文章基本信息

标题：INHIBITORY EFFECT OF DILTIAZEM ON DIAZEPAM METABOLISM IN THE MOUSE HEPATIC MICROSOMES
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作者：Norihiko IHARA ; Takatoshi KOKUFU ; Nobuyuki SUGIOKA 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1993
卷号：16
期号：3
页码：331-333
DOI：10.1248/bpb.16.331
出版社：The Pharmaceutical Society of Japan
摘要：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(K_i) 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.
关键词：cytochrome P-450;enzyme inhibition;diltiazem;drug interaction;diazepam