Drug Detail

Etravirine

Last Updated June 10, 2016

Trade Names

Intelence

Drug Classification

Nonnucleoside reverse transcriptase inhibitor antiretroviral

Formulations

100 mg tablets; should not be prescribed with rifampicin or rifapentine.* See dosing recommendations for use with rifabutin.*

Indications and Pharmacology

Indication: treatment of HIV infection in combination with other antiretrovirals after virologic failure on other NNRTI-containing regimens.

Mechanism of action*: binds directly to reverse transcriptase, which interferes with HIV viral RNA–dependent DNA polymerase inhibiting viral replication.

Pharmacokinetics*: metabolized in the liver by CYP 3A4, 2C9, 2C19. CYP 3A4 inducer; CYP 2C9 and 2C19 inhibitor. Half-life: 41 hours (± 20 hours).

Dosage

Adult Dose: 200 mg twice daily, taken after meals.

Use in Renal or Hepatic Insufficiency*:

  • No dose adjustments needed in renal insufficiency.
  • No dose adjustment in mild to moderate hepatic impairment. No data in severe hepatic impairment.

Use in Pregnancy and Breastfeeding: Avoid in pregnancy; safety is not established in lactation.

Use in Children: No recommendations.

Warnings

Reports of severe, potentially life-threatening and fatal skin reactions have been reported.

Drug–Drug Interactions

Increased concentrations of concomitant medication: warfarin, voriconazole, diazepam, digoxin, boceprevir, ethinyl estradiol, fluvastatin, pitavastatin*

Decreased concentrations of concomitant medication: antiarrhythmics, itraconazole,
ketoconazole, clarithromycin, artemether, lumefantrine, rifabutin (if etravirine is used with a ritonavir-boosted PI, rifabutin should not be given, otherwise dose rifabutin 300 mg once daily), telaprevir, atorvastatin, lovastatin, simvastatin, buprenorphine, sildenafil, tadalafil, vardenafil, cyclosporine, sirolimus, tacrolimus, clopidogrel.*

Increased concentrations of etravirine with concomitant medication: fluconazole, itraconazole,
ketoconazole, posaconazole, voriconazole, clarithromycin.*

Decreased concentrations of etravirine with concomitant medication: boceprevir, St. John's wort, dexamethasone, rifabutin, rifampin, rifapentine, carbamazepine, phenobarbital, phenytoin.*

Drug interactions between etravirine and other antiretrovirals*:

Considerations for Special Populations

No recommendations for use in pregnancy.

Adverse Effects

Rash including Stevens-Johnson syndrome, hypersensitivity reaction, nausea, diarrhoea, triglyceridemia.

*Information from US prescribing information.