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

被引：52

作者：

Weiss, Johanna ^{[1
]}

Weis, Nicola ^{[1
]}

Ketabi-Kiyanvash, Nahal ^{[1
]}

Storch, Caroline H. ^{[1
]}

Haefeli, Walter E. ^{[1
]}

机构：

[1] Univ Heidelberg, Dept Internal Med 4, D-69120 Heidelberg, Germany

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 2008年 / 579卷 / 1-3期

关键词：

P-glycoprotein; NNRTIs (non-nucleoside reverse transcriptase inhibitors); NRTIs (nucleoside reverse transcriptase inhibitors); NtRTI (nucleotide reverse transcriptase inhibitor); induction; drug interactions;

D O I：

10.1016/j.ejphar.2007.11.007

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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 mu M) having the largest effect. (C) 2007 Elsevier B.V. All rights reserved.

引用

页码：104 / 109

页数：6

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