Single and divided doses of penbutolol

Penbutolol, a nonselective beta-adrenoreceptor antagonist, induced reduction of exercise-induced heartbeats for at least 24 hr after a single 40-mg oral dose, and was equipotent with respect to a 2 X 20-mg regimen over the same period. Ingestion for 7 days did not influence the pharmacodynamics or p...

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Bibliographic Details
Published inClinical pharmacology and therapeutics Vol. 25; no. 5 Pt 1; p. 528
Main Authors Müller, F O, Hundt, H K, Bromley, P A, Torres, J, Vanderbeke, O
Format Journal Article
LanguageEnglish
Published United States 01.05.1979
Subjects
Adult
Drug Administration Schedule
Heart Rate - drug effects
Humans
Kinetics
Male
Penbutolol - administration & dosage
Penbutolol - adverse effects
Penbutolol - blood
Penbutolol - pharmacology
Physical Exertion
Propanolamines - administration & dosage
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Summary:Penbutolol, a nonselective beta-adrenoreceptor antagonist, induced reduction of exercise-induced heartbeats for at least 24 hr after a single 40-mg oral dose, and was equipotent with respect to a 2 X 20-mg regimen over the same period. Ingestion for 7 days did not influence the pharmacodynamics or pharmacokinetics of penbutolol, and there was no cumulation of drug in serum. A relationship was found between the logarithms of measurable serum concentrations of penbutolol and the percentage reduction of total heartbeats. Absorption of oral penbutolol appeared to be reduced when administered in the evening. Since beta-adrenoceptor activity was relatively unchanged between 13 and 24 hr after a single 40-mg dose of penbutolol, there is a possibility that an active metabolite or metabolites may contribute to prolonged duration of action.
ISSN:0009-9236
DOI:10.1002/cpt1979255part1528