tipranavir (Aptivus, TPV)

Indications

• combination antiretroviral treatment of HIV-1
  • evidence of viral replication, or
  • highly treatment-experienced, or
  • HIV-1 strains resistant to multiple protease inhibitors

Dosage

• 500 mg PO BID
• must be coadministered with ritonavir*

Capsules: 250 mg

Pharmacokinetics

• bioavailability increased by high-fat meal
• metabolized by cyt P450 3A4*

Monitor

• liver function tests baseline & then frequently
• discontinue if serum ALT or serum AST > 10X upper limit of normal or serum ALT or serum AST > 5-10X upper limit of normal with serum bilirubin increase

Adverse effects

• diarrhea, nausea & vomiting
• fatigue
• headache
• sulfonamide allergy
• intracranial hemorrhage in combination with ritonavir*
• hyperlipidemia, lipodystrophy syndrome
• hepatitis

• drug adverse effects of antiretroviral protease inhibitors
• drug adverse effects of antiretroviral agents
• drug adverse effects of sulfonamides

Drug interactions

• plasma levels increased by drugs that inhibit cyt P350 3A4
  • ritonavir* -intracranial hemorrhage

• drug interaction(s) anticonvulsants with anti-bacterial agents
• drug interaction(s) of fluticasone with HIV1 protease inhibitors
• drug interaction(s) of antiretroviral protease inhibitor in combination with ritonavir
• drug interaction(s) of statins with antiviral protease inhibitors
• drug interaction(s) of antibiotics with warfarin

Laboratory

• tipranavir in serum

More general terms

• antiretroviral protease inhibitor
• sulfonamide

Additional terms

• Acquired Immuno-Deficiency Syndrome (HIV infection stage 3, AIDS)

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=65027
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=133089
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=456177
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=163296
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=456351