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Loxapine P-glycoprotein Interactions in Vitro

Loxapine P-glycoprotein Interactions in Vitro

Andrea Reed, Keith Huie, Elke S Perloff, James V Cassella, Lori H Takahashi

Drug Metab Lett. 2012 Mar;6(1):26-32.

PMID: 22300294

Abstract:

The antipsychotic drugs risperidone, paliperidone, olanzapine, quetiapine, aripiprazole, clozapine, haloperidol, and chlorpromazine have been reported to have various degrees of interaction (substrate or inhibitor) with the multidrug resistance transporter, P-glycoprotein (P-gp). An interaction of the antipsychotic drug loxapine with P-gp was recently reported, but an IC50 value was not determined. Loxapine (as the succinate salt) was evaluated as a P-gp substrate, and inhibitor of P-gp mediated transport of digoxin in vitro in Caco-2 cells. Loxapine was not a substrate for P-gp but did exhibit weak-to-moderate inhibition (IC50 = 9.1 μM). Since the typical steady state maximal plasma concentrations of loxapine in clinical use have been reported to be in the nanomolar range, pharmacokinetic interactions due to the inhibition of P-gp activity are not expected.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP27833643-B	Loxapine succinate salt		27833-64-3	Price

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