Drug Guide
Rilpivirine Hydrochloride
Classification
Therapeutic: Antiretroviral, HIV-1 reverse transcriptase inhibitor
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 the non-nucleoside reverse transcriptase enzyme, causing direct inhibition of viral replication by non-competitively binding to the enzyme and causing conformational changes that inhibit DNA synthesis.
Dosage and Administration
Adult: 25 mg orally once daily with a meal
Pediatric: Not indicated for pediatric use
Geriatric: No specific dosage adjustment required, but caution advised due to comorbidities
Renal Impairment: No dosage adjustment necessary
Hepatic Impairment: Use with caution; no specific dosage recommendations available
Pharmacokinetics
Absorption: Rapidly absorbed, food increases absorption
Distribution: High protein binding (~99%)
Metabolism: Primarily hepatic via CYP3A4 enzyme
Excretion: Fecal excretion (major), minimal renal clearance
Half Life: 39 hours
Contraindications
- Concurrent use with certain drugs that induce CYP3A4 or with drugs that prolong QT interval
Precautions
- Cautious use in patients with history of QT prolongation, cardiac arrhythmias, or concomitant medications that affect QT interval; hepatic impairment; pregnancy category B
Adverse Reactions - Common
- Headache (Common)
- Insomnia (Common)
- Nausea (Common)
- rash (Common)
Adverse Reactions - Serious
- QT prolongation (Less common)
- Drug hypersensitivity reactions including hypersensitivity syndrome (Rare)
Drug-Drug Interactions
- Concurrent use with strong CYP3A4 inducers (e.g., rifampin, carbamazepine) reduces effectiveness of rilpivirine.
- CYP3A4 inhibitors (e.g., ketoconazole) may increase rilpivirine levels.
Drug-Food Interactions
- Food enhances absorption; take with a meal.
Drug-Herb Interactions
- Avoid St. John’s Wort (CYP3A4 inducer).
Nursing Implications
Assessment: Monitor for symptoms of HIV breakthrough, check for history of cardiac arrhythmias or QT prolongation.
Diagnoses:
- Risk for ineffective tissue perfusion r/t cardiac arrhythmias.
Implementation: Advise to take consistently with a meal. Monitor for adverse reactions such as rash, mood changes.
Evaluation: Assess viral load periodically to evaluate effectiveness.
Patient/Family Teaching
- Take medication with food to enhance absorption.
- Report any symptoms of arrhythmia, such as palpitations or dizziness.
- Inform about potential side effects and when to seek medical attention.
Special Considerations
Black Box Warnings:
- None specific for rilpivirine.
Genetic Factors: Genetic variations affecting CYP3A4 activity may influence drug levels.
Lab Test Interference: May interfere with certain laboratory tests, consult lab for specifics.
Overdose Management
Signs/Symptoms: Nausea, vomiting, dizziness, somnolence, seizures.
Treatment: Supportive care; no specific antidote. Contact poison control for guidance.
Storage and Handling
Storage: Store at room temperature, 20°C to 25°C (68°F to 77°F). Keep in original container.
Stability: Stable for the duration of the labeled expiration date if stored properly.