Dosing & Uses
Dosage Forms & Strengths
tablet
- 25mg
HIV-1 Infection
Indicated in combination with other antiretroviral agents for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in treatment-naïve adult patients with HIV-1 RNA <100,000 copies/mL
25 mg PO qDay; administer with a meal
Dose during pregnancy
- May continue use for pregnant patients on a stable rilpivirine regimen before pregnancy and who are virologically suppressed (ie, HIV-1 RNA <50 copies/mL)
- 25 mg PO qDay; administer with a meal
- Lower exposures of rilpivirine were observed during pregnancy, therefore viral load should be monitored closely
Dosage Modifications
Renal impairment
- Mild-to-moderate renal impairment: No dose adjustment required
- Severe renal impairment or ESRD: Used with caution and with increased monitoring for adverse effects, plasma concentrations may be increased because of altered drug absorption, distribution, and metabolism secondary to renal dysfunction
- Dialysis: Highly bound to plasma proteins, unlikely to be significantly removed by hemodialysis or peritoneal dialysis
Hepatic impairment
- Mild-to-moderate hepatic impairment (Child-Pugh Classes A and B): No dose adjustment required
- Severe hepatic impairment (Child-Pugh Class C): Has not been studied
Dosage Forms & Strengths
tablet
- 25mg
HIV-1 Infection
Indicated in combination with other antiretroviral agents for treatment of HIV-1 infection in treatment-naïve adolescents aged 12-17 yr with HIV-1 RNA ≤100,000 copies/mL
<12 years: Safety and efficacy not established
12-17 years (weight ≥35 kg): 25 mg PO qDay; administer with a meal (see Administration)
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Adverse Effects
1-10%
Depressive disorders (4%)
Insomnia (3%)
Headache (3%)
Rash (3%)
Increased AST (2%; grade 3 or higher)
ALT increased (19%)
Abnormal dreams (1%)
Nausea (1%)
Suicidal ideation (4-8%)
Abdominal pain (1%)
Vomiting (1%)
Fatigue (1%)
Dizziness (1%)
Posmarketing reports
Severe skin and hypersensitivity reactions including DRESS (Drug Reaction with Eosinophilia and Systemic Symptoms)
Warnings
Contraindications
Hypersensitivity
Coadministration with drugs (eg, CYP inducers like phenobarbital, dexamethasone, oxcarbazepine, phenytoin, or carbamazepine) where significant decreases in rilpivirine plasma concentrations may occur, which may result in loss of virologic response and possible resistance and cross-resistance to other NNRTIs
Contraindicated with drugs that increase gastric pH (eg, esomeprazole, lansoprazole, omeprazole, pantoprazole, rabeprazole) that may decrease rilpivirine absorption and result in decreased rilpivirine plasma concentrations
Cautions
Coadministration with other NNRTIs may either increase or decrease rilpivirine; avoid use with other NNRTIs
May increase risk for depressive disorders
Hepatic adverse effects reported; patients with underlying hepatitis B or C, or marked increased transaminases prior to treatment may be at increased risk; monitor for hepatotoxicity before initiating and during treatment
Redistribution/accumulation of body fat, including central obesity, dorsocervical fat enlargement (buffalo hump), peripheral wasting, facial wasting, breast enlargement, and “cushingoid appearance” have been observed in patients receiving antiretroviral therapy
Immune reconstitution syndrome: During initial phase of combination ART treatment, patients whose immune system responds may develop an inflammatory response to indolent or residual opportunistic infections (eg, Mycobacterium avium complex, CMV, Pneumocystis pneumonia, TB)
Severe skin and hypersensitivity reactions reported, including cases of drug reaction with eosinophilia and systemic symptoms (DRESS), with rilpivirine-containing regimens; immediately discontinue treatment if hypersensitivity or rash with systemic symptoms or elevations in hepatic serum biochemistries develop and closely monitor clinical status, including hepatic serum biochemistries
Virologic failure & resistance
- More rilpivirine treated individuals with HIV-1 RNA >100,000 copies/mL at the start of therapy experienced virologic failure compared to those with <100,000 copies/mL
- Observed virologic failure rate in rilpivirine treated individuals conferred a higher rate of overall treatment resistance and cross-resistance to the NNRTI class compared to efavirenz
- More individuals treated with rilpivirine developed lamivudine/emtricitabine associated resistance compared to efavirenz
Drug interaction overview
- Drugs that induce or inhibit CYP3A may affect clearance of rilpivirine
- Coadministration with CYP3A4 inducers may decrease plasma concentrations of rilpivirine and result in loss of virologic response and possible resistance to rilpivirine OR to non-nucleoside reverse transcriptase inhibitors (NNRTIs)
- Coadministration with CYP3A4 inhibitors may increase plasma concentrations of rilpivirine
- Coadministration with drugs that increase gastric pH may decrease plasma concentrations of rilpivirine and result in loss of virologic response and possible resistance to rilpivirine or to NNRTIs
- In healthy subjects, rilpivirine 75 mg PO qDay (3 times rilpivirine dose) and 300 mg PO qDay (12 times rilpivirine dose) have been shown to prolong the QTc interval; consider alternatives when coadministered with a drug with a known risk of torsade de pointes
Pregnancy & Lactation
Pregnancy
Healthcare providers are encouraged to register patients by call the Antiretroviral Pregnancy Registry (APR) 1-800-258-4263
Available data from the APR show no difference in the overall risk of birth defects for rilpivirine compared with the background rate for major birth defects of 2.7% in the Metropolitan Atlanta Congenital Defects Program (MACDP) reference population
Lactation
Unknown whether distributed in human breast milk
The CDC recommends that women in the United States should not breastfeed their infants because of risk of the following
- Postnatal HIV transmission (in HIV-negative infants)
- Developing viral resistance (in HIV-positive infants)
- Adverse reactions in nursing infants
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Antiviral agent; diarylpyrimidine non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1
Inhibits HIV-1 replication by noncompetitive inhibition of HIV-1 reverse transcriptase
Does not inhibit the human cellular DNA polymerases alpha, beta, and gamma
Absorption
Bioavailability: Absolute bioavailability unknown
Peak Plasma Time: 4-5 hr
Peak Plasma Concentration: 80 ng/mL (mean)
AUC: 2397 ng•h/mL (mean)
Food: Exposure ~40% lower when taken in a fasted condition as compared to a normal caloric meal (533 kcal) or high-fat high-caloric meal (928 kcal); when taken with only a protein-rich nutritional drink, exposures were 50% lower than when taken with a meal
Distribution
Protein Bound: 99.7% (primarily to albumin)
Metabolism
Metabolized primarily by CYP3A
Elimination
Half-life: 50 hr
Excretion: feces (85%), urine (6.1%) bile, other
Administration
Oral Administration
Must administer with a meal
Must be able to take with a meal of at least 500 calories on a regular schedule (a protein drink alone does not constitute a meal)
If coadministered with antacids should only be administered either at least 2 hr before or at least 4 hr after rilpivirine
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Patient Handout
Formulary
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