Application of Nevirapine as the Non-Nucleoside Reverse Transcriptase Inhibitor

Chemical name: 11-cyclopropyl-5,11-dihydro-4-methyl-6-hydrogen-bipyridine-[3,2-b: 2,3-e][1,4]diazepine- 6-ketone

Sold under the brandname in China: Nevirapine

Appearance: white or off-white powder, odorless.

English name: Nevirapine (NVP for short).

Structural features: dipyridodiazepine.

Nucleoside mechanism: It needs to be converted into a triphosphate form to work.

Non-nucleosides: not required, not used alone, used in combination with nucleosides.

Nevirapine is a non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI) that blocks RNA-dependence and the activity of DNA-dependent DNA polymerase by direct ligation with HIV-1 reverse transcriptase (RT) and by rupturing the catalytic end of this enzyme. It does not compete with substrate or nucleoside triphosphate, and can be used in combination with other antiretroviral drugs to treat HIV-1 infection. In June 1996, Nevirapine was approved for medical use in the treatment of HIV infection in adults together with nucleoside drugs by the US Food and Drug Administration (FDA). 

At present, the common adverse reactions include: rash, liver problems, feeling tired, fever, headache, drowsiness, and adverse reactions to the digestive tract, myalgia, severe liver damage, liver failure and allergic reactions. In January 2005, the FDA posted a message on its official website to remind medical staff of patients with high CD4 cell counts (women with CD4 count >250/mm3 and men >400/mm3) having higher potential of liver damage. Therefore, for patients who have not previously received antiviral therapy, if the CD4 cell counts are higher than the above two thresholds, Nevirapine should be avoided.
 

Referrence

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