Inhibition of the metabolism of brotizolam by erythromycin in humans: in vivo evidence for the involvement of CYP3A4 in brotizolam metabolism.

Abstract:

AIMS:To obtain in vivo evidence for the involvement of cytochrome P450 (CYP) 3A4 in the metabolism of brotizolam. METHODS:Fourteen healthy male volunteers received erythromycin 1200 mg day(-1) or placebo for 7 days in a double-blind randomized crossover manner. On the 6th day they received a single oral 0.5-mg dose of brotizolam, and blood samplings were performed for 24 h. RESULTS:Erythromycin treatment significantly increased the peak plasma concentration (P < 0.05), total area under the plasma concentration-time curve (P < 0.01), and elimination half-life (P < 0.01) of brotizolam. CONCLUSIONS:The present study provides in vivo evidence for the involvement of CYP3A4 in brotizolam metabolism.

journal_name

Br J Clin Pharmacol

authors

Tokairin T,Fukasawa T,Yasui-Furukori N,Aoshima T,Suzuki A,Inoue Y,Tateishi T,Otani K

doi

10.1111/j.1365-2125.2005.02380.x

keywords:

subject

Has Abstract

pub_date

2005-08-01 00:00:00

pages

172-5

issue

2

eissn

0306-5251

issn

1365-2125

pii

BCP2380

journal_volume

60

pub_type

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