Nurses Compass
Drug Guide
Raltegravir potassium
Classification
Therapeutic: Antiretroviral agent for HIV-1 infection
Pharmacological: Integrase strand transfer inhibitor
FDA Approved Indications
- Treatment of HIV-1 infection in adults and pediatric patients (4 weeks and older)
Mechanism of Action
Raltegravir inhibits the HIV integrase enzyme, preventing the integration of viral DNA into the host cell genome, which inhibits viral replication.
Dosage and Administration
Adult: 600 mg twice daily; for some patients, 1200 mg once daily may be used, depending on co-administered drugs and clinical judgment.
Pediatric: Dose varies by weight and age; typically 4 mg/kg twice daily for children aged 4 weeks to less than 2 years, 25 mg twice daily for children 2 to less than 12 years and weighing 11 kg or more.
Geriatric: No specific dosage adjustment; consider renal, hepatic status.
Renal Impairment: No dose adjustment required for mild to moderate impairment; data limited for severe impairment.
Hepatic Impairment: No specific adjustment suggested; caution advised.
Pharmacokinetics
Absorption: Rapid absorption with peak plasma concentrations in 1 to 2 hours.
Distribution: Extensive plasma protein binding (~83%).
Metabolism: Primarily via UGT1A1-mediated glucuronidation; minor CYP3A4 contributions.
Excretion: Mostly fecal (~53%) and renal (~31%), primarily as metabolites.
Half Life: ~9 hours.
Contraindications
- Hypersensitivity to raltegravir or any component of the formulation.
Precautions
- Use with caution in patients with hepatic impairment.
- May cause hepatotoxicity; monitor liver function.
- Potential for hypersensitivity reactions.
Adverse Reactions - Common
- Nausea (20-30%)
- Diarrhea (10-19%)
- Headache (10-19%)
- Elevated liver enzymes (<10%)
Adverse Reactions - Serious
- Musculoskeletal symptoms (including myopathy and rhabdomyolysis) (Rare)
- Hypersensitivity reactions including rash, eosinophilia, and systemic symptoms (Rare)
- Hepatotoxicity leading to liver failure (Rare)
Drug-Drug Interactions
- Potential interactions with drugs metabolized by UGT1A1 and CYP3A4; avoid concomitant use with rifampin, carbamazepine, phenobarbital, or other strong inducers.
Drug-Food Interactions
N/ADrug-Herb Interactions
N/ANursing Implications
Assessment: Monitor HIV viral load and CD4 counts; assess liver function periodically.
Diagnoses:
- Risk for infection due to immunosuppression.
- Risk for adverse drug reactions.
Implementation: Administer medication as prescribed; counsel patient on adherence.
Evaluation: Evaluate viral suppression and monitor for adverse effects.
Patient/Family Teaching
- Take medication consistently at the same times each day.
- Report any rash, allergic symptoms, or signs of liver problems.
- Maintain regular follow-up appointments for lab tests.
Special Considerations
Black Box Warnings:
- None explicitly assigned; however, monitor for hypersensitivity reactions.
Genetic Factors: None specifically noted.
Lab Test Interference: May cause false-positive tests for cannabinoids and other drugs of abuse.
Overdose Management
Signs/Symptoms: Nausea, vomiting, hypotension, somnolence.
Treatment: Supportive care; no specific antidote; consider activated charcoal if ingestion was recent.
Storage and Handling
Storage: Store at controlled room temperature 20°C to 25°C (68°F to 77°F).
Stability: Stable under recommended conditions until expiration date.