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

 S K Cho  ;  J S Yoon  ;  M G Lee  ;  D H Lee  ;  L A Lim  ;  K Park  ;  M S Park  ;  J-Y Chung 
 Clinical Pharmacology & Therapeutics, Vol.89(3) : 416-421, 2011 
Journal Title
 Clinical Pharmacology & Therapeutics 
Issue Date
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.
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1. College of Medicine (의과대학) > Dept. of Pharmacology (약리학교실) > 1. Journal Papers
1. College of Medicine (의과대학) > Dept. of Pediatrics (소아청소년과학교실) > 1. Journal Papers
Yonsei Authors
Park, Kyungsoo(박경수) ORCID logo https://orcid.org/0000-0002-6972-1143
Park, Min Soo(박민수) ORCID logo https://orcid.org/0000-0002-4395-9938
Lee, Dong Hwan(이동환)
Lee, Min Goo(이민구) ORCID logo https://orcid.org/0000-0001-7436-012X
Lim, Lay Ahyoung(임아영)
Chung, Jae Yong(정재용)
Cho, Sung Kweon(조성권)
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