Ritonavir, efavirenz, and nelfinavir inhibit CYP2B6 activity in vitro: potential drug interactions with bupropion.

Article Details

Citation

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
DrugEnzymeKindOrganismPharmacological ActionActions
AmprenavirCytochrome P450 2B6ProteinHumans
Unknown
Inhibitor
Details
EfavirenzCytochrome P450 2B6ProteinHumans
Unknown
Substrate
Inducer
Details
NelfinavirCytochrome P450 2B6ProteinHumans
Unknown
Inhibitor
Details
RitonavirCytochrome P450 2B6ProteinHumans
No
Inhibitor
Inducer
Details
Drug Interactions
DrugsInteraction
Bupropion
Ritonavir
The metabolism of Bupropion can be increased when combined with Ritonavir.
Interactions
Improve patient outcomes
Build effective decision support tools with the industry’s most comprehensive drug-drug interaction checker.
Learn more