Therapeutic Classification: antiretrovirals
Pharmacologic Classification: non nucleoside reverse transcriptase inhibitors
Absorption: Well absorbed following oral administration.
Distribution: Unknown.
Protein Binding: 99.7%.
Metabolism/Excretion: Mostly metabolized by the liver by the CYP3A isoenzyme; 25% excreted in feces unchanged, <1% excreted unchanged in urine.
Half-Life: 50 hr.
- Tablets and tablets for oral suspension are not interchangeable.
Treatment-Naive Patients With HIV Infection
- PO (Adults and Children ≥2 yr and ≥25 kg): 25 mg once daily (tablets only); Pregnant patients on stable rilpivirine regimen prior to pregnancy and virologically suppressed (HIV RNA <50 copies/mL): 25 mg once daily; Concurrent use of rifabutin: 50 mg once daily (↓ to 25 mg once daily when rifabutin discontinued).
- PO (Children ≥2 yr and 20–<25 kg): 15 mg once daily (tablets for oral suspension only).
- PO (Children ≥2 yr and 14–<20 kg): 12.5 mg once daily (tablets for oral suspension only).
Combination Therapy With Cabotegravir for HIV Infection
- PO (Adults and Children ≥12 yr and ≥35 kg): Oral lead-in therapy to assess tolerability of rilpivirine: 25 mg once daily (with oral cabotegravir 30 mg once daily) for ≥28 days; then switch to cabotegravir/rilpivirine extended-release injection. To replace planned missed cabotegravir/rilpivirine extended-release injections for patients on monthly dosing schedule (if patient plans to miss scheduled monthly injection by >7 days): 25 mg once daily (with oral cabotegravir 30 mg once daily) initiated at the same time as missed injection of cabotegravir/rilpivirine; then continued until day the cabotegravir/rilpivirine extended-release injection is restarted (oral replacement therapy can be continued for up to 2 mo). To replace planned missed cabotegravir/rilpivirine extended-release injections for patients on every 2-mo dosing schedule (if patient plans to miss scheduled every 2-mo injection by >7 days): 25 mg once daily (with oral cabotegravir 30 mg once daily) initiated the same time as missed injection of cabotegravir/rilpivirine; then continued until day the cabotegravir/rilpivirine extended-release injection is restarted (oral replacement therapy can be continued for up to 2 mo).
