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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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