emtricitabine + rilpivirine hydrochloride + tenofovir disoproxil fumarate: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
emtricitabine + rilpivirine hydrochloride + tenofovir disoproxil fumarate: clinical details
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).
emtricitabine + rilpivirine hydrochloride + tenofovir disoproxil fumarate preparations and strengths
Tablet
Route: Oral
Strengths: 200 mg + 25 mg + 245 mg
emtricitabine + rilpivirine hydrochloride + tenofovir disoproxil fumarate interactions
Rilpivirine absorption and CYP3A metabolism create important interactions, while tenofovir can add to kidney toxicity.
Proton-pump inhibitors, including omeprazole and lansoprazole
Contraindicated because they can substantially reduce rilpivirine exposure and compromise HIV control.
Antacids and H2-receptor antagonists
Can reduce rilpivirine absorption and require separation as directed by the prescriber or pharmacist.
Carbamazepine, oxcarbazepine, phenobarbital or phenytoin
Contraindicated because they can lower rilpivirine concentrations and undermine treatment.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.