超低剂量纳洛酮对阿片类药物镇痛效能的影响及可能机制

Ultra-low Dose Naloxone Enhances the Antinociceptive Effects of Opioids

纳洛酮作为纯阿片受体拮抗剂,常被用于拮抗阿片类药物所引起的不良反应,如呼吸抑制、恶心、呕吐或阿片类药物中毒等。但超低剂量的纳洛酮(<1μg/kg)近些年分别在离体实验、动物实验和临床试验中被证实与阿片类药物联用可以减轻后者的副作用,甚至可增强镇痛作用。其还可减轻大剂量瑞芬太尼诱发的患者术后痛觉过敏,降低或阻止啮齿类动物的阿片类药物耐受,可能的相关机制是其选择性的抑制阿片受体的兴奋性。

Naloxone as pure opioid receptor antagonist, is often used to antagonism adverse reactions caused by opioid, such as respiratory depression, nausea, vomiting and opioid overdoses. Some in vitro evidence, in addition to information gathered from animals and human clinical studies, have demonstrated that ultra-low doses of naloxone, along with opioids, could increase analgesia. In addition, it could reduce opioid-induced side effects. An ultra-low doses of naloxone preserves the antinociceptive effect of morphine in morphine tolerant rats and it can block remifentanil-induced hyperalgesia.