Document Detail


Converting enzyme inhibitors and the role of the sulfhydryl group in the potentiation of exo- and endogenous nitrovasodilators.
MedLine Citation:
PMID:  1720843     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
In this study, the effect of bradykinin on coronary flow in the isolated rat heart was significantly potentiated when cysteine or the sulfhydryl-containing converting enzyme inhibitors captopril and zofenoprilat were administered simultaneously. In contrast, the effect of concomitant administration of enalaprilat only slightly increased the effect of bradykinin on coronary flow. In nitrate-tolerant hearts of rats pretreated with isosorbide dinitrate (15 mg daily), the increase in coronary flow by nitroglycerin and bradykinin was significantly less when compared to control hearts. The effect of captopril was not affected by pretreatment. The involvement of endothelium-derived relaxing factor (EDRF) in the effect of captopril was apparent from experiments with L-arginine, the precursor of EDRF, and L-NMMA, the "false" precursor of EDRF. L-Arginine increased the effect of captopril, whereas L-NMMA showed a competitive antagonism for the effect of captopril on coronary flow in the isolated rat heart. Clinically, the effect of captopril was studied in 10 patients with stable, exercise-induced angina pectoris that had been treated for 3 weeks with slow-release isosorbide dinitrate (20 mg four times daily). At day 7, a baseline exercise test was obtained. Subsequently, patients with chest pain and at least 1-mm ST-segment depression on the ECG during exercise were included. They received on day 14 and 21 either captopril (25 mg) or placebo 1 h before exercise testing in a randomized, double-blind, crossover design. Captopril significantly improved the combined score of maximal ST-segment depression, maximal workload, and time to angina when compared to placebo. No differences in the pressure-rate index at rest and during exercise were seen. These results indicate that the sulfhydryl group of certain angiotensin converting enzyme inhibitors can potentiate their effect on the endogenous nitrovasodilator EDRF. In the clinical situation, this may lead to an improved exercise performance in patients with stable angina pectoris during chronic nitrate treatment, independent of its systemic vascular effects.
Authors:
W H van Gilst; P A de Graeff; M J de Leeuw; E Scholtens; H Wesseling
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Publication Detail:
Type:  Clinical Trial; In Vitro; Journal Article; Randomized Controlled Trial    
Journal Detail:
Title:  Journal of cardiovascular pharmacology     Volume:  18     ISSN:  0160-2446     ISO Abbreviation:  J. Cardiovasc. Pharmacol.     Publication Date:  1991 Sep 
Date Detail:
Created Date:  1992-01-14     Completed Date:  1992-01-14     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  7902492     Medline TA:  J Cardiovasc Pharmacol     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  429-36     Citation Subset:  IM    
Affiliation:
Department of Pharmacology/Clinical Pharmacology, University of Groningen, The Netherlands.
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MeSH Terms
Descriptor/Qualifier:
Aged
Angina Pectoris / drug therapy
Angiotensin-Converting Enzyme Inhibitors / pharmacology*
Animals
Arginine / analogs & derivatives,  pharmacology
Blood Pressure / drug effects
Bradykinin / antagonists & inhibitors,  pharmacology
Captopril / pharmacology
Coronary Circulation / drug effects
Cysteine / pharmacology
Dose-Response Relationship, Drug
Humans
Isosorbide Dinitrate / pharmacology
Male
Middle Aged
Nitric Oxide / physiology
Nitro Compounds / pharmacology*
Rats
Rats, Inbred Strains
Sulfhydryl Compounds / pharmacology*
Vasodilator Agents / pharmacology*
omega-N-Methylarginine
Chemical
Reg. No./Substance:
0/Angiotensin-Converting Enzyme Inhibitors; 0/Nitro Compounds; 0/Sulfhydryl Compounds; 0/Vasodilator Agents; 10102-43-9/Nitric Oxide; 17035-90-4/omega-N-Methylarginine; 52-90-4/Cysteine; 58-82-2/Bradykinin; 62571-86-2/Captopril; 74-79-3/Arginine; 87-33-2/Isosorbide Dinitrate

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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