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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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