Elimination
CYP3A4 inhibitor and substrate
Dosage adjustment in hepatic insufficiency recommended
Serum/ Half-life
7 hrs
Storage
Room temperature (up to 25ºC or 77ºF)
Adverse Events
▶ Indirect hyperbilirubinemia ▶ Prolonged PR interval—first degree symptomatic AV block in some pts
▶ Use with caution in pts with underlying conduction defects or on concomitant medications that can cause PR prolongation
▶ Hyperglycemia ▶ Fat maldistribution ▶ Possible increased bleeding episodes in pts with hemophilia
▶ Nephrolithiasis ▶ Skin rash (20%) ▶ Serum transaminase elevations ▶ Hyperlipidemia (especially with RTV boosting)
CYP3A4 inhibitor and substrate
15 hrs (when combined
with RTV)
Room temperature (up to 25ºC or 77ºF)
▶ Skin rash (10%)—DRV has a sulfonamide moiety; Stevens-Johnson syndrome and erythrema multiforme have been reported
▶ Hepatotoxicity ▶ Diarrhea, nausea ▶ Headache ▶ Hyperlipidemia ▶ Transaminase elevation ▶ Hyperglycemia ▶ Fat maldistribution ▶ Possible increased bleeding episodes in pts with hemophilia
Amprenavir is a CYP3A4 substrate, inhibitor, and inducer
Dosage adjustment in hepatic insufficiency recommended
(amprenavir) Room 7.7 hrs
temperature (up to 25ºC or 77ºF)
▶ Skin rash (19%) ▶ Diarrhea, nausea, vomiting ▶ Headache ▶ Hyperlipidemia ▶ Transaminase elevation ▶ Hyperglycemia ▶ Fat maldistribution ▶ Possible increased bleeding episodes in pts with hemophilia ▶ Nephrolithiasis
CYP3A4 inhibitor and substrate
Dosage adjustment in hepatic insufficiency recommended
1.5-2 hrs
Room temperature (15º-30ºC/ 59º-86ºF) Protect from moisture
▶ Nephrolithiasis ▶ GI intolerance, nausea ▶ Indirect hyperbilirubinemia ▶ Hyperlipidemia ▶ Headache, asthenia, blurred vision, dizziness, rash, metallic taste, thrombocytopenia, alopecia, and hemolytic anemia
▶ Hyperglycemia ▶ Fat maldistribution ▶ Possible increased bleeding episodes in pts with hemophilia
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