Antiretroviral Agents in HIV-1 (2014)

DHHS Adult HIV 2014

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Table 2. Advantages and Disadvantages of Antiretroviral Components Recommended as Initial Antiretroviral Therapy (continued) ARV Class ARV Agent(s) Advantages Disadvantages INSTIs DTG • Once-daily dosing • DTG-containing regimens have higher rates of virologic suppression than EFV- or DRV/r- containing regimens, largely because of fewer drug discontinuations. • May have higher barrier to resistance than EVG or RAL • Demonstrated virologic potency with both TDF/ FTC and ABC/3TC regardless of pre-ART HIV RNA level • Effective at double dose (50 mg twice daily) against some RAL- and EVG-resistant viruses • No food requirement • No CYP3A4 interactions • Inhibits renal tubular secretion of creatinine and can increase serum creatinine without affecting glomerular function • Oral absorption can be reduced by simultaneous administration with products containing polyvalent cations (eg, Al +++ , Ca ++ , or Mg ++ containing antacids or supplements, or multivitamin tablets with minerals) • UGT substrate: potential for drug interactions EVG • Co-formulated with cobi/TDF/FTC • Once daily dosing • Non-inferior to EFV/ TDF/FTC and ATV/r plus TDF/FTC • EVG is only recommended for patients with baseline CrCl ≥70 mL/min; therapy should be discontinued if CrCl decreases to <50 mL/min. • Cobi is a potent CYP3A4 inhibitor, which can result in significant interactions with CYP3A substrates. • Oral absorption can be reduced by simultaneous administration with antacids containing polyvalent cations, such as Al +++ or Mg ++ . • Cobi inhibits active tubular secretion of creatinine and can increase serum creatinine, without affecting renal glomerular function. • Has potential for new onset or worsening of renal impairment • May have lower genetic barrier to resistance than seen with boosted • PI- or DTG-based regimens • Food requirement 5

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