emtricitabine + rilpivirine hydrochloride + tenofovir disoproxil fumarate: clinical use

Prescribing considerations

• Confirm the licensed viral-load criterion and review genotypic or historical resistance data; evidence is insufficient after previous NNRTI failure.
• Assess renal, hepatic and bone risk, concurrent nephrotoxins, acid-suppressing treatment and CYP3A inducers.
• Screen for hepatitis B co-infection and plan continued HBV-active management and follow-up before discontinuation.
• Consider reduced rilpivirine exposure and closer virological monitoring during pregnancy.

Contraindications and cautions

• Hypersensitivity to an active substance or excipient.
• Concurrent carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifampicin, rifapentine, proton-pump inhibitors, repeated systemic dexamethasone or St John's wort.
• Not recommended with moderate or severe renal impairment or severe hepatic impairment.

Monitoring

• HIV viral load, adherence and emergence of resistance.
• Creatinine clearance and serum phosphate before treatment and periodically; investigate suspected renal-tubule dysfunction.
• Liver function, particularly with pre-existing disease or viral hepatitis co-infection.
• Bone pain, fractures or suspected osteomalacia, especially with renal-tubule dysfunction or osteoporosis.
• Metabolic parameters according to established HIV practice; monitor viral load closely during pregnancy.

Clinical pharmacology

Emtricitabine and intracellular tenofovir metabolites competitively inhibit HIV reverse transcriptase and terminate viral DNA chains. Rilpivirine is a non-competitive NNRTI primarily metabolised through CYP3A; its absorption is food-dependent and reduced when gastric pH rises.

Formulation and product differences

• The fixed combination does not permit individual component adjustment; separate preparations are required when a component must be modified or discontinued.
• The film-coated tablet should remain intact because chewing, crushing or splitting may alter absorption.
• The product contains lactose and sunset yellow aluminium lake (E110).

Tablet

Route: Oral

Strengths: 200 mg + 25 mg + 245 mg