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ANTIINFECTIVES FOR SYSTEMIC USE › ANTIVIRALS FOR SYSTEMIC USE › DIRECT ACTING ANTIVIRALS › Non-nucleoside reverse transcriptase inhibitors
rilpivirine
J05AG05
Forms & Strengths
- Oral tablets: 25 mg
- Extended-release injectable suspension (Cabenuva co-pack): 600 mg/3 mL, 900 mg/3 mL
Adult Dosing
- Oral: 25 mg once daily taken with a meal, co-administered with other antiretroviral agents
- Injectable (as part of complete regimen with cabotegravir): 900 mg IM monthly or 1200 mg IM every 2 months after lead-in oral therapy
Pediatric Dosing
- Pediatric patients 12 years and older weighing at least 35 kg: 25 mg oral tablet once daily with a meal
- Safety and efficacy not established in children weighing less than 35 kg
Indications
- Treatment of HIV-1 infection in antiretroviral treatment-naive patients with baseline viral load <= 100,000 copies/mL
- Certain virologically suppressed patients for replacement of current antiretroviral regimen
Mechanism of Action
- Non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1
- Non-competitively inhibits HIV-1 reverse transcriptase, causing DNA chain termination
Contraindications
- Co-administration with strong CYP3A inducers (e.g., carbamazepine, oxcarbazepine, phenobarbital, phenytoin)
- Co-administration with systemic rifampin and rifapentine
- Co-administration with St. John's wort (Hypericum perforatum)
Adverse Reactions
- Depressive disorders (including depression, depressed mood, suicide attempt, suicidal ideation)
- Insomnia and headache
- Rash
- Elevated transaminases and total bilirubin
- Increased total cholesterol and LDL
Drug Interactions
- Strong CYP3A inducers significantly decrease rilpivirine plasma concentrations, risking loss of virologic response
- Drugs that increase gastric pH (proton pump inhibitors, H2-receptor antagonists, antacids) decrease rilpivirine absorption; avoid PPIs
- Co-administration with drugs that prolong the QTc interval requires caution
Curated Content: Needs Vetting Before Put to Clinical Use