Guidelines for the Use of Antiretroviral Agents in Adults and Adolescents with HIV
The information in the brief version is excerpted directly from the full-text guidelines. The brief version is a compilation of the tables and boxed recommendations.
Appendix B: Drug Characteristics Tables
Characteristics of Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)
Last Updated: December 18, 2019; Last Reviewed: December 18, 2019
Appendix B, Table 4. Characteristics of Non-Nucleoside Reverse Transcriptase Inhibitors
The older NNRTI DLV is no longer commonly used in clinical practice and is not listed this table. Please refer to the FDA product label for DLV for information regarding this drug.
|Formulations||Dosing Recommendationsa||Elimination/ Metabolic Pathway||Serum
||CYP3A4/5 substrate||15 hours||Nausea
Note: Generic product is available.
See Appendix B, Table 1 for dosing information for STRs that contain EFV.
|Metabolized by CYP2B6 (primary), 3A4, and 2A6
CYP3A4 mixed inducer/inhibitor (more an inducer than an inhibitor)
CYP2B6 and 2C19 inducer
Serum transaminase elevations
Use of EFV may lead to false-positive results with some cannabinoid and benzodiazepine screening assays
QT interval prolongation
||CYP3A4, 2C9, and 2C19 substrate
CYP2C9 and 2C19 inhibitor
|41 hours||Rash, including Stevens-Johnson syndromed
HSRs, characterized by rash, constitutional findings, and sometimes organ dysfunction (including hepatic failure), have been reported.
Viramune or Viramune XR
Note: Generic products are available.
Repeat lead-in period if therapy is discontinued for >7 days.
In patients who develop mild-to-moderate rash without constitutional symptoms, continue lead-in dose until rash resolves, but do not extend lead-in period beyond 28 days total.
CYP3A4 and 2B6 inducer
Contraindicated in patients with moderate to severe hepatic impairment.
Dose adjustment is recommended in patients on hemodialysis (see Appendix B, Table 10).
|25–30 hours||Rash, including Stevens-Johnson syndromed
See Appendix B, Table 1 for dosing information for STRs that contain RPV.
|CYP3A4 substrate||50 hours||Rashd
Depression, insomnia, headache
QT interval prolongation
a For dose adjustments in patients with renal or hepatic insufficiency, see Appendix B, Table 10. When no food restriction is listed, the ARV drug can be taken with or without food.
b Also see Table 17.
c See Appendix B, Table 1 for information about these formulations.
d Rare cases of Stevens-Johnson syndrome have been reported with the use of most NNRTIs; the highest incidence of rash was seen among patients who were receiving NVP.
e Adverse events can include dizziness, somnolence, insomnia, abnormal dreams, depression, suicidality (e.g., suicide, suicide attempt or ideation), confusion, abnormal thinking, impaired concentration, amnesia, agitation, depersonalization, hallucinations, and euphoria. Approximately 50% of patients who are receiving EFV may experience any of these symptoms. Symptoms usually subside spontaneously after 2–4 weeks, but discontinuation of EFV may be necessary in a small percentage of patients. Late-onset neurotoxicities, including ataxia and encephalopathy, have been reported.
Key: 3TC = lamivudine; ARV = antiretroviral; CD4 = CD4 T lymphocyte; CYP = cytochrome P; DLV = delavirdine; DOR = doravirine; DTG = dolutegravir; EFV = efavirenz; ETR = etravirine; FDC = fixed-dose combination; FTC = emtricitabine; HSR = hypersensitivity reaction; NNRTI = non-nucleoside reverse transcriptase inhibitor; NVP = nevirapine; RPV = rilpivirine; STR = single-tablet regimen; TAF = tenofovir alafenamide; TDF = tenofovir disoproxil fumarate; XR = extended release