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Nevirapine ( NVP ), marketed under the trade name Viramune among others, is a medication used to treat and prevent HIV/AIDS, specifically HIV-1.
Common side effects include rash, headache, nausea, feeling tired, and liver problems.
Nevirapine was approved for medical use in the United States in 1996.
1 Medical uses
1.1 Preventing mother-to-child transmission
2 Adverse effects
3 Drug interactions
4 Mechanism of action
5 History
6 Society and culture
7 References
Medical uses
Nevirapine is used in adults and in children 6 years of age infected with HIV-1 as part of combination antiretroviral treatment (ART or cART). Mono treatment use of nevirapine is not indicated due to increased risk of resistance.
Nevirapine in triple combination therapy has been shown to suppress viral load effectively when used as initial antiretroviral therapy ( i.e., in antiretroviral-naive patients).
This drug is generally only to be considered for used in HIV-1 infected population once CD4 cell counts are very low.
Although concerns have been raised about nevirapine-based regimens in those starting therapy with high viral load or low CD4 count, some analyses suggest that nevirapine may be effective in this group of people.
Nevirapine may also form a useful component of salvage regimens after virological failure, usually in combination with one or more PIs as well as nucleotide reverse transcriptase inhibitor (NRTIs), especially in those who have not previously taken an NNRTI.
Dosing in children is based on body surface area (BSA),
Preventing mother-to-child transmission
A single dose of nevirapine given to both mother and child reduced the rate of HIV transmission by almost 50% compared with a very short course of zidovudine (AZT) prophylaxis, in a clinical trial in Uganda.
A major concern with this approach is that NNRTI resistance mutations are commonly observed in both mothers and infants after single-dose nevirapine,
Adverse effects
The most common adverse effect of nevirapine is the development of mild or moderate rash (13%).
Nevirapine may cause severe or life-threatening liver toxicity, usually emerging in the first six weeks of treatment.
Cases of immune reconstitution syndrome and fat redistribution have also been observed with this drug.
U.S. Food and Drug Administration recommends stopping nevirapine if a person experiencing:
sign and symptoms of liver issues such as hepatitis
increased transaminases in addition to rash or systemic symptoms
formation of rash with systemic symptoms
severe skin or hypersensitivity reactions
Additionally, U.S. FDA recommends monitoring closely for first 6 weeks of therapy for above symptoms as there is high risk during this time. Monitor for up to the first 18 weeks of treatment and if a patient experiences 1) hepatitis plus rash or other systemic symptoms or 2) severe hypersensitivity or skin rash, nervirapine should not be restarted.
Drug interactions
Nevirapine is a substrate for liver CYP3A and CYP2B6 enzymes. Concomitant administration of drugs that are inhibitors of these enzymes may increase serum nevirapine levels significantly. Some examples of these drugs include ritonavir, fosamprenavir, and fluconazole. On the other hand, drugs that are inducers of these enzymes such as rifampicin may lower serum nevirapine levels.
In addition, concomitant use of St. John’s wort (Hypericum perforatum) or St. John’s wort containing products may significantly lower nevirapine levels.
Nevirapine is an inducer of cytochrome P450 isoenzymes CYP3A4 and CYP2B6. It may reduce levels of several co-administered drugs including the antiretrovirals efavirenz, indinavir, lopinavir, nelfinavir and saquinavir, as well as clarithromycin, ketoconazole, forms of hormonal contraception, and methadone.
Mechanism of action
Nevirapine shown in ball and stick structure.
Nevirapine falls in the non-nucleoside reverse transcriptase inhibitor (NNRTI) class of antiretrovirals.
Nevirapine is not effective against HIV-2, as the pocket of the HIV-2 reverse transcriptase has a different structure, which confers intrinsic resistance to the NNRTI class.
Resistance to nevirapine develops rapidly if viral replication is not completely suppressed. As all NNRTIs bind within the same pocket, viral strains which are resistant to nevirapine are usually also resistant to the other NNRTIs, efavirenz and delavirdine. However, second generation NNRTIs like rilpivirine and etravirine are effective in treatment for HIV strains resistant to nevirapine and other first generation drugs in that same class.
Nevirapine was discovered by Hargrave et al. at Boehringer Ingelheim Pharmaceuticals, Inc., one of the Boehringer Ingelheim group of companies. It is covered by U.S. Patent 5,366,972 and corresponding foreign patents. Nevirapine was the first NNRTI approved by the U.S. Food and Drug Administration (FDA). It was approved June 21, 1996 for adults and September 11, 1998 for children. It was also approved in Europe in 1997.
Society and culture
Former U.S. President George W. Bush ‘s PEPFAR funding of $500 million to help combat the African AIDS epidemic included nevirapine, among other medications and programs.

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