Trimethoprim-metformin interaction and its genetic modulation by OCT2 and MATE1 transporters.

ABSTRACT:

Aims

Metformin pharmacokinetics depends on the presence and activity of membrane-bound drug transporters and may be affected by transport inhibitors. The aim of this study was to investigate the effects of trimethoprim on metformin pharmacokinetics and genetic modulation by organic cation transporter 2 (OCT2) and multidrug and toxin extrusion 1 (MATE1) polymorphisms.

Methods

Twenty-four healthy volunteers received metformin 500 mg three times daily for 10 days and trimethoprim 200 mg twice daily from day 5 to 10. Effects of trimethoprim on steady-state metformin pharmacokinetics were analysed.

Results

In the population as a whole, trimethoprim significantly reduced the apparent systemic metformin clearance (CL/F) from 74 to 54 l h(-1) and renal metformin clearance fro

SUBMITTER: Grun B 

PROVIDER: S-EPMC3853537 | biostudies-literature | 2013 Nov

REPOSITORIES: biostudies-literature