Neuraminidase Inhibitors
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Neuraminidase Inhibitors
Neuraminidase inhibitors (NAIs) are a class of drugs which block the neuraminidase enzyme. They are a commonly used antiviral drug type against influenza. Viral neuraminidases are essential for influenza reproduction, facilitating viral budding from the host cell. Oseltamivir (Tamiflu), zanamivir (Relenza), laninamivir (Inavir), and peramivir belong to this class. Unlike the M2 inhibitors, which work only against the influenza A virus, NAIs act against both influenza A and influenza B. The NAIs oseltamivir and zanamivir were approved in the US and Europe for treatment and prevention of influenza A and B. Peramivir acts by strongly binding to the neuraminidase of the influenza viruses and inhibits activation of neuraminidase much longer than oseltamivir or zanamivir. However, laninamivir in the cells is slowly released into the respiratory tract, resulting in long-lasting anti-influenza virus activity. Thus the mechanism of the long-lasting activity of laninamivir is basically differ ...
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Drug
A drug is any chemical substance that causes a change in an organism's physiology or psychology when consumed. Drugs are typically distinguished from food and substances that provide nutritional support. Consumption of drugs can be via insufflation (medicine), inhalation, drug injection, injection, smoking, ingestion, absorption (skin), absorption via a dermal patch, patch on the skin, suppository, or sublingual administration, dissolution under the tongue. In pharmacology, a drug is a chemical substance, typically of known structure, which, when administered to a living organism, produces a biological effect. A pharmaceutical drug, also called a medication or medicine, is a chemical substance used to pharmacotherapy, treat, cure, preventive healthcare, prevent, or medical diagnosis, diagnose a disease or to promote well-being. Traditionally drugs were obtained through extraction from medicinal plants, but more recently also by organic synthesis. Pharmaceutical drugs may be used ...
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Vomiting
Vomiting (also known as emesis and throwing up) is the involuntary, forceful expulsion of the contents of one's stomach through the mouth and sometimes the Human nose, nose. Vomiting can be the result of ailments like Food-poisoning, food poisoning, gastroenteritis, pregnancy, motion sickness, or hangover; or it can be an after effect of diseases such as brain tumors, elevated intracranial pressure, or overexposure to ionizing radiation. The feeling that one is about to vomit is called nausea; it often precedes, but does not always lead to vomiting. Impairment due to Alcoholic drink, alcohol or anesthesia can cause inhalation of vomit, leading to suffocation. In severe cases, where dehydration develops, intravenous fluid may be required. Antiemetics are sometimes necessary to suppress nausea and vomiting. Self-induced vomiting can be a component of an eating disorder such as bulimia nervosa, bulimia, and is itself now classified as an eating disorder on its own, purging di ...
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Discovery And Development Of Neuraminidase Inhibitors
Neuraminidase inhibitors inhibit enzymatic activity of the enzyme neuraminidase (sialidase). These type of inhibitors have been introduced as anti-influenza drugs as they prevent the virus from exiting infected cells and thus stop further spreading of the virus. Neuraminidase inhibitors for human neuraminidase (hNEU) have the potential to be useful drugs as the enzyme plays a role in several signaling pathways in cells and is implicated in diseases such as diabetes and cancer.Christopher W. Cairo. (2014) Inhibitors of the human neuraminidase enzymes. ''Med. Chem. Commun.'', 2014, 5, 1067.DOI: 10.1039/c4md00089g History The first neuraminidase Inhibitors (NAIs) were synthesized in the 1960s by Edmond et al.,Edmond, J. D., Johnston, R. G., Kidd, D., Rylance, H. J. and Sommerville, R. G. (1966) The Inhibition Of Neuraminidase And Antiviral Action. ''Br. J. Pharmacol. Chemother''., 1966, 27: 415–426. doi: 10.1111/j.1476-5381.1966.tb01673.x through an attempt to understand the c ...
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Berberine
Berberine is a quaternary ammonium salt from the protoberberine group of benzylisoquinoline alkaloids found in such plants as ''Berberis vulgaris'' (barberry), ''Berberis aristata'' (tree turmeric), ''Mahonia aquifolium'' (Oregon grape), ''Hydrastis canadensis'' (goldenseal), ''Xanthorhiza simplicissima'' (yellowroot), ''Phellodendron amurense'' (Amur cork tree), ''Coptis chinensis'' (Chinese goldthread), ''Tinospora cordifolia'', ''Argemone mexicana'' (prickly poppy), and ''Eschscholzia californica'' (Californian poppy). Berberine is usually found in the roots, rhizomes, stems, and bark. Due to its yellow color, ''Berberis'' species were used to dye wool, leather, and wood. Under ultraviolet light, berberine shows a strong yellow fluorescence, making it useful in histology for staining heparin in mast cells. As a natural dye, berberine has a color index of 75160. Research and adverse effects The safety of using berberine for any condition is not adequately defined by high-qua ...
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Coptisine
Coptisine is an alkaloid found in Chinese goldthread (''Coptis chinensis''), greater celandine, and opium. Famous for the bitter taste that it produces, it is used in Chinese herbal medicine along with the related compound berberine Berberine is a quaternary ammonium salt from the protoberberine group of benzylisoquinoline alkaloids found in such plants as ''Berberis vulgaris'' (barberry), '' Berberis aristata'' (tree turmeric), '' Mahonia aquifolium'' (Oregon grape), '' Hyd ... for digestive disorders caused by bacterial infections. References Isoquinoline alkaloids Benzodioxoles Quaternary ammonium compounds {{alkaloid-stub ...
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Black Elderberry
''Sambucus nigra'' is a species complex of flowering plants in the family Adoxaceae native to most of Europe. Common names include elder, elderberry, black elder, European elder, European elderberry, European black elderberry and tramman (Isle of Man). It grows in a variety of conditions including both wet and dry fertile soils, primarily in sunny locations. The plant is widely grown as an ornamental shrub or small tree. Both the flowers and the berries have a long tradition of culinary use, primarily for cordial and wine. Although elderberry is commonly used in dietary supplements and traditional medicine, there is no scientific evidence that it provides any benefit for maintaining health or treating diseases. Description Elderberry is a deciduous shrub or small tree growing to tall and wide, rarely reaching tall. The bark, light gray when young, changes to a coarse gray outer bark with lengthwise furrowing, lenticels prominent. The leaves are arranged in opposite pairs, ...
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Natural Products
A natural product is a natural Chemical compound, compound or chemical substance, substance produced by a living organism—that is, found in nature. In the broadest sense, natural products include any substance produced by life. Natural products can also be prepared by chemical synthesis (both semisynthesis and total synthesis) and have played a central role in the development of the field of organic chemistry by providing challenging synthetic targets. The term natural product has also been extended for commercial purposes to refer to cosmetics, dietary supplements, and foods produced from natural sources without added artificial ingredients. Within the field of organic chemistry, the definition of natural products is usually restricted to organic compounds isolated from natural sources that are produced by the pathways of primary metabolite, primary or secondary metabolite, secondary metabolism. Within the field of medicinal chemistry, the definition is often further restric ...
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Zanamivir Structure
Zanamivir is a medication used to treat and prevent influenza caused by influenza A and influenza B viruses. It is a neuraminidase inhibitor and was developed by the Australian biotech firm Biota Holdings. It was licensed to Glaxo in 1990 and approved in the US in 1999, only for use as a treatment for influenza. In 2006, it was approved for prevention of influenza A and B. Zanamivir was the first neuraminidase inhibitor commercially developed. It is marketed by GlaxoSmithKline under the trade name Relenza as a powder for oral inhalation. Medical uses Zanamivir is used for the treatment of infections caused by influenza A and influenza B viruses, but in otherwise-healthy individuals, benefits overall appear to be small. It decreases the risk of one's getting symptomatic, but not asymptomatic influenza. The combination of diagnostic uncertainty, the risk for virus strain resistance, possible side effects and financial cost outweigh the small benefits of zanamivir for the prophyla ...
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Zanamivir
Zanamivir is a medication used to treat and prevent influenza caused by influenza A and influenza B viruses. It is a neuraminidase inhibitor and was developed by the Australian biotech firm Biota Holdings. It was licensed to Glaxo in 1990 and approved in the US in 1999, only for use as a treatment for influenza. In 2006, it was approved for prevention of influenza A and B. Zanamivir was the first neuraminidase inhibitor commercially developed. It is marketed by GlaxoSmithKline under the trade name Relenza as a powder for oral inhalation. Medical uses Zanamivir is used for the treatment of infections caused by influenza A and influenza B viruses, but in otherwise-healthy individuals, benefits overall appear to be small. It decreases the risk of one's getting symptomatic, but not asymptomatic influenza. The combination of diagnostic uncertainty, the risk for virus strain resistance, possible side effects and financial cost outweigh the small benefits of zanamivir for the prophylax ...
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Peramivir
Peramivir (trade name Rapivab) is an antiviral drug developed by BioCryst Pharmaceuticals for the treatment of influenza. Peramivir is a neuraminidase inhibitor, acting as a transition-state analogue inhibitor of influenza neuraminidase and thereby preventing new viruses from emerging from infected cells. It is approved for intravenous administration. In October 2009, the U.S. Food and Drug Administration (FDA) issued an emergency use authorization (EUA) for the use of peramivir based on safety data from phase I, phase II, and limited phase III trial data. The emergency use authorization for peramivir expired in June 2010. On 19 December 2014, the FDA approved peramivir to treat influenza infection in adults. History An intramuscular (IM) peramivir phase II study for seasonal influenza in 2008–2009 found no effect for the primary endpoint of improvement in the median time to alleviation of symptoms in subjects with confirmed, acute, uncomplicated influenza infection versus p ...
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Laninamivir
Laninamivir (CS-8958) is a neuraminidase inhibitor that is a drug used for the treatment and prophylaxis of Influenzavirus A and Influenzavirus B ''Influenza B virus'' is the only species in the genus ''Betainfluenzavirus'' in the virus family ''Orthomyxoviridae''. Influenza B virus is known only to infect humans and seals. This limited host range is apparently responsible for the lack o .... It is currently in Phase III clinical trials. It is a long-acting neuraminidase inhibitor administered by nasal inhalation. Laninamivir was approved for influenza treatment in Japan in 2010 and for prophylaxis in 2013. It is currently marketed under the name Inavir by Daiichi Sankyo. Biota Pharmaceuticals and Daiichi Sankyo co-own Laninamivir. On 1 April 2011, BARDA awarded up to an estimated U$231m to Biota Pharmaceuticals (Formerly Biota Holdings Ltd) wholly owned subsidiary, Biota Scientific Management Pty Ltd, for the advanced development of Laninamivir in the US. It is under clinic ...
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Delirium
Delirium (also known as acute confusional state) is an organically caused decline from a previous baseline of mental function that develops over a short period of time, typically hours to days. Delirium is a syndrome encompassing disturbances in attention, consciousness, and cognition. It may also involve other neurological deficits, such as psychomotor disturbances (e.g. hyperactive, hypoactive, or mixed), impaired sleep-wake cycle, emotional disturbances, and perceptual disturbances (e.g. hallucinations and delusions), although these features are not required for diagnosis. Delirium is caused by an acute organic process, which is a physically identifiable structural, functional, or chemical problem in the brain that may arise from a disease process ''outside'' the brain that nonetheless affects the brain. It may result from an underlying disease process (e.g. infection, hypoxia), side effect of a medication, withdrawal from drugs, over-consumption of alcohol, usage of hall ...
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