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Tipranavir

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Tipranavir, Aptivus, TPV

  • See Also
  1. Anti-Retroviral Therapy
  2. Protease Inhibitor
  • Indications
  1. HIV Infection as part of combination therapy (not a first-line agent)
    1. Indicated for resistance to other Protease Inhibitors
  • Contraindications
  1. Sulfonamide Allergy (Exercise caution if used)
  2. Moderate to severe hepatic Impairment (Chil-Pugh Class B or C)
  • Mechanism
  1. See Protease Inhibitor
  • Medications
  1. Capsules: 250 mg
    1. Do not break, swallow whole
    2. Keep refrigerated
  2. Oral Solution (100 mg/ml)
    1. Contains Vitamin E (avoid combining with Vitamin E supplements)
  • Dosing
  1. General
    1. Use with Ritonavir, in addition to other Antiretrovirals as part of combination therapy
    2. Indicated as second line agent in HIV Treatment experienced patients with resistance to other Protease Inhibitors
  2. Adult
    1. Tipranavir 500 mg orally twice daily AND
    2. Ritonavir 200 mg orally twice daily
  3. Child (age >=2 years)
    1. Tipranavir 14 mg/kg (or 375 mg/m2) orally twice daily AND
    2. Ritonavir 6 mg/kg (or 150 mg/m2) orally twice daily
  • Adverse Effects
  1. See Protease Inhibitor for adverse effects attributed to the class
  2. Hepatotoxicity
    1. Severe hepatitis (fatalities have occurred)
    2. Higher risk in Hepatitis B and Hepatitis CVirus coinfection
    3. Avoid in Moderate to severe hepatic Impairment (Chil-Pugh Class B or C)
  3. Intracranial Hemorrhage (rare)
    1. Higher risk in CNS neoplasm, Closed Head Injury, Coagulopathy or Anticoagulants
  • Safety
  1. Avoid in Lactation
  2. Avoid in pregnancy
  • Drug Interactions
  1. Multiple Drug Interactions
    1. See Protease Inhibitor
    2. Ritonavir, even at its lower boosting dose, has numerous Drug Interactions
    3. As with other Protease Inhibitors, check a formal Drug Interaction application before prescribing
  2. CYP3A4 Substrates (e.g. Atorvastatin, Etravirine. other Protease Inhibitors)
    1. Avoid in combination with Tipranavir (risk of significant toxicity)
  3. Oral Contraceptives (OCP)
    1. Decreased OCP effectiveness
    2. Use backup or alternative Contraception
  4. Voriconazole
    1. Ritonavir decreases Voriconazole levels and efficacy
    2. Avoid concurrent use if possible
  5. Tricyclic Antidepressants
    1. Monitor levels
  6. Immunosuppressants
    1. Monitor levels
  7. Clarithromycin
    1. Decrease Clarithromycin dose if Creatinine Clearance <60 ml/min
  • Resources
  1. Tipranavir (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=08982e49-d2eb-4b25-b01a-1be52fd669ef
  • References
  1. Hamilton (2020) Tarascon Pocket Pharmacopoeia
  2. (2009) Treat Guidel Med Lett 7(78): 11-22 [PubMed]
  3. Reust (2011) Am Fam Physician 83(12): 1443-51 [PubMed]