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

Autor: Tokairin, Takaki, Fukasawa, Takashi, Yasui-Furukori, Norio, Aoshima, Toshiaki, Suzuki, Akihito, Inoue, Yoshimasa, Tateishi, Tomonori, Otani, Koichi
Předmět:
Zdroj: British Journal of Clinical Pharmacology; Aug2005, Vol. 60 Issue 2, p172-175, 4p
Abstrakt: To obtain in vivo evidence for the involvement of cytochrome P450 (CYP) 3A4 in the metabolism of brotizolam. 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. 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. The present study provides in vivo evidence for the involvement of CYP3A4 in brotizolam metabolism. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index