Page 229 - HIV/AIDS Guidelines

Appendix B, Table 2. Characteristics of Non-Nucleoside Reverse Transcriptase Inhibitors* (NNRTIs)
(Last updated October 14, 2011; last reviewed March 27, 2012) (page 1 of 2)

*DLV is not included in this table. Please refer to the DLV FDA package insert for related information.

Dosing
Recommendations
Generic Name
Serum/
Adverse Events
(abbreviation)/ Formulations (For dosage adjustment Elimination Half-life (Also see Table 13)
in renal or hepatic
Trade Name
insufficiency, see
Appendix B, Table 7.)
Efavirenz • 50-, 200-mg 600 mg once daily at or Metabolized by 40–55 hrs • Rash a
(EFV)/ capsules before bedtime CYPs 2B6 and • Neuropsychiatric symptoms b
Sustiva 3A4
• 600-mg tablet Take on an empty stomach • Increased transaminase levels
Also available as to reduce side effects. CYP3A4 mixed
component of inducer/inhibitor • Hyperlipidemia
fixed-dose (more an inducer • False-positive results with some
combination: than an inhibitor) cannabinoid and benzodiazepine
Atripla (EFV 600 mg + 1 tablet once daily at or screening assays reported.
EFV FTC 200 mg + before bedtime. • Teratogenic in nonhuman primates
with TDF + FTC TDF 300 mg) tablet and potentially teratogenic in humans
Etravirine (ETR)/ • 100-, 200-mg 200 mg BID CYP3A4, 2C9, 41 hrs • Rash, including Stevens-Johnson
Intelence tablets and 2C19 syndrome a
Take following a meal.
substrate
• HSRs, characterized by rash,
3A4 inducer; 2C9 constitutional findings, and
and 2C19 sometimes organ dysfunction,
inhibitor including hepatic failure, have been
reported.
• Nausea
Nevirapine • 200-mg tablet 200 mg once daily for 14 CYP450 substrate, 25–30 hrs • Rash, including Stevens-Johnson
(NVP)/ • 400-mg XR tablet days (lead-in period); inducer of 3A4 syndrome a
Viramune or thereafter, 200 mg BID or and 2B6; 80% • Symptomatic hepatitis, including
Viramine XR • 50-mg/5-mL oral 400 mg (Viramune XR excreted in urine fatal hepatic necrosis, has been
suspension tablet) once daily (glucuronidated reported:
metabolites, <5%
Take without regard to - rash reported in approximately
meals. unchanged); 10%
in feces 50% of cases;
Repeat lead-in period if - occurs at significantly higher
therapy is discontinued for frequency in ARV-naive female
more than 7 days.
patients with pre-NVP CD4 counts
3
In patients who develop >250 cells/mm and in ARV-naive
mild-to-moderate rash male patients with pre-NVP CD4
3
without constitutional counts >400 cells/mm . NVP
symptoms, continue lead-in should not be initiated in these
period until rash resolves but patients unless the benefit clearly
not longer than 28 days total. outweighs the risk.

Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents O-4

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