Table 7. Advantages and Disadvantages of Antiretroviral
Components Recommended as Initial Antiretroviral Therapy
ARV
Agent(s) Advantages Disadvantages
NNRTIs
a
(cont'd)
RPV • Once-daily dosing
• Coformulated with
TDF/FTC
• Compared with EFV:
▶ Fewer
discontinuations
for CNS adverse
effects
▶ Fewer lipid effects
▶ Fewer rashes
• More virologic failures in patients with
pretreatment HIV RNA >100,000 copies/mL
than with EFV-based regimen
• More NNRTI- and 3TC-associated mutations
at virological failure than with regimen
containing EFV + two NRTIs
• Food requirement
• Absorption depends on lower gastric pH
• Contraindicated with PPIs
• RPV-associated depression reported
• Use RPV with caution when coadministered with
a drug having a known risk of torsades de pointes
PIs
a
PI class advantages:
• Higher genetic
barrier to resistance
than NNRTIs and
RAL
• PI resistance
uncommon with
failure while on first
PI regimen
PI class disadvantages:
• Metabolic complications such as dyslipidemia,
insulin resistance, hepatotoxicity
• GI adverse effects
• CYP3A4 inhibitors and substrates: potential
for drug interactions (more pronounced with
RTV-based regimens)
ATV • Fewer adverse effects
on lipids than other
PIs
• Once-daily dosing
• Low pill burden
• Good GI tolerability
• Signature mutation
(I50L) not associated
with broad PI cross-
resistance
• Indirect hyperbilirubinemia sometimes leading
to jaundice or scleral icterus
• PR interval prolongation: generally
inconsequential unless ATV combined with
another drug with similar effect
• Cannot be coadministered with TDF, EFV, or
NVP (see ATV/r)
• Nephrolithiasis, cholelithiasis
• Skin rash
• Food requirement
• Absorption depends on food and low gastric pH
ATV/r • RTV boosting :
higher trough ATV
concentration and
greater antiviral effect
• Once-daily dosing
• Low pill burden
• More adverse effects on lipids than unboosted
ATV
• More hyperbilirubinemia and jaundice than
unboosted ATV
• Food requirement
• Absorption depends on food and low gastric pH
• 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
• Nephrolithiasis, cholelithiasis
a
Agents listed in alphabetical order.
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