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Appendix B, Table 3. Characteristics of Protease Inhibitors (PIs) (Last updated October 14, 2011; last
reviewed March 27, 2012) (page 2 of 5)
Dosing
Recommendations
Generic Name Serum/ Adverse Events
(abbreviation)/ Formulations (For dosage adjustment Elimination Half-life Storage (Also see Table 13)
in renal or hepatic
Trade Name
insufficiency, see
Appendix B, Table 7.)
Fosamprenavir • 700-mg tablet ARV-naive patients: APV is a CYP3A4 7.7 hrs Room • Skin rash (12%–19%): FPV has a
(FPV)/ • FPV 1400 mg BID or substrate, (APV) temperature sulfonamide moiety
• 50-mg/mL oral
Lexiva (a prodrug suspension • (FPV 1400 mg + RTV 100– inhibitor, and (up to 25ºC • Diarrhea, nausea, vomiting
of amprenavir 200 mg) once daily or inducer or 77ºF) • Headache
[APV]) Dosage
• (FPV 700 mg + RTV • Hyperlipidemia
100 mg) BID adjustment in
patients with • Serum transaminase elevation
PI-experienced patients hepatic
(once-daily dosing not insufficiency • Hyperglycemia
recommended): recommended • Fat maldistribution
• (FPV 700 mg + RTV (See Appendix B,
100 mg) BID Table 7.) • Possible increased bleeding
episodes in patients with
With EFV: hemophilia
• (FPV 700 mg + RTV
100 mg) BID or • Nephrolithiasis
• (FPV 1400 mg + RTV
300 mg) once daily
Tablet: Take without regard
to meals (if not boosted with
RTV tablet)
Suspension: Take without
food
FPV with RTV tablet: Take
with meals
Indinavir 100-, 200-, 400- 800 mg every 8 hrs CYP3A4 inhibitor 1.5–2 hrs Room • Nephrolithiasis
(IDV)/ mg capsules Take 1 hour before or 2 and substrate temperature • GI intolerance, nausea
Crixivan (15º–30ºC/
hours after meals; may take Dosage • Hepatitis
with skim milk or low-fat adjustment in 59º–86ºF)
meal patients with Protect • Indirect hyperbilirubinemia
hepatic from
With RTV: • Hyperlipidemia
(IDV 800 mg + insufficiency moisture • Headache, asthenia, blurred
RTV 100–200 mg) BID recommended
(See Appendix B, vision, dizziness, rash, metallic
Take without regard to meals Table 7.) taste, thrombocytopenia, alopecia,
and hemolytic anemia
• Hyperglycemia
• Fat maldistribution
• Possible increased bleeding
episodes in patients with
hemophilia
Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents O-7
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