Tipranavir

What is Tipranavir

Tipranavir is a non-peptidic protease inhibitor (PI), indicated for use in combination with ritonavir and other antiretroviral medications to treat HIV-1 infected patients who are treatment-experienced and infected with HIV-1 strains resistant to more than 1 PI.

The non-peptidic structure theoretically exhibits greater flexibility in conforming to HIV protease variants that are resistant to current PIs, and may also decrease the rate of developing resistance.

Tipranavir MUST be “boosted” with ritonavir; failure to do so will result in tipranavir plasma concentrations that are insufficient to achieve the desired antiviral effect.

Hepatotoxicity, including some fatalities, has been reported in tipranavir-treated patients; thus, use of the drug is contraindicated in patients with moderate or severe (Child-Pugh B or C) hepatic impairment.

The FDA-approved labeling contains a Black Box Warnings (BBW) regarding an increased risk of drug-induced hepatotoxicity in patients coinfected with hepatitis B or C.

The BBW also advises of the association of the drug with fatal and non-fatal intracranial hemorrhage.

Brand Name

Aptivus

Indications

  • human immunodeficiency virus (HIV)
  • human immunodeficiency virus (HIV) infection

Side Effects

  1. abdominal pain
  2. anemia
  3. anorexia
  4. bleeding
  5. cough
  6. Cushingoid features
  7. dehydration
  8. diabetes mellitus
  9. diarrhea
  10. dizziness
  11. drowsiness
  12. dyspepsia
  13. dyspnea
  14. elevated hepatic enzymes
  15. epistaxis
  16. erythema
  17. fatigue
  18. fever
  19. flatulence
  20. gastroesophageal reflux
  21. gynecomastia
  22. headache
  23. hepatic failure
  24. hepatitis
  25. hepatotoxicity
  26. hyperamylasemia
  27. hyperbilirubinemia
  28. hypercholesterolemia
  29. hyperglycemia
  30. hyperlipidemia
  31. hypertriglyceridemia
  32. influenza
  33. insomnia
  34. intracranial bleeding
  35. lipodystrophy
  36. maculopapular rash
  37. malaise
  38. muscle cramps
  39. myalgia
  40. nausea
  41. neutropenia
  42. pancreatitis
  43. peripheral neuropathy
  44. photosensitivity
  45. pruritus
  46. QT prolongation
  47. rash
  48. steatosis
  49. thrombocytopenia
  50. urticaria
  51. vomiting
  52. weight loss

Monitoring Parameters

  • blood glucose
  • CBC with differential
  • CD4+ T cell count
  • hepatitis B serology
  • LFTs
  • plasma hepatitis C RNA
  • plasma HIV RNA
  • pregnancy testing
  • serum bilirubin (total and direct)
  • serum cholesterol profile
  • serum lipid profile
  • serum triglycerides
  • urinalysis

Contraindications

  • alcoholism
  • anticoagulant therapy
  • autoimmune disease
  • bleeding
  • breast-feeding
  • children
  • coagulopathy
  • diabetes mellitus
  • Graves’ disease
  • Guillain-Barre syndrome
  • head trauma
  • hemophilia
  • hepatic decompensation
  • hepatic disease
  • hepatitis
  • hepatitis B and HIV coinfection
  • hepatitis C and HIV coinfection
  • hepatotoxicity
  • human immunodeficiency virus (HIV) infection resistance
  • hypercholesterolemia
  • hyperlipidemia
  • hypertension
  • hypertriglyceridemia
  • immune reconstitution syndrome
  • infants
  • intracranial bleeding
  • jaundice
  • neonates
  • pancreatitis
  • pregnancy
  • serious rash
  • sulfonamide hypersensitivity
  • surgery

Interactions

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