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Propranolol pharmacokinetics and pharmacodynamics after single doses and at steady-state.

Abstract：

:The duration and extent of cardiac beta-blockade and their relationship to propranolol pharmacokinetics were assessed in nine healthy volunteers. Each subject received 160 mg of regular propranolol (R), 160 mg of sustained-release propranolol (SR) and no drug (control), both as single doses and once daily for 7 days. After single doses and at steady-state, both products caused a decrease in exercise heart rate for at least 24 h, compared to control. The time course of effect was similar to the time course of serum propranolol concentration. The oral clearance of propranolol decreased from single doses to steady-state for both R and SR; however, the difference achieved statistical significance only for R. These changes were reflected in mean accumulation ratios (AUC steady-state 0-24 h/AUC single dose 0-infinity) of 1.49 and 1.68 for R and SR, respectively. The pharmacokinetic data are consistent with a decrease in intrinsic hepatic clearance of propranolol, leading to an increase in bioavailability at steady-state. Despite a two-fold difference in the bioavailability of R and SR, there was no difference in the area under the effect-time curve at steady-state.

journal_name

Eur J Clin Pharmacol

journal_title

European journal of clinical pharmacology

authors

Lalonde RL,Pieper JA,Straka RJ,Bottorff MB,Mirvis DM

doi

10.1007/BF00637569

subject

Has Abstract

pub_date

1987-01-01 00:00:00

pages

315-8

issue

3

eissn

0031-6970

issn

1432-1041

journal_volume

33

pub_type

杂志文章

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