Verapamil decreases the glucose-lowering effect of metformin in healthy volunteers.

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Cho SK, Kim CO, Park ES, Chung JY

Verapamil decreases the glucose-lowering effect of metformin in healthy volunteers.

Br J Clin Pharmacol. 2014 Dec;78(6):1426-32. doi: 10.1111/bcp.12476.

PubMed ID

25060604 [ View in PubMed

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Abstract

AIM: The organic cation transporter 1 (OCT1) plays a key role in the cellular transport of metformin and its subsequent glucose-lowering effect. A recent non-clinical study reported that metformin uptake into hepatocytes is regulated via OCT1, and that uptake was strongly inhibited by verapamil. Therefore, we investigated the effects of verapamil co-administration on the pharmacokinetics and pharmacodynamics of metformin in humans. METHODS: We evaluated the pharmacokinetics and the anti-hyperglycaemic effects of metformin using an oral glucose tolerance test (OGTT) in 12 healthy participants, before (day 1) and after metformin treatment (day 2), and again on days 15 and 16 after co-administration with verapamil. RESULTS: Verapamil inhibited the ability of metformin to reduce maximum blood glucose concentrations (DeltaGmax ) by 62.5% (P = 0.008) and decreased the area under the glucose concentration-time curve (DeltaAUCgluc ) by 238% (P = 0.015). However, verapamil did not significantly alter the Cmax and the AUC of metformin, nor its renal clearance. CONCLUSIONS: Our results suggest that verapamil remarkably decreases the glucose-lowering effect of metformin, possibly by acting as a competitive inhibitor of OCT1.

DrugBank Data that Cites this Article

Drug Transporters

Drug	Transporter	Kind	Organism	Pharmacological Action	Actions
Verapamil	Solute carrier family 22 member 1	Protein	Humans	Unknown	Inhibitor	Details

Drug Interactions

Drugs	Interaction
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