Comparative effects of rifabutin and rifampicin on hepatic microsomal enzyme activity in normal subjects.

Abstract:

:The comparative enzyme inducing effects of rifabutin and the chemically related drug rifampicin have been investigated in 8 normal subjects. Rifampicin 600 mg daily for 7 days caused considerable shortening of the antipyrine half-life and a marked increase in antipyrine clearance, associated with an increased rate of conversion to norantipyrine and, to a lesser extent, 4-hydroxyantipyrine and 3-hydroxymethylantipyrine. The urinary excretion of 6-beta-hydroxycortisol was also markedly increased, while plasma GGT activity showed only a slight albeit statistically significant elevation. In the same subjects, rifabutin in the proposed therapeutic dosage (300 mg daily) for 7 days also enhanced the metabolic elimination of antipyrine, with preferential stimulation of the demethylation pathway, and increased the excretion of 6-beta-hydroxycortisol, but the magnitude of the effects was significantly less than after rifampicin. No significant change in plasma GGT was seen. The results indicate that, contrary to the findings in animals, rifabutin does have enzyme inducing properties in man, although at the dosages assessed they were considerably less than those of rifampicin.

journal_name

Eur J Clin Pharmacol

authors

Perucca E,Grimaldi R,Frigo GM,Sardi A,Mönig H,Ohnhaus EE

doi

10.1007/BF00615223

subject

Has Abstract

pub_date

1988-01-01 00:00:00

pages

595-9

issue

6

eissn

0031-6970

issn

1432-1041

journal_volume

34

pub_type

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