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Nevirapine


ACCESSION NB: DB00238 (APRD00705)


TYPE: small molecule


GROUP: approved


DESCRIPTION:
A potent, non-nucleoside reverse transcriptase inhibitor used in combination with nucleoside analogues for treatment of HIV infection and AIDS. [PubChem]

VOLUME OF DISTRIBUTION: 1.21 ± 0.09 L/kg

CATEGORIES:
Anti-HIV Agents Nonnucleoside Reverse Transcriptase Inhibitors Reverse Transcriptase Inhibitors

ABSORPTION: 90% (absolute bioavailability 93 ± 9%)

INDICATION:
For use in combination with other antiretroviral drugs in the ongoing treatment of HIV-1 infection.

PHARMACODYNAMICS:
Nevirapine is a non-nucleoside reverse transcriptase inhibitor (nNRTI) with activity against Human Immunodeficiency Virus Type 1 (HIV-1). HIV-2 RT and eukaryotic DNA polymerases (such as human DNA polymerases alpha, beta, or sigma) are not inhibited by nevirapine. Nevirapine is, in general, only prescribed after the immune system has declined and infections have become evident. It is always taken with at least one other HIV medication such as Retrovir or Videx. The virus can develop resistance to nevirapine if the drug is taken alone, although even if used properly, nevirapine is effective for only a limited time.

MECHANISM OF ACTION:
Nevirapine binds directly to reverse transcriptase (RT) and blocks the RNA-dependent and DNA-dependent DNA polymerase activities by causing a disruption of the enzyme's catalytic site. The activity of nevirapine does not compete with template or nucleoside triphosphates.

PROTEIN BINDING:
60%

METABOLISM:
Hepatic. In vivo studies in humans and in vitro studies with human liver microsomes have shown that nevirapine is extensively biotransformed via cytochrome P450 3A4 metabolism to several hydroxylated metabolites. Enzyme Metabolite Reaction Km Vmax Cytochrome P450 3A5 12-Hydroxynevirapine Cytochrome P450 3A5 2-Hydroxynevirapine Cytochrome P450 2D6 12-Hydroxynevirapine Cytochrome P450 2D6 8-Hydroxynevirapine Cytochrome P450 3A4 12-Hydroxynevirapine Cytochrome P450 3A4 2-Hydroxynevirapine Cytochrome P450 3A4 8-Hydroxynevirapine Cytochrome P450 2C9 12-Hydroxynevirapine Cytochrome P450 2B6 8-Hydroxynevirapine Cytochrome P450 2B6 3-Hydroxynevirapine

TOXICITY:
Symptoms of overdose include edema, erythema nodosum, fatigue, fever, headache, insomnia, nausea, pulmonaryinfiltrates, rash, vertigo, vomiting, and weight decrease.

AFECTED ORGANISMS:
Human Immunodeficiency Virus