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)
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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.