Nevirapine

Nevirapine is a nonnucleoside reverse transcriptase inhibitor. The drug inhibits replication of human immunodeficiency virus type 1 (HIV-1) by interfering with viral RNA- and DNA-directed polymerase activities of reverse transcriptase. Nevirapine binds directly to HIV-1 reverse transcriptase and exerts a virustatic effect by acting as a specific, noncompetitive HIV-1 reverse transcriptase inhibitor. Nevirapine is a highly specific antiretroviral agent with a very limited spectrum of activity.

Pharmacokinetics: Nevirapine is administered orally. The drug may be taken without regard to meals. Systemic availability of nevirapine is not affected by concomitant administration with a substantial meal, an antacid, or with didanosine formulated with an alkaline buffering agent. Because nevirapine is extensively metabolized by the liver and nevirapine metabolites are extensively eliminated by the kidneys, the drug should be used with caution in patients with renal or hepatic dysfunction. The manufacturer states that data currently are insufficient to recommend a nevirapine dosage for patients who have hepatic dysfunction or renal insufficiency or are undergoing hemodialysis.

Oral nevirapine is labeled for use in combination with dideoxynucleoside reverse transcriptase inhibitors for the treatment of HIV-1 infections in adults.

Resistance: Strains of HIV-1 with reduced susceptibility to nevirapine have been produced in vitro. Strains of HIV-1 resistant to nevirapine may be cross-resistant to some other nonnucleoside reverse transcriptase inhibitors.

Adverse effects: The drug appears to be well tolerated when administered in combination with zidovudine (with or without didanosine). The major toxicity associated with nevirapine to date is rash, including severe or life-threatening rash. Manifestations of severe rash or rash associated with constitutional symptoms.