etravirine: clinical use

Prescribing considerations

• Initiate and supervise treatment through an experienced HIV service.
• Review resistance results, treatment history and the complete interaction profile, including herbal and non-prescription products.
• Use caution with previous NNRTI-associated rash, moderate hepatic impairment, viral hepatitis co-infection, pregnancy and older age.

Contraindications and cautions

• Hypersensitivity to etravirine or a formulation excipient.
• Concomitant elbasvir/grazoprevir.

Monitoring

• HIV viral load, adherence and emergence of resistance.
• Rash and systemic hypersensitivity features, especially early in treatment.
• Liver function, particularly with hepatitis B or C co-infection.
• Blood lipids, glucose and clinically indicated haematology or renal tests.
• Interaction-specific monitoring, such as INR with warfarin or concentrations of selected narrow-therapeutic-index medicines.

Clinical pharmacology

Etravirine is an HIV-1 NNRTI that disrupts reverse transcriptase activity. It is highly protein-bound, metabolised mainly through CYP3A4, CYP2C9 and CYP2C19, weakly induces CYP3A4 and weakly inhibits CYP2C9, CYP2C19 and P-glycoprotein. Food materially increases exposure.

Formulation and product differences

• The selected tablet can be swallowed whole or dispersed in water; it should not be chewed.
• The selected formulation is essentially sodium-free and does not list lactose among its excipients, whereas some lower-strength formulations contain lactose.
• Keep tablets in the tightly closed original bottle with the desiccant pouches to protect them from moisture.

Tablet

Route: Oral

Strengths: 100 mg, 200 mg