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ANTIINFECTIVES FOR SYSTEMIC USE › ANTIVIRALS FOR SYSTEMIC USE › DIRECT ACTING ANTIVIRALS › Non-nucleoside reverse transcriptase inhibitors
etravirine
J05AG04
Forms & Strengths
- Tablets: 25 mg
- Tablets: 100 mg
- Tablets: 200 mg
Adult Dosing
- 200 mg (one 200 mg tablet or two 100 mg tablets) orally twice daily
- Administer following a meal
- Swallow whole or disperse in 5 mL of water
Pediatric Dosing
- Pediatric patients 6 years and older: Dosed by weight, administered twice daily with food
- 10 kg to < 20 kg: 100 mg twice daily
- 20 kg to < 25 kg: 125 mg twice daily
- 25 kg to < 30 kg: 150 mg twice daily
- At least 30 kg: 200 mg twice daily
Indications
- Treatment of human immunodeficiency virus type 1 (HIV-1) infection in treatment-experienced adult and pediatric patients aged 6 years and older
- Used in combination with other antiretroviral agents
Mechanism of Action
- Non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1
- Binds directly to reverse transcriptase and blocks RNA-dependent and DNA-dependent DNA polymerase activities
- Retains activity against many NNRTI-resistant HIV-1 strains due to its molecular flexibility
Contraindications
- Hypersensitivity to etravirine or any of its excipients
- Co-administration with drugs that are strong inducers of CYP3A, CYP2C9, or CYP2C19 (e.g., carbamazepine, phenobarbital, phenytoin, rifampin, rifapentine, St. John's wort) due to significant decreases in etravirine plasma concentrations
Adverse Reactions
- Rash (including severe cutaneous adverse reactions such as Stevens-Johnson syndrome and toxic epidermal necrolysis)
- Hypersensitivity reactions accompanied by fever, general malaise, fatigue, muscle or joint aches, blisters, oral lesions, conjunctivitis, facial edema, hepatitis, and/or eosinophilia
- Nausea
- Diarrhea
- Fatigue
- Peripheral neuropathy
- Elevated transaminases and lipids (total cholesterol, triglycerides)
Drug Interactions
- Strong CYP3A, CYP2C9, and CYP2C19 inducers (e.g., rifampin, carbamazepine, St. John's wort): Significantly decrease etravirine levels; co-administration is contraindicated
- CYP2C9/2C19 inhibitors (e.g., fluconazole): May increase etravirine exposure
- Protease inhibitors (e.g., atazanavir/ritonavir, darunavir, fosamprenavir): Altered concentrations may require dosage adjustments or careful monitoring
- Statins (e.g., atorvastatin, simvastatin): Concentrations may be decreased by etravirine; monitor lipid response
- Hormonal contraceptives: Etravirine may decrease systemic exposure of hormonal contraceptives; alternative or additional contraceptive measures recommended
Curated Content: Needs Vetting Before Put to Clinical Use