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Ritonavir, Efavirenz, and Nelfinavir Inhibit CYP2B6 Activity in Vitro: Potential Drug Interactions with Bupropion

Ritonavir, Efavirenz, and Nelfinavir Inhibit CYP2B6 Activity in Vitro: Potential Drug... Abstract Since antiretroviral drugs are known to inhibit many cytochrome P450 isoforms, the inhibition of CYP2B6 by non-nucleoside reverse transcriptase inhibitors and viral protease inhibitors was studied in vitro in human liver microsomes using bupropion hydroxylation as the CYP2B6 index reaction. Mean IC 50 values (μM) for inhibition of bupropion hydroxylation were: nelfinavir (2.5), ritonavir (2.2), and efavirenz (5.5). The reaction was only weakly inhibited by indinavir, saquinavir, amprenavir, delavirdine, and nevirapine. The inhibition of bupropion hydroxylation in vitro by nelfinavir, ritonavir, and efavirenz indicates inhibitory potency versus CYP2B6 and suggests the potential for clinical drug interactions. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Drug Metabolism and Disposition Am. Soc for Pharma & Experimental Therapeutics

Ritonavir, Efavirenz, and Nelfinavir Inhibit CYP2B6 Activity in Vitro: Potential Drug Interactions with Bupropion

Ritonavir, Efavirenz, and Nelfinavir Inhibit CYP2B6 Activity in Vitro: Potential Drug Interactions with Bupropion

Drug Metabolism and Disposition , Volume 29 (2): 100 – Feb 1, 2001

Abstract

Abstract Since antiretroviral drugs are known to inhibit many cytochrome P450 isoforms, the inhibition of CYP2B6 by non-nucleoside reverse transcriptase inhibitors and viral protease inhibitors was studied in vitro in human liver microsomes using bupropion hydroxylation as the CYP2B6 index reaction. Mean IC 50 values (μM) for inhibition of bupropion hydroxylation were: nelfinavir (2.5), ritonavir (2.2), and efavirenz (5.5). The reaction was only weakly inhibited by indinavir, saquinavir, amprenavir, delavirdine, and nevirapine. The inhibition of bupropion hydroxylation in vitro by nelfinavir, ritonavir, and efavirenz indicates inhibitory potency versus CYP2B6 and suggests the potential for clinical drug interactions.

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Publisher
Am. Soc for Pharma & Experimental Therapeutics
Copyright
Copyright © Drug Metabolism and Disposition
ISSN
0090-9556
eISSN
1521-009X
Publisher site

Abstract

Abstract Since antiretroviral drugs are known to inhibit many cytochrome P450 isoforms, the inhibition of CYP2B6 by non-nucleoside reverse transcriptase inhibitors and viral protease inhibitors was studied in vitro in human liver microsomes using bupropion hydroxylation as the CYP2B6 index reaction. Mean IC 50 values (μM) for inhibition of bupropion hydroxylation were: nelfinavir (2.5), ritonavir (2.2), and efavirenz (5.5). The reaction was only weakly inhibited by indinavir, saquinavir, amprenavir, delavirdine, and nevirapine. The inhibition of bupropion hydroxylation in vitro by nelfinavir, ritonavir, and efavirenz indicates inhibitory potency versus CYP2B6 and suggests the potential for clinical drug interactions.

Journal

Drug Metabolism and DispositionAm. Soc for Pharma & Experimental Therapeutics

Published: Feb 1, 2001

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