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Eur J Pharmacol. 2008 Jan 28;579(1-3):104-9. Epub 2007 Nov 13.

Comparison of the induction of P-glycoprotein activity by nucleotide, nucleoside, and non-nucleoside reverse transcriptase inhibitors.

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Department of Internal Medicine VI, Clinical Pharmacology and Pharmacoepidemiology, University of Heidelberg, Im Neuenheimer Feld 410, D-69120 Heidelberg, Germany.


Combination therapy against human immunodeficiency virus (HIV)-infection is complicated by drug-drug interactions between antiretrovirals and also between anti-HIV drugs and drugs used to treat co-morbidity. P-glycoprotein represents one important site for drug interactions and induction of its function could reduce the effectiveness of drugs that are P-glycoprotein substrates. We therefore investigated induction of P-glycoprotein function in LS180 cells by non-nucleoside and nucleoside reverse transcriptase inhibitors (NNRTIs and NRTIs) and tenofovir as essential components of antiretroviral combination therapy. P-glycoprotein activity was increased by all NNRTIs and some NRTIs with delavirdine (5.3-fold at 100 muM) having the largest effect.

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