US DHHS Guidelines with Australian commentary
Characteristics of Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)
Last Updated: October 25, 2018;
Last Reviewed: October 25, 2018
Note: DLV is not included in this table. Please refer to the DLV Food and Drug Administration package insert for related infor
|Formulations||Dosing Recommendationsa||Elimination/ Metabolic Pathway||Serum
||CYP3A4/5 substrate||15 hours||
Note: Generic product is available.
||Metabolized by CYPs 2B6 (primary), 3A4, and 2A6
CYP3A4 mixed inducer/inhibitor (more an inducer than an inhibitor) CYP2C9 and 2C19 inhibitor; 2B6 inducer
||CYP3A4, 2C9, and 2C19 substrate
3A4 inducer; 2C9 and 2C19 inhibitor
Viramune or Viramune XR
Note: Generic is available for 200 mg tablets and oral suspension.
||CYP450 substrate, inducer of 3A4 and 2B6; 80% excreted in urine (glucuronidated metabolites, <5% unchanged); 10% in feces
Contraindicated in patients with moderate to severe hepatic impairment.
Dose adjustment is recommended in patients on hemodialysis (see Appendix B, Table 8).
||CYP3A4 substrate||50 hours||
|a For dose adjustments in patients with renal or hepatic insufficiency, see Appendix B, Table 8.
b Also see Table 15.
c Rare cases of Stevens-Johnson syndrome have been reported with most NNRTIs; the highest incidence of rash was seen with NVP.
d Adverse events can include dizziness, somnolence, insomnia, abnormal dreams, depression, suicidality (suicide, suicide attempt or ideation), confusion, abnormal thinking, impaired concentration, amnesia, agitation, depersonalization, hallucinations, and euphoria. Approximately 50% of patients receiving EFV may experience any of these symptoms. Symptoms usually subside spontaneously after 2 to 4 weeks but may necessitate discontinuation of EFV in a small percentage of patients.
Key to Acronyms: 3TC = lamivudine; ARV = antiretroviral; BID = twice daily; CD4 = CD4 T lymphocyte; CYP = cytochrome P; DLV = delavirdine; DOR = doravirine; DTG = dolutegravir; EFV = efavirenz; ETR = etravirine; FTC = emtricitabine; HSR = hypersensitivity reaction; NNRTI = non-nucleoside reverse transcriptase inhibitor; NVP = nevirapine; RPV = rilpivirine; TAF = tenofovir alafenamide; TDF = tenofovir disoproxil fumarate; XR = extended release