Nevirapine

11 -cyclopropyl -4-methyl -5 ,11 -dihydro -6H- dipyrido [ 3,2-b :2,3 -e ] - [ 1,4] diazepin- 6-one

J05AG01

White to off- white powder

Antiviral, non-nucleoside reverse transcriptase inhibitors

Non- competitive inhibition of reverse transcriptase

247-249 ° C

2.8

Practically insoluble in water, slightly soluble to slightly soluble in dichloromethane, sparingly soluble in methanol

400 mg · kg -1 ( LD50, rat, oral)

Template: Infobox chemical / molecular formula search available

Nevirapine ( Viramune ® trade name, manufacturer Boehringer Ingelheim) is a drug used to treat HIV -1 -infected patients under antiretroviral combination therapy.

History

Nevirapine was the first professional representatives the class of non-nucleoside reverse transcriptase inhibitors ( NNRTI). The approved in 1996 in the U.S. and in Europe in 1997.

Pharmacology

Nevirapine binds non- competitively to the reverse transcriptase of HIV-I, near the substrate binding site for nucleosides. Wherein the catalytically active site is blocked. It can now bind less nucleosides and the polymerization is slowed significantly. Due to the mechanism of the development of resistance of the HIV virus is already possible by simple mutation of the binding site. This results in additional resistance to other non-nucleoside RT inhibitors, as these have a common binding site. Therefore, a use is recommended only in combination therapy. An effect on HIV - II does not, because it has a different binding site.