Efavirenz

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Efavirenz, a non-nucleoside reverse transcriptase inhibitor.

Efavirenz (EFV) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) and is used as part of highly active antiretroviral therapy (HAART) for the treatment HIV-1. It is a synthetic purine derivative similar to zidovudine, zalcitabine, and stavudine. Efavirenz and lamivudine with either zidovudine or tenofovir is the preferred NNRTI-based regimen for HIV infections not previously treated. It is also used in combination with other anti-HIV drugs in expanded prophylactic treatment upon possible HIV exposure. It is sold under the brand names Sustiva® and Stocrin®.

Its IUPAC chemical name is (4S)-6-chloro-4-(2-cyclopropylethynyl)-4-(trifluoromethyl)-1H-3,1-benzoxazin-2-one and its chemical formula is C14H9ClF3NO2 (MW = ).


Drug interactions

St. John's Wort and saquinavir decrease the antiretroviral effects of efavirenz, and efavirenz decreases the levels and/or effects of atazanavir, clarithromycin, cyclosporin, indinavir, methadone and voriconazole.

Efavirenz may increase the toxicity of ergot derivatives, including dihydroergotamine, dihydroergotoxine, ergotamine, methylergonovine and methysergide and some statin drugs, including atorvastatin, lovastatin and simavstatin. An increased risk of cardiotoxicity and arrhythmias occurs when efavirenz is taken with astemizole or cisapride or terfenadine. Increased toxicity of benzodiazepine is noted when taken with alprazolam, midazolam or triazolam.

External Links

  • {{DailyMed}