| 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. |
| Absorption |
90% (absolute bioavailability 93 ± 9%) |
| Volume of distribution |
|
| 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. |
| Route of elimination |
Thus cytochrome P450 metabolism, glucuronide conjugation, and
urinary excretion of glucuronidated metabolites represent the primary
route of nevirapine biotransformation and elimination in humans. Only a
small fraction (<5%) of the radioactivity in urine (representing
<3% of the total dose) was made up of parent compound; therefore,
renal excretion plays a minor role in elimination of the parent
compound. |
| Half life |
45 hours |
| Clearance |
Not Available |
| Toxicity |
Symptoms of overdose include edema, erythema nodosum, fatigue,
fever, headache, insomnia, nausea, pulmonaryinfiltrates, rash, vertigo,
vomiting, and weight decrease. |
