INHIBITORY EFFECT OF DILTIAZEM ON DIAZEPAM METABOLISM IN THE MOUSE HEPATIC MICROSOMES

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 const...

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Veröffentlicht in:	Biological & pharmaceutical bulletin 1993/03/15, Vol.16(3), pp.331-333
Hauptverfasser:	IHARA, Norihiko, KOKUFU, Takatoshi, SUGIOKA, Nobuyuki, OHTA, Toshio, NOSAKA, Kazuto
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antianginal agents. Coronary vasodilator agents Biological and medical sciences Cardiovascular system cytochrome P-450 Cytochrome P-450 Enzyme Inhibitors Cytochrome P-450 Enzyme System diazepam Diazepam - metabolism Diazepam - pharmacokinetics diltiazem Diltiazem - pharmacology drug interaction enzyme inhibition In Vitro Techniques Male Medical sciences Mice Mice, Inbred Strains Microsomes, Liver - drug effects Microsomes, Liver - metabolism Nordazepam - metabolism Oxidoreductases, N-Demethylating - antagonists & inhibitors Pharmacology. Drug treatments
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Zusammenfassung:	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.
ISSN:	0918-6158 1347-5215
DOI:	10.1248/bpb.16.331