Why is morphine not the ultimate analgesic and what can be done to improve it?
Why is morphine not the ultimate analgesic and what can be done to improve it?
复制标题
DOI：
10.1054/jpai.2000.9820
复制
发表时间：
2000-09-01
期刊：
影响因子：
4
通讯作者：
Machelska, H
中科院分区：
文献类型：
--
作者：
Stein, C;Schäfer, M;Machelska, H
虽然阿片类药物在治疗急性和癌症疼痛方面是无与伦比的，但它们在慢性非癌症疼痛中的应用显然是有限的。本文讨论了一些开放和有争议的问题，如疼痛缓解和副作用之间的平衡，是否所有类型的疼痛都可以用阿片类药物治疗，以及目前开发阿片类药物的努力，改善疗效-副作用比。虽然呼吸抑制或耐受性通常不是长期使用阿片类药物的主要问题，但当疼痛有主要情感成分或习得性疼痛行为是主要问题时，阿片类药物是否能在某些类型的疼痛中产生镇痛反应似乎值得怀疑。改善阿片样物质的努力传统上旨在增强阿片样物质受体配体对μ-、δ-和κ-受体的选择性。另一个主要策略是寻找作用于中枢神经系统外阿片受体的阿片类镇痛剂，其前景是避免中枢介导的副作用。
Although opioids are unsurpassed in the treatment of acute and cancer pain, their use in chronic noncancer pain is clearly limited. This review discusses some open and controversial issues such as the balance between pain relief and side effects, whether all types of pain can be treated with opioids, and current efforts to develop opioids with an improved efficacy-side effect ratio. Whereas respiratory depression or tolerance are usually not major issues in long-term opioid use, it seems questionable whether opioids can produce an analgesic response in certain types of pain when there is a major affective component to the pain or when learned pain behavior is the main problem. Efforts to improve opioids have traditionally aimed at enhancing the selectivity of opioid receptor ligands towards mu-, delta-, and kappa-receptors. Another major strategy has been the search for opioid analgesics acting at opioid receptors outside the central nervous system, with the prospect to avoid centrally mediated side effects.