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

Authors
 Sung Kweon Cho  ;  Choon Ok Kim  ;  Eun Seok Park  ;  Jae-Yong Chung 
Citation
 BRITISH JOURNAL OF CLINICAL PHARMACOLOGY, Vol.78(6) : 1426-1432, 2014 
Journal Title
 BRITISH JOURNAL OF CLINICAL PHARMACOLOGY 
ISSN
 0306-5251 
Issue Date
2014
MeSH
Adult ; Blood Glucose/analysis ; Drug Interactions ; Humans ; Hypoglycemic Agents/pharmacology* ; Male ; Metformin/pharmacokinetics ; Metformin/pharmacology* ; Organic Cation Transport Proteins/antagonists & inhibitors ; Organic Cation ; Transporter 1/antagonists & inhibitors ; Verapamil/pharmacology*
Keywords
OCT1 ; drug interaction ; metformin ; verapamil
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 (ΔGmax ) by 62.5% (P = 0.008) and decreased the area under the glucose concentration-time curve (ΔAUCgluc ) 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.
Files in This Item:
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DOI
10.1111/bcp.12476
Appears in Collections:
1. College of Medicine (의과대학) > Dept. of Pharmacology (약리학교실) > 1. Journal Papers
Yonsei Authors
Kim, Choon Ok(김춘옥) ORCID logo https://orcid.org/0000-0002-2319-1108
Cho, Sung Kweon(조성권)
URI
https://ir.ymlib.yonsei.ac.kr/handle/22282913/165028
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