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

Appendix B: Drug Characteristics Tables

Characteristics of Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)

(Last updated:2/12/2013; last reviewed:2/12/2013)

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

Appendix B, Table 2. Characteristics of Non-Nucleoside Reverse Transcriptase Inhibitors* (NNRTIs)
Generic Name (Abbreviation)/ Trade Name Formulations Dosing Recommendations
(For dosage adjustment in renal or hepatic insufficiency, see
Appendix B, Table 7.)
Elimination Serum
Half-life
Adverse Events
(Also see Table 13.)

Efavirenz (EFV)/
Sustiva
Also available as a component of fixed-dose combination:
  • 50 and 200 mg capsules
  • 600 mg tablet
600 mg once daily, at or before bedtime

Take on an empty stomach to reduce side effects.
Metabolized by CYPs 2B6 and 3A4

CYP3A4 mixed inducer/inhibitor (more an inducer than an inhibitor)
40-55 hours
  • Rasha
  • Neuropsychiatric symptomsb
  • Increased transaminase levels
  • Hyperlipidemia
  • False-positive results with some cannabinoid and benzodiazepine screening assays reported.
  • Teratogenic in non-human primates and potentially teratogenic in humans
Atripla
EFV with
TDF + FTC
(EFV 600 mg + FTC 200 mg + TDF 300 mg) tablet 1 tablet once daily, at or before bedtime
Etravirine (ETR)/ Intelence
  • 25, 100, and 200 mg tablets
200 mg BID

Take following a meal.
CYP3A4, 2C9, and 2C19 substrate

3A4 inducer; 2C9 and 2C19 inhibitor
41 hours
  • Rash, including Stevens-Johnson syndromea
  • HSRs, characterized by rash, constitutional findings, and sometimes organ dysfunction, including hepatic failure, have been reported.
  • Nausea
Nevirapine
(NVP)/
Viramune or Viramine XR

Generic available for 200 mg tablets
  • 200 mg tablet
  • 400 mg XR tablet
  • 50 mg/5 mL oral suspension
200 mg once daily for 14 days (lead-in period); thereafter, 200 mg BID, or 400 mg (Viramune XR tablet) once daily Take without regard to meals Repeat lead-in period if therapy is discontinued for more than 7 days In patients who develop mild-to-moderate rash without constitutional symptoms, continue lead-in period until rash resolves but not longer than 28 days total. CYP450 substrate, inducer of 3A4 and 2B6; 80% excreted in urine (glucuronidated metabolites, <5% unchanged); 10% in feces 25-30 hours
  • Rash, including Stevens-Johnson syndromea
  • Symptomatic hepatitis, including fatal hepatic necrosis, has been reported:
    • Rash reported in approximately 50% of cases
    • Occurs at significantly higher frequency in ARV-naive female patients with pre-NVP CD4 counts >250 cells/mm3 and in ARV-naive male patients with pre-NVP CD4 counts >400 cells/mm3. NVP should not be initiated in these patients unless the benefit clearly outweighs the risk.
Rilpivirine
(RPV)/
Edurant

Also available as component of fixed-dose combination:
  • 25 mg tablet
25 mg once daily

Take with a meal
CYP3A4 substrate 50 hours
  • Rasha
  • Depression, insomnia, headache
  • Hepatotoxicity
Complera
RPV with TDF + FTC
Complera
(RPV 25 mg +
TDF 300 mg +
FTC 200 mg) tablet
1 tablet once daily with a meal

Key to Abbreviations: ARV = antiretroviral, BID = twice daily, CYP = cytochrome P, DLV = delavirdine, EFV = efavirenz, ETR = etravirine, FDA = Food and Drug Administration, FTC = emtricitabine, HSR = hypersensitivity reaction, NNRTI = non-nucleoside reverse transcriptase inhibitor, NVP = nevirapine, RPV = rilpivirine, TDF = tenofovir disoproxil fumarate, XR = extended release

a
Rare cases of Stevens-Johnson syndrome have been reported with most NNRTIs; the highest incidence of rash was seen with NVP.
b Adverse events can include dizziness, somnolence, insomnia, abnormal dreams, confusion, abnormal thinking, impaired concentration, amnesia, agitation, depersonalization, hallucinations, and euphoria. Approximately 50% of patients receiving EFV may experience any of these symptoms. Symptoms usually subside spontaneously after 2 to 4 weeks but may necessitate discontinuation of EFV in a small percentage of patients.