Page 235 - HIV/AIDS Guidelines

Appendix B, Table 3. Characteristics of Protease Inhibitors (PIs) (Last updated October 14, 2011; last
reviewed March 27, 2012) (page 5 of 5)

Dosing
Generic Name Recommendations
(abbreviation)/ Formulations (For dosage adjustment Elimination Serum/ Storage Adverse Events
Trade Name in renal or hepatic Half-life (Also see Table 13)
insufficiency, see
Appendix B, Table 7.)

Tipranavir (TPV)/ • 250-mg (TPV 500 mg + CYP P450 3A4 6 hrs after Refrigerate • Hepatotoxicity: Clinical
Aptivus capsule RTV 200 mg) BID inducer and single capsules. hepatitis (including hepatic
substrate dose of decompensation and hepatitis-
• 100-mg/mL Unboosted TPV is not Capsules can be
oral solution recommended. Net effect when TPV/r stored at room associated fatalities) has been
combined with temperature reported; monitor closely,
TPV taken with RTV tablets: especially in patients with
Take with meals. RTV (CYP 3A4, (25ºC or 77ºF) for underlying liver diseases.
2D6 inhibitor) up to 60 days.
TPV taken with RTV • Skin rash (3%–21%): TPV has
capsules or solution: Take Oral solution a sulfonamide moiety; use
without regard to meals. should not be with caution in patients with
refrigerated or
frozen and known sulfonamide allergy.
should be used • Rare cases of fatal and
within 60 days nonfatal intracranial
after bottle is hemorrhages have been
opened. reported. Risks include brain
lesion, head trauma, recent
neurosurgery, coagulopathy,
hypertension, alcoholism, use
of anti-coagulant or anti-
platelet agents including
vitamin E.
• Hyperlipidemia
• Hyperglycemia
• Fat maldistribution
• Possible increased bleeding
episodes in patients with
hemophilia

Key to Abbreviations: APV = amprenavir, ARV = antiretroviral, ATV = atazanavir, AV = atrioventricular, BID = twice daily, CYP = cytochrome P,
DRV = darunavir, EFV = efavirenz, FPV = fosamprenavir, GI = gastrointestinal, IDV = indinavir, LPV = lopinavir, LPV/r = lopinavir + ritonavir,
msec = millisecond, NFV = nelfinavir, NVP = nevirapine, PI = protease inhibitor, PPI = proton pump inhibitor, RTV = ritonavir, SQV = saquinavir,
TDF = tenofovir disoproxil fumarate, TID = three times a day, TPV = tipranavir

Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents O-10

Downloaded from http://aidsinfo.nih.gov/guidelines on 12/8/2012 EST.