Biological and Pharmaceutical Bulletin
Online ISSN : 1347-5215
Print ISSN : 0918-6158
ISSN-L : 0918-6158
INHIBITORY EFFECT OF DILTIAZEM ON DIAZEPAM METABOLISM IN THE MOUSE HEPATIC MICROSOMES
井原 憲彦国府 孝敏杉岡 信幸太田 利夫野坂 和人
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1993 年 16 巻 3 号 p. 331-333

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In order to elucidate the drug interaction between diltiazem and diazepam, the effect of diltiazem on the N-demethylation of diazepam in the mouse hepatic microsomes was investigated. Kinetic study showed that diltiazem noncompetitively inhibited the N-demethylation of diazepam with inhibition constant(Ki) value of 247.8 μM, indicating that diltiazem exhibits an inhibitory effect on the hepatic oxidative metabolism of diazepam. It was therefore suggested that diltiazem may impair the metabolism of diazepam in vivo.

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