Efavirenz

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
  • Efavirenz 200 mg
  • Efavirenz 30 mg
  • Efavirenz 600 mg
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