Generic Name (Abbreviation) 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 STRs That Contain DORc
| Pifeltro
See Appendix A, 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)
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
| Intelence
| 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
STRs that Contain RPVc
Copackaged Intramuscular Regimen
| Edurant
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
|
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 |