Methadone inhibits rhodamine123 transport in Caco-2 cells.

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Stormer E, Perloff MD, von Moltke LL, Greenblatt DJ

Methadone inhibits rhodamine123 transport in Caco-2 cells.

Drug Metab Dispos. 2001 Jul;29(7):954-6.

PubMed ID

11408360 [ View in PubMed

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Abstract

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 (IC(50) = 7.5 microM) of rhodamine123 B to A transport across Caco-2 cell monolayers, causing a reduction to 25% of control at 100 microM 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.

DrugBank Data that Cites this Article

Drug Transporters

Drug	Transporter	Kind	Organism	Pharmacological Action	Actions
Methadone	P-glycoprotein 1	Protein	Humans	Unknown	Inhibitor	Details

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Methadone	P-glycoprotein 1	IC 50 (nM)	7500	N/A	N/A	Details