Elimination
Cytochrome P450 3A4 inducer and substrate
Net effect when combined with RTV (CYP 3A4, 2D6 inhibitor)
Serum/ Half-life
6 hrs after single dose of TPV/r
Storage
Refrigerate capsules
Capsules can be stored at room temperature (25ºC or 77ºF) for up to 60 days.
Oral solution should not be refrigerated or frozen and should be used within 60 days after opening the bottle.
Adverse Events
▶ Hepatotoxicity—clinical hepatitis, (including hepatic decompensation and hepatitis-associated fatalities) has been reported; monitor closely, especially in pts with underlying liver diseases.
▶ Skin rash—TPV has a sulfonamide moiety; use with caution in pts with known sulfonamide allergy.
▶ Rare cases of fatal and nonfatal intracranial hemorrhages have been reported. Most pts had underlying comorbidity, such as brain lesion, head trauma, recent neurosurgery, coagulopathy, hypertension, or alcoholism or were on medication with increased risk of bleeding.
▶ Hyperlipidemia (especially hypertriglyceridemia)
▶ Hyperglycemia ▶ Fat maldistribution ▶ Possible increased bleeding episodes in pts with hemophilia
Serum/Half-life Route of Metabolism ~9 hrs
UGT1A1-mediated glucuronidation
Adverse Events
▶ Nausea ▶ Headache ▶ Diarrhea ▶ Pyrexia ▶ CPK elevation, muscle weakness, myopathy and rhabdomyolysis
▶ Rare severe skin and sysemic reactions
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