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

A high-performance liquid chromatographic method for the quantitative determination of the HIV reverse transcriptase inhibitor lamivudine ((-)-2'-deoxy-3'-thiacytidine, 3TC, Epivir) in human plasma, saliva and cerebrospinal fluid is described. Lamivudine was extracted from samples using silica extraction columns prior to reversed-phase high-performance liquid chromatography with ultraviolet detection at 270 nm. The method has been validated over the range of 10 (lower limit of quantitation) to 5000 ng/ml using a 0.5-ml sample volume. Between-day and within-day precisions ranged from 3.5 to 9.0%. The assay has been used for the quantitative analysis of lamivudine in plasma and cerebrospinal fluid of HIV-1 infected patients.
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PMID:Quantitative determination of (-)-2'-deoxy-3'-thiacytidine (lamivudine) in human plasma, saliva and cerebrospinal fluid by high-performance liquid chromatography with ultraviolet detection. 974 54

(1) Combivir is a fixed-dose combination of two HIV reverse transcriptase inhibitors: zidovudine (300 mg) + lamivudine (150 mg). (2) A meta-analysis of four trials shows that this combination is more effective clinically than zidovudine monotherapy. One trial also shows that clinical efficacy is even better with the triple combination of the protease inhibitor indinavir with zidovudine + lamivudine. (3) The risk of anaemia and neutropaenia necessitates blood cell monitoring during treatment. (4) Compared with lamivudine and zidovudine taken separately, Combivir does not reduce the frequency of doses (two a day), but the daily number of tablets falls from four to two, provided that the patient does not require dose adjustment.
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PMID:Zidovudine + lamivudine: new preparation. Fewer tablets required. 1084 57

While it appears that protease inhibitors in combination therapies are saving lives, questions continue: (1) which combinations of protease inhibitors and other antiretroviral agents are most effective in restoring immune function, (2) how these combinations can be used most effectively, and (3) what is the best time to start using them? An evaluation is presented on the immunological value of specific drug cocktail combinations and a comparison of the best and worst drug combinations and the reasons for this assessment. It indicates that Norvir is the most effective of all four protease inhibitors in preventing opportunistic infections, lymphomas, and cancers. D4T and 3TC are the safest and most effective of the nucleosides for preventing or remitting opportunistic infections when used with protease inhibitors. Rescriptor is the most therapeutic of the two non-nucleoside reverse transcriptase inhibitors in increasing absorption of protease inhibitors. The best drug combination therapies are listed as follows: Norvir plus Rescriptor; Norvir plus D4T; Norvir plus 3TC; Norvir, Rescriptor, and D4T; Norvir, Rescriptor, and 3TC; Norvir, D4T, and 3TC; and Crixivan or Viracept plus Rescriptor plus either D4T or 3TC. The worst drug combination therapies are listed as follows: AZT plus ddI (used in combination with a protease inhibitor); AZT or ddI or Combivir (used in combinations with a protease inhibitor); and any two protease inhibitors used together in any person with active hepatitis or elevated liver enzymes or impaired kidney function.
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PMID:An evaluation of drug cocktail combinations for their immunological value in preventing/remitting opportunistic infections. 1136 16

During the past two years, two new classes of drugs have emerged that are effective in treating HIV infection. Since protease inhibitors and non-nucleoside reverse transcriptase inhibitors are highly effective but difficult to take, pharmaceutical manufacturers have developed new formulations of some of these drugs. People taking AZT and ritonavir can sometimes switch to a product called Combivir, a combination of the two. Saquinavir patients may be able to switch to a gel formulation of the same drug, Fortovase, that is more readily absorbed by the body. Potential side effects and impacts on treatment are reviewed.
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PMID:New ways to take old drugs. 1136 12

Abacavir (ABC), an experimental nucleoside reverse transcriptase inhibitor created by Glaxo Wellcome, appears as effective in combination therapy as protease inhibitors, when ABC is combined with Combivir. Combivir is a two-drugs-in-one combination comprised of AZT and 3TC. ABC was developed as an investigational treatment for HIV and is currently in Phase III trials for adults and children. This is the first time that three drugs in the same class have effectively reduced the viral load of treatment-naive patients to levels usually only seen with protease inhibitors. Trial results are nearly identical to those where AZT, 3TC, and a protease inhibitor have been combined. ABC can potentially change the way treatment is initiated because it involves a simple regimen. Due to its potency, fewer pills are necessary. There are also very few side effects or serious drug interactions associated with ABC.
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PMID:New abacavir data open door to a better treatment paradigm. 1136 47

A non-nucleoside reverse transcriptase inhibitor, Sustiva (efavirenz, formerly DMP 266), received FDA approval for use by children and adults. Dosing is recommended at bedtime to avert side effects, which are described. People who receive the drug should avoid driving. Women should not become pregnant while taking this medication. Triple combination therapy with Sustiva and AZT/ Epivir (3TC) may be as effective as the combination of Crixivan with AZT/Epivir (3TC), preliminary trials showed. The drug costs about $4,000 a year. Contact information for obtaining financial assistance in the purchasing the drug is provided.
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PMID:Sustiva (efavirenz) is approved. 1136 71

Elderberry, chondroitin, and glucosamine sulfate have been found to block HIV replication at three distinct points in the replication cycle. For quadruple therapy, a reverse transcriptase inhibitor such as olive leaf extract or Epivir (3TC) could be added. In one case, a female, taking no HIV drugs, used an elderberry extract, called Sambucol, with olive leaf extract and experienced a viral load drop from 17,000 to 4,000. Instructions are given for making both alcohol-free and alcohol-based elderberry extracts. In 1993, researchers at Jerusalem?s Hebrew University Medical School found in a placebo-controlled double-blind study that Sambucol led to a rapid recovery from influenza and inhibited replication of nine other strains of the flu virus. A theory is that elderberry renders viruses nonfunctional by staining and coating them. Another promising treatment is soil based organisms, which improved Natural Killer cell function in a person with CFIDS.
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PMID:A new triple combination therapy. 1136 42

The non-nucleoside reverse transcriptase inhibitors (NNRTIs) are commonly used in combination antiretroviral therapy and are associated with hypersensitivity reactions on induction therapy. We report a case of recurrent hypersensitivity associated with Combivir, when there was a delay in determining the cause as the NNRTIs were considered to be the more likely cause.
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PMID:Recurrent hypersensitivity to Combivir. 1186 Jul 1

For the last several years, the combination of ddI (didanosine, Videx) and d4T (stavudine, Zerit) as a backbone of three-drug therapy has been popular both in treatment and in research. Together, the two nucleoside analog reverse transcriptase inhibitor (NARTI) drugs offered relatively high strength and fairly simple use. Despite this, some researchers have long questioned the wisdom of the combination as it violates one of the key rules of combining drugs: combine only drugs with different side effect profiles. Both drugs are associated with the development of peripheral neuropathy and pancreatitis. Pancreatitis is more commonly seen with ddI and neuropathy with d4T, but both occur to a significant degree with each drug and to a higher degree than was seen with other drugs of their class. However, few if any studies were run comparing the ddI/d4T combination to alternatives such as AZT/3TC (Combivir) or even 3TC/d4T. Both ddI and d4T come from the same company, Bristol Myers Squibb.
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PMID:New questions about an old combination--ddI + d4T. 1264 75

The FDA approved FTC (emtricitabine, Emtriva) in July 2003 for use by adults in combination with other anti-HIV drugs. FTC is a nucleoside analog reverse transcriptase inhibitor (NRTI). Other drugs in this class include 3TC, abacavir, AZT, Combivir, d4T, d4T XR, ddC, ddI, ddI EC and Trizivir.
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PMID:FTC (emtricitabine, Emtriva). 1469 67


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