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CONBINATION OF A NMDA NR2B SELECTIVE ANTAGONIST AND A COX-2 INHIBITOR.
CONBINATION OF A NMDA NR2B SELECTIVE ANTAGONIST AND A COX-2 INHIBITOR.
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机译:NMDA NR2B选择性拮抗剂和COX-2抑制剂的组合。
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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.
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