Neurotransmitters and their receptor subtypes

Nevirapine is a nonnucleoside reverse-transcriptase inhibitor that inhibits replication of retroviruses, including HIV. In combination with other antiretroviral agents it is used for treatment of HIV-1 infection. 

Nevirapine is a dipyridodiazepinone NNRTl with potent activity against HIV-1. The in vitro ICjg of this drug ranges from 10 to 100 nM. Like other compounds in this class, nevirapine does not have significant activity against HlV-2 or other retroviruses. 

Nevirapine is a noncompetitive inhibitor that binds to a site on the HIV-1 reverse transcriptase that is distant from the active site, inducing a conformational change that disrupts catalytic activity. As the target site is HIV-1-specific and is not essential for the enzyme, resistance can develop rapidly. A single mutation at either codon 103 or codon 181 of reverse transcriptase decreases susceptibility more than a hundredfold. Nevirapine resistance is also associated 

Nevirapine is well absorbed, and its bioavailability is not altered by food or antacids. The drug readily crosses the placenta and has been found in breast milk, a feature that has encouraged use of nevirapine for prevention of mother-to-child transmission of HIV. 

The most frequent adverse event associated with nevirapine is rash, which occurs in approximately 16% of patients. Mild macular or papular eruptions commonly involve the trunk, face, and extremities and generally occur within the first 6 weeks of therapy. Pruritus is also common. In the majority of patients, the rash resolves with continued administration of drug. Up to 7% of patients discontinue therapy owing to rash, and administration glucocorticoids may cause a more severe rash. Life-threatening Stevens-Johnson syndrome is rare but occurs in up to 0 3% of recipients. 

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