Indications |
Oral HIV infection Adult: Combined with other antiretrovirals: 600 mg once daily. Dosing at bedtime recommended during 1st 2-4 wk of therapy to improve tolerability. Child: Combined with other antiretrovirals: >3 yr, 10-14 kg: 200 mg; 15-19 kg: 250 mg; 20-24 kg: 300 mg; 25-32.4 kg: 350 mg; 32.5-39 kg: 400 mg; ≥40 kg: 600 mg. To be taken once daily. |
Contraindications |
Severe hepatic impairment; hypersensitivity; lactation. |
Warnings / Precautions |
Mild to moderate liver disease; renal impairment. Monitor liver enzymes and cholesterol. Discontinue if severe skin rash or fever develops; known or suspected hepatitis B or infection. History of mental illness or seizures; elderly. Pregnancy. Children. |
Adverse Reactions |
Rash including Stevens-Johnson syndrome and erythema multiforme; CNS effects e.g. dizziness, headache, insomnia, somnolence, abnormal dreams, fatigue, impaired concentration. Nausea, less frequently, vomiting, diarrhoea, hepatitis, depression, anxiety, psychosis, amnesia and ataxia, stupor, vertigo, abdominal pain, hepatic failure, pancreatitis, convulsions, gynaecomastia, pruritus, blurred vision. |
Overdose Reactions |
Treatment is supportive. Activated charcoal may be used to remove unabsorbed drug. Dialysis may not be useful as drug is highly protein-bound. |
Drug Interactions |
Hormonal contraceptives; antibacterial e.g. rifampicin, rifabutin, clarithromycin; enzyme inducers. St. John's wort may decrease serum level. Ethanol (hepatic and CNS adverse effects). Potentially Fatal: Life-threatening adverse effects when used with terfenadine, astemizole, cisapride, midazolam, triazolam and ergot alkaloids. See Below for More efavirenz Drug Interactions |
Lab Interactions |
False-positive results in some urinary cannabinoid tests. Raised liver enzymes and serum cholesterol values. |
Food Interactions |
High-fat meals increase absorption of efavirenz. Grapefruit juice inhibits its metabolism. |
Mechanism of Actions |
Efavirenz, a non-nucleoside reverse transcriptase inhibitor with activity against HIV, blocks the RNA-dependent and DNA-dependent polymerase activities including HIV replication. Absorption: Absorbed after oral doses; plasma concentrations peak after about 5 hr. Distribution: >99% bound to plasma proteins. Metabolism: Metabolised mainly by CYP3A4 and CYP2B6. Excretion: About 14-34% of a dose is excreted in the urine as metabolites, and 16-61% in the faeces. |
Administration |
Should be taken on an empty stomach. (Take on an empty stomach, preferably at bedtime.) |
Storage Conditions |
Oral: Store at 15-30°C. |
ATC Classification |
J05AG03 - efavirenz ; Belongs to the class of non-nucleoside reverse transcriptase inhibitors. Used in the systemic treatment of viral infections. |
Storage |
Oral: Store at 15-30°C. |
Available As |
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Efavirenz
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Efavirenz Containing Brands
Efavirenz is used in following diseases
Drug - Drug Interactions of Efavirenz
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