羟考酮纳洛酮缓释片治疗中重度疼痛的研究进展

Research progress of oxycodone and naloxone sustained-release tablets in the treatment of moderate to severe pain

羟考酮纳洛酮缓释片是一种包含固定剂量阿片受体激动剂和阿片受体拮抗剂的复方制剂,用于治疗中重度疼痛。制剂中羟考酮发挥镇痛作用,而纳洛酮由于口服生物利用率低在不影响镇痛效果的同时,通过在肠壁的局部拮抗作用可以对抗羟考酮引起的便秘。大量已发表的临床试验和观察性研究表明,与单方羟考酮制剂及其他阿片类药物相比,按说明书规定标准剂量口服羟考酮纳洛酮缓释片可以为中重度癌痛和非癌痛类型的患者提供有效的镇痛并缓解阿片类药物诱导产生的肠功能障碍。本文对羟考酮纳洛酮缓释片的药理特性、治疗中重度疼痛的研究进展等文献进行梳理并形成综述,以期为医药领域专业人员提供全面、精准及系统的参考。

Oxycodone and naloxone sustained-release tablets is fixed-dose combination of receptor antagonist and opioid receptor antagonist used clinically for the management of moderate to severe pain.Oxycodone in this formulation provides analgesic effect,while naloxone,due to its low oral bioavailability,counteracts oxycodone-induced constipation through the local antagonist effect in the gut wall while maintaining analgesia.Data from numerous published clinical trials and observational studies suggest that oral oxycodone and naloxone prolonged-release tablets at standard labeled doses provide effective analgesia and alleviate opioid-induced bowel dysfunction in patients with moderate to severe cancer and non-cancer pain when compared to oxycodone formulations and other opioids.This paper reviews the pharmacological properties,the research progress of oxycodone and naloxone sustained-release tablets in the treatment of moderate to severe pain,in order to provide a comprehensive,accurate and systematic reference for professionals in the pharmaceutical field.