NNRTI (HIV) Pregnancy: eMC §4.6: a moderate amount of data on pregnant women (between 300 and 1000 pregnancy outcomes) indicate no malformative or feto/neonatal toxicity of rilpivirine. Lower exposures of rilpivirine were observed during pregnancy, therefore viral load should be monitored closely. Animal studies do not indicate reproductive toxicity. The use of rilpivirine may be considered during pregnancy, if necessary. Breast-feeding: it is not known whether rilpivirine is excreted in human milk (it is excreted in rat milk); because of the potential for adverse reactions in breastfed infants, mothers should be instructed not to breast-feed if they are receiving rilpivirine, and to avoid transmission of HIV to the infant it is recommended that women living with HIV do not breast-feed. Fertility: no human data; no clinically relevant effects in animal studies.

Rilpivirine

Brand names: Edurant

Rilpivirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used as part of combination antiretroviral therapy for HIV-1 infection.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: One 25 mg tablet once daily

Route: Oral. Must be taken with a meal; the film-coated tablet should be swallowed whole with water and not chewed or crushed.

Frequency: Once daily

eMC §4.2 (Edurant 25 mg film-coated tablets). Therapy should be initiated by a physician experienced in the management of HIV infection. The recommended dose in adult AND paediatric patients weighing at least 25 kg is one 25 mg tablet once daily, taken with a meal. DOSE ADJUSTMENT: for patients concomitantly receiving rifabutin the EDURANT dose should be INCREASED to 50 mg (two 25 mg tablets) once daily; when rifabutin co-administration is stopped the dose should be decreased back to 25 mg once daily. MISSED DOSE: if missed within 12 hours of the usual time, take with a meal as soon as possible and resume the normal schedule; if missed by more than 12 hours, do not take the missed dose and resume the usual schedule. VOMITING: if the patient vomits within 4 hours of taking the dose, another tablet should be taken with a meal; if more than 4 hours after, no further dose is needed until the next scheduled dose. ELDERLY: limited information above 65 years; no dose adjustment required but use with caution. HEPATIC IMPAIRMENT: no dose adjustment in mild or moderate impairment (Child-Pugh A or B), use with caution in moderate impairment; not studied in and not recommended for severe impairment (Child-Pugh C). PREGNANCY: lower rilpivirine exposures were observed during pregnancy, so viral load should be monitored closely; alternatively switching to another ART regimen could be considered. PAEDIATRIC: EDURANT is also available as EDURANT 2.5 mg DISPERSIBLE tablets for paediatric patients aged 2 to less than 18 years weighing at least 14 kg and less than 25 kg, with the recommended dosage based on body weight - the specific weight-band figures are NOT contained in the fetched text, so no paediatric per-kg or per-band dose can be given here. A difference in bioavailability between one 25 mg film-coated tablet and ten 2.5 mg dispersible tablets was observed, therefore THE TWO FORMULATIONS ARE NOT INTERCHANGEABLE. Safety and efficacy in children under 2 years or weighing less than 14 kg have not been established. US labelling notes trials of weight-adjusted doses of 25, 15 and 12.5 mg daily in children aged 2 years and older weighing at least 14 kg. Verify all under-18 dosing against a children's formulary and the dispersible-tablet SPC. CARDIOVASCULAR (§4.4): at supra-therapeutic doses (75 and 300 mg once daily) rilpivirine has been associated with QTc prolongation; the recommended 25 mg once-daily dose is not associated with a clinically relevant effect on QTc, but use with caution with medicinal products with a known risk of Torsade de Pointes.

Dose adjustments

Renal

eMC §4.2: rilpivirine has mainly been studied in patients with normal renal function. No dose adjustment is required in mild or moderate renal impairment. In severe renal impairment or end-stage renal disease, rilpivirine should be used with caution, and the combination of rilpivirine with a strong CYP3A inhibitor (e.g. a ritonavir-boosted HIV protease inhibitor) should only be used if the benefit outweighs the risk. Treatment resulted in an early small increase of mean serum creatinine which remained stable over time and is not considered clinically relevant.

Dose auto-extracted from UK Summary of Product Characteristics (SPC) via the eMC; US FDA prescribing information (openFDA / DailyMed) — cross-check; US labelling may differ from UK — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.

Contraindications

Hypersensitivity to the active substance or to any of the excipients (§4.3)
Co-administration with the anticonvulsants carbamazepine, oxcarbazepine, phenobarbital or phenytoin (§4.3)
Co-administration with the antimycobacterials rifampicin or rifapentine (§4.3)
Co-administration with proton pump inhibitors such as omeprazole, esomeprazole, lansoprazole, pantoprazole or rabeprazole (§4.3)
Co-administration with systemic dexamethasone, except as a single dose treatment (§4.3)
Co-administration with St John's wort (Hypericum perforatum) (§4.3)

Side effects

Very common: insomnia; headache; dizziness; nausea; increased transaminases; increased pancreatic amylase; increased total cholesterol (fasted) and increased LDL cholesterol (fasted)
Common: depression, abnormal dreams, sleep disorders, depressed mood; somnolence; abdominal pain, vomiting, abdominal discomfort, dry mouth, increased lipase; decreased appetite
Common: decreased white blood cell count, decreased haemoglobin, decreased platelet count; increased bilirubin; increased triglycerides (fasted)
Common: rash; fatigue
Uncommon: immune reactivation syndrome. The most frequently reported adverse drug reactions of at least moderate intensity in the phase 3 trials were depression (4.1%), headache (3.5%), insomnia (3.5%), rash (2.3%) and abdominal pain (2.0%)

Interactions

Contraindicated co-medications (§4.3) cause significant decreases in rilpivirine plasma concentrations through CYP3A induction or gastric pH increase, which may result in loss of therapeutic effect: carbamazepine, oxcarbazepine, phenobarbital, phenytoin; rifampicin, rifapentine; proton pump inhibitors; systemic dexamethasone (except a single dose); St John's wort
Rifabutin - requires the rilpivirine dose to be increased to 50 mg once daily while co-administered, reverting to 25 mg once daily when rifabutin is stopped (§4.2)
CYP3A inducers and inhibitors generally (US labelling §7) - rilpivirine is primarily metabolised by CYP3A; inducers may cause decreased plasma concentrations, loss of virologic response and possible resistance to rilpivirine or the NNRTI class, while inhibitors may increase plasma concentrations
Drugs that increase gastric pH (US labelling §7) - may result in decreased rilpivirine plasma concentrations, loss of virologic response and possible resistance
Medicinal products with a known risk of Torsade de Pointes - use rilpivirine with caution when co-administered (§4.4)
The eMC §4.5 interaction section was not captured in this bundle - clinician to review the full SPC interaction table

Clinical monograph

How it works

It binds to and inhibits HIV-1 reverse transcriptase, blocking transcription of viral RNA into DNA.

Prescribing in practice

Acid-reducing agents such as proton pump inhibitors are contraindicated because they markedly reduce rilpivirine absorption and risk virological failure.
It should be taken with a meal to ensure adequate absorption.
Efficacy is reduced in patients with a high baseline viral load, so it is preferred for those with lower viral loads.

Monitoring

Monitor HIV viral load and CD4 count to confirm virological response, with attention to adherence and food intake.

Counselling the patient

Always take this medicine with a meal, not on an empty stomach.
Do not use proton pump inhibitor indigestion remedies; check other antacids with your clinician.
Take every dose to keep the virus under control and prevent resistance.

Evidence & guidelines

Rilpivirine is an established NNRTI option in UK and international HIV treatment guidelines for appropriate patients.

Reference: BHIVA; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Curated clinical cross-links plus same-class fallbacks.

Pathways