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PMID: 1233266 Published · ppublish English Journal Article

Induction of drug metabolism in man after rifampicin treatment measured by increased hexobarbital and tolbutamide clearance.

European journal of clinical pharmacology ·Vol. 9 ·No. 2-3 ·1975-12-19 ·Pages 219-27

Zilly W, Breimer DD, Richter E

Abstract

Five healthy volunteers took 1.2 g rifampicin daily for 8 days, and before and afterwards each received hexobarbital (7.32 mg/kg) and tolbutamide (20 mg/kg) by i.v. infusion on two consecutive days. The plasma concentrations of the two drugs were determined during and after infusion. The average elimination half-life of hexobarbital had decreased from 325 to 122 min and of tolbutamide from 418 to 183 min following rifampicin treatment. It was calculated that the metabolic clearance of hexobarbital had increased about three-fold and that of tolbutamide more than two-fold. Significant changes in the distribution kinetics of the two drugs were not observed. The results suggest that rifampicin is capable of inducing drug metabolism in man, which leads to an increased rate of elimination of drugs that undergo biotransformation in the liver.

MeSH Terms
Adult Creatine/blood Half-Life Hexobarbital/metabolism Humans Kinetics Liver Function Tests Male Metabolic Clearance Rate Models, Biological Rifampin/pharmacology Tolbutamide/metabolism
Chemicals
Tolbutamide Hexobarbital Creatine Rifampin
Authors & Affiliations
3 authors, click to expand affiliations / ORCID
Zilly W
Breimer D D
Richter E
References (31)
31 references, click to expand
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Article Info
Journal
European journal of clinical pharmacology
Abbr.
Eur J Clin Pharmacol
ISSN
0031-6970
DOI
10.1007/BF00614021
Published
1975-12-19
Pages
219-27
Language
English
Region
Germany
NLM ID
1256165
Subset
IM
External Links
PubMed source DOI: 10.1007/BF00614021 View journal details
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