Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: EC:2.7.7.49 (reverse transcriptase)
 31,746 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

A new class of anti-HIV drugs has entered the treatment arena. Non-nucleoside reverse transcriptase inhibitors (NNRTIs) interfere with infected cells and suppress their ability to replicate. Delaviradine (Rescriptor) and nevirapine (Viramune) are described, including drug interactions, trial results, and the potential for resistance.
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PMID:A new class of anti-HIV drugs. 1136 16

Now available in pharmacies, the first of a new class of non-nucleoside reverse transcriptase inhibitors (NNRTIs) has been licensed. Nevirapine (marketed as Viramune) is different from nucleoside reverse transcriptase inhibitors because it binds at a different location on the HIV-1 virus and at a different point in the reproduction process in its effort to block HIV replication. Also, HIV-1 mutant strains, which become resistant to other drugs, have remained sensitive to nevirapine. The Food and Drug Administration (FDA) Antiviral Drugs Advisory Committee recommended that nevirapine be used only in combination therapy, but did not complicate the label by stating whether to include one or two additional drugs. They recommended approval for both treatment-naive and experienced individuals. Although suppression of viral replication is modest, the NNRTIs appear to penetrate the central nervous system and offer an alternative for people either intolerant of or resistant to the currently available nucleoside analogs. A major side effect of the drug is the development of a severe rash. The manufacturer, Boehringer Ingelheim, has promised to issue a booklet on how to manage a nevirapine-related rash. Individuals interested in the patient assistance program may call Boehringer Ingelheim for more information.
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PMID:Nevirapine, the first of a new class of NNRTI drugs arrives in pharmacies. 1136 27

Manufacturers of nevirapine (Viramune) report that studies of the interaction of this non-nucleoside reverse transcriptase drug and indinavir and saquinavir are underway. About 21 patients have been treated with nevirapine and saquinavir, and 22 patients have been treated with nevirapine and ritonavir. These studies will determine whether nevirapine can be safely taken with protease inhibitors. Preliminary interaction studies suggested that nevirapine decreases the drug levels of saquinavir by about 17 percent. Currently, nevirapine is labeled for combination with nucleoside analogues only.
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PMID:Nevirapine-plus-protease studies under way. 1136 56

Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are the latest drugs used to treat HIV infection. Three NNRTIs are introduced: Viramune (nevirapine), Rescriptor (delavirdine), and Viracept (nelfinavir). Recommended doses, rates of absorption, side effects, distribution throughout the body, clinical studies, reactions with other drugs, and how the drugs are metabolized are given. A list of agents that may inhibit the effect of Rescriptor and Viracept, such as antihistamines, antibiotics and anti-convulsions, is presented.
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PMID:[New combination medications]. 1136 1

Voluntary HIV testing of pregnant women and perinatal treatment with AZT have caused a decline in the rate of transmission of HIV to infants during delivery. Researchers are now looking at whether AZT in combination with other antiretrovirals will be even more effective in reducing infection rates. At the 37th Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) held in Toronto, researchers from the Centers for Disease Control and Prevention (CDC) reported that up to 80 percent of mothers whose HIV-positive children were identified by HIV/AIDS surveillance knew their health status before giving birth. A total of 77 percent of women received perinatal prophylaxis in 1996, compared to 36 percent in 1994. The CDC also reported a 12 percent infection rate in children who received perinatal treatment from September 1994 to December 1995, compared to 30 percent in those who received no treatment. The CDC is using this surveillance data to help States to determine how close they are to meeting the new guidelines of the Ryan White CARE Act. One requirement is to inform 95 percent of all pregnant women about their HIV status, thereby reducing perinatal infections by half. Of the new treatments being tested to reduce transmission rates, a Phase III study of nevirapine (Viramune) is the farthest along. The ACTG 316 study has begun enrolling women at 18 centers in the United States to test the non-nucleoside reverse transcriptase inhibitor. When combined with European sites, the study population should be large enough to guarantee statistical significance.
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PMID:Perinatal HIV down as treatment increases. 1136 70

Recent progress in treatment methods and medicines has made HIV more manageable. Factors contributing to this progress include advances in testing; the use and approval of protease inhibitors, non-nucleoside reverse transcriptase inhibitors, and other nucleosides; and the success of highly active antiretroviral regimens (HAART) and combination therapy. Nucleoside reverse transcriptase inhibitors, such as Zidovudine and Didanosine, and non-nucleoside reverse transcriptase inhibitors (NNRTIs) such as Nevirapine (Viramune) and Delavirdine (Rescriptor), are recommended for use in combination therapy. The pharmacology, side effects, and contraindications of these types of drugs are provided. Dosages and common side effects are also mentioned.
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PMID:Understanding the reverse transcriptase inhibitors in HIV. 1136 42

Nevirapine (Viramune), a non-nucleoside reverse transcriptase inhibitor, is now approved for use in children. It should be used as part of a three-drug combination for maximum effectiveness and to prevent resistance. In adults Nevirapine is often paired with two nucleoside analogues. Recommended doses for children and possible side effects are presented.
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PMID:Nevirapine in children. 1136

None of the studies conducted on people who have reduced the number of antivirals taken in their regimen have shown good results. Research has consistently shown that these people have an increased viral load count when one or more drugs are discontinued. Results from a French study show some promise in switching from a protease inhibitor to a nonnucleoside analogue reverse transcriptase inhibitor (NNRTI) such as Viramune (Nevirapine) or Sustiva (efavirenz). Fifteen out of sixteen participants maintained viral load levels below 200 copies when they changed to an NNRTI regimen. The one person whose viral load increased had taken an NNRTI drug before, although its use was prohibited in eligibility requirements. The strategy may work for people at varying stages of the disease, but larger studies are needed to confirm the results. Also, a fifth protease inhibitor, Amprenavir (Agenerase) has received FDA approval. Trial results are summarized, and side effects and drug interactions with Amprenavir are described.
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PMID:New treatment options. 1136 13

Nevirapine (Viramune, Boehringer Ingelheim) is a non-nucleoside reverse transcriptase (RT) inhibitor (NNRTI) effective in the treatment of HIV-1 infected antiretroviral-naive and -experienced patients. Some recent studies have suggested that nevirapine-based regimens may have an efficacy similar to protease inhibitor (PI)-based regimens, at least in naive patients with CD4+ > 200 microl, while it lacks the drawbacks inherent in PI-containing regimens, such as lipodystrophy and metabolic alterations. Switching from a PI-containing regimen to a nevirapine-containing regimen seems to retain the virological response to therapy and it may also limit or reverse the development of some metabolic disorders induced by PIs. Nevirapine is also effective in preventing mother-to-child transmission of HIV-1 disease and in the treatment of HIV-1 infected children. Nevirapine is well-tolerated, rash being the most common severe adverse effect observed. Hepatotoxicity may also appear with nevirapine, mainly in patients with chronic hepatitis C and/or altered liver function tests. This side effect may occasionally be life-threatening but it can be safely managed in most patients.
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PMID:The role of nevirapine in the treatment of HIV-1 disease. 1182 35

It was previously found that certain nonnucleoside reverse transcriptase inhibitors (NNRTI) possess virucidal activity against human immunodeficiency virus type 1 (HIV-1), and it was suggested that the tight-binding mode of inhibition of reverse transcriptase might be important for this virucidal activity (Borkow et al., J. Virol. 71:3023-3030, 1997). To test this, we compared six different NNRTI, including three tight-binding NNRTI, namely UC781, efavirenz (EFV) (Sustiva), and 5-chloro-3-phenylsulfonylindole-2-carboxamide (CSIC), and three rapid-equilibrium NNRTI, delavirdine (DLV) (Rescriptor), nevirapine (NVP) (Viramune), and UC84, in a variety of virucidal tests. Incubation of isolated HIV-1 virions with UC781, EFV, or CSIC rapidly inactivated the virus, whereas DLV, NVP, and UC84 were ineffective in this respect. Exposure of H9+ cells chronically infected by HIV-1 to the tight-binding NNRTI abolished the infectivity of nascent virus subsequently produced by these cells following removal of extracellular drug, thereby preventing cell-to-cell virus transmission in the absence of exogenous drug. In contrast, cell-to-cell transmission of HIV was blocked by DLV, NVP, and UC84 only when the drug remained in the extracellular medium. Pretreatment of uninfected lymphocytoid cells with UC781, EFV, or CSIC, but not DLV, NVP, or UC84, protected these cells from subsequent HIV-1 infection in the absence of extracellular drug. The protective effect was dependent on both the dose of NNRTI and the viral load. The overall virucidal efficacy of the tight-binding NNRTI tested was CSIC > UC781 approximately EFV. We conclude that the tight-binding mode of inhibition is an essential characteristic for virucidal NNRTI and that antiviral potency is an insufficient predictor for virucidal utility of NNRTI.
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PMID:A tight-binding mode of inhibition is essential for anti-human immunodeficiency virus type 1 virucidal activity of nonnucleoside reverse transcriptase inhibitors. 1201


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