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Guidelines for the Use of Antiretroviral Agents in Pediatric HIV Infection

Non-Nucleoside Analogue Reverse Transcriptase Inhibitors (NNRTIs)

Rilpivirine

(Last updated:2/12/2014; last reviewed:2/12/2014)

Rilpivirine (RPV, Edurant, TMC 278)

Rilpivirine (RPV, Edurant, TMC 278)

For additional information see Drugs@FDA: http://www.accessdata.fda.gov/scripts/cder/drugsatfda/index.cfm

Formulations

Tablet:
25 mg
Combination Tablet:

With Emtricitabine and Tenofovir Disoproxil Fumarate (Tenofovir):

  • Rilpivirine 25 mg + Emtricitabine 200 mg + Tenofovir 300 mg (Complera)

Dosing Recommendations

Neonate/Infant Dose:
  • Not approved for use in neonates/infants.
Pediatric Dose:
  • Not approved for use in children. A clinical trial in treatment-naive adolescents (aged 12–18 years) is under way using a 25-mg dose.
Adolescent (>18 years)/Adult Dose (Antiretroviral-Naive Patients Only):
  • 25 mg once daily

Selected Adverse Events

  • Depression, mood changes
  • Insomnia
  • Headache
  • Rash

Special Instructions

  • Instruct patients to take rilpivirine with a meal of at least 500 calories (a protein drink alone does not constitute a meal).
  • Do not use rilpivirine with other non-nucleoside reverse transcriptase inhibitors.
  • Do not use rilpivirine with proton pump inhibitors.
  • Antacids should only be taken either at least 2 hours before or at least 4 hours after rilpivirine.
  • Use rilpivirine with caution when co-administered with a drug with a known risk of torsades de pointes (http://www.qtdrugs.org/).
  • Do not start rilpivirine in patients with HIV RNA >100,000 copies/mL because of increased risk of virologic failure.

Metabolism

  • Cytochrome P450 (CYP) 3A substrate
  • Dosing in patients with hepatic impairment: No dose adjustment is necessary in patients with mild or moderate hepatic impairment.
  • Dosing in patients with renal impairment: No dose adjustment is required in patients with mild or moderate renal impairment.
  • Use rilpivirine with caution in patients with severe renal impairment or end-stage renal disease. Increase monitoring for adverse effects because rilpivirine concentrations may be increased in patients with severe renal impairment or end-stage renal disease.

Drug Interactions

  • Metabolism: Rilpivirine is a CYP 3A substrate and requires dosage adjustments when administered with CYP 3A-modulating medications.
  • Before rilpivirine is administered, a patient’s medication profile should be carefully reviewed for potential drug interactions.

Major Toxicities

  • More common: Insomnia, headache, and rash
  • Less common (more severe): Depression or mood changes

Resistance

The International Antiviral Society-USA (IAS-USA) maintains a list of updated resistance mutations (see http://www.iasusa.org/resistance_mutations/index.html).

Pediatric Use

Rilpivirine is approved in combination with other ARV agents for treatment-naive, HIV-infected adults with viral load ≤100,000 copies/mL. The pharmacokinetics, safety, and efficacy of rilpivirine in pediatric patients have not been established. An international trial currently under way is investigating a 25-mg dose of rilpivirine in combination with two nucleoside reverse transcriptase inhibitors in antiretroviral-naive children aged 12 to <18 years who weigh ≥32 kg and have a viral load ≤100,000 copies/mL.1

Reference

  1. ClinicalTrials.gov. A Study to Evaluate the Pharmacokinetics, Safety, Tolerability, and Antiviral Efficacy of TMC278 in Human Immunodeficiency Virus Infected Adolescents. ClinicalTrials.gov Identifier: NCT00799864. Available at http://clinicaltrials.gov/show/NCT00799864.