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
收藏
页码：104 / 109
页数：6
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