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首页> 外文期刊>Current opinion in anaesthesiology >Differences between and combinations of opioids re-visited.
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Differences between and combinations of opioids re-visited.

机译：再次探讨了阿片类药物及其组合之间的差异。

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PURPOSE OF REVIEW: Recent studies highlighting between-opioid differences in patient outcomes, opioid receptor interactions and animal study findings implicating a 'fine control' mechanism underpinning potential diversity in opioid receptor signalling that could potentially be exploited to develop novel opioid analgesics with improved tolerability are reviewed. RECENT FINDINGS: Recent clinical trials confirm the success of 'opioid rotation' for improving opioid tolerability and restoring analgesia in most patients who would otherwise experience intolerable side effects and poor pain relief. These findings suggest that individual strong opioids may interact, at least in part, with different opioid receptor sub-populations or modulate mu opioid receptor signalling in subtly different ways. Identification of novel mu opioid splice variants with different intron 1 sizes that heterodimerize with, and modulate the function of, native mu opioid receptors provide insight into potential diversity in opioid signalling. Oxycodone, unlike other strong opioids, does not cause potassium current desensitization nor does it displace [3H]-morphine binding, consistent with its different in-vivo pharmacological profile to morphine. Opioid analgesic combinations administered as tethered bivalent ligands or admixture demonstrate good pain relief with improved side effect profiles. SUMMARY: Enhanced understanding of diversity in opioid signalling has the potential to produce novel strong opioid analgesics with improved tolerability.
机译：审查目的：最近的研究强调了阿片类药物在患者预后之间的差异，阿片类药物受体之间的相互作用以及动物研究结果，这些隐含了一种“精细控制”机制，可支持阿片类药物受体信号转导的潜在多样性，这些潜在的潜在潜力可用于开发具有改善的耐受性的新型阿片类镇痛药。已审查。最近的发现：最近的临床试验证实了“阿片类药物旋转”疗法在改善阿片类药物耐受性和恢复镇痛的大多数患者中的成功，否则这些患者会出现无法忍受的副作用和较差的疼痛缓解。这些发现表明，单独的强阿片样物质可能至少部分地与不同的阿片样物质受体亚群相互作用或以微妙的不同方式调节μ阿片样物质受体信号传导。与天然mu阿片受体异二聚体并调节其功能的具有不同内含子1大小的新型mu阿片样物质剪接变体的鉴定提供了对阿片样物质信号转导中潜在多样性的了解。羟考酮与其他强阿片类药物不同，不会引起钾电流脱敏，也不会取代[3H]-吗啡结合，这与其对吗啡的体内药理学特征是一致的。以栓系二价配体或混合物形式给药的阿片类镇痛药组合物可缓解疼痛，并改善副作用。摘要：对阿片类药物信号传导多样性的加深了解可能产生具有改善的耐受性的新型强效阿片类镇痛药。

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