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Torsemide: A Comprehensive Review

机译:Torsemide:全面审查

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摘要

Torsemide (l-isopropyl-3-{[4-(3-methyl-phenylamino)pyridine]-3-sulfonyl} urea), a lipophilic anilinopyrimidine sulfonylurea derivative and one of the high-ceiling loop diuretics, is effective in the treatment of both acute and chronic congestive heartfailure (HF). Its mechanism of diuretic action is blockade of the Na+/K+/2CF co-transporter in the thick ascending loop of Henle. Despite its similar site of action to other loops diuretics (e.g., furosemide), torsemide it not structurally related. Torsemide's unique chemical structure is responsible for its pharmacokinetic/pharmacodynamic properties, including: a long half-life, antifibrotic effects, potassium sparing effects, and anti-aldosterone/mineralocorticoid effects. Torsemide has been evaluated in murine and canine models of heart disease (failure) as well as spontaneous HF in humans, dogs, cats and horses. Given the potential beneficial effects of torsemide and unique pharmacokinetic properties a comprehensive understanding of this drug andits current and potential clinical uses is essential.
机译:织物(L-异丙基-3 - {[4-(3-甲基 - 苯基氨基)吡啶] -3-磺酰基}尿素),亲脂性苯胺嘧啶磺酰脲衍生物和高吊环利尿剂之一,可有效治疗急性和慢性充血性心脏(HF)。其利尿作用的机制是封闭的Na + / k + / 2CF共传输液,其厚的Henle上升环。尽管其与其他环路利尿剂(例如,呋塞米)相似的行动部位,但它在结构上没有结构上有关。扭转物体独特的化学结构负责其药代动力学/药效学特性,包括:长半衰期,抗灰度效应,钾盐钾效果和抗醛固酮/矿物质效应。在鼠和犬心脏病(失败)和犬类模型以及人类,狗,猫和马匹中的自发性HF进行了评估。鉴于躯体肌瘤和独特的药代动力学性能潜在的有益效果,对这种药物的全面了解,并且潜在的临床用途至关重要。

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