Document Detail

In vitro interactions of captopril with H2-receptor antagonists.
MedLine Citation:
PMID:  17416569     Owner:  NLM     Status:  MEDLINE    
Captopril is effective in the treatment of hypertension of all grades of severity. H2-receptors antagonists block gastric acid secretion and some cardiovascular effects of histamine. In view of the fact that, simultaneous administration of both drugs may alter the antihypertensive effect of captopril, present paper deals with the in vitro availability studies of captopril in presence of commonly used H2-receptor antagonists like cimetidine, ranitidine and famotidine. In order to simulate various pH levels in GI tract and to find out the kinetics and energetics of captopril-H2-receptor antagonist interactions, these studies were carried out in buffers of pH 4, 7.4 and 9 at 37 degrees C and at elevated temperatures. These studies clearly indicate that most of the H2-receptor antagonists bind to captopril, forming charge-transfer complexes. As a result, the availability of captopril was affected by the concurrent administration of H2-receptor antagonists. Accordingly coadministration of both the drugs should be avoided.
Najma Sultana; M Saeed Arayne; Reeshanul Quraish
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Pakistan journal of pharmaceutical sciences     Volume:  20     ISSN:  1011-601X     ISO Abbreviation:  Pak J Pharm Sci     Publication Date:  2007 Apr 
Date Detail:
Created Date:  2007-04-09     Completed Date:  2007-07-03     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9426356     Medline TA:  Pak J Pharm Sci     Country:  Pakistan    
Other Details:
Languages:  eng     Pagination:  132-9     Citation Subset:  IM    
Department of Pharmaceutical Chemistry, Research Institute of Pharmaceutical Sciences, Faculty of Pharmacy, University of Karachi, Karachi-75270, Pakistan.
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MeSH Terms
Angiotensin-Converting Enzyme Inhibitors / chemistry*,  metabolism
Anti-Ulcer Agents / chemistry*,  pharmacology
Antihypertensive Agents / chemistry*,  metabolism
Captopril / chemistry*,  metabolism
Cimetidine / chemistry
Drug Interactions
Famotidine / chemistry
Gastric Juice / chemistry
Histamine H2 Antagonists / chemistry*,  pharmacology
Hydrogen-Ion Concentration
Models, Chemical
Ranitidine / chemistry
Reg. No./Substance:
0/Angiotensin-Converting Enzyme Inhibitors; 0/Anti-Ulcer Agents; 0/Antihypertensive Agents; 0/Histamine H2 Antagonists; 51481-61-9/Cimetidine; 62571-86-2/Captopril; 66357-35-5/Ranitidine; 76824-35-6/Famotidine

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