首页> 外国专利> CONBINATION OF A NMDA NR2B SELECTIVE ANTAGONIST AND A COX-2 INHIBITOR.

CONBINATION OF A NMDA NR2B SELECTIVE ANTAGONIST AND A COX-2 INHIBITOR.

机译:NMDA NR2B选择性拮抗剂和COX-2抑制剂的组合。

摘要

A product comprising a selective NMDA NR2B antagonist and a COX-2 inhibitor in the form of a combined preparation for simultaneous, separate or sequential use in the treatment or prevention of pain or nociception. The present specification surprisingly demonstrates that NMDA NR2B antagonists possess antinoniceptive effects in rat models of inflammatory and neuropathic pain with an improvement in the window of side effects on noncompetitive NMDA antagonists (ataxic / antinoniceptive), when combined with an opioid, the combination is better tolerated than expected. Cyclooxygenase-2 inhibitors are a subclass of the class of drugs known as non-steroidal anti-inflammatory drugs (abbreviated in English NSAID). NSAIDs are active in reducing prostaglandin-induced pain and swelling associated with the inflammatory process but they are also active in affecting other prostaglandin-regulated processes not associated with the inflammatory process. So, the use of high doses of the most common NSAIDs can cause serious side effects, including life-threatening ulcers, which limit their therapeutic potential. An alternative to NSAIDs is the use of corticosteroids, which have even more drastic side effects, especially when long-term therapy is involved.
机译:以组合制剂的形式包含选择性NMDA NR2B拮抗剂和COX-2抑制剂的产品,可同时,分别或依次用于治疗或预防疼痛或伤害感受。本说明书令人惊讶地证明,NMDA NR2B拮抗剂在炎性和神经性疼痛的大鼠模型中具有抗神经肽作用,并改善了对非竞争性NMDA拮抗剂(抗抑郁/抗神经肽)的副作用窗口,当与阿片类药物联合使用时,该组合的耐受性更好超出预期。环氧合酶2抑制剂是被称为非甾体类抗炎药(英文NSAID的缩写)的一类药物。 NSAIDs可以有效减轻前列腺素引起的与炎症过程相关的疼痛和肿胀,但它们也可以有效地影响其他与炎症过程无关的前列腺素调节过程。因此,大剂量使用最常见的非甾体抗炎药会导致严重的副作用,包括威胁生命的溃疡,从而限制了它们的治疗潜力。 NSAID的替代方法是使用皮质类固醇,其副作用更为严重,尤其是在涉及长期治疗时。

著录项

  • 公开/公告号ES2220047T3

    专利类型

  • 公开/公告日2004-12-01

    原文格式PDF

  • 申请/专利权人 MERCK SHARP & DOHME LTD.;

    申请/专利号ES19990906366T

  • 发明设计人 BOYCE SUSAN;

    申请日1999-02-26

  • 分类号A61K45/06;A61K31/445;

  • 国家 ES

  • 入库时间 2022-08-21 22:14:56

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