Nevirapine, an antiretroviral drug |NNRTI

Nevirapine belongs to a group of medicines called antiretrovirals, used in the treatment of Human Immunodeficiency Virus (HIV-1) infection. The active substance of your medicine is called nevirapine. Nevirapine belongs to a class of anti-HIV medicines called non-nucleoside reverse transcriptase inhibitors (NNRTIs). Reverse transcriptase is an enzyme that HIV needs in order to multiply.
Nevirapine is a dipyridodiazepinone compound.




Nevirapine stops reverse transcriptase from working. By stopping reverse transcriptase from working, Nevirapine helps control HIV-1 infection. Nevirapine is indicated for the treatment of HIV-1 infected adults, adolescents, and children of any age. You must take Nevirapine together with other antiretroviral medicines. Your doctor will recommend the best medicines for you.




Class: Nevirapine is a dipyridodiazepinone compound.

Antiviral Activity: Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are highly selective for HIV-1 but do not exhibit activity against other viruses.

Pharmacodynamics
In vitro IC50 for nevirapine ranges between 0.01 and 0.1 μM.

Pharmacokinetics

Nevirapine is well absorbed after oral administration. Its absolute bioavailability appears to be greater than 90% and maximum concentrations are generally achieved by 4 hours after an oral dose. It is approximately 60% bound to plasma proteins. Nevirapine is extensively metabolized by the cytochrome P450 system, mainly 3A4. Nevirapine is an inducer of CYP450 3A4, which leads to auto-induction.

Therapeutic indications

Nevirapine Teva is indicated in combination with other anti-retroviral medicinal products for the treatment of HIV-1 infected adults, adolescents, and children of any age.
Most of the experience with nevirapine is in combination with nucleoside reverse transcriptase inhibitors (NRTIs). The choice of a subsequent therapy after nevirapine should be based on clinical experience and resistance testing

Mechanism of Action

Nevirapine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1. 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. HIV-2 RT and eukaryotic DNA polymerases (such as human DNA polymerases α, ß, γ, or δ) are not inhibited by nevirapine.

Dose and method of administration

Adults 16 years and older

The recommended dose  is one 200 mg tablet daily for the first 14 days (this lead-in period should be used because it has been found to lessen the frequency of rash), followed by one 200 mg tablet twice daily, in combination with at least two additional antiretroviral agents. For concomitantly administered nucleoside therapy, the manufacturer's recommended dosage and monitoring should be followed.

Pediatric Dosing


  • 2 months up to 8 years of age - 4 mg/kg once daily for the first 14 days followed by 7 mg/kg twice daily thereafter.
  • 8 years and older - 4 mg/kg once daily followed by 4 mg/kg twice daily thereafter (Total nevirapine dose should not exceed 400mg)

Contraindications/Warnings/Precautions

Hypersensitivity to the active substance or to any of the excipients. Severe, life threatening, and in some cases fatal hepatotoxicity, including fulminant and cholestatic hepatitis, hepatic necrosis and hepatic failure and severe, life threatening skin reactions have been reported with the use of nevirapine.

Drug Interactions

Nevirapine is an inducer of hepatic cytochrome P450 3A. Therefore medications that are metabolized by CYP3A may interact with nevirapine.

Pregnancy

Category C: Risk unknown. Human studies inadequate.
Nevirapine is well studied and tolerated as an antiretroviral agent to prevent perinatal transmission. However, there is concern over the emergence of resistance after using nevirapine to prevent mother to child transmission.



Reference
https://aidsinfo.nih.gov/drugs/116/nevirapine/0/patient
https://www.webmd.com/drugs/2/drug-13802-6268/nevirapine-oral/nevirapine-oral/details
https://www.aidsmap.com/about-hiv/arv-background-information/nevirapine-viramune
http://www.antimicrobe.org/drugpopup/nevirapine.htm
https://www.drugbank.ca/drugs/DB00238
https://www.drugs.com/mtm/nevirapine.html
https://reference.medscape.com/drug/viramune-viramune-xr-nevirapine-342623
https://clinicaltrials.gov/ct2/show/NCT00074412

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