Rilpivirine is a next-generation NNRTI with good tolerability and lower rates of neuropsychiatric effects compared to efavirenz. Requires a low viral load for efficacy.
Also known as: Edurant, RPV
Proton pump inhibitors (omeprazole) raise gastric pH, reducing rilpivirine absorption by ~40-50%. Avoid coadministration or use alternative.
Rilpivirine is a weak base that requires acidic gastric pH (pH <3) for adequate dissolution and absorption. Proton pump inhibitors like omeprazole raise gastric pH to >4, significantly reducing rilpivirine oral bioavailability (~40-50% reduction in AUC). The rilpivirine label (Edurant) lists PPIs as a relative contraindication. Alternative: if an antacid is needed, use an H2-receptor antagonist (ranitidine 150 mg) with at least 12 hours apart, or aluminium/magnesium antacids with 4 hours apart. Monitor viral load if PPI is unavoidable.
Rilpivirine + omeprazole: PPI reduces rilpivirine absorption by ~40-50%. Avoid coadministration or use H2B with interval.
Rilpivirine is a weak base that requires acidic pH for adequate absorption. Omeprazole raises gastric pH, significantly reducing oral bioavailability.
Monitor viral load if PPI is unavoidable.
Clinically significant reduction in rilpivirine levels → risk of virological failure.
Avoid coadministration. If necessary, use antacids (aluminium/magnesium hydroxide) with at least 4 hours apart. Alternative: H2-receptor antagonist (ranitidine) with at least 12 hours apart.
DailyMed/FDA (NIH/NLM) — approved Rilpivirine (Edurant) label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=03880372-2c68-45c6-a53a-f420c49541d6 ; approved Omeprazole label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=eb575720-d081-4261-ab09-432c30d13c07
Antacids (aluminium/magnesium hydroxide) may reduce rilpivirine absorption. Administer at least 4 hours apart.
Antacids containing polyvalent cations (aluminium hydroxide, magnesium hydroxide) may form insoluble complexes with rilpivirine in the gastrointestinal tract, reducing its absorption. The effect is less marked than PPIs but clinically relevant if antacids are used regularly. The rilpivirine label recommends an interval of at least 4 hours between antacid and rilpivirine administration. For patients requiring frequent antacids, consider alternatives such as ranitidine (H2B) or omeprazole (with the restrictions above).
Rilpivirine + antacids: polyvalent cations (Al³⁺/Mg²⁺) reduce absorption. 4-hour interval.
Antacids containing polyvalent cations (Al³⁺, Mg²⁺) may form insoluble complexes with rilpivirine, reducing its absorption.
Monitor viral load if antacids are used regularly.
Reduced rilpivirine absorption → risk of virological failure.
Administer antacids at least 4 hours before or 4 hours after rilpivirine.
DailyMed/FDA (NIH/NLM) — approved Rilpivirine (Edurant) label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=03880372-2c68-45c6-a53a-f420c49541d6
Rilpivirine requires fatty foods for adequate absorption. Without fat, bioavailability decreases ~50%.
Always take with a meal containing fat (e.g. milk, butter, olive oil).
DailyMed/FDA (NIH/NLM) — approved Rilpivirine (Edurant) label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=03880372-2c68-45c6-a53a-f420c49541d6
No documented disease interactions.
Limited human data. Animal studies did not demonstrate teratogenicity. Use with caution.
Can be used in the 2nd and 3rd trimesters with caution.
Excreted in breast milk. Artificial feeding is recommended for HIV-positive mothers.
Reliable contraceptive methods are recommended.
DailyMed/FDA (NIH/NLM) — approved Rilpivirine (Edurant) label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=03880372-2c68-45c6-a53a-f420c49541d6
Clinical and educational support tool. The information does not replace a medical prescription or the opinion of a qualified healthcare professional.
Rilpivirine is a next-generation NNRTI with good tolerability and lower rates of neuropsychiatric effects compared to efavirenz.
Binds to HIV-1 reverse transcriptase with high affinity and selectivity, blocking viral DNA synthesis. Flexible structure accommodates resistance mutations (good activity against NNRTI mutations).
Oral bioavailability: significantly increased by food (79% vs fasting). Tmax: 4-5 hours. MUST be taken with a meal containing fat.
Metabolised by CYP3A4 (primarily). Induced by rifampicin, rifabutin, carbamazepine, phenytoin, phenobarbital. Inhibited by CYP3A4 inhibitors (ketoconazole, erythromycin).
~50 hours. Elimination: 85% faeces (metabolites), <10% urine. Long half-life allows once-daily dosing.
Medicines from the same therapeutic group (ATC classification) or the same pharmacological class.
