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Inhibition of the metabolism of brotizolam by erythromycin in humans: in vivo evidence for the involvement of CYP3A4 in brotizolam metabolism
Author(s) -
Tokairin Takaki,
Fukasawa Takashi,
YasuiFurukori Norio,
Aoshima Toshiaki,
Suzuki Akihito,
Inoue Yoshimasa,
Tateishi Tomonori,
Otani Koichi
Publication year - 2005
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.2005.02380.x
Subject(s) - cyp3a4 , crossover study , placebo , erythromycin , in vivo , pharmacokinetics , medicine , metabolism , endocrinology , pharmacology , chemistry , cytochrome p450 , biology , antibiotics , biochemistry , microbiology and biotechnology , alternative medicine , pathology
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.