox CR, Altace, Capozide, Monopril/Monopril HCT, Furadantin

The FDA has approved revisions to the safety labeling for fluvoxamine, ramipril, captopril plus hydrochlorothiazide, fosinopril, fosinopril plus hydrochlorothiazide, and nitrofurantoin. Medscape Medical News (Source: Medscape PublicHealth Headlines)

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  FDA Safety Changes: Luvox/Luvox CR, Altace, Capozide, Monopril/Monopril HCT, Furadantin

The FDA has approved revisions to the safety labeling for fluvoxamine, ramipril, captopril plus hydrochlorothiazide, fosinopril, fosinopril plus hydrochlorothiazide, and nitrofurantoin. Medscape Medical News (Source: Medscape Today Headlines)

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  Captopril induced hyperkalemia in a child.

Authors: Sunder RA, Rakesh G, Rudingwa P, Chanderlekha PMID: 19335351 [PubMed - in process] (Source: Paediatric Anaesthesia)

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  Acute hypertension provokes acute trafficking of distal tubule Na-Cl cotransporter (NCC) to subapical cytoplasmic vesicles

When blood pressure (BP) is elevated above baseline, a pressure natriuresis-diuresis response ensues, critical to volume and BP homeostasis. Distal convoluted tubule Na+-Cl– cotransporter (NCC) is regulated by trafficking between the apical plasma membrane (APM) and subapical cytoplasmic vesicles (SCV). We aimed to determine whether NCC trafficking contributes to pressure diuresis by decreasing APM NCC or compensates for increased volume flow to the DCT by increasing APM NCC. BP was raised 50 mmHg (high BP) in rats by arterial constriction for 5 or 20–30 min, provoking a 10-fold diuresis at both times. Kidneys were excised, and NCC subcellular distribution was analyzed by 1) sorbitol density gradient fractionation and immunoblotting and 2) immunoelectron microscopy (immuno-EM)....

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  Angiotensin II Activates IκB Kinase Phosphorylation of RelA at Ser536 to Promote Myofibroblast Survival and Liver Fibrosis

Conclusions: An autocrine pathway that includes angiotensin II, IKK, and P-Ser536-RelA regulates myofibroblast survival and can be targeted to stimulate therapeutic regression of liver fibrosis. (Source: Gastroenterology)

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  Angiotensin II activates I?B kinase phosphorylation of RelA at Ser536 to promote myofibroblast survival and liver fibrosis.

CONCLUSIONS:: An autocrine pathway that includes angiotensin II, IKK and P-Ser536-RelA regulates myofibroblast survival and can be targeted to stimulate therapeutic regression of liver fibrosis. PMID: 19303015 [PubMed - as supplied by publisher] (Source: Gastroenterology)

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  Impact of renin-angiotensin system polymorphisms on renal haemodynamic responsiveness to acute angiotensin-converting enzyme inhibition in type 2 diabetes mellitus

Conclusions. Our data indicate that the heterogeneity of patients' response to ACE inhibition is, at least partly, genetically determined, and the genetic polymorphisms in RAS might predict the acute responsiveness to ACE inhibitors. (Source: Journal of the Renin-Angiotensin-Aldosterone System : JRAAS)

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  captopril, Capoten

Title: captopril, CapotenCategory: MedicationsCreated: 12/31/1997Last Editorial Review: 3/12/2009 (Source: MedicineNet High Blood Pressure General)

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  Gene profiling of left ventricle eccentric hypertrophy in aortic regurgitation in rats: rationale for targeting the {beta}-adrenergic and renin-angiotensin systems

Aortic valve regurgitation (AR) imposes a severe volume overload to the left ventricle (LV), which results in dilation, eccentric hypertrophy, and eventually loss of function. Little is known about the impact of AR on LV gene expression. We, therefore, conducted a gene expression profiling study in the LV of rats with acute and severe AR. We identified 64 genes that were specifically upregulated and 29 that were downregulated out of 21,910 genes after 2 wk. Of the upregulated genes, a good proportion was related to the extracellular matrix. We subsequently studied a subset of 19 genes by quantitative RT-PCR (qRT-PCR) to see if the modulation seen in the LV after 2 wk persisted in the chronic phase (after 6 and 12 mo) and found that it did persist. Knowing that the adrenergic and renin-angi...

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  Lack of interaction between the peptidomimetic substrates captopril and cephradine.

Authors: Foster DR, Yee S, Bleske BE, Carver PL, Shea MJ, Menon SS, Ramachandran C, Welage LS, Amidon GL Intestinal peptide transporters, including hPEPT1, facilitate the absorption of cephalosporins and angiotensin-converting enzyme inhibitors, and have been investigated as a means to improve oral drug absorption. Renal peptide transporters including hPEPT2, may also facilitate renal reabsorption of such compounds. In vitro and animal studies suggest that co-administration of peptidomimetic compounds may alter oral pharmacokinetics, although this has not been well studied in humans. The purpose of this study was to determine whether co-administration of the hPEPT substrates captopril and cephradine alters the oral pharmacokinetics of either agent. Nine healthy male volunteers received...

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  Study of the acute cardiovascular effects of several antihypertensive agents with the measurement of plasma catecholamines in mice.

In this study, the method was applied to mouse plasma, and it was determined that only 10 mul of mouse plasma was necessary for the selective and reproducible determination of catecholamines. Studies were then conducted in acute cardiovascular effects of sodium nitroprusside, nicardipine, captopril (angiotensin-converting enzyme (ACE) inhibitor), candesartan, and olmesartan (type 1 angiotensin receptor antagonists (AT(1) antagonists)) by this method. Sodium nitroprusside and nicardipine elevated plasma NE concentrations significantly, whereas the ACE inhibitor and the AT(1) antagonists did not change plasma NE concentrations in anesthetized mice. These results suggested that angiotensin II-induced augmentation may be mainly carried through the central baroreflex pathway. PMID: 19234691...

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  Reno-prevention vs. reno-protection: a critical re-appraisal of the evidence-base from the large RAAS blockade trials after ontarget--a call for more circumspection

The ACEI, captopril was introduced into clinical medicine in the early 1970s for hypertension. Other ACEIs and the ARBs were introduced subsequently. Following several RAAS blockade trials, we now have an expanded set of clinical indications for these agents. Despite the escalated use of these agents, we continue to experience an unexplained epidemic of ESRD/CKD/ARF. There are concerns regarding potential iatrogenic renal failure arising from these agents. A case, it would appear, of unintended consequences. Our publication of several reports on the previously unrecognized syndrome of late onset renal failure from angiotensin blockade (LORFFAB) in 2008 adds to this evolving literature. At the same time, some recent reports have questioned the veracity of claims of superior reno-protection ...

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  Study on effect of astragalus on left ventricular collagen remodeling after myocardial infarction in rats

Conclusion: Astragalus is effective in lowering the elevation of MC after infarction and changing the MC I /H ratio, therefore, is beneficial to improve the systolic and diastolic function of left ventricle after acute myocardial infarction. Content Type Journal ArticleCategory Experimental Work and ResearchDOI 10.1007/BF02970586Authors Haiming Shi, Shanghai Medical University Cardiac Division, Huashan Hospital (200040) ShanghaiXingping Luo, Shanghai Medical University Cardiac Division, Huashan Hospital (200040) ShanghaiZhiyu Zeng, Shanghai Medical University Cardiac Division, Huashan Hospital (200040) ShanghaiWeihu Fan, Shanghai Medical University Cardiac Division, Huashan Hospital (200040) ShanghaiRuihong Dai, Shanghai Medical University Cardiac Division, Huashan Hospital (200040) ...

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

Altaf M A, Sreedharan, Charyulu NIndian Journal of Pharmaceutical Sciences 2008 70(5):655-658A new oral drug delivery system was developed utilizing both the concepts of controlled release and mucoadhesiveness, in order to obtain a unique drug delivery system which could remain in stomach and control the drug release for longer period of time. Captopril microcapsules were prepared with a coat consisting of alginate and a mucoadhesive polymer such as hydroxy propyl methyl cellulose, carbopol 934p, chitosan and cellulose acetate phthalate using emulsification ionic gelation process. The resulting microcapsules were discrete, large, spherical and free flowing. Microencapsulation efficiency was 41.7-89.7% and high percentage efficiency was observed with (9:1) alginate-chitosan microcaps...

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

Altaf M A, Sreedharan, Charyulu NIndian Journal of Pharmaceutical Sciences 2008 70(5):545-548A new oral drug delivery system was developed utilizing both the concepts of controlled release and mucoadhesiveness, in order to obtain a unique drug delivery system which could remain in stomach and control the drug release for longer period of time. Captopril microcapsules were prepared with a coat consisting of alginate and a mucoadhesive polymer such as hydroxy propyl methyl cellulose, carbopol 934p, chitosan and cellulose acetate phthalate using emulsification ionic gelation process. The resulting microcapsules were discrete, large, spherical and free flowing. Microencapsulation efficiency was 41.7-89.7% and high percentage efficiency was observed with (9:1) alginate-chitosan microcaps...

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  Inhibition of brain renin-angiotensin system improved diastolic cardiac function following myocardial infarction in rats.

Authors: Araujo IG, de Castro Trindade D, Mecawi AS, Sonoda-Côrtes R, Werneck-de-Castro JP, Costa-E-Sousa RH, Reis LC, Olivares EL 1. We have recently demonstrated that oral captopril treatment improved diastolic function and attenuated cardiac remodeling after myocardial infarction in rats. Considering the feasible role of brain renin-angiotensin system (RAS) in heart failure, herein we studied the role of the captopril injected intracerebroventricularly (i.c.v.) on progression of cardiac dysfunction. 2. Male Wistar rats underwent experimental myocardial infarction (MI) or sham-operation. Infarcted animals received daily i.c.v. injection of captopril (~200 micrograms/Kg, MI + Cap) or saline (MI) between 11d and 18d post-infarction. Electro and echocardiogram assessments were made...

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  A case of Parkinson's disease worsened by captopril: An unexpected adverse effect

No abstract. (Source: Movement Disorders)

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  Molecular Imaging for Efficacy of Pharmacologic Intervention in Myocardial Remodeling

Conclusions Radiolabeled CRIP allows for the evaluation of the efficacy of neurohumoral antagonists after MI and reconfirms superiority of combination therapy. If proven clinically, molecular imaging of the myocardial healing process may help plan an optimal treatment for patients susceptible to heart failure. (Source: Journal of the American College of Cardiology: Cardiovascular Imaging)

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  Hemodynamic effects of benazepril, an angiotensin-converting enzyme inhibitor, as studied in conscious normotensive dogs

Summary  Hemodynamic effects and inhibitory effects on the pressor response to exogenous angiotensin I of benazepril (CGS 14824A), a new angiotensin-converting enzyme (ACE) inhibitor, were examined in conscious chronically instrumented normotensive dogs in comparison with those of captorpil. Oral administration of benazepril (1–10 mg/kg) and captopril (3 and 10 mg/kg) reduced the blood pressure and inhibited the pressor response to angiotensin I dose-dependently. The blood-pressure-lowering effect of benazepril was as potent as that of captopril. The onset of effects of benazepril was slower and the duration longer than that of captopril. There was no close correlation between the attenuation of pressor response to exogenous angiotensin I and the blood-pressure-lowering e...

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  Determination and Applications of the Molar Absorptivity of Phenolic Adducts with Captopril and Mesna

Journal of Agricultural and Food Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable). (Source: Journal of Agricultural and Food Chemistry)

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  Effect of different vasodilators on NTPDase activity in healthy and hypertensive patients.

CONCLUSION: It is postulated that there was an interaction between vasodilators, NO donors and inhibition of NTPDase. PMID: 19174306 [PubMed - as supplied by publisher] (Source: Thrombosis Research)

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  Prediction of renal impairment in elderly patients with congestive heart failure treated with captopril

This study assessed the usefulness of the oral captopril test in the prediction of renal impairment among elderly patients with congestive heart failure (CHF). Fortyseven patients aged ≥65 years with CHF (EF <40%) participated in a prospective nonrandomized series. Blood samples for plasma renin activity (PRA) were drawn before and 60 minutes after 50 mg of oral captopril. Twenty-four hours later, captopril was administered (up to 75 mg/day over a 4 day period), and renal laboratory and clinical assessment were performed at baseline and for a 9 day period. In 7 of 47 patients (14.9%), deterioration of renal function was observed. During the captopril test, the PRA increased significantly after 1 hour in almost all patients and the mean blood pressure decreased from 99.2±14.6 mm...

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  Acute hypertension provokes acute trafficking of distal tubule Na-Cl- co-transporter (NCC) to subapical cytoplasmic vesicles.

Authors: Lee DH, Riquier AD, Yang LE, Leong PK, Maunsbach AB, McDonough AA When blood pressure (BP) is elevated above baseline, a pressure natriuresis-diuresis response ensues, critical to volume and BP homeostasis. Distal convoluted tubule Na(+)-Cl(-) cotransporter (NCC) is regulated by trafficking between apical plasma membrane (APM) and sub-apical cytoplasmic vesicles (SCV). We aimed to determine whether NCC trafficking contributes to pressure diuresis by decreasing APM NCC or compensates for increased volume flow to the DCT by increasing APM NCC. BP was raised 50 mmHg (high BP) in rats by arterial constriction for 5 or 20-30 min provoking a 10 fold diuresis at both times. Kidneys were excised and NCC subcellular distribution analyzed by: 1) sorbitol density gradient fractionation a...

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  Synthesis of N -[3′-(acetylthio)alkanoyl] and N -[3′-mercaptoalkanoyl]-4-α(s)-(phenylmethyl) pyroglutamic acids and prolines as potent ACE inhibitors

Abstract  Angiotensin converting enzyme (ACE) inhibitors have emerged as a revolution in antihypertensive therapy. Introduction of captopril, the first rationally designed ACE inhibitor, has encouraged researchers all over the world to design and synthesize target molecules controlling hypertension based on these lines. It has been observed that replacing proline part of captopril with 4-substituted prolines or 5-oxo-prolines led to significant enhancement in ACE inhibitory activity, and this observation prompted us to design and synthesize N-acyl 4-substituted pyroglutamates and prolinates with the objective of developing therapeutically better ACE inhibitors. Herein we describe an easy approach for N-acylation of 4-α(S)-(phenylmethyl) pyroglutamates with the aim of synthe...

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  Chronic angiotensin-converting enzyme inhibition up-regulates mouse kidney growth arrest specific-6 protein and the AXL subfamily of receptor tyrosine kinases

Conclusions. These findings suggest that GAS-6 may not be a final common pathway for nitric oxide synthase inhibition-induced renal disease. Renal tubular GAS-6 expression following captopril treatment was unexpected and could be beneficial in preventing tubular atrophy following the onset of persistent systemic hypertension. (Source: Journal of the Renin-Angiotensin-Aldosterone System : JRAAS)

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  Gene profiling of left ventricle eccentric hypertrophy in aortic regurgitation in rats: rationale for targeting the {beta}-adrenergic and renin-angiotensin systems.

Authors: Champetier S, Bojmehrani A, Beaudoin J, Lachance D, Plante E, Roussel E, Couet J, Arsenault M Aortic valve regurgitation (AR) imposes a severe volume overload to the left ventricle (LV) which results in dilation, eccentric hypertrophy and eventually loss of function. Little is known about the impact of AR on LV gene expression. We therefore conducted a gene expression profiling study in the LV of rats with acute and severe AR. We identified 64 genes that were specifically up-regulated and 29 that were down-regulated out of 21910 genes after 2 weeks. Of the up-regulated genes, a good proportion was related to the extracellular matrix. We subsequently studied a subset of 19 genes by quantitative RT-PCR (qRT-PCR) to see if the modulation seen in the LV after two weeks persisted i...

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  Albumin caused the increasing production of angiotensin II due to the dysregulation of ACE/ACE2 expression in HK2 cells.

CONCLUSION: These findings suggested a novel insight on the albuminuria induced activation of intrarenal RAS by upregulation of ACE and downregulation of ACE2. PMID: 19141296 [PubMed - as supplied by publisher] (Source: International Journal of Clinical Chemistry)

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  Erythropoietin levels in heart failure after an acute myocardial infarction: determinants, prognostic value, and the effects of captopril versus losartan.

CONCLUSION: In this substudy of the OPTIMAAL trial, the correlation between Epo and hemoglobin disappeared in early post-acute myocardial infarction heart failure patients. Furthermore, elevated Epo levels at baseline predicted increased mortality. PMID: 19081402 [PubMed - in process] (Source: American Heart Journal)

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  Superiority of Tc-99m MAG3 to Tc-99m DTPA in treating a patient with mild renal artery stenosis

Abstract  A 22-year-old female patient with severe hypertension underwent both Technetium-99m diethylenetriaminepentaacetate and Technetium-99m mercaptoacetyltriglycine basal and captopril renal scintigraphy. While no significant change was seen with Tc-99m DTPA, there was left sided parenchymal retention of captopril Tc-99m MAG3 suggesting renal artery stenosis which was confirmed by angiography. Content Type Journal ArticleCategory Case ReportsDOI 10.1007/BF03012130Authors Pinar Özgen Kiratli, Hacettepe University Medical School Department of Nuclear Medicine 06100 Sihhtye, Ankara TurkeyBiray CanerBülent Altun, Hacettepe University Medical Centre Department of Nephrology Ankara TurkeySaruhan Çekirge, Hacettepe University Medical Centre Department of Radiology Ankara T...

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  L-Arginine Fails to Prevent Ventricular Remodeling and Heart Failure in the Spontaneously Hypertensive Rat.

ConclusionThese data demonstrate that in contrast to captopril, long-term treatment with L-arginine exacerbates age-related cardiac hypertrophy, fibrosis, and did not prevent contractile dysfunction or the development of HF in aging SHR.American Journal of Hypertension 2008; doi:10.1038/ajh.2008.334American Journal of Hypertension 2008; doi:10.1038/ajh.2008.334. PMID: 19057517 [PubMed - as supplied by publisher] (Source: American Journal of Hypertension)

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  Different Effects of Angiotensin Converting Enzyme Inhibitors on Endothelin-1 and Nitric Oxide Balance in Human Vascular Endothelial Cells: Evidence of an Oxidant-Sensitive Pathway

In conclusion, among the four tested ACE-I, zofenoprilat was more effective in improving endothelin-1/nitric oxide balance in HUVECs likely because of its greater antioxidant properties. (Source: Mediators of Inflammation)

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  Molecular Imaging of Interstitial Alterations in Remodeling Myocardium After Myocardial Infarction

Conclusions Radiolabeled CRIP allows for noninvasive visualization of interstitial alterations during cardiac remodeling, and is responsive to antiangiotensin treatment. If proven clinically feasible, such a strategy would help identify post-MI patients likely to develop heart failure. (Source: Journal of the American College of Cardiology)

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  The potential role of MLC phosphatase and MAPK signalling in the pathogenesis of vascular dysfunction in heart failure.

Conclusions. PMID: 19120700 [PubMed - in process] (Source: J Cell Mol Med)

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  Successful Treatment of Fosinopril-Induced Severe Cholestatic Jaundice with Plasma Exchange (December).

CONCLUSIONS: Plasma exchange therapy may play a valuable role in the treatment of fosinopril-induced cholestatic jaundice and liver failure. This intervention can be considered for temporary liver support until recovery or OLT. PMID: 19017832 [PubMed - as supplied by publisher] (Source: The Annals of Pharmacotherapy)

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  Sex Differences in Blood Pressure Response to Antihypertensive Therapy in Chinese Patients with Hypertension (December).

CONCLUSIONS: Women have better blood pressure responses to HCTZ and atenolol and experience more adverse effects with sustained-release nifedipine and captopril than do men, indicating that sex should be taken into account when selecting antihypertensive drugs. PMID: 19017831 [PubMed - as supplied by publisher] (Source: The Annals of Pharmacotherapy)

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  Angiotensin receptor blockers are superior to angiotensin-converting enzyme inhibitors in the suppression of hepatic fibrosis in a bile duct-ligated rat model

Conclusions  Both ARB and ACEI attenuate hepatic fibrosis through inhibiting hepatic stellate cell activation, and the inhibitory effect of ARBs on hepatic fibrosis is superior to that of ACEIs in the BDL rat model. Content Type Journal ArticleCategory Liver, Pancreas, and Biliary TractDOI 10.1007/s00535-008-2239-9Authors Moon Young Kim, Yonsei University Wonju College of Medicine Department of Internal Medicine and Institute of Lifelong Health 162 Ilsan-dong Wonju 220-701 South KoreaSoon Koo Baik, Yonsei University Wonju College of Medicine Department of Internal Medicine and Institute of Lifelong Health 162 Ilsan-dong Wonju 220-701 South KoreaDong Hun Park, Yonsei University Wonju College of Medicine Department of Internal Medicine and Institute of Lifelong Health 162...

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  Captopril/enalapril: Renal disorders and hyperkalaemia: 5 case reports

(Source: Reactions)

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  Captopril/enalapril: Renal disorders and hyperkalaemia: 5 case reports.

Page: 12 (Source: Reactions Weekly)

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  High-pressure NMR characterization of triacetyl-beta-cyclodextrin in supercritical carbon dioxide.

Authors: Ivanova GI, Vão ER, Temtem M, Aguiar-Ricardo A, Casimiro T, Cabrita EJ Cyclodextrins are used in many drug formulations since their cavities provide microenvironments where drug molecules can enter and form inclusion complexes for controlled drug delivery. Supercritical carbon dioxide (scCO(2)) is an alternative to organic solvents and a very attractive medium for the preparation of these inclusion complexes. The potential ability of triacetyl-beta-cyclodextrin (TA-beta-CD) to form inclusion complexes in addition to its high miscibility in liquid and scCO(2) could offer a chance for an economical and environmental friendly chemical processing. In this work, high-pressure NMR studies were performed in order to obtain information on the molecular structure and dynamics of T...

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  Incidental Atherosclerotic Renal Artery Stenosis in Patients Undergoing Elective Coronary Angiography: Are These Lesions Significant?

Conclusions: In cardiac patients diagnosed with iARAS, the presence of known anatomic lesions did not correlate with captopril renogram positivity. Uncertainty remains as to whether nuclear renography is a poor functional test in this population, or the lesions are not functionally significant. These results lead us to question both the significance of such lesions, and the utility of conducting renograms in this population. PMID: 19011276 [PubMed - as supplied by publisher] (Source: American Journal of Nephrology)

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  Ginkgo biloba extract prevents glucose-induced accumulation of ECM in rat mesangial cells

This study evaluated the effects of Ginkgo biloba extract (GbE) on the metabolism of the ECM in rat mesangial cells cultured in hyperglycemic conditions. The cultured mesangial cells in high glucose conditions were allotted into six groups: normal control group, high glucose group, low concentration of GbE group, moderate concentration of GbE group, high concentration of GbE group, and captopril group. In the presence of high glucose, the levels of matrix metalloproteinase-2 (MMP-2), matrix metalloproteinase-9 (MMP-9) and extracellular matrix metalloproteinase inducer (EMMPRIN) were decreased significantly, and the levels of tissue inhibitor of metalloproteinase-2 (TIMP-2), tissue inhibitor of metalloproteinase-1 (TIMP-1) and plasminogen activator inhibitor-1 (PAI-1) were increased signifi...

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  Nerve stimulation induced overflow of neuropeptide Y and modulation by angiotensin II in spontaneously hypertensive rats

The sympathetic nervous system and renin-angiotensin system are both thought to contribute to the development and maintenance of hypertension in experimental models such as the spontaneously hypertensive rat (SHR). We demonstrated that periarterial nerve stimulation (NS) increased the perfusion pressure (PP) and neuropeptide Y (NPY) overflow from perfused mesenteric arterial beds of SHRs at 4–6, 10–12, and 18–20 wk of age, which correspond to prehypertensive, developing hypertensive, and maintained hypertensive stages, respectively, in the SHR. NS also increased PP and NPY overflow from mesenteric beds of Wistar-Kyoto (WKY) normotensive rats. NS-induced increases in PP and NPY were greater in vessels obtained from SHRs of all three ages compared with WKY rats. ANG II prod...

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  Ameliorative effect of captopril and valsartan on an animal model of diabetic cardiomyopathy.

The objective of this study was to clarify the relationship between angiotensin II and the pathogenesis of diabetic cardiomyopathy by observing the effects of related drugs on diabetic cardiomyopathy in rats. Captopril and Valsartan, an automatic biochemical analyzer, and radioimmunoassay technology were used to an experimental rat model of diabetic cardiomyopathy to dynamically measure the levels of creatine kinase-MB, lactate dehydrogenase-1 in the serum, and angiotensin I and II in the plasma, and to observe changes in the myocardial ultrastructure. The content of angiotensin I and II was increased and the renin-angiotensin system was in a hyperfunctional state in experimental rats with myocardial damage. Angiotensin-converting enzyme inhibitors and angiotensin II receptor 1 antagonists...

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  [Effects of Tangxinping Capsule on angiotensin II and its type 1 receptor and myocardial ultrastructure in diabetic rats.]

Conclusion: Tangxinping may adjust the disorder of renin-angiotensin system to protect myocardial tissue in rats with cardiomyopathy due to diabetes. PMID: 18990343 [PubMed - in process] (Source: Zhong xi yi jie he xue bao : Journal of Chinese Integrative Medicine.)

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  Effect of carvedilol on pulse pressure and left ventricular hypertrophy in spontaneously hypertensive rats with adriamycin nephropathy.

In conclusion, carvedilol alone, but more strongly in combination with captopril, significantly reduced blood pressure, PP, LVH, renal blood vessel changes and chronic renal failure progression. PMID: 19013753 [PubMed - as supplied by publisher] (Source: Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie)

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  Comparison of Nifedipine and Captopril in Children with Pulmonary Hypertension due to Broncopneumonia

This study included 40 children, who were diagnosed with pneumonia and pulmonary hypertension (from the radiographic and clinical features), was performed at Yuzuncu Yil University Faculty of Medicine, Department of Pediatrics, from September 2003 to July 2005. Patients who had pneumonia and congenital heart disease or systemic hypertension or renal and liver disease together were excluded from the study. Blood gas analysis and oxygen concentration, measured with pulse oximetry, were performed in all patients. Besides chest X-ray, electrocardiography and echocardiographic search was also carried out. Echocardiographic examination was performed by using M mode, two-dimensional echocardiography and colored Doppler sonotron Vingmed CFM 725. At echocardiographic examination, pulmonary hyperten...

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  Nerve Stimulation Induced Overflow of Neuropeptide Y and Modulation by Angiotensin II in Spontaneously Hypertensive Rats.

Authors: Byku M, Macarthur H, Westfall TC The sympathetic nervous system (SNS) and the renin angiotensin system (RAS) are both thought to contribute to the development and maintenance of hypertension in experimental models such as the Spontaneously Hypertensive Rat (SHR). We demonstrated that periarterial nerve stimulation (NS) increased the perfusion pressure (PP) and NPY overflow from the perfused mesenteric arterial bed of SHR at 4-6, 10-12 , and 18-20 weeks of age; which correspond to a prehypertensive, developing hypertensive and maintained hypertensive stages respectively in the SHR. NS also increased PP and NPY overflow from the mesenteric beds of Wistar Kyoto (WKY) normotensive rats. The NS-induced increase in PP and NPY was greater in vessels obtained from SHR of all 3 ages co...

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  Improvement of diastolic function after regression of left ventricular hypertrophy.

CONCLUSIONS: Some indexes of diastolic function improved after regression of left ventricular hypertrophy and good blood pressure control with captopril and chlortalidone. PMID: 19205547 [PubMed - in process] (Source: Archivos de Cardiologia de Mexico)

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  [Causation] Enalapril and captopril increased mortality compared with ramipril in elderly patients with heart failure

(Source: Evidence-Based Nursing)

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  Effects of angiotensin converting enzyme inhibition on cardiac innervation and ventricular arrhythmias after myocardial infarction.

CONCLUSION: In this study, prolonged captopril treatment was effective in preventing VAs in healed MI, partly by attenuating the spatial heterogeneity of cardiac innervation. PMID: 18682043 [PubMed - in process] (Source: Clinical and Investigative Medicine)

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  Rural treatment of acute cardiogenic pulmonary edema: applying the evidence to achieve success with failure.

Authors: Bosomworth J Rural management of acute cardiogenic pulmonary edema should be based on avoidance of adverse outcomes such as in-hospital mortality, the need for intensive care unit care, and the need for intubation and mechanical ventilation. Current evidence suggests that early noninvasive continuous positive airway pressure and early aggressive preload reduction with intravenous nitroglycerin are first-line interventions. Afterload reduction with sublingual captopril, with or without nitroglycerin, improves outcomes and is a second-line intervention. Furosemide is associated with adverse outcomes when used alone and should be given only after vasodilator therapy as a third-line intervention. Inotropes should be used only with demonstrably poor perfusion as they do not improve...

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  Catalysis reaction between sodium 1,2-naphthoquinone-4-sulfonate and hydroxyl ion using captopril as catalyzer and determination of captopril.

Authors: Gao L, Wu L, Li Q A novel and simple spectrophotometric method for the determination of Captopril with sodium 1,2-naphthoquinone-4-sulfonate is established in this paper. The detailed reaction mechanism is proposed and discussed. It is based on the fact that captopril can catalyze the reaction between sodium 1,2-naphthoquinone-4-sulfonate and hydroxyl ion to form 2-hydroxy-1,4-naphthoquinone in buffer solution of pH 13.00. Beer's law is obeyed in a range of 0.64-80 mugmL(-1) at the maximal absorption wavelength of 442 nm. The equation of linear regression is A=0.05815+0.00589C (mugmL(-1)), with a linear regression correlation coefficient of 0.9981. The detection limit is 0.3 mugmL(-1), R.S.D. is 0.77% and the recovery rate is in range of 96.0-103.8%. Furthermore, the method ha...

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  Structure-activity relationships for dipeptide prodrugs of acyclovir: Implications for prodrug design.

Authors: Santos CR, Capela R, Pereira CS, Valente E, Gouveia L, Pannecouque C, De Clercq E, Moreira R, Gomes P A series of water-soluble dipeptide ester prodrugs of the antiviral acyclovir (ACV) were evaluated for their chemical stability, cytotoxicity, and antiviral activity against several strains of Herpes Simplex-1 and -2, vaccinia, vesicular stomatitis, cytomegalovirus and varicella zoster viruses. ACV dipeptide esters were very active against herpetic viruses, independently of the rate at which they liberate the parent drug. Their minimum cytotoxic concentrations were above 100muM and the resulting MCC/EC(50) values were lower than those of ACV. When comparing the reactivity of Phe-Gly esters and amides (ACV, zidovudine, paracetamol, captopril and primaquine) in pH 7.4 buffer it ...

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  The Effect of Pentoxifylline on Proteinuria in Diabetic Kidney Disease: A Meta-analysis

Conclusions: Available evidence suggests that pentoxifylline may decrease proteinuria in patients with diabetic nephropathy. To confirm these findings, large high-quality studies are required. (Source: American Journal of Kidney Diseases)

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  Captopril as a potential inhibitor of lung tumor growth and metastasis.

Authors: Attoub S, Gaben AM, Al-Salam S, Al Sultan MA, John A, Nicholls MG, Mester J, Petroianu G Lung cancer is the most common form of cancer in the world, and 90% of patients die from their disease. The angiotensin converting enzyme (ACE) inhibitors are used widely as antihypertensive agents, and it has been suggested that they decrease the risk of some cancers, although available data are conflicting. Accordingly, we investigated the anticancer activity of the ACE inhibitor, captopril, in athymic mice injected with highly tumorigenic LNM35 human lung cells as xenografts. Using this model, we demonstrated that daily IP administration of captopril (2.8 mg/mouse) for 3 weeks resulted in a remarkable reduction of tumor growth (58%, P < 0.01) and lymph node metastasis (50%, P= 0.088)...

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  A study of in vivo antihypertensive properties of enzymatic hydrolysate from chicken leg bone protein

In this study, the best ACE inhibitory hydrolysate (A4) (which was derived from chicken leg bone protein by Alcalase after 4 h incubation) was orally administrated (50 mg/kg bw) in spontaneously hypertensive rats (SHRs) to investigate its antihypertensive effects. After oral administration of A4, a maximal reduction activity of about 26 mmHg was found at 4 h and maintained to 8 h. Moreover, SHRs treated with A4 (50 mg/kg bw/day) for eight weeks exhibited a reduction in systolic blood pressure, which is as significant as the effects of Captopril (P < 0.05). These results suggested that chicken leg bones have a high potential for utilization to develop ACE inhibitors as potential food ingredients intended to alleviate hypertension. (Source: Animal Science Journal)

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  Pharmacologic Effects of Grain Weevil Extract on Isolated Guinea Pig Tracheal Smooth Muscle

Abstract  The grain weevil, an insect (pest) that infects grain, is a frequent contaminant of processed wheat, and its presence may contribute to respiratory abnormalities in grain workers. We studied the in vitro effects of an extract of grain weevil (GWE) on airway smooth muscle. Pharmacologic studies included in vitro challenge of guinea pig trachea with GWE, in parallel organ baths, pretreated with mediator-modifying agents or a control solution. Dose-related contractions of nonsensitized guinea pig trachea (GPT) were demonstrated using this extract. Pharmacologic studies were performed by pretreating guinea pig tracheal tissue with drugs known to modulate smooth muscle contraction: atropine, indomethacin, pyrilamine, acivicin, NDGA, BPB, TMB8, captopril, and capsaicin....

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  Matrix metalloproteinase-9/tissue inhibitors of metalloproteinase-1 expression and atrial structural remodeling in a dog model of atrial fibrillation: inhibition with angiotensin-converting enzyme.

CONCLUSIONS: Altered expression of matrix metalloproteinase-9 and tissue inhibitors of metalloproteinase-1 contributes to atrial extracellular matrix remodeling and atrial dilatation. Angiotensin-II-mediated intracellular Ca(2+) overload may be the mechanism of altered expression of matrix metalloproteinase-9 and tissue inhibitors of metalloproteinase-1. Angiotensin-converting enzyme inhibitor treatment may attenuate atrial structural remodeling by normalizing the balance between matrix metalloproteinase-9 and tissue inhibitors of metalloproteinase-1. PMID: 18706834 [PubMed - as supplied by publisher] (Source: Cardiovascular Pathology)

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  Opposed effects of prostaglandin E2 on perfusion of rat renal cortex and medulla: interactions with the renin–angiotensin system

In conclusion, in rat renal cortex the dominating stable PGE2 effect is vasoconstriction, most probably mediated by EP3 receptors and unrelated to activation of the RAS. Prostaglandin E2 applied to the cortical or medullary interstitium, a natural route for paracrine agents, induces medullary vasodilatation. (Source: Experimental Physiology)

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  RAS inhibitors decrease apoptosis of acinar cells and increase elimination of pancreatic stellate cells after in the course of experimental chronic pancreatitis induced by dibutyltin dichloride.

Authors: Madro A, Korolczuk A, Czechowska G, Celiński K, Słomka M, Prozorow-Król B, Korobowicz E Chronic pancreatitis (CP) is a progressive disease, in which the exocrine function of the gland is gradually lost and fibrosis develops due to repeated episodes of acute pancreatitis. The aim of the study was to investigate the effects of RAS inhibitors on the apoptosis of acinar cells and pancreatic stellate cells (PSCs) elimination in experimental CP induced by dibutyltin dichloride (DBTC). CP was induced by administration of DBTC to the femoral vein. Simultaneously captopril, losartan, enalapril and lisinopril were administered intraperitoneally. The rats were decapitated after 60 days and tissue of pancreas was collected. In rats treated by DBTC the features of inflamma...

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  Captopril: Lichen planus pemphigoides in an elderly patient: case report

(Source: Reactions)

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  The characterization of selected drugs with infrared laser desorption/tunable synchrotron vacuum ultraviolet photoionization mass spectrometry.

Authors: Pan Y, Yin H, Zhang T, Guo H, Sheng L, Qi F Some selected drugs including captopril, fudosteine and racecadotril have been analyzed by infrared (IR) laser desorption/tunable synchrotron vacuum ultraviolet (VUV) photoionization mass spectrometry (PIMS). The molecular ions of captopril and racecadotril are exclusively observed without any fragments at near threshold single-photon ionization (SPI). However, fudosteine easily forms fragments even at a photon energy near the ionization threshold, indicating the instability of its molecular ion. For these drugs, a number of fragments are yielded with the increase of photon energy. The structures of such fragments proposed by IR LD/VUV PIMS are supported by electron ionization time-of-flight mass spectrometry (EI-TOFMS) results. Frag...

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  Design and Evaluation of a Sustained Release Gastroretentive Dosage Form of Captopril: A Technical Note.

Authors: Patel P, Dand N, Somwanshi A, Kadam VJ, Hirlekar RS PMID: 18626773 [PubMed - as supplied by publisher] (Source: AAPS PharmSciTech)

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  Chronic high dose captopril decreases total heart rate variability and increases heart rate in C57BL/6J mice

Abstract: The effects of high dose captopril, within the therapeutic range, on autonomic activity are unknown in those with normal cardiovascular function. Thus the study aims were to assess the effects of high dose captopril on autonomic function in mice. Autonomic activity was measured using heart rate variability (HRV). ECG recordings were obtained from 18 Male C57BL/6J mice (20–25 g) subdivided into control (N=8) or mice receiving oral captopril (0.688 mg/ml captopril in the drinking water for 6 weeks, N=10). HRV results for linear and non-linear parameters were attenuated following chronic captopril for 6 weeks compared to control. Captopril was associated with a trend for an increase in average heart rate and approximate entropy (ApEn), a non-linear measure of HRV decreased sig...

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  Lesions of medullary catecholaminergic neurons increase salt intake in rats.

Authors: Colombari DS, Pedrino GR, Freiria-Oliveira AH, Korim WS, Maurino IC, Cravo SL Several findings suggest that catecholaminergic neurons in the caudal ventrolateral medulla (CVLM) contribute to body fluid homeostasis and cardiovascular regulation. From the CVLM other areas in central nervous system involved in cardiovascular regulation and hydroelectrolyte balance can be activated. Therefore, the aim of the present study was to investigate the effects of lesions of these neurons on 0.3M NaCl and water intake induced by subcutaneous injection of furosemide (FURO)+captopril (CAP) or 36h of water deprivation/partial hydration with only water (WD/PR). Male Wistar rats (320-360g) were submitted to medullary catecholaminergic neuron lesions by microinjection of anti-dopamine-beta-hydro...

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

Authors: Zicha J, Dobesová Z, Kunes J Spontaneously hypertensive rats (SHR) are characterized by enhanced nifedipine-sensitive component of sympathetic vasoconstriction. Our study tried to elucidate the mechanisms responsible for long-term reduction of blood pressure (BP) in SHR subjected to early transient captopril treatment. Adult untreated SHR aged 30-34 weeks were compared with animals subjected to chronic captopril treatment for 6 weeks either in youth (between 4 and 10 weeks of age) or in adulthood (between 24 and 30 weeks of age). Antihypertensive effects of captopril were more pronounced in young than adult SHR. This was due to greater attenuation of sympathetic and nifedipine-sensitive BP components and prevention of residual BP rise in young captopril-treated SHR in whi...

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  Chronic high dose captopril decreases total heart rate variability and increases heart rate in C57BL/6J mice.

In conclusion high dose captopril reduces total HRV and increases heart rate in normotensive mice with normal cardiac function. PMID: 18606470 [PubMed - as supplied by publisher] (Source: International Journal of Cardiology)

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

CONCLUSIONS: Acting via B(2) receptor, BK contributes to the antihypertrophic and antiproliferative effects of captopril on cardiomyocytes and CFs. In the absence of B(2) receptor, B(1) receptor may act a compensatory mechanism for the B(2) receptor and contribute to the inhibition of cardiomyocyte hypertrophy and CFs proliferation by captopril. NO and cGMP play an important role in the effect of B(1) receptor. PMID: 18710643 [PubMed - in process] (Source: Chinese Medical Journal)

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  Renal and Hormonal Responses to Direct Renin Inhibition With Aliskiren in Healthy Humans.

Conclusions-Renal vasodilation in healthy people with the potent renin inhibitor aliskiren exceeded responses seen previously with angiotensin-converting enzyme inhibitors and angiotensin receptor blockers. The effects were longer lasting and were associated with significant natriuresis. These results indicate that aliskiren may provide more complete and thus more effective blockade of the renin-angiotensin system. PMID: 18559696 [PubMed - as supplied by publisher] (Source: Circulation)

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  A mouse model for Costello syndrome reveals an Ang II-mediated hypertensive condition

Germline activation of H-RAS oncogenes is the primary cause of Costello syndrome (CS), a neuro-cardio-facio-cutaneous developmental syndrome. Here we describe the generation of a mouse model of CS by introduction of an oncogenic Gly12Val mutation in the mouse H-Ras locus using homologous recombination in ES cells. Germline expression of the endogenous H-RasG12V oncogene, even in homozygosis, resulted in hyperplasia of the mammary gland. However, development of tumors in these mice was rare. H-RasG12V mutant mice closely phenocopied some of the abnormalities observed in patients with CS, including facial dysmorphia and cardiomyopathies. These mice also displayed alterations in the homeostasis of the cardiovascular system, including development of systemic hypertension, extensive vascular re...

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  Effect of various surfactants and their concentration on controlled release of captopril from polymeric matrices.

In this study, the effects of various polymers such as hydroxypropyl methylcellulose (HPMC), ethylcellulose (EC) and sodium carboxymethylcellulose (CMC) and surfactants (sodium lauryl sulphate, cetyltrimethylammonium bromide and Arlacel 60) on the release rate of captopril were investigated. The results showed that an increase in the amount of HPMC K15M resulted in reduction of the release rate of captopril from these matrices. When HPMC was partly replaced by NaCMC (the ratio of HPMC/NaCMC was 5:1), the release rate of the drug significantly decreased. However, there was no significant difference in release rate of captopril from matrices produced with ratios of 5:1 and 2:1 of HPMC/NaCMC. The presence of lactose in matrices containing HPMC and NaCMC increased the release rate of captopril...

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  Captopril decreases plasminogen activator inhibitor-1 in rats with ventilator-induced lung injury.

Page: 1880DOI: 10.1097/CCM.0b013e31817c911dAuthors: Chen, Chung-Ming MD, PhD; Chou, Hsiu-Chu PhD; Wang, Leng-Fang MS; Lang, Yaw-Dong MS (Source: Critical Care Medicine)

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  Minimally invasive treatment of urethral strictures in men

Abstract  Minimally invasive treatments of urethral strictures in men intend to durably restore normal anatomy and function with relief of urinary symptoms and avoidance of morbidity. Minimally invasive treatments for bulbar urethral strictures include bougienage and coaxial balloon dilation, endoscopic urethrotomy with a cold-knife or laser, and urethral wall stents. Adjunctive techniques including brachytherapy and the injection of steroids, mitomycin C, or captopril, have been employed to reduce the high restricture rates with minimally invasive treatments for bulbar urethral strictures. This review discusses recently published data concerning indications for these commonly performed minimally invasive procedures, along with their efficacy, durability, and potential for ...

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  Investigation of the Arterial Stiffness on Renal Artery Doppler Sonograms

This study aims to identify the effect of stiffness on renal artery Doppler sonograms by using a curve fitting approach. The study includes 20 patients with suspected renovascular hypertension. Each patient underwent recordings during renal artery examinations before and after administration of Captopril 25 mg (Kapril tablet, MN Pharmaceuticals, Istanbul, Turkey). Doppler signals were analyzed with short time Fourier transformation, followed by curve fitting to sonograms using Savitzky–Golay method. Doppler parameters obtained from pre- and post-Captopril curve-fitted sonograms were statistically compared with “Paired-Samples t-Test”. Captopril administration resulted in a significant decrease in the mean frequency and a significant increase in Pulsatility Index of the per...

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