Document Detail


Influence of pentobarbital on effect and plasma levels of alprenolol and 4-hydroxy-alprenolol.
MedLine Citation:
PMID:  428186     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Six healthy subjects were given placebo and a single oral 0.2-gm dose of alprenolol (Aptin) before and after 0.1 gm pentobarbital at bedtime for 10 days. The plasma concentrations of alprenolol and its metabolite 4-hydroxy-alprenolol and the inhibition of exercise tachycardia were studied for 7 hr after the alprenolol. Alprenolol and 4-hydroxy-alprenolol plasma levels were decreased by about 40% by pentobarbital but plasma half-lives were unchanged. The inhibition of exercise tachycardia during a 7-hr period was reduced from 14.0% to 10.7% by pentobarbital. The reduction was proportional to the decreased drug plasma levels. There was a significant contribution of the metabolite to alprenolol effect. The estimation of relative potency of metabolite against parent compound was 0.9 before pentobarbital and 1.9 after pentobarbital.
Authors:
P Collste; P Seideman; K O Borg; K Haglund; C von Bahr
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Clinical pharmacology and therapeutics     Volume:  25     ISSN:  0009-9236     ISO Abbreviation:  Clin. Pharmacol. Ther.     Publication Date:  1979 Apr 
Date Detail:
Created Date:  1979-06-29     Completed Date:  1979-06-29     Revised Date:  2008-11-21    
Medline Journal Info:
Nlm Unique ID:  0372741     Medline TA:  Clin Pharmacol Ther     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  423-7     Citation Subset:  AIM; IM    
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MeSH Terms
Descriptor/Qualifier:
Adult
Alprenolol / blood*,  pharmacology
Drug Interactions
Heart Rate / drug effects
Humans
Hydroxylation
Male
Pentobarbital / pharmacology*
Physical Exertion
Time Factors
Chemical
Reg. No./Substance:
13655-52-2/Alprenolol; 76-74-4/Pentobarbital

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


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