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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