16 Oct stavudine mechanism of action
CD4 + lymphocytes isolated from asymptomatic stavudine-treated patients had reduced basal mitochondrial oxygen consumption compared with untreated HIV-infected patients and uninfected controls. Neuropathy tends to appear after 3 months of therapy and resolves slowly with medication discontinuation. M. Lartey, ... C.I.S. Medicine India is just a publishing medium for medicine related information and does not provide services or sales of medicines including stavudine. The authors suggested that in resource-poor settings, otherwise unexplained weight loss may prove a useful indicator of stavudine-associated lipoatrophy. However, its use has been limited by delayed toxicity, notably peripheral neuropathy and myopathy caused by mitochondrial damage. It improves the seroconversion of e-antigen positive hepatitis B and also improves histology staging of the liver. Lamivudine is administered by mouth, and it is rapidly absorbed with a bio-availability of over 80%. Gabapentin can be used, and it showed benefit in one placebo controlled trial (Hahn et al., 2004). He was not rechallenged with the drug. Stavudine is indicated for use in combination with other antiretroviral agents for the treatment of HIV-1 infection. For the three-coach British electric trains sometimes known as 3TC, see, InChI=1S/C8H11N3O3S/c9-5-1-2-11(8(13)10-5)6-4-15-7(3-12)14-6/h1-2,6-7,12H,3-4H2,(H2,9,10,13)/t6-,7+/m1/s1, nucleoside reverse transcriptase inhibitor, World Health Organization's List of Essential Medicines, "Lamivudine resistance in children with chronic hepatitis B", "National Institutes of Health: Moving Research from the Bench to the Bedside", "The Wide-Ranging Effects of Nucleoside Analogs:A Look at Mitochondrial Toxicity", Bictegravir/emtricitabine/tenofovir alafenamide, Darunavir/cobicistat/emtricitabine/tenofovir alafenamide, Elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide, Elvitegravir/cobicistat/emtricitabine/tenofovir, Emtricitabine/rilpivirine/tenofovir alafenamide, GlaxoSmithKline Services Unlimited v Commission, 2013−2016 West African Ebola virus epidemic, 1967 Marburg virus outbreak in West Germany, https://en.wikipedia.org/w/index.php?title=Lamivudine&oldid=983526601, Nucleoside analog reverse transcriptase inhibitors, World Health Organization essential medicines, Drugboxes which contain changes to verified fields, Wikipedia medicine articles ready to translate, Creative Commons Attribution-ShareAlike License, Do not prescribe lamivudine/zidovudine, abacavir/lamivudine, or abacavir/lamivudine/zidovudine to patients taking, Long-term use of lamivudine can trigger a resistant, HIV or HBV-infected women on lamivudine are warned to discontinue, Use with caution for patients with impaired, Epivir tablets (GlaxoSmithKline; US and UK) for the treatment of HIV, Epivir-HBV tablets (GlaxoSmithKline; US only) for the treatment of hepatitis B, Zeffix tablets (GlaxoSmithKline; UK only) for the treatment of hepatitis B, 3TC tablets (GlaxoSmithKline; South Africa) for the treatment of HIV, This page was last edited on 14 October 2020, at 18:58. No distinction was made between HIV-induced and stavudine-associated neuropathy. [13][14], Lamivudine was approved by the Food and Drug Administration (FDA) on November 17, 1995 for use with zidovudine (AZT) and again in 2002 as a once-a-day dosed medication. Cells from the stavudine-treated patients also had reduced maximal oxygen consumption. Its mechanism of action is similar to that of zidovudine. Inhibition of mitochondrial DNA synthesis is proposed to induce depletion of cellular mitochondrial DNA and it is ultimately responsible for the delayed toxicity observed with the use of stavudine and other nucleoside reverse transcriptase inhibitors (NRTIs).
Barker, in. Stavudine (2′,3′-didehydro, 3′-deoxythymidine) is a thymidine analogue with significant activity against HIV-1, having inhibitory concentrations, which range from 0.01 to 4.1 μmol l −1. A regimen that includes D4T and lamivudine (3TC) and a protease inhibitor (indinavir or ritonavir) was found to be associated with immune restoration and thyroid-specific immunity resulting in Graves’ disease in five patients. There was a higher incidence of TB in the 30 mg group [167c]. ScienceDirect ® is a registered trademark of Elsevier B.V. ScienceDirect ® is a registered trademark of Elsevier B.V. URL: https://www.sciencedirect.com/science/article/pii/B9780444537171014670, URL: https://www.sciencedirect.com/science/article/pii/B9780702062858001520, URL: https://www.sciencedirect.com/science/article/pii/B9780123739445001784, URL: https://www.sciencedirect.com/science/article/pii/B9780323189071000780, URL: https://www.sciencedirect.com/science/article/pii/B9780444634078000290, URL: https://www.sciencedirect.com/science/article/pii/B9780128013175000141, URL: https://www.sciencedirect.com/science/article/pii/B9780444537416000295, URL: https://www.sciencedirect.com/science/article/pii/B978012408078200007X, URL: https://www.sciencedirect.com/science/article/pii/B9780444594990000295, URL: https://www.sciencedirect.com/science/article/pii/B9780702040887000900, Clinical Pharmacology (Eleventh Edition), 2012, Meyler's Side Effects of Drugs (Sixteenth Edition), Painful bilateral gynecomastia and hypersexuality, possibly related to the use of, Encyclopedia of Microbiology (Third Edition), Endocrinology: Adult and Pediatric (Seventh Edition), A worldwide yearly survey of new data in adverse drug reactions, Isobel D. Ramsay, ... Charlotte I.S. She was found to be acidotic with hypokalaemia and hypophosphataemia and was polyuric. Due to the risk of a fatal lactic acidosis, combination treatment with didanosine and stavudine should only be used in cases where no alternatives are available (Bristol-Myers Squibb 2001). Stavudine is converted to stavudine 5'-triphosphate which competes with thymidine 5'-triphosphate for incorporation into viral DNA. Lamivudine, commonly called 3TC, is an antiretroviral medication used to prevent and treat HIV/AIDS. Lamivudine treatment has been shown to restore zidovudine sensitivity of previously resistant HIV. [7] A better explanation of the data is that lamivudine continues to have a partial anti-viral effect even in the presence of the M184V mutation. It is phosphorylated to active metabolites that compete for incorporation into viral DNA. Stavudine is used for HIV infection in combination with other anti-HIV agents. Of those with lactic acidosis 22% died; these patient all had a baseline CD4 count less than 10 × 106/l before the start of therapy. This indication is based on the results of several studies, including a study in zidovudine-experienced patients of monotherapy with stavudine versus zidovudine that showed stavudine significantly delayed clinical progression;15 a study of stavudine versus zidovudine, each in combination with lamivudine and indinavir demonstrating comparable virologic efficacy;16 and a study of stavudine and didanosine versus zidovudine and lamivudine, each in combination with indinavir, demonstrating comparable or superior virologic efficacy.17 Subsequent studies and clinical experience revealed the toxicity of stavudine and the combination of stavudine and didanosine and these are used uncommonly today. In 152 patients (8.8%) the plasma venous lactate was raised (over 2.2 mmol/l); 45 (41 women and 4 men) were admitted to hospital because of lactic acidosis. Other resistance mutations are L80V/I, V173L and L180M.[9]. It can inhibit both types (1 and 2) of HIV reverse transcriptase and also the reverse transcriptase of hepatitis B virus. Mechanism of Action Stavudine, a nucleoside analogue of thymidine, is phosphorylated by cellular kinases to the active metabolite stavudine triphosphate.
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