Appendix A, Table 4. Characteristics of Non-Nucleoside Reverse Transcriptase Inhibitors

Body
Generic Name (Abbreviation) Trade NameFormulationsDosing RecommendationsaElimination/ Metabolic PathwaySerum Half-LifeAdverse Eventsb
Doravirine
(DOR)
Pifeltro

Pifeltro

  • 100-mg tablet

Also available as part of the STR Delstrigo (DOR/TDF/3TC)c

STRs That Contain DORc

  • Delstrigo (DOR/TDF/3TC)

Pifeltro

  • DOR 100 mg PO once daily

See Appendix A, Table 1 for dosing information for Delstrigo.

 

CYP3A4/5 substrate15 hours

Nausea

Dizziness

Abnormal dreams

Efavirenz
(EFV)

Note: The branded product Sustiva has been discontinued.

Efavirenz (generic)

  • 600-mg tablet

STRs that Contain EFVc

  • EFV/TDF/FTC (generic)
  • Symfi (EFV 600 mg/TDF/3TC)
  • Symfi Lo (EFV 400 mg/TDF/3TC)

Efavirenz (generic)

  • EFV 600 mg PO once daily on an empty stomach, preferably at or before bedtime

See Appendix A, 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

40–55 hours

Rashd

Neuropsychiatric symptomse

Serum transaminase elevations

Hyperlipidemia

QT interval prolongation

Use of EFV may lead to false-positive results with some cannabinoid and benzodiazepine screening assays.

Etravirine
(ETR)
Intelence

Intelence

  • 100-mg, and 200-mg tablets

Intelence

  • ETR 200 mg PO twice daily following a meal.

CYP3A4, 2C9, and 2C19 substrate

CYP3A4 inducer

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.

Nausea

Rilpivirine
(RPV)
Edurant

Edurant

  • 25-mg tablet

STRs that Contain RPVc

  • Complera (RPV/TDF/FTC)
  • Juluca (DTG/RPV)
  • Odefsey (RPV/TAF/FTC)

Copackaged Intramuscular Regimen

  • Cabenuva (CAB plus RPV)

Edurant

  • RPV 25 mg PO once daily with food.

See Appendix A, Table 1 for dosing information for coformulated and copackaged regimens that contain RPV.

 

 

CYP3A4 substrate

PO: 50 hours

IM: 13-28 weeks

Rashd

Depression, insomnia, headache

Hepatotoxicity

QT interval prolongation

IM Formulation Only

  • Injection-site reactions (pain, induration, swelling, nodules)
  • Rare post-injection reaction (dyspnea, agitation, abdominal cramps, flushing) occurring within a few minutes after RPV IM injection; possibly associated with inadvertent IV administration.

a For dose adjustments in people with renal or hepatic insufficiency, see Appendix B. When no food restriction is listed, the antiretroviral drug can be taken with or without food.

b Also see Table 20.

c See Appendix A, Table 1 for information about these formulations.

d Rare cases of Stevens-Johnson syndrome have been reported with the use of most NNRTIs.

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 people 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 people. Late-onset neurotoxicities, including ataxia and encephalopathy, have been reported.

Key: 3TC = lamivudine; ARV = antiretroviral; CAB = cabotegravir; CD4 = CD4 T lymphocyte; CYP = cytochrome P; DOR = doravirine; DTG = dolutegravir; EFV = efavirenz; ETR = etravirine; FTC = emtricitabine; HSR = hypersensitivity reaction; IM = intramuscular; IV = intravenous; NNRTI = non-nucleoside reverse transcriptase inhibitor; PO = orally; RPV = rilpivirine; STR = single-tablet regimen; TAF = tenofovir alafenamide; TDF = tenofovir disoproxil fumarate

 

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