Efavirenz Bupropion

B6 Artemisinin, bupropion, cyclophosphamide, efavirenz, ifosfamide, ketamine, S-mephobarbital, S-mephenytoin (/V-demethylation to nirvanol), methadone, nevirapine, propofol, selegiline, sertraline, ticlopidine Phenobarbital, cyclophosphamide Ticlopidine, clopidogrel... 

The query used is labeled multiple objects and is available under the section Dmg Queries (Fig. 1). The objects used for the search are bupropion and efavirenz. 

Figure 2 List of precipitants evaluated with the substrates bupropion and efavirenz and which have shown more than 20% effect in in vivo inhibition. Display from the Metabolism and Transport Drug Interaction Database (http //www.druginteractioninfo...

Substrates shown to be at least partially metabolized by CYP2B6. bBold Inhibitor tested in vivo and in vitro with bupropion or efavirenz. Italic In vitro Inhibitors with no effects in vivo on efavirenz. 

BUPROPION 1. ANTICANCER DRUGS - thiotepa 2. ANTIDEPRESSANTS-fluoxetine, fluvoxamine, paroxetine, sertraline 3. ANTIVIRALS - efavirenz, protease inhibitors t plasma concentrations of bupropion and risk of adverse effects Inhibition of CYP2B6 Warn patients about adverse effects and use alternatives when possible. Avoid co-administration of bupropion with protease inhibitors. Co-adminis-ter efavirenz and bupropion with caution. A retrospective study showed that two patients received a combination without reported adverse effects. Potential T risk of seizures... 

Ritonavir, efavirenz and nelfinavir inhibit the cytochrome P450 isoenzyme CYP2B6 in vitro and may, theoretically, increase bupropion levels. However, an in vivo study su ests that ritonavir may decrease bupropion levels. 

One diagnostic substrate is efavirenz [569], which also has clinical issues (Sect. 7.7.7, vide infra). Perhaps the most widely accepted reference substrate for P450 2B6 (in vitro) is bupropion [570, 571]. Efavirenz has been utilized as a marker in vivo [572]. 

Some of the clinical issues have been reviewed recently by Zanger and Klein [607]. The major issues are interindividual variations due to induction and genetic variation as well as some inhibitions. The effects of genetic variation have been reported for the drag efavirenz (used for HIV) [608-611]. Another drag in which genetic variations make an in vivo difference is bupropion, used in smoking cessation therapy [612, 613]. Efavirenz-bupropion interactions have also been reported [614]. 

Robertson SM, Maldarelli F, Natarajan V, Formen-tini E, Alfaro RM, Penzak SR (2008) Efavirenz induces CYP2B6-mediated hydroxylation of bupropion in healthy subjects. J Acquir Immune Defic Syndr 49 513-519... 

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