Last Updated June 10, 2016
Nonnucleoside reverse transcriptase inhibitor antiretroviral.
Indication: treatment of HIV infection in combination with other antiretrovirals, reduction of perinatal transmission of HIV.
Mechanism of action*: binds directly to reverse transcriptase, which interferes with HIV viral RNA–dependent DNA polymerase inhibiting viral replication.
Pharmacokinetics: metabolized in the liver by CYP 3A4 and 2B6. CYP 3A4 and 2B6 inducer. Half life: 25-30 hours; autoinducer.
Adult Dose: 200 mg once daily x 14 days, then 200 mg twice daily.
Prevention of mother-to-child transmission: 200 mg to mother at onset of labour, 2 mg/kg to infant within 72 hours.
Use in Renal or Hepatic Insufficiency:
Use in Pregnancy and Breastfeeding: Category B. Excreted into breast milk. Safety in lactation not established.
Use in Children:
US Prescribing Information Boxed Warning: severe hepatotoxic reactions may occur (fulminant and cholestatic hepatitis, hepatic necrosis) and, in some cases, have resulted in hepatic failure and death. The greatest risk of these reactions is within the initial 6 weeks of treatment, in patients with chronic or acute hepatitis, and in patients with higher CD4+ cell counts. Intensive monitoring is required during the initial 18 weeks of therapy to detect potentially life-threatening hepatic reactions.*
US Prescribing Information Boxed Warning: severe life-threatening skin reactions (eg, Stevens-Johnson syndrome, toxic epidermal necrolysis, hypersensitivity reactions with rash and organ dysfunction), including fatal cases, have occurred. The greatest risk of these reactions is within the initial 6 weeks of treatment; intensive monitoring is required during the initial 18 weeks of therapy to detect potentially life-threatening dermatologic and hypersensitivity reactions.*
Liver function monitoring is recommended at baseline, Weeks 2, 4, and 8, and periodically thereafter.
If nevirapine discontinuation is required, continue companion drugs and substitute with a PI to avoid development of resistance. The optimal time for staggered discontinuation has not been established.
Coadministration not recommended*: St John’s wort, other NNRTIs, atazanavir, ketoconazole, itraconazole, rifampin (Southern African HIV Clinician Society provides guidance on coadministration†), boceprevir, telaprevir.
Increased concentrations of concomitant medication*: warfarin, rifabutin (dose 300 mg/day†).
Decreased concentrations of concomitant medication*: methadone, antiarrhythmics, warfarin, carbamazepine, itraconazole, ketoconazole, ergotamine, clarithromycin, diltiazem, verapamil, nifedipin, ethinyl estradiol, norethindrone, cyclosporine, tacrolimus, sirolimus, cyclophosphamide, cisapride, fentanyl.
Increased concentrations of nevirapine with concomitant medication*: fluconazole, itraconazole, ketoconazole.
Decreased concentrations of nevirapine with concomitant medication*: carbamazepine, clonazepam, ethosuximide, rifampin.
Drug interactions between nevirapine and other antiretrovirals and recommended dosing changes*:
Efficacy of oral contraceptives may be reduced.
See above for pregnancy and lactation and paediatric dosing.
Clinical hepatitis is common but abnormal liver function tests are more common and both occur within the first 8 weeks.
*Information from US prescribing information.
†Recommendation from Southern African HIV Clinician Society Guidelines.