Stein C
J Pain Symptom Manage. 1991 Apr;6(3):119-24. doi: 10.1016/0885-3924(91)90960-c.
This paper will review experimental and clinical studies investigating analgesic effects of opioids outside the central nervous system. The experimental data indicate that 1) opioids can produce antinociceptive effects in the periphery mediated by local opioid receptors, 2) three different receptor types (mu, delta, kappa) can become active in peripheral tissue, 3) inflammatory hyperalgesic conditions are especially amenable to peripheral opioid actions and 4) the activation of opioid receptors located on primary afferent neurons is the most likely mechanism of action. The evidence from clinical studies is equivocal so far, partly because of methodological shortcomings. More extensive controlled studies investigating the effects of local application of opioids in the vicinity of peripheral nerve terminals or of compounds unable to cross the blood-brain barrier are warranted in view of the potential avoidance of central side effects such as respiratory depression, dependence, nausea or sedation.
本文将综述研究阿片类药物在中枢神经系统以外镇痛作用的实验和临床研究。实验数据表明：1）阿片类药物可通过局部阿片受体在外周产生抗伤害感受作用；2）三种不同的受体类型（μ、δ、κ）在外周组织中均可激活；3）炎症性痛觉过敏状态尤其适合外周阿片类药物发挥作用；4）位于初级传入神经元上的阿片受体激活是最可能的作用机制。目前临床研究的证据尚不明确，部分原因是方法学上的缺陷。鉴于有可能避免呼吸抑制、成瘾、恶心或镇静等中枢副作用，有必要开展更广泛的对照研究，以探讨在外周神经末梢附近局部应用阿片类药物或无法透过血脑屏障的化合物的效果。
