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Generic Name and Formulations:
Efavirenz 50mg, 200mg; caps.
Indications for SUSTIVA:
HIV-1 infection, in combination with other antiretroviral agents.
Adults and Children:
Swallow whole; do not break tabs. If unable to swallow tabs or caps: may sprinkle capsule content and mix in 1–2tsps of soft food (eg, applesauce, grape jelly, yogurt) or 2tsps of room temperature infant formula; administer within 30mins of mixing. Give once daily on an empty stomach, preferably at bedtime. Consider pretreating with antihistamine (for children) or steroid to minimize rash. <3mos or <3.5kg: not recommended. ≥3mos (3.5kg to <5kg): 100mg; (5kg to <7.5kg): 150mg; (7.5kg to <15kg): 200mg; (15kg to <20kg): 250mg; (20kg to <25kg): 300mg; (25kg to <32.5kg): 350mg; (32.5kg to <40kg): 400mg; (≥40kg) and adults: 600mg. Concomitant voriconazole: increase voriconazole maintenance dose to 400mg every 12hrs and decrease efavirenz dose to 300mg once daily using capsule form. Concomitant rifampin (patient ≥50kg): increase efavirenz dose to 800mg once daily.
CNS or psychiatric disturbances. QTc prolongation. Underlying hepatic disease (including hepatitis B or C coinfection). Hepatic impairment: moderate or severe: not recommended; mild: monitor. Monitor liver function before and during therapy in all patients; consider discontinuing in persistent serum transaminase elevations to >5×ULN and discontinue if elevation is accompanied by signs/symptoms of hepatitis or hepatic decompensation. History of seizures. Monitor cholesterol and triglycerides before starting and periodically thereafter. Discontinue if severe rash (w. blistering, desquamation, mucosal involvement, or fever) occurs. Obtain (–) pregnancy test before starting; use adequate (barrier + hormonal) contraception during and for 12 weeks after discontinuation. Elderly. Embryo-fetal toxicity. Pregnancy: avoid (esp. during 1st trimester). Nursing mothers: not recommended.
Avoid concomitant other efavirenz-containing products (eg, Atripla unless needed for dose adjustment with rifampin), atazanavir (treatment-experienced), posaconazole, boceprevir, simeprevir, atovaquone/proguanil, pibrentasvir/glecaprevir, velpatasvir/sofosbuvir/voxilaprevir, alcohol, psychoactive, other NNRTIs or hepatotoxic drugs. Caution with drugs metabolized by, or that affect activity of, CYP2B6 or CYP3A4. Efavirenz levels decreased by carbamazepine, phenytoin, phenobarbital, rifampin (adjust dose). May decrease levels of indinavir, amprenavir, atazanavir, saquinavir, anticonvulsants, clarithromycin, calcium channel blockers (eg, diltiazem, felodipine, nicardipine, nifedipine, verapamil), itraconazole, ketoconazole, lopinavir (adjust dose: see full labeling), maraviroc, bupropion, methadone, rifabutin (increase dose; see full labeling), sertraline, simvastatin, atorvastatin, pravastatin, hormonal contraceptives (eg, norgestimate, etonogestrel), immunosuppressants (eg, cyclosporine, sirolimus, tacrolimus), artemether/lumefantrine. May affect or be affected by voriconazole (adjust dose). Levels of both drugs increased with ritonavir (monitor liver function and for adverse events). Closely monitor warfarin, anticonvulsants (esp. phenytoin, phenobarbital, carbamazepine), others. Consider alternatives when concomitant drugs with a risk of QT prolongation (eg, clarithromycin, artemether/lumefantrine). May cause false (+) cannabis screening test results.
Non-nucleoside reverse transcriptase inhibitor.
CNS effects (eg, dizziness, headache, insomnia, impaired concentration, somnolence, abnormal dreams), psychiatric effects (eg, severe depression, suicidal ideation/attempt, aggression, paranoia, mania, delusions, psychosis), rash (may be severe; eg, Stevens-Johnson, erythema multiforme), nausea, vomiting, fatigue; immune reconstitution syndrome, fat redistribution, hepatotoxicity, dyslipidemia.
Register pregnant patients exposed to efavirenz by calling (800) 258-4263.
Hepatic (CYP3A, CYP2B6); 99% protein bound.
Fecal (primary), renal.
Caps 50mg—30; 200mg—90; Tabs 600mg—30