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glyburide + fluconazole + rifampin is a drug combination used in a Phase 1 pharmacokinetic drug-drug interaction study conducted by the University of California, San Francisco. The study investigated the complex effects of metabolic and transporter-mediated interactions on glyburide, a second-generation sulfonylurea used for type 2 diabetes mellitus. Glyburide works by inhibiting ATP-sensitive potassium channels in pancreatic beta cells to stimulate insulin release. Fluconazole acts as a CYP2C9 inhibitor, while rifampin serves as both an acute inhibitor of hepatic uptake transporters (OATP) and a chronic inducer of CYP2C9 enzymes. This research aimed to understand how these co-administered drugs alter glyburide exposure and its glucose-lowering efficacy.
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