Nurses Compass
Drug Guide
Rilpivirine
Classification
Therapeutic: Antiretroviral agent for HIV-1 infection
Pharmacological: Non-nucleoside reverse transcriptase inhibitor (NNRTI)
FDA Approved Indications
- Treatment of HIV-1 infection in combination with other antiretroviral agents
Mechanism of Action
Rilpivirine binds to reverse transcriptase enzyme and causes direct inhibition of viral DNA synthesis, preventing viral replication.
Dosage and Administration
Adult: 25 mg once daily with a meal
Pediatric: Not approved for pediatric use
Geriatric: No specific recommendations; dose adjustment generally not required, but caution in renal/hepatic impairment
Renal Impairment: No dose adjustment necessary, but use with caution
Hepatic Impairment: Use caution in severe hepatic impairment; no specific dose adjustment established
Pharmacokinetics
Absorption: Well absorbed with food, especially meals containing fat
Distribution: Widely distributed in tissues, plasma protein binding ~99.7%
Metabolism: Primarily via CYP3A enzymes, mainly CYP3A4
Excretion: Metabolized extensively, with minimal unchanged drug excreted in urine and feces
Half Life: ~50 hours
Contraindications
- Concurrent use with proton pump inhibitors (PPIs) due to decreased absorption and efficacy
Precautions
- Use with caution in patients with hepatic impairment, history of hypersensitivity, or concomitant medications that prolong QT interval
Adverse Reactions - Common
- Insomnia (Common)
- Depressive symptoms (Common)
- Headache (Common)
- Nausea (Less common)
Adverse Reactions - Serious
- QT prolongation, Torsades de Pointes (Rare)
- Severe skin reactions, including Stevens-Johnson syndrome (Rare)
- Hepatotoxicity (Rare)
Drug-Drug Interactions
- Interactions with PPIs reducing efficacy; significant interactions with certain anticonvulsants, rifampin, and herbal products like St. John’s Wort
Drug-Food Interactions
- High-fat meals increase absorption
Drug-Herb Interactions
- St. John’s Wort may reduce effectiveness
Nursing Implications
Assessment: Monitor for signs of adverse reactions, adherence, and efficacy of ART
Diagnoses:
- Risk for ineffective tissue perfusion related to cardiac conduction abnormalities
- Imbalanced nutrition: less than body requirements due to nausea or anorexia
Implementation: Ensure administration with meal, monitor ECG in patients at risk for QT prolongation, regularly review medication compatibility
Evaluation: Assess viral load and CD4 counts regularly to evaluate treatment effectiveness
Patient/Family Teaching
- Take medication with a meal to improve absorption
- Report signs of hypersensitivity, skin rash, or serious side effects promptly
- Avoid concomitant use of PPIs and discuss any other medications
Special Considerations
Black Box Warnings:
- QT interval prolongation and risk of Torsades de Pointes
Genetic Factors: Genetic polymorphisms may affect drug metabolism but not routinely tested for
Lab Test Interference: May affect hepatic function tests
Overdose Management
Signs/Symptoms: Nausea, vomiting, dizziness, somnolence, QT prolongation
Treatment: Supportive care, cardiac monitoring, possibly activated charcoal if recent ingestion, no specific antidote
Storage and Handling
Storage: Store at room temperature, 20°C to 25°C (68°F to 77°F) in a dry place
Stability: Stable under recommended storage conditions for the duration of the labeled expiration date