Updated
Reviewed
Jun. 03, 2021

Appendix B: Drug Characteristics Tables

Characteristics of Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)

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

The older non-nucleoside reverse transcriptase inhibitor (NNRTI) delavirdine (DLV) is no longer used commonly in clinical practice and is not listed this table. Please refer to the Food and Drug Administration product label for DLV for information regarding this drug.

Generic Name (Abbreviations) Trade Name Formulations Dosing Recommendationsa Elimination/ Metabolic Pathway Serum Half-Life Adverse Eventsb
Doravirine (DOR)
Pifeltro

Pifeltro:

  • 100-mg tablet

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

Pifeltro:

  • DOR 100 mg PO once daily

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

CYP3A4/5 substrate 15 hours

Nausea

Dizziness

Abnormal dreams

Efavirenz (EFV)
Sustiva

Note: Generic product is available.

Sustiva:

  • 50-mg and 200-mg capsules
  • 600-mg tablet

Generic:

  • 600-mg tablet

STRs that Contain EFV:c

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

Sustiva:

  • EFV 600 mg PO once daily, at or before bedtime

Take on an empty stomach to reduce side effects.

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

40–55 hours

Rashd

Neuropsychiatric symptomse

Serum transaminase elevations

Hyperlipidemia

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

QT interval prolongation

Etravirine (ETR) Intelence

Intelence:

  • 25-mg, 100-mg, and 200-mg tablets

Intelence:

  • ETR 200 mg PO twice daily

Take 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

Nevirapine (NVP)
Viramune or
Viramune XR

Note: Generic products are available.

Viramune:

  • 200-mg tablet
  • 50-mg/5-mL oral suspension

Viramune XR:

  • 400-mg tablet

Generic:

  • 200-mg tablet
  • 400-mg extended release tablet 50-mg/5-mL oral suspension

Viramune:

  • NVP 200 mg PO once daily for 14 days (lead-in period); thereafter, NVP 200 mg PO twice daily, or
  • NVP 400 mg (Viramune XR tablet) PO once daily

Take without regard to meals.

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.

CYP450 substrate

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 11).

25–30 hours

Rash, including Stevens-Johnson syndromed

Symptomatic Hepatitis:

  • Symptomatic hepatitis, including fatal hepatic necrosis, has been reported.
  • Rash has been reported in approximately 50% of cases.
  • Symptomatic hepatitis occurs at a 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

Edurant:

  • 25 mg tablet

Coformulated STRs that Contain RPV:c

  • 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

Take with a meal.

See Appendix B, 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 patients with renal or hepatic insufficiency, see Appendix B, Table 11. When no food restriction is listed, the ARV drug can be taken with or without food.

b Also see Table 20.

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; 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; NVP = nevirapine; PO = orally; RPV = rilpivirine; STR = single-tablet regimen; TAF = tenofovir alafenamide; TDF = tenofovir disoproxil fumarate; XR = extended release

Appendix B: Drug Characteristics Tables

Characteristics of Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)

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

The older non-nucleoside reverse transcriptase inhibitor (NNRTI) delavirdine (DLV) is no longer used commonly in clinical practice and is not listed this table. Please refer to the Food and Drug Administration product label for DLV for information regarding this drug.

Generic Name (Abbreviations) Trade Name Formulations Dosing Recommendationsa Elimination/ Metabolic Pathway Serum Half-Life Adverse Eventsb
Doravirine (DOR)
Pifeltro

Pifeltro:

  • 100-mg tablet

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

Pifeltro:

  • DOR 100 mg PO once daily

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

CYP3A4/5 substrate 15 hours

Nausea

Dizziness

Abnormal dreams

Efavirenz (EFV)
Sustiva

Note: Generic product is available.

Sustiva:

  • 50-mg and 200-mg capsules
  • 600-mg tablet

Generic:

  • 600-mg tablet

STRs that Contain EFV:c

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

Sustiva:

  • EFV 600 mg PO once daily, at or before bedtime

Take on an empty stomach to reduce side effects.

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

40–55 hours

Rashd

Neuropsychiatric symptomse

Serum transaminase elevations

Hyperlipidemia

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

QT interval prolongation

Etravirine (ETR) Intelence

Intelence:

  • 25-mg, 100-mg, and 200-mg tablets

Intelence:

  • ETR 200 mg PO twice daily

Take 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

Nevirapine (NVP)
Viramune or
Viramune XR

Note: Generic products are available.

Viramune:

  • 200-mg tablet
  • 50-mg/5-mL oral suspension

Viramune XR:

  • 400-mg tablet

Generic:

  • 200-mg tablet
  • 400-mg extended release tablet 50-mg/5-mL oral suspension

Viramune:

  • NVP 200 mg PO once daily for 14 days (lead-in period); thereafter, NVP 200 mg PO twice daily, or
  • NVP 400 mg (Viramune XR tablet) PO once daily

Take without regard to meals.

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.

CYP450 substrate

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 11).

25–30 hours

Rash, including Stevens-Johnson syndromed

Symptomatic Hepatitis:

  • Symptomatic hepatitis, including fatal hepatic necrosis, has been reported.
  • Rash has been reported in approximately 50% of cases.
  • Symptomatic hepatitis occurs at a 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

Edurant:

  • 25 mg tablet

Coformulated STRs that Contain RPV:c

  • 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

Take with a meal.

See Appendix B, 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 patients with renal or hepatic insufficiency, see Appendix B, Table 11. When no food restriction is listed, the ARV drug can be taken with or without food.

b Also see Table 20.

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; 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; NVP = nevirapine; PO = orally; RPV = rilpivirine; STR = single-tablet regimen; TAF = tenofovir alafenamide; TDF = tenofovir disoproxil fumarate; XR = extended release

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