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Generic Name (Abbreviation)/ Trade Name
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Formulations
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Dosing Recommendations
(For dosage adjustment in renal or hepatic insufficiency, see
Appendix B, Table 7.)
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Elimination
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Serum
Half-life
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Adverse Events
(Also see Table 13.)
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Efavirenz (EFV)/
Sustiva
Also available as a component of fixed-dose combination:
|
- 50 and 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 hours |
- Rasha
- Neuropsychiatric symptomsb
- Increased transaminase levels
- Hyperlipidemia
- False-positive results with some cannabinoid and benzodiazepine screening assays reported.
- Teratogenic in non-human 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 |
- 25, 100, and 200 mg tablets
|
200 mg BID
Take following a meal. |
CYP3A4, 2C9, and 2C19 substrate
3A4 inducer; 2C9 and 2C19 inhibitor |
41 hours |
- 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
Generic available for 200 mg tablets |
- 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 hours |
- 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 once daily
Take with a meal
|
CYP3A4 substrate |
50 hours |
- Rasha
- Depression, insomnia, headache
- Hepatotoxicity
|
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.
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