Nurses Compass
Drug Guide
Tipranavir
Classification
Therapeutic: Antiretroviral, Protease Inhibitor
Pharmacological: Non-peptidic Protease Inhibitor
FDA Approved Indications
- Treatment of HIV-1 infections in combination with other antiretroviral agents in patients with evidence of viral replication and HIV-1 resistance to multiple protease inhibitors
Mechanism of Action
Tipranavir inhibits the HIV-1 protease enzyme, which is necessary for the maturation of infectious viral particles. By blocking this enzyme, it prevents the cleavage of the Gag-Pol polyprotein, resulting in the production of immature, noninfectious viral particles.
Dosage and Administration
Adult: 600 mg twice daily in combination with ritonavir 200 mg twice daily.
Pediatric: Not indicated for pediatric use.
Geriatric: Use with caution; no specific dosage adjustments necessary, but renal and hepatic function should be considered.
Renal Impairment: Use with caution; specific dosage adjustments are not well established.
Hepatic Impairment: Use with caution; hepatic function should be monitored closely.
Pharmacokinetics
Absorption: Rapidly absorbed, with peak plasma concentrations occurring approximately 2 hours after dosing.
Distribution: Extensively bound to plasma proteins (~99%).
Metabolism: Metabolized primarily by the cytochrome P450 enzyme system, notably CYP3A4.
Excretion: Excreted mainly in feces (about 83%), minimal renal excretion.
Half Life: Approximately 4-6 hours.
Contraindications
- Hypersensitivity to tipranavir or any component of the formulation.
Precautions
- History of hypersensitivity reactions, such as rash or allergy; hepatic impairment; sulfa allergy risk; neurologic side effects; bleeding disorders; carefully monitor for hepatitis and liver-related adverse effects.
Adverse Reactions - Common
- N/V, diarrhea (Common)
- Rash (Common)
- Elevated liver enzymes (Common)
Adverse Reactions - Serious
- Hepatic decompensation, hepatic failure (Serious)
- Intracranial hemorrhage (Serious)
- Allergic reactions, including rash and hypersensitivity (Serious)
Drug-Drug Interactions
- CYP3A4 inducers and inhibitors (e.g., rifampin, ketoconazole), other antiretrovirals, anticoagulants, statins.
Drug-Food Interactions
- High-fat meals may decrease absorption; administration should be consistent with or without food.
Drug-Herb Interactions
- St. John's Wort and other herbal products inducing CYP3A4 may reduce tipranavir levels.
Nursing Implications
Assessment: Monitor liver function tests, for signs of bleeding, neurologic symptoms, and hypersensitivity reactions.
Diagnoses:
- Risk for hepatic injury
- Risk for bleeding
- Altered mental status
Implementation: Administer with ritonavir; monitor for allergic reactions and adverse effects; counsel on adherence.
Evaluation: Assess viral load and CD4 counts regularly; evaluate for adverse reactions and drug interactions.
Patient/Family Teaching
- Take medication exactly as prescribed.
- Report any signs of allergic reactions, bleeding, neurologic symptoms, or hepatic issues.
- Maintain regular follow-up appointments and lab tests.
- Use contraception if applicable, as medication may affect pregnancy.
Special Considerations
Black Box Warnings:
- Hepatic adverse reactions, including hepatitis and hepatic failure.
Genetic Factors: Consider screening for HLA-B*5701 allele, although primarily associated with abacavir.
Lab Test Interference: May affect liver function tests.
Overdose Management
Signs/Symptoms: Nausea, vomiting, dizziness, hypotension, possible hepatic toxicity.
Treatment: Supportive care, gastric lavage if recent ingestion, monitor liver function, provide symptomatic treatment.
Storage and Handling
Storage: Store at 20°C to 25°C (68°F to 77°F), excursions permitted to 15°C to 30°C (59°F to 86°F).
Stability: Stable under recommended storage conditions for the duration specified in the package insert.