7
INSTIs
(cont'd)
RAL • Compared to other
INSTIs, has longest
post-marketing
experience
• No food
requirement
• No CYP3A4
interactions
• Favorable lipid
profile
• Lower genetic barrier to
resistance than boosted PI- or
DTG-based regimens
• Increases in creatine kinase,
myopathy, and rhabdomyolysis
have been reported.
• Rare cases of severe HSRs
(including SJS and TEN) have
been reported.
• Higher pill burden than other
INSTI-based regimens.
• No fixed-dose combination
formulation.
• 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.
• Depression and suicidal
ideation (rare; usually in
patients with preexisting
psychiatric conditions).
NNRTIs EFV • Coformulated with
TDF/FTC
• Long term clinical
experience
EFV-based regimens
(except for EFV plus
ABC/3TC) have well-
documented efficacy
in patients with high
HIV RNA.
• Short- and long-term
neuropsychiatric (CNS) side
effects, including depression and,
in some studies, suicidality.
• Teratogenic in non-human
primates.
• Dyslipidemia.
• Rash.
• QTc interval prolongation;
consider an alternative to EFV in
patients taking medications with
known risk of causing TdP, or in
those at higher risk of TdP.
• Transmitted resistance more
common than with PIs and
INSTIs.
• Greater risk of resistance at the
time of treatment failure than
with PIs.
• Potential for CYP450 drug
interactions.
• Should be taken on an empty
stomach (food increases drug
absorption and CNS toxicities).
Table 2. Advantages and Disadvantages of Antiretroviral
Components Recommended as Initial ART (cont'd)
ARV
Class
ARV
Agent(s) Advantages Disadvantages
