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 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.

Appendix B, Table 4. Characteristics of Non-Nucleoside Reverse Transcriptase Inhibitors
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:
  • One tablet 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 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 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, 100, and 200 mg tablets
Intelence:
  • ETR 200 mg 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 once daily for 14 days (lead-in period); thereafter, NVP 200 mg twice daily, or
  • NVP 400 mg (Viramune XR tablet) 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 total.
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 10).
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
STRs that Contain RPV:c
  • Complera (RPV/TDF/FTC)
  • Juluca (DTG/RPV)
  • Odefsey (RPV/TAF/FTC)
Edurant:
  • RPV 25 mg once daily
Take with a meal.

See Appendix B, Table 1 for dosing information for STRs that contain RPV.
CYP3A4 substrate 50 hours Rashd

Depression, insomnia, headache

Hepatotoxicity

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  

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 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.

Appendix B, Table 4. Characteristics of Non-Nucleoside Reverse Transcriptase Inhibitors
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:
  • One tablet 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 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 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, 100, and 200 mg tablets
Intelence:
  • ETR 200 mg 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 once daily for 14 days (lead-in period); thereafter, NVP 200 mg twice daily, or
  • NVP 400 mg (Viramune XR tablet) 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 total.
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 10).
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
STRs that Contain RPV:c
  • Complera (RPV/TDF/FTC)
  • Juluca (DTG/RPV)
  • Odefsey (RPV/TAF/FTC)
Edurant:
  • RPV 25 mg once daily
Take with a meal.

See Appendix B, Table 1 for dosing information for STRs that contain RPV.
CYP3A4 substrate 50 hours Rashd

Depression, insomnia, headache

Hepatotoxicity

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  
Updated
Reviewed
Dec. 18, 2019

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