Efavirenz

Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used in combination with other antiretroviral agents for HIV-1 infection. It blocks RNA- and DNA-dependent polymerase activities including HIV replication. Recommended dose is 600 mg once daily on an empty stomach, preferably at bedtime. For children, dose is weight-based. Common side effects include headache, dizziness, insomnia, somnolence, nausea, vomiting, diarrhea, fatigue, rash and abnormal dreams. Contraindicated in severe hepatic impairment, hypersensitivity and lactation. Category D during pregnancy.

• HIV-1 infection (in combination with other antiretroviral agents)

Efavirenz is a synthetic antiretroviral agent, a non-nucleoside reverse transcriptase inhibitor (NNRTI). It blocks RNA- and DNA-dependent polymerase activities including HIV-1 replication.

Efavirenz, a non-nucleoside reverse transcriptase inhibitor with activity against HIV, blocks the RNA-dependent and DNA-dependent polymerase activities including HIV replication.

Adult Dose: 600 mg once daily, in combination with other antiretrovirals. Dosing at bedtime recommended during first 2-4 weeks to improve tolerability.

Child Dose (>3 years): Weight-based: 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. Once daily.

Hepatic Dose: Mild (Child-Pugh A): No adjustment needed, use caution; Moderate-severe (B or C): Not recommended.

Oral tablet/capsule. Take in the dose and duration as advised. Swallow whole. Do not chew, crush or break. Take on empty stomach, preferably at bedtime.

If you miss a dose of Efavirenz, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular schedule. Do not double the dose.

Common Side Effects:

• Headache
• Dizziness
• Agranulocytosis
• Insomnia
• Sleepiness
• Vomiting
• Allergic reaction
• Nausea
• Abnormal dreams
• Fatigue
• Increased liver enzymes
• Anxiety
• Fever
• Itching
• Difficulty in paying attention
• Increased triglycerides
• Rash

Serious: Lipodystrophy, osteonecrosis, hyperglycemia, hypertriglyceridemia

• Efavirenz is used in combination with other medicines for HIV treatment.
• Take on an empty stomach, preferably at bedtime to reduce side effects.
• Do not skip doses and finish the full course of treatment even if you feel better.
• HIV or HBV can be passed to others. Don't share needles or personal items.
• Liver function will be monitored regularly. Inform doctor if yellowing of eyes/skin, dark urine, or stomach pain occurs.
• Dizziness or abnormal dreams may occur during initial days. Consult doctor if bothersome.
• Use reliable contraception while taking this medicine.

• Severe hepatic impairment
• Hypersensitivity
• Lactation
• Concomitant administration with terfenadine, astemizole, cisapride, midazolam, triazolam, pimozide, bepridil, ergot alkaloids, St John's wort

Additive CNS effects with psychoactive drugs. May alter plasma warfarin concentrations. May reduce plasma concentrations of HIV integrase inhibitors, other NNRTIs, HMG-CoA reductase inhibitors. Reduced plasma concentrations with rifampicin. St. John's wort may decrease serum level. Ethanol causes hepatic and CNS adverse effects.

Caution is advised when consuming alcohol with Efavirenz. Please consult your doctor.

Efavirenz is unsafe during pregnancy. There is definite evidence of risk to the developing baby. However, doctor may prescribe in life-threatening situations if benefits outweigh risks.

Efavirenz may pass through breast milk and cause serious harm to the baby. Should not be used during lactation.

Not studied in pediatric patients below 3 years or weighing less than 10 kg.

Limited information available regarding dose adjustment for elderly patients.

Renal impairment: Probably safe in kidney disease. Dose adjustment may not be needed.

Hepatic impairment: Use with caution. Dose adjustment may be needed. Not recommended in moderate and severe liver disease.

Symptoms: Increased CNS adverse effects including involuntary muscle contractions. Management: Supportive and symptomatic treatment. May administer activated charcoal.

Store at 25°C.

Efavirenz