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Nevirapine
- indication:For use in combination with other antiretroviral drugs in the ongoing treatment of HIV-1 infection.
- pharmacologypharmacology:
- mechanism: 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.
- toxicity: Symptoms of overdose include edema, erythema nodosum, fatigue, fever, headache, insomnia, nausea, pulmonaryinfiltrates, rash, vertigo, vomiting, and weight decrease.
- absorprion: 90% (absolute bioavailability 93 ± 9%)
- halflife: 45 hours
- roouteelimination: 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.
- volumedistribution: * 1.21 ± 0.09 L/kg
- clearance: