Efavirenz
Mechanism :
Efavirenz (EFV) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) of human immunodeficiency virus type 1 (HIV-1). EFV activity is mediated predominantly by non-competitive inhibition of HIV-1 reverse transcriptase (RT). HIV-2 RT and human cellular DNA polymerases a, b, g, and d are not inhibited by EFV.
Indication :
Contraindications :
Contraindicated in patients with clinically significant hypersensitivity to any of its components. Avoided in pregnant women in view of potential teratogenicity. Not recommended in children less than 3 years of age.
Dosing :
Under 3 months:
Safety and efficacy not established.
Above 3 months:
Oral
3.5 to 5 kg:
100 mg OD
5 to 7.5 kg:
150 mg OD
7.5 to 15 kg:
200 mg OD
15 to 20 kg:
250 mg OD
20 to 25 kg:
300 mg OD
25 to 33 kg:
350 mg OD
33 to 40 kg:
400 mg OD
>40 kg:
600 mg OD
Adverse Effect :
Psychiatric symptoms, rash, increased total cholesterol, diarrhea, depression, anxiety, headache, nausea, fatigue, dizziness, insomnia, vomiting.
Interaction :
Astemizole, Cisapride, Midazolam, Triazolam, or Ergot Derivatives: Should not be administered concurrently with astemizole, cisapride, midazolam, triazolam, or ergot derivatives because competition for CYP3A4 by efavirenz could result in inhibition of metabolism of these drugs and create the potential for serious and/or life-threatening adverse events (e.g., cardiac arrhythmias, prolonged sedation, or respiratory depression).
Voriconazole: Efavirenz should not be administered concurrently with voriconazole because it significantly decreases voriconazole plasma concentrations.
Renal Dose :
Dose in Renal Impairment GFR (mL/min)
| 20-50 | Dose as in normal renal function |
| 10-20 | Dose as in normal renal function |
| <10 | Dose as in normal renal function |
Dose in Patients undergoing Renal Replacement Therapies
| CAPD | Not dialysed. Dose as in normal renal function |
| HD | Not dialysed. Dose as in normal renal function |
| HDF/High flux | Not dialysed. Dose as in normal renal function |
| CAV/VVHD | Not dialysed. Dose as in normal renal function |
Hepatic Dose :
Mild hepatic impairment: No dosage adjustment needed.
Moderate and severe hepatic impairment: Use is not recommended.