Ritonavir, efavirenz, and nelfinavir inhibit CYP2B6 activity in vitro: potential drug interactions with bupropion.
Article Details
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Hesse LM, von Moltke LL, Shader RI, Greenblatt DJ
Ritonavir, efavirenz, and nelfinavir inhibit CYP2B6 activity in vitro: potential drug interactions with bupropion.
Drug Metab Dispos. 2001 Feb;29(2):100-2.
- PubMed ID
- 11159797 [ View in PubMed]
- 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 (microM) 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.
DrugBank Data that Cites this Article
- Drug Enzymes
Drug Enzyme Kind Organism Pharmacological Action Actions Amprenavir Cytochrome P450 2B6 Protein Humans UnknownInhibitorDetails Efavirenz Cytochrome P450 2B6 Protein Humans UnknownSubstrateInducerDetails Nelfinavir Cytochrome P450 2B6 Protein Humans NoInhibitorDetails Ritonavir Cytochrome P450 2B6 Protein Humans NoInhibitorInducerDetails - Drug Interactions