Gintzler Alan R, Liu Nai-Jiang
Department of Obstetrics and Gynecology, State University of New York, Downstate Medical Center, Brooklyn, New York.
J Opioid Manag. 2019 Jan/Feb;16(1):67-72. doi: 10.5055/jom.2020.0552.
To review evidence demonstrating efficacy and feasibility of harnessing the activity of endogenous opioid analgesic systems for pain management.
The authors sought to summarize a wealth of data that establish proof of concept that the analgesic activity of endogenous opioids can be exploited to clinically benefit from the enormous pain-relieving abilities of these peptides without contributing to the current crisis of death by synthetic opioid overdose.
There is a plethora of studies demonstrating that not only can endogenous opioids mediate placebo-induced antinociception but they are also active in modulating clinical pain. Earlier studies convincingly demonstrate the effec-tiveness of psychological strategies to coopt endogenous opioid analgesic systems to produce pain relief. The challenge is to define pharmacological targets for activating endogenous opioid analgesia reliably in a clinical setting. Based on insights gleaned from mechanisms underlying the ebb and flow of analgesic responsiveness to the spinal application of endomorphin 2, multiple signaling proteins were identified that activate endogenous spinal opioid analgesia. Notably, this was achieved in the absence of any exogenous synthetic opioid.
Utilization of drugs that harness endogenous opioid antinociception in accordance with varying physiological states represents a novel approach for effective pain management while mitigating the present epidemic of death by synthetic opioid overdose.
回顾有关利用内源性阿片类镇痛系统的活性进行疼痛管理的有效性和可行性的证据。
作者试图总结大量数据，这些数据确立了概念验证，即内源性阿片类药物的镇痛活性可被利用，从而在临床上受益于这些肽巨大的止痛能力，同时又不会加剧当前因合成阿片类药物过量导致的死亡危机。
大量研究表明，内源性阿片类药物不仅可以介导安慰剂诱导的抗伤害感受，而且在调节临床疼痛方面也具有活性。早期研究令人信服地证明了心理策略在利用内源性阿片类镇痛系统以减轻疼痛方面的有效性。挑战在于确定在临床环境中可靠激活内源性阿片类镇痛的药理学靶点。基于从内吗啡肽2脊髓应用镇痛反应性的起伏机制中获得的见解，鉴定出多种激活内源性脊髓阿片类镇痛的信号蛋白。值得注意的是，这是在没有任何外源性合成阿片类药物的情况下实现的。
根据不同生理状态利用内源性阿片类抗伤害感受的药物，是一种有效的疼痛管理新方法，同时可缓解当前因合成阿片类药物过量导致的死亡流行。
