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:
Also available as part of the STR Delstrigo (DOR/TDF/3TC)c |
Pifeltro:
See Appendix B, Table 1 for dosing information for Delstrigo. |
CYP3A4/5 substrate | 15 hours |
Nausea Dizziness Abnormal dreams |
Efavirenz (EFV) Note: Generic product is available. |
Sustiva:
Generic:
STRs that Contain EFV:c
|
Sustiva:
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:
|
Intelence:
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) Note: Generic products are available. |
Viramune:
Viramune XR:
Generic:
|
Viramune:
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:
|
Rilpivirine (RPV) Edurant |
Edurant:
Coformulated STRs that Contain RPV:c
Copackaged Intramuscular Regimen:
|
Edurant:
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:
|
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:
Also available as part of the STR Delstrigo (DOR/TDF/3TC)c |
Pifeltro:
See Appendix B, Table 1 for dosing information for Delstrigo. |
CYP3A4/5 substrate | 15 hours |
Nausea Dizziness Abnormal dreams |
Efavirenz (EFV) Note: Generic product is available. |
Sustiva:
Generic:
STRs that Contain EFV:c
|
Sustiva:
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:
|
Intelence:
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) Note: Generic products are available. |
Viramune:
Viramune XR:
Generic:
|
Viramune:
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:
|
Rilpivirine (RPV) Edurant |
Edurant:
Coformulated STRs that Contain RPV:c
Copackaged Intramuscular Regimen:
|
Edurant:
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:
|
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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