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Trends Pharmacol Sci. 2012 Jun;33(6):312-22. doi: 10.1016/ Epub 2012 Apr 2.

Drug interactions with oral antidiabetic agents: pharmacokinetic mechanisms and clinical implications.

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Department of Clinical Pharmacology, University of Helsinki and HUSLAB, Helsinki University Central Hospital, Tukholmankatu 8C, FIN-00290 Helsinki, Finland.


There is a growing epidemic of type 2 diabetes (T2DM), and it is associated with various comorbidities. Patients with T2DM are usually treated with multiple drugs, and are therefore at an increased risk of harmful drug-drug interactions (DDIs). Several potentially life-threatening DDIs concerning oral antidiabetic drugs have been identified. This has mostly been initiated by case reports but, more recently, the understanding of their mechanisms has greatly increased. In this article, we review the pharmacokinetic DDIs concerning oral antidiabetics, including metformin, sulfonylureas, meglitinide analogs, thiazolidinediones and dipeptidyl peptidase-4 inhibitors, and the underlying mechanistic basis that can help to predict and prevent DDIs. In particular, the roles of membrane transporters and cytochrome P450 (CYP) enzymes in these DDIs are discussed.

[Indexed for MEDLINE]

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