Antiretroviral Agents in HIV-1 (2018)

Antiretroviral Agents in HIV-1 Pocket Guide

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8 Selecting a Treatment Regimen NNRTIs (cont'd) RPV • Coformulated with TDF/FTC and TAF/FTC. • RPV/TDF/FTC and RPV/TAF/ FTC have smaller pill size than other coformulated ARV drugs. • Compared with EFV: ▶ Fewer CNS adverse effects ▶ Fewer lipid effects ▶ Fewer rashes • NOT recommended in patients with pre-ART HIV RNA >100,000 copies/mL or CD4 count <200 cells/mm 3 because of higher rate of virologic failure in these patients. • Depression and suicidality • QTc interval prolongation; consider an alternative to RPV in patients taking medications with known risk of causing TdP, or in those at higher risk of TdP. • Rash. • Transmitted resistance more common than with PIs and INSTIs. • More NNRTI-, TDF-, and 3TC- associated mutations at virological failure than with regimen containing EFV and two NRTIs. • Potential for CYP450 drug interactions. • Food requirement (>390 kcal). • Requires acid for adequate absorption. ▶ Contraindicated with PPIs ▶ Use with H2 antagonists or antacids with caution PIs ATV/c or ATV/r • Higher genetic barrier to resistance than NNRTIs, EVG, and RAL. • PI resistance at the time of treatment failure uncommon with PK- enhanced PIs. • ATV/c and ATV/r have similar virologic activity and toxicity profiles. • Observational cohort studies have found an association between some PIs (DRV, LPV/r, FPV, IDV) and an increased risk of CV events, while this has not been seen with ATV. Further study is needed. • Commonly causes indirect hyperbilirubinemia, which may manifest as scleral icterus or jaundice. • Food requirement. • Absorption depends on food and low gastric pH. • Nephrolithiasis, cholelithiasis, nephrotoxicity. • GI adverse effects. • CYP3A4 inhibitors and substrates: potential for drug interactions. Table 2. Advantages and Disadvantages of Antiretroviral Components Recommended as Initial ART (cont'd) ARV Class ARV Agent(s) Advantages Disadvantages

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