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Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents

Appendix B: Drug Characteristics Tables

Table 2

(Last updated:10/14/2011; last reviewed:3/27/2012)

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Appendix B, Table 2. Characteristics of Non-Nucleoside Reverse Transcriptase Inhibitors* (NNRTIs)

*DLV is not included in this table. Please refer to the DLV FDA package insert for related information.

Generic Name (abbreviation)/ Trade Name Formulations Dosing Recommendations
(For dosage adjustment in renal or hepatic insufficiency, see
Appendix B, Table 7.)		 Elimination Serum
Half-life		 Adverse Events
(Also see Table 13)
Efavirenz (EFV)/
Sustiva

Also available as component of fixed-dose combination:

 • 50-, 200-mg capsules

• 600-mg tablet
 600 mg once daily at or before bedtime

Take on an empty stomach to reduce side effects.		 Metabolized by CYPs 2B6 and 3A4

CYP3A4 mixed inducer/inhibitor (more an inducer than an inhibitor)		 40-55 hrs • Rasha
• Neuropsychiatric symptomsb
• Increased transaminase levels
• Hyperlipidemia
• False-positive results with some cannabinoid and benzodiazepine screening assays reported.
• Teratogenic in nonhuman primates and potentially teratogenic in humans
Atripla
EFV
with TDF + FTC		 (EFV 600 mg + FTC 200 mg + TDF 300 mg) tablet 1 tablet once daily at or before bedtime.
Etravirine (ETR)/ Intelence • 100-, 200-mg tablets 200 mg BID
Take following a meal.		 CYP3A4, 2C9, and 2C19 substrate

3A4 inducer; 2C9 and 2C19 inhibitor		 41 hrs • Rash, including Stevens-Johnson syndromea
• HSRs, characterized by rash, constitutional findings, and sometimes organ dysfunction, including hepatic failure, have been reported.
• Nausea
Nevirapine
(NVP)/
Viramune or Viramine XR		 • 200-mg tablet

• 400-mg XR tablet

• 50-mg/5-mL oral suspension		  200 mg once daily for 14 days (lead-in period); thereafter, 200 mg BID or 400 mg (Viramune XR tablet) once daily

Take without regard to meals.

Repeat lead-in period if therapy is discontinued for more than 7 days.

In patients who develop mild-to-moderate rash without constitutional symptoms, continue lead-in period until rash resolves but not longer than 28 days total.

 CYP450 substrate, inducer of 3A4 and 2B6; 80% excreted in urine (glucuronidated metabolites, <5% unchanged); 10% in feces 25-30 hrs • Rash, including Stevens-Johnson syndromea
• Symptomatic hepatitis, including fatal hepatic necrosis, has been reported:
- rash reported in approximately 50% of cases;
- occurs at 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

Also available as component of fixed-dose combination:		 • 25-mg tablet 25 mg once daily
Take with a meal.
 CYP3A4 substrate 50 hrs • Rasha
• Depression, insomnia, headache
Complera
RPV with TDF + FTC		 Complera
(RPV 25 mg +
TDF 300 mg +
FTC 200 mg) tablet		 1 tablet once daily with a meal

Key to Abbreviations: ARV = antiretroviral, BID = twice daily, CYP = cytochrome P, DLV = delavirdine, EFV = efavirenz, ETR = etravirine, FDA = Food and Drug Administration, FTC = emtricitabine, HSR = hypersensitivity reaction, NNRTI = non-nucleoside reverse transcriptase inhibitor, NVP = nevirapine, RPV = rilpivirine, TDF = tenofovir disoproxil fumarate, XR = extended release

a Rare cases of Stevens-Johnson syndrome have been reported with most NNRTIs; the highest incidence of rash was seen with NVP.
b Adverse events can include dizziness, somnolence, insomnia, abnormal dreams, 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.