KETOCONAZOLE - A POTENT INHIBITOR OF CYTOCHROME P-450-DEPENDENT DRUG-METABOLISM IN RAT-LIVER
- 1 January 1984
- journal article
- research article
- Vol. 12 (5), 603-606
Abstract
Ketoconazole, an orally active imidazole antimycotic agent, is a potent inhibitor of drug N-demethylase activities of liver microsomes from rats pretreated with phenobarbital or pregnenolone-16.alpha.-carbonitrile, and an inhibitor of 7-ethoxyresorufin O-deethylase activity of liver microsomes from rats pretreated with 5,6-benzoflavone. Spectrophotometric studies reveal that the imidazole compound binds to the cytochrome P-450 component of the monooxygenase complex, and has little effect on NADPH-cytochrome c (P-450) reductase activity. Cytochrome P-450 is apparently the site of action of this potent inhibitor of drug metabolism in liver microsomes.This publication has 6 references indexed in Scilit:
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