Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI) with activity against HIV-1. It blocks the RNA- and DNA-dependent polymerase activities including HIV-1 replication.
Oral HIV infection Adult: In combination w/ other antiretrovirals: As cap or tab: 600 mg once daily. As soln: 720 mg once daily. Doses are given preferably at bedtime esp during the 1st 2-4 wk to improve tolerability. Child: In combination w/ other antiretrovirals: 3-17 yr As cap: 13-<15 kg: 200 mg; 15-<20 kg: 250 mg; 20-<25 kg: 300 mg; 25-<32.5 kg: 350 mg; 32.5-<40 mg: 400 mg; -40 kg: 600 mg. As soln: 13-<15 kg: <5 yr 360 mg; -5 yr 270 mg. 15-<20 kg: <5 yr 390 mg; -5 yr 300 mg. 20-<25 kg: <5 yr 450 mg; -5 yr 360 mg. 25-<32.5 kg: <5 yr 510 mg; -5 yr 450 mg. 32.5-<40 kg: -5 yr 510 mg. -40 kg: -5 yr 720 mg. Doses are given once daily, preferably at bedtime esp during the 1st 2-4 wk to improve tolerability. Should be taken on an empty stomach. Take preferably at bedtime.
Additive CNS effects w/ psychoactive drugs. May alter plasma warfarin concentrations. May reduce plasma concentrations of HIV integrase inhibitors (e.g. dolutegravir), other HIV NNRTIs (e.g. etravirine), HMG-CoA reductase inhibitors (e.g. simvastatin). Plasma concentrations of efavirenz is increased and that of voriconazole is reduced when given concomitantly. Reduced plasma concentrations w/ rifampicin.
Hypersensitivity. Severe hepatic impairment. Lactation. Concomitant admin w/ terfenadine, astemizole, cisapride, midazolam, triazolam, pimozide, bepridil, ergot alkaloids, St John’s wort. Patient w/ history of seizures and psychiatric disorders; acute porphyria. Patients receiving voriconazole or rifampicin (weighing ?50 kg). Discontinue if severe rash or fever develops. Moderate hepatic and severe renal impairment. Childn. Pregnancy.
Rashes, psychiatric or CNS disturbances, amnesia, agitation, confusion, dizziness, vertigo, headache, euphoria, insomnia or somnolence, impaired concentration, abnormal thinking or dreaming, depersonalisation, convulsions, hallucinations, nausea, vomiting, diarrhoea, pancreatitis, fatigue, hepatic failure, photoallergic dermatitis; autoimmune disorders (e.g. Graves’ disease, polymyositis, Guillain-Barre syndrome), osteonecrosis. Accumulation or redistribution of body fat (lipodystrophy) including central obesity, peripheral and facial wasting, buffalo hump, breast enlargement, cushingoid appearance. Metabolic abnormalities e.g. hypercholesterolaemia, hyperglycaemia, hypertriglyceridaemia, hyperlactataemia, insulin resistance. Potentially Fatal: Stevens-Johnson syndrome, erythema multiforme, toxic skin eruptions.
Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
Symptoms: Increased adverse CNS effects including involuntary muscle contractions.
Management: Supportive and symptomatic treatment. May administer activated charcoal.
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