Inhibitory Effect of Glyburide on Human Cytochrome P450 Isoforms in Human Liver Microsomes

Abstract

This article is available online at http://dmd.aspetjournals.org ABSTRACT:The However, glyburide showed no appreciable inhibitory effect on CYP1A2, CYP2C8, CYP2C19, CYP2E1, or CYP2D6. In summary, glyburide showed potent inhibition on CYP2C9 and weak inhibition on CYP3A4, whereas it had minimal or no inhibitory effect on the other cytochromes P450 examined. It is anticipated that clinically significant drug-drug interactions will ensue when glyburide is coadministered with agents that are cleared primarily by the CYP2C9-mediated pathway and those with narrow therapeutic ranges.

Impact of Age, CYP2C9 Genotype and Concomitant Medication on the Rate of Rise for Prothrombin Time During the First 30 Days of Warfarin Therapy

“…30 Like warfarin, most sulfonylureas are also metabolized by CYP2C9. Sulfonylurea use is known to inhibit the metabolism of other drugs in a competitive fashion, 31,32 and sulfonylureas are often used as probe substrates for CYP2C9 activity. 33,34 The potential for a warfarin-sulfonylurea drug interaction is therefore substantial.…”

Inhibition of cytochrome P450 activities by oleanolic acid and ursolic acid in human liver microsomes

“…After preincubation, probe substrates were added either with or without the NADPH-regenerating system. The incubation conditions, including incubation times, concentration of microsomes, probe substrate concentrations, and quenching methods, have been reported elsewhere (Shin et al, 2002;Kim and Park, 2003;Park and Kim, 2003). The time of incubation and concentration of microsomes used in each assay were determined to be in the linear range for the rate of metabolite formation.…”

Pseudoporphyria induced by voriconazole

“…CYP3A4 is inhibited by diltiazem 61 and glyburide. 59 Thus there are multiple potential competitive drug interactions that could lead to increased concentrations of voriconazole, thereby increasing the risk of pseudoporphyria.…”