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Vol. 29, Issue 7, 954-956, July 2001

SHORT COMMUNICATION
Methadone Inhibits Rhodamine123 Transport in Caco-2 Cells

Elke Störmer, Michael D. Perloff, Lisa L. von Moltke, and David J. Greenblatt

Department of Pharmacology
and Experimental Therapeutics,
Tufts University School of Medicine,
Boston, Massachusetts

This study investigated the effects of racemic methadone (MET) on P-glycoprotein (P-gp) activity in cell culture. MET showed no differential rates of passage between the basolateral to apical (B to A) and apical to basolateral (A to B) direction across Caco-2 cell monolayers in a transwell system. MET transport in either direction was not importantly influenced by the P-gp inhibitor verapamil. However, MET was a potent inhibitor (IC50 = 7.5 µM) of rhodamine123 B to A transport across Caco-2 cell monolayers, causing a reduction to 25% of control at 100 µM MET. In this model of Caco-2 monolayers, rates of MET passage between B to A and A to B directions could not be distinguished. However, MET can inhibit P-gp activity at intraluminal concentrations that might be achieved clinically. This may lead to increased bioavailability of coadministered compounds.

Copyright © 2001 by The American Society for Pharmacology and Experimental Therapeutics


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Copyright © 2001 by the American Society for Pharmacology and Experimental Therapeutics.