Characterization of kinetics of human cytochrome P450s involved in bioactivation of flucloxacillin: inhibition of CYP3A ‐catalyzed hydroxylation by sulfaphenazole

Conclusions and implicationsThe combined results show that the 5 ’‐hydroxylation of FLX is primarily catalysed by CYP3A4, CYP3A7 and CYP2C9. The large variability of the hepatic expression of these enzymes could affect the formation of 5’‐hydroxymethylfucloxacillin, which may determine the differences in susceptibility to flucloxacillin‐induced liver in jury. Additionally, the strong inhibition in CYP3A‐catalyzed flucloxacillin metabolism by sulfaphenazole suggest that unanticipated drug‐drug interactions could occur with coadministered drugs.

Source: British Journal of Pharmacology - November 17, 2018 Category: Drugs & Pharmacology Authors: Stefan J Dekker, Floor Dohmen, Nico P E Vermeulen, Jan N M Commandeur Tags: RESEARCH PAPER Source Type: research