Product Information
Registration Status: ActiveVIRAMUNE XR TABLET 400mg is approved to be sold in Singapore with effective from 2013-01-24. It is marketed by BOEHRINGER INGELHEIM SINGAPORE PTE LTD, with the registration number of SIN14299P.
This product contains Nevirapine 400mg in the form of TABLET, EXTENDED-RELEASE. It is approved for ORAL use.
This product is manufactured by Boehringer Ingelheim Roxane Inc in UNITED STATES.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
A potent, non-nucleoside reverse transcriptase inhibitor (NNRTI) used in combination with nucleoside analogues for treatment of Human Immunodeficiency Virus Type 1 (HIV-1) infection and AIDS. [PubChem] Structurally, nevirapine belongs to the dipyridodiazepinone chemical class.
Indication
For use in combination with other antiretroviral drugs in the ongoing treatment of HIV-1 infection.
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.
Pharmacokinetics
- Absorption
- Nevirapine is readily absorbed (greater than 90%) after oral administration in healthy subjects and adults with HIV-1 infection. The absolute bioavailability in healthy adults following a single dose administration is 93 ± 9% (mean ± SD) for a 50 mg tablet and 91 ± 8% for an oral solution. Peak plasma nevirapine concentrations of 2 ± 0.4 mcg/mL (7.5 micromolar) were attained by 4 hours following a single 200 mg dose. Nevirapine tablets and suspension have been shown to be comparably bioavailable and interchangeable at doses up to 200 mg. When the oral tablet is given with a high-fat meal, the extent of absorption is compared to that of the fasted-state.
- Distribution
- * 1.21 ± 0.09 L/kg [apparent volume of distribution, healthy adults, IV] Nevirapine is capable of crossing the placenta and is found in breast milk.
- 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.
- Elimination
Toxicity
Symptoms of overdose include edema, erythema nodosum, fatigue, fever, headache, insomnia, nausea, pulmonaryinfiltrates, rash, vertigo, vomiting, and weight decrease. The most common adverse reaction is rash.
Active Ingredient/Synonyms
11-cyclopropyl-5,11-dihydro-4-methyl-6H-dipyrido(3,2-b:2',3'-e)(1,4)diazepin-6-one | NEV | Nevirapine anhydrous | Nevirapine, anhydrous | NVP | Nevirapine |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.