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Naloxegol: A Review of Its Use in Patients with Opioid-Induced Constipation

机译:Naloxegol:阿片类药物诱导便秘患者使用的综述

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摘要

Oral naloxegol (Movantik (TM), Moventig((R))), a peripherally acting mu-opioid receptor antagonist, inhibits opioid binding in mu-opioid receptors in the gastrointestinal tract. This article reviews the pharmacological properties of naloxegol and its clinical efficacy and tolerability in patients with opioid-induced constipation. It demonstrated clinical efficacy and was well tolerated in placebo-controlled trials in patients with non-cancer pain and opioid-induced constipation, including those with an inadequate response to laxatives, and was well tolerated in a long-term safety study. As a PEGylated naloxone derivative, naloxegol is associated with significant improvements in spontaneous bowel movements, while maintaining levels of opioid-related analgesia (a result of its reduced ability to cross the blood-brain barrier). Naloxegol is a useful option in the treatment of opioid-induced constipation.
机译:口服纳洛酮酚(Movantik TM,Moventig)是一种外周作用的μ阿片受体拮抗剂,可抑制胃肠道中μ阿片受体中的阿片结合。本文综述了纳洛西尔的药理特性及其在阿片类药物致便秘患者中的临床疗效和耐受性。它显示出临床疗效,并且在非癌症疼痛和阿片类药物引起的便秘的患者(包括对泻药反应不足的患者)的安慰剂对照试验中得到了很好的耐受,并且在长期安全性研究中也得到了很好的耐受。作为聚乙二醇化的纳洛酮衍生物,纳洛西酚可显着改善自发性肠蠕动,同时维持与阿片类药物相关的镇痛水平(由于其穿过血脑屏障的能力降低)。纳洛索酚是治疗阿片类药物引起的便秘的有用选择。

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