作者
Damilola Alex OMOBOYOWA, Parker Elijah JOSHUA, LWB OLANIYAN
发表日期
2011
期刊
Int J Cur Biomed Phar Res
卷号
1
期号
4
页码范围
186-189
简介
Nevirapine is highly lipophilic and is essentially non-ionized at physiologic pH Nevirapine readily crosses the placenta and is also found in breast milk. Nevirapine is about 60% bound to plasma proteins in the plasma concentration range of 1-10μg/ml [1]. The side effects of nevirapine toxicity include hepatotoxicity (up to 15%, defined as an increase in transaminases to at least three times the upper limit of normal). Liver function tests should be monitored bi-weekly for the first two months, rash which is often pruritic and usually occurring within the first six weeks can generally be treated with antihistamines if mucous membranes are not involved and transaminases are normal [2]. Nevirapine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1; that binds directly to reverse transcriptase (RT) and blocks the RNA-dependent and DNA-dependent DNA polymerase activities by causing a disruption of the enzymes' catalytic site. The activity of nevirapine does not compete with template or nucleoside triphosphate. HIV-2 reverse transcriptase and eukaryotic DNA polymerases (such as human DNA polymerases α β or δ) are not inhibited by nevirapine [1]. Nevirapine is used successfully for the prevention of mother-tochild transmission of HIV. As with all NNRTIs, a single point mutation is sufficient to develop high-level resistance with very good long-term tolerability. Hepatotoxicity within the first month of treatment is a problem with neverapine administration [2].
In vitro studies in humans with human liver microsomes have shown that Nevirapine is extensively bio-transformed via cytochrome p-450 metabolism to several metabolizing …
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