Efavirenz

Dosing

원내

HIV infection

  • 600 mg PO q24h

  • Take at bedtime, without food. Food may increase serum concentration, which can lead to elevated risk of adverse events.No renal dose adjustment

원내

Safety and efficacy in pediatric patients <3m of age or <3.5 kg of BW have not been established

  • BW 3.5-5 kg 100 mg PO q24h

  • BW 5-7.5 kg 150 mg PO q24h

  • BW 7.5-15 kg 200 mg PO q24h

  • BW 15-20 kg 250 mg PO q24h

  • BW 20-25 kg 300 mg PO q24h

  • BW 25-32.5 kg 350 mg PO q24h

  • BW 32.5-40 kg 400 mg PO q24h

  • BW >40 kg 600 mg PO q24hNo renal dose adjustment

Mild or moderate hepatic impairment No dose adjustment

Severe hepatic impairment No data

General Information

Treatment of HIV infection.

Indicated for use as a NNRTI agent as part of a 3-drug combination regimen.

Monitor viral load prior to initiation or modification of treatment.

Monitor CD4 cell counts prior to initiation or with modification of ARV treatment and every 3-6 months; thereafter during at least the first 2 years of treatment.

Monitor hepatitis B screening.

Perform hepatitis C antibody testing prior to initiation or modification of ARV treatment.

Common

  • Rash

  • Pruritus

  • Diarrhea

  • Nausea

  • Vomiting

  • Dizziness

  • Headache

  • Fatigue

  • Insomnia

  • Serum cholesterol and serum triglycerides raised

  • Increased liver enzymes

Serious

  • Prolonged QT interval

  • Torsades de pointes

  • Erythema multiforme

  • Stevens-Johnson syndrome

  • Liver failure

  • Neurotoxicity

  • Depression

  • Psychiatric effects

  • Paritaprevir - increased efavirenz plasma concentrations, elevated liver enzymes

  • St John's wort - increased risk of antiretroviral resistance and treatment

  • QT interval prolonging drugs

  • Ritonavir

  • Voriconazole

  • Elbasvir

  • Grazoprevir

  • Carbamazepine

Multiple drug-drug interactions

Antimicrobial class: Antiretroviral agent, Non-nucleoside reverse transcriptase inhibitor

Pregnancy category: D

Average serum half life: 40-55 hours

Urine penetration: Therapeutic

CSF penetration: Therapeutic

Precautions: Monotherapy should not be used as viral cross-resistance may develop if used alone or added as a sole agent to a failing regimen.

Liver function monitoring recommended for all patients.

Not recommended in patients with moderate to severe hepatic impairment.

Late-onset neurotoxicity may occur months to years after beginning therapy, especially in patients with CYP2B6 genetic polymorphisms associated with increased efavirenz levels; discontinuation may be warranted.

Immediate medical evaluation recommended for serious psychiatric symptoms.

Negative pregnancy test warranted prior to therapy initiation.

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