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 NNRTIs EFV • Virologic responses non- inferior or superior to most comparators • Virologic potency persists regardless of baseline HIV RNA • Once-daily dosing • Co-formulated with TDF/FTC • Long-term clinical experience • Transmitted resistance more common than with PIs • Short-and long-term neuropsychiatric side effects, including depression and suicidality • Teratogenic in non-human primates; avoid use in women who are trying to conceive or who are sexually active and not using contraception • Dyslipidemia • Greater risk of resistance at the time of treatment failure than with PIs • Skin rash • Potential for CYP450 drug interactions • Should be taken on an empty stomach (food increases drug absorption and CNS toxicities) RPV • Once-daily dosing • Co-formulated with TDF/FTC • Smaller pill size than co- formulated EFV/TDF/ FTC or EVG/cobi/ TDF/FTC • Compared with EFV: > Fewer discontinuations for CNS adverse effects > Fewer lipid effects > Fewer rashes > Smaller pill size • 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 • Transmitted resistance more common than with PIs • More NNRTI-, TDF-, and 3TC-associated mutations at virological failure than with regimen containing EFV and two NRTIs • Potential for CYP450 drug interactions • Meal requirement • Requires acid for adequate absorption • Contraindicated with PPIs • Use with H2 antagonists or antacids with caution • RPV-associated depression reported • Use with caution when co- administered with a drug having a known risk of torsades de pointes. 3

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