Title : Kinetic characterization and identification of the enzymes responsible for the hepatic biotransformation of adinazolam and N-desmethyladinazolam in man.

Pub. Date : 1998 Mar

PMID : 9600717






2 Functional Relationships(s)
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1 Ketoconazole, a relatively specific CYP 3A4 inhibitor, inhibited the reaction; the concentration resulting in 50% of maximum inhibition, IC50, was 0.15 microM and the inhibition constant, Ki, was < 0.04 microM in five of six livers tested. Ketoconazole cytochrome P450 family 4 subfamily F member 3 Homo sapiens
2 Co-administration of adinazolam with CYP 3A4 inhibitors such as ketoconazole or erythromycin might lead to reduced efficacy, since adinazolam by itself has relatively weak benzodiazepine agonist activity, with much of the pharmacological activity of adinazolam being attributable to its active metabolite NDMAD. Ketoconazole cytochrome P450 family 4 subfamily F member 3 Homo sapiens