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Rifampin enhances the glucose-lowering effect of metformin and increases OCT1 mRNA levels in healthy participants

Authors
 S K Cho ; J S Yoon ; J-Y Chung ; M S Park ; K Park ; L A Lim ; D H Lee ; M G Lee 
Citation
 Clinical Pharmacology & Therapeutics, Vol.89(3) : 416~421, 2011 
Journal Title
 Clinical Pharmacology & Therapeutics 
ISSN
 0009-9236 
Issue Date
2011
Abstract
We evaluated the effect of the pregnane X receptor (PXR) agonist rifampin on metformin pharmacokinetics, organic cation transporter 1 (OCT1) and OCT2 mRNA levels, and glucose levels, using the oral glucose tolerance test (OGTT) in 16 healthy subjects. The glucose-lowering effects of metformin were evaluated by OGTT before and after metformin treatment on days 1 and 2 and again on days 13 and 14 after a 10-day course of rifampin. Rifampin increased the difference in maximum glucose levels (ΔG(max)) by 41.9% (P = 0.024) and the area under the concentration-time curve (AUC) during the first 60 min after glucose ingestion (ΔAUC(gluc60)) by 54.5% (P = 0.020). Renal clearance (CL(R)) of metformin was increased by 16% (P = 0.008), but the systemic exposure was only slightly increased (13%, P = 0.049), possibly because of increased absorption. Rifampin increased OCT1 mRNA levels 4.1-fold in peripheral blood cells (P = 0.001); however, OCT2 mRNA was not detected. Our results suggest that rifampin increases OCT1 expression and hepatic uptake of metformin, leading to enhanced glucose-lowering action.
URI
http://ir.ymlib.yonsei.ac.kr/handle/22282913/92771
DOI
10.1038/clpt.2010.266
Appears in Collections:
1. 연구논문 > 1. College of Medicine > Dept. of Pharmacology
1. 연구논문 > 1. College of Medicine > Dept. of Pediatrics
Yonsei Authors
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Link
 http://www.nature.com/clpt/journal/v89/n3/full/clpt2010266a.html
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