Page 77 - HIV/AIDS Guidelines

Table 6. Advantages and Disadvantages of Antiretroviral Components Recommended as
Initial Antiretroviral Therapy (page 1 of 4)

ARV
ARV Class Advantages Disadvantages
Agent(s)
NNRTIs (in NNRTI Class Advantages: NNRTI Class Disadvantages:
alphabetical • Long half-lives • Greater risk of resistance at the time of treatment failure with
order) NNRTIs than with PIs
• Potential for cross resistance
• Skin rash
• Potential for CYP450 drug interactions (See Tables 14, 15b, and
16b.)
• Transmitted resistance more common with NNRTIs than with
PIs
EFV • Virologic responses equivalent or • Neuropsychiatric side effects
superior to all comparators to date • Teratogenic in nonhuman primates. Several cases of neural tube
• Once-daily dosing defect in infants born to women who were exposed to EFV in the
• Coformulated with TDF/FTC first trimester of pregnancy reported. EFV use should be avoided
in women with potential for pregnancy and is contraindicated in
the first trimester.
• Dyslipidemia

NVP • No food effect • Higher incidence of rash, including rare but serious HSRs (SJS
• Fewer lipid effects than EFV or TEN), than with other NNRTIs
• Once-daily dosing with extended- • Higher incidence of hepatotoxicity, including serious and even
release tablet formulation fatal cases of hepatic necrosis, than with other NNRTIs
• Contraindicated in patients with moderate or severe (Child-Pugh
B or C) hepatic impairment
• Some data suggest that ART-naive patients with high pre-NVP
3 3
CD4 counts (>250 cells/mm for females, >400 cells/mm for
males) are at higher risk of symptomatic hepatic events. NVP is
not recommended in these patients unless benefit clearly
outweighs risk.
• Early virologic failure of NVP + TDF + (FTC or 3TC) in small
clinical trials
RPV • Once-daily dosing • More virologic failures in patients with pretreatment HIV RNA
• Coformulated with TDF/FTC >100,000 copies/mL than with EFV-based regimen
• Compared with EFV: • More NNRTI- and 3TC-associated mutations at virological failure
than with regimen containing EFV + two NRTIs
• Fewer discontinuations for CNS
adverse effects • Food requirement
• Fewer lipid effects • Absorption depends on lower gastric pH. (See Table 15a for
detailed information regarding interactions with H2 antagonists
• Fewer rashes
and antacids.)
• Contraindicated with PPIs
• RPV-associated depression reported
• Use RPV with caution when coadministered with a drug having a
known risk of torsades de pointes.

Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents F-16

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