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Table 6. Advantages and Disadvantages of Antiretroviral Components Recommended as
            Initial Antiretroviral Therapy (page 2 of 4)


                             ARV
              ARV Class                      Advantages                            Disadvantages
                           Agent(s)
             PIs (in                 PI Class Advantages:          PI Class Disadvantages:
             alphabetical            • Higher genetic barrier to resistance  • Metabolic complications such as dyslipidemia, insulin
             order)                   than NNRTIs and RAL           resistance, hepatotoxicity
                                     • PI resistance uncommon with failure  • GI adverse effects
                                      while on first PI regimen    • CYP3A4 inhibitors and substrates: potential for drug
                                                                    interactions (more pronounced with RTV-based regimens)
                                                                    (See Tables 14 and 15a.)



                          ATV        • Fewer adverse effects on lipids than  • Indirect hyperbilirubinemia sometimes leading to jaundice or
                                      other PIs                     scleral icterus
                                     • Once-daily dosing           • PR interval prolongation: generally inconsequential unless ATV
                                     • Low pill burden              combined with another drug with similar effect
                                     • Good GI tolerability        • Cannot be coadministered with TDF, EFV, or NVP (See ATV/r.)
                                     • Signature mutation (I50L) not  • Nephrolithiasis
                                      associated with broad PI cross  • Skin rash
                                      resistance                   • Food requirement
                                                                   • Absorption depends on food and low gastric pH. (See Table
                                                                    15a for detailed information regarding interactions with H2
                                                                    antagonists, antacids, and PPIs.)

                          ATV/r      • RTV boosting: higher trough ATV  • More adverse effects on lipids than unboosted ATV
                                      concentration and greater antiviral  • More hyperbilirubinemia and jaundice than unboosted ATV
                                      effect
                                                                   • Food requirement
                                     • Once-daily dosing
                                                                   • Absorption depends on food and low gastric pH. (See Table
                                     • Low pill burden              15a for interactions with H2 antagonists, antacids, and PPIs.)
                                                                   • RTV boosting required with TDF and EFV. With EFV, use ATV
                                                                    400 mg and RTV 100 mg once daily (PI-naive patients only).
                                                                   • Should not be coadministered with NVP
                          DRV/r      • Once-daily dosing           • Skin rash
                                     • Potent virologic efficacy   • Food requirement

                          FPV/r      • Twice-daily dosing resulted in efficacy  • Skin rash
                                      comparable to LPV/r          • Hyperlipidemia
                                     • RTV boosting results in higher trough  • Once-daily dosing results in lower APV concentrations than
                                      APV concentration and greater  twice-daily dosing
                                      antiviral effect
                                                                   • For FPV 1400 mg + RTV 200 mg: requires 200 mg of RTV and
                                     • Once-daily dosing possible with RTV  no coformulation
                                      100 mg or 200 mg daily
                                                                   • Fewer data on FPV 1400 mg + RTV 100 mg dose than on
                                     • No food effect               DRV/r and ATV/r















            Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents         F-17

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