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Rilpivirine

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Rilpivirine, Edurant

  • See Also
  1. Non-Nucleoside Reverse Transcriptase Inhibitor
  2. Anti-Retroviral Therapy
  • Indications
  1. HIV Infection (part of combination therapy)
    1. FDA approved in 2011 for treatment-naive HIV patients (with HIV RNA <100,000 copies)
    2. High risk of induced HIV resistance
      1. Never use NNRTIs as monotherapy in HIV Infection
  • Mechanism
  1. See Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI)
  2. Second-generation Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI)
  3. Rilpivirine is a diarylpyrimidine
  • Medications
  1. Oral: 25 mg tablets
  2. Combination agents
    1. Cabenuva (Cabotegravir/Rilpivirine) monthly IM Injections
    2. Juluca (Dolutegravir/Rilpivirine)
  1. For treatment naive patients and HIV RNA <100,000 copies
  2. Administer in combination with other Antiretrovirals
  3. Protect medication from light (keep in original packaging)
  4. Adult (and child age >12 years or weight >35 kg)
    1. Take 25 mg orally daily with food
  • Efficacy
  1. Higher failure rates than Efavirenz when HIV RNA >100,000 copies
  2. Higher failure rates when CD4 Count <200 cells/mm3
  • Adverse Effects
  1. See Non-Nucleoside Reverse Transcriptase Inhibitor
  2. QTc Prolongation
    1. Increased risk with high serum levels of Rilpivirine
    2. Avoid with known QTc Prolongation or other medications that cause Drug-Induced QTc Prolongation
  3. Hepatotoxicity
    1. Obtain Liver Function Tests at baseline and periodically (esp. in known liver disease)
  • Safety
  1. Avoid in Lactation
  2. Pregnancy
    1. May use in pregnancy if risk outweighs benefit
    2. Monitor viral loads in pregnancy
    3. Pregnancy registry exists
  • Drug Interactions
  1. Rifabutin
    1. Increase Doravirine dose to 50 mg orally daily with food
  2. Drug-Induced QTc Prolongation
    1. Avoid with other agents that prolong QTc
  3. Metabolized by CYP3A4
    1. Avoid with strong CYP3A4 Inducers (e.g. Carbamazepine, Phenobarbital, Phenytoin, Rifampin)
  4. Antacids
    1. Antacid Salts (e.g. Aluminum and Magnesium Salt Antacid, Calcium Carbonate)
      1. Take at least 2 hours before or 4 hours after Rilpivirine
    2. H2 Blockers
      1. Take at least 12 hours before or 4 hours after Rilpivirine
  5. Methadone
    1. Rilpivirine may reduce Methadone effects
  • Resources
  1. Rilpivirine (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=03880372-2c68-45c6-a53a-f420c49541d6