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tipranavir (Aptivus, TPV)
Indications:
- combination antiretroviral treatment of HIV-1
a) evidence of viral replication, or
b) highly treatment-experienced, or
c) HIV-1 strains resistant to multiple protease inhibitors
Dosage:
1) 500 mg PO BID
2) must be coadministered with ritonavir*
Capsules: 250 mg
Pharmacokinetics:
1) bioavailability increased by high-fat meal
2) metabolized by cyt P450 3A4*
Monitor:
- liver function tests baseline & then frequently [5]
- 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 [5]
Adverse effects:
1) diarrhea, nausea & vomiting
2) fatigue
3) headache
4) sulfonamide allergy
5) intracranial hemorrhage [3] in combination with ritonavir* [3]
6) hyperlipidemia, lipodystrophy syndrome [4]
7) hepatitis [4]
Drug interactions:
- plasma levels increased by drugs that inhibit cyt P350 3A4
- ritonavir* -intracranial hemorrhage [3]
Laboratory:
- tipranavir in serum
Interactions
drug interactions
drug adverse effects (more general classes)
Related
Acquired Immuno-Deficiency Syndrome (HIV infection stage 3, AIDS)
General
antiretroviral protease inhibitor
sulfonamide
Properties
INHIBITS: protease
Database Correlations
PUBCHEM correlations
References
- Prescriber's Letter 12(8): 2005
New Drug: Tipranavir (Aptivus)
Detail-Document#: 210805
(subscription needed) http://www.prescribersletter.com
- Department of Veterans Affairs, VA National Formulary
- FDA Medwatch
http://www.fda.gov/medwatch/safety/2006/safety06.htm#Aptivus
- Medical Knowledge Self Assessment Program (MKSAP) 14, 15, 17.
American College of Physicians, Philadelphia 2006, 2009, 2015
- Prescriber's Letter 17(7): 2010
Recommended Lab Monitoring for Common Medications
Liver Function Test Scheduling
Detail-Document#: 260704
(subscription needed) http://www.prescribersletter.com