Generic Name (Abbreviation) Trade Name | Formulations | Dosing Recommendationsa | Elimination/ Metabolic Pathway | Serum Half-Life | Adverse Eventsb |
---|---|---|---|---|---|
Doravirine |
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 Note: The branded product Sustiva has been discontinued. |
Efavirenz (generic)
STRs that Contain EFVc
|
Efavirenz (generic)
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 QT interval prolongation Use of EFV may lead to false-positive results with some cannabinoid and benzodiazepine screening assays. |
Etravirine |
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 Note: Generic products are available. |
Viramune
Viramune XR
Generic
50-mg/5-mL oral suspension |
Viramune
Take without regard to food. 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 12). |
25–30 hours |
Rash, including Stevens-Johnson syndromed Symptomatic Hepatitis
|
Rilpivirine |
Edurant
Coformulated STRs that Contain RPVc
Copackaged Intramuscular Regimen
|
Edurant
Take with food. 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 12. When no food restriction is listed, the antiretroviral 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 |