Influence of smoking and gender on the disposition kinetics of metoprolol.

Abstract:

:The purpose of this study was to examine the influence of cigarette smoking and gender on the pharmacokinetics of metoprolol. Eighteen volunteers with no evidence of clinical disease each randomly received the following doses of metoprolol tartrate: 100 mg orally, 200 mg orally and 20 mg as a constant-rate intravenous infusion over 20 min. The only significant difference between smokers (S) and nonsmokers (NS) was that S had a larger steady-state volume of distribution (3.3 vs 2.5 l/kg). There were no differences in half-life, systemic clearance or bioavailability (f). No differences were observed between males (M) and females (FM) for any of the kinetic parameters examined. Systemic bioavailability varied markedly between subjects (range: 15 to 92%). In fifteen of the eighteen subjects, f was higher after the 200-mg dose compared to the 100-mg dose. These results suggest that metoprolol may be subject to saturable presystemic elimination and extend the previous observations of Johnsson et al. [1] who showed that f increased from 31% to 46% when doses were increased from 20 to 100 mg. However, the difference in f as the dose is increased is unlikely to be clinically significant since the mean difference is smaller than the variation in f among subjects.

journal_name

Eur J Clin Pharmacol

authors

Schaaf LJ,Campbell SC,Mayersohn MB,Vagedes T,Perrier DG

doi

10.1007/BF00637630

subject

Has Abstract

pub_date

1987-01-01 00:00:00

pages

355-61

issue

4

eissn

0031-6970

issn

1432-1041

journal_volume

33

pub_type

临床试验,杂志文章,随机对照试验
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