Rilpivirine

Rilpivirine is a prescription medication used to treat the symptoms of HIV-1 Infection. 

• Rilpivirine is available under the following different brand names: Edurant

Common side effects of Rilpivirine include:

• Sleep problems (insomnia),
• Depression,
• Skin rash,
• Headache, and
• Change in the shape or location of body fat (especially in your arms, legs, face, neck, breasts, and waist)

Serious side effects of Rilpivirine include:

• Hives,
• Difficulty breathing,
• Swelling of the face, lips, tongue, or throat,
• Fever,
• Sore throat,
• Burning in the eyes,
• Skin pain,
• Red or purple skin rash that spreads and causes and peeling,
• Swollen glands,
• Flu-like symptoms,
• Muscle aches,
• Severe weakness,
• Unusual bruising,
• Yellowing of the skin or eyes,
• Mood changes,
• Anxiety,
• Sadness,
• Hopeless,
• Thoughts about self-harm,
• Right-sided upper stomach pain,
• Dark urine,
• Yellowing of the skin or eyes (jaundice),
• Mood changes,
• Feelings of low self-worth,
• Loss of interest in things once enjoyed,
• New sleep problems,
• Night sweats,
• Cold sores,
• Cough,
• Wheezing,
• Diarrhea,
• Weight loss,
• Trouble speaking,
• Difficulty swallowing,
• Problems with balance or eye movement,
• Weakness or prickly feeling,
• Swelling in the neck or throat (enlarged thyroid),
• Menstrual changes, and
• Impotence

Rare side effects of Rilpivirine include:

• none

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, loss of coordination, feeling unsteady, very stiff muscles, high fever, profuse sweating, or tremors;
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out. 

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult and pediatric dosage

Tablet

• 25 mg

HIV-1 Infection

Adult dosage

• 25 mg orally once a day; administer with a meal

Dose during pregnancy

• 25 mg orally once a day; administer with a meal

Pediatric dosage

• Children below 12 years: Safety and efficacy not established
• Children 12-17 years (weight above 35 kg): 25 mg orally once a day; administer with a meal (see Administration)

HIV Infection in Combination with Cabotegravir

Adult dosage

• Oral lead-in dosing prior to Cabenuva
• 25 mg orally once a day plus cabotegravir 30 mg orally once a day for at least 28 days to assess tolerability
• Take the last oral dose on the same day injections with Cabenuva started
• Oral replacement dose for planned missed Cabenuva injections
• If a patient plans to miss scheduled Cabenuva (cabotegravir; rilpivirine) extended-release injectable suspensions by above 7 days, take daily oral therapy to replace up to 2 consecutive monthly or 1 scheduled every-2-month injection visit(s)
• 25 mg orally once a day plus cabotegravir 30 mg orally once a day as a replacement for up to 2 consecutive months
• Take the first dose of oral therapy at approximately the same time as the planned missed injection and continue until the day injection dosing restarted

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Rilpivirine has severe interactions with at least 21 other drugs.
• Rilpivirine has serious interactions with at least 34 other drugs.
• Rilpivirine has moderate interactions with at least 137 other drugs.
• Rilpivirine has minor interactions with the following drugs
  • chloroquine
  • crizotinib

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all your products. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, or if you have health questions or concerns.

Contraindications

• Hypersensitivity
• Coadministration with drugs (e.g, 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 (. g, esomeprazole, lansoprazole, omeprazole, pantoprazole, rabeprazole) that may decrease rilpivirine absorption and result in decreased rilpivirine plasma concentrations

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Rilpivirine?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Rilpivirine?”

Cautions

• Coadministration with other NNRTIs may either increase or decrease rilpivirine; avoid use with other NNRTIs
• May increase the 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 the initial phase of combination ART treatment, patients whose immune system responds may develop an inflammatory response to indolent or residual opportunistic infections (.g, 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 above 100,000 copies/mL at the start of therapy experienced virologic failure compared to those with below 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 the 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 orally once a day (3 times rilpivirine dose) and 300 mg orally once a day (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 and Lactation

• Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 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
• Based on the experience of HIV-1-infected pregnant women who completed a clinical trial through the postpartum period with a rilpivirine-based regimen, no dose adjustments are required for pregnant patients who are already on a stable dose regimen prior to pregnancy and who are virologically suppressed (HIV-1 RNA less than 50 copies per mL); the recommended dosage is one 25 mg tablet once daily taken orally with a meal; lower exposures of the drug were observed during pregnancy, therefore viral load should be monitored closely
• Lactation
  • Unknown whether distributed in human breast milk; there are no data on the presence of drug in human milk, its effects on the breastfed infant, or on milk production; the drug is present in rat milk
  • The CDC recommends that women in the United States should not breastfeed their infants because of the risk of the following
  • Postnatal HIV transmission (in HIV-negative infants)
  • Developing viral resistance (in HIV-positive infants)
  • Adverse reactions in nursing infants