a Laboratory of Quality of Life Research, Chair and Department of Palliative Medicine , Poznan University of Medical Sciences , Poznan , Poland.
b Department of Interdisciplinary Intensive Care , Jagiellonian University Medical College , Krakow , Poland.
Expert Opin Pharmacother. 2019 Apr;20(5):511-522. doi: 10.1080/14656566.2018.1561863. Epub 2019 Jan 9.
Common opioid adverse effects (AE) of the gastrointestinal tract include opioid-induced constipation (OIC) and opioid-induced bowel dysfunction (OIBD) with traditional laxatives being of limited efficacy, having AEs and not addressing the pathophysiology of OIC or OIBD. Targeted treatment comprises of PAMORA (peripherally acting mu-opioid receptor antagonists) and a combination of an opioid receptor agonist with its antagonist, namely prolonged-release oxycodone with prolonged-release naloxone (OXN) tablets at a fixed ratio of 2:1. Oxycodone provides analgesia, whereas naloxone prevents binding or displaces it from opioid receptors located in the gut wall. Areas covered: The authors review the role of OXN in the management of patients with pain and OIC. A literature search was performed using the search terms 'oxycodone/naloxone' and 'opioid-induced constipation' using the PubMed database up to October 2018. Expert opinion: OXN delivers analgesia comparable (or superior versus placebo and in observational studies) to oxycodone alone and other opioids with a limited or decreased disturbing effect on bowel function. OXN in daily doses of up to 160 mg/80 mg provides effective analgesia with little negative impact on bowel function. OXN may be successfully used in patients with chronic pain, to prevent or treat symptoms of OIC and OIBD.
常见的阿片类药物胃肠道不良反应(AE)包括阿片类药物引起的便秘(OIC)和阿片类药物引起的肠道功能障碍(OIBD),传统的泻药疗效有限,且具有不良反应,不能解决 OIC 或 OIBD 的病理生理学问题。靶向治疗包括 PAMORA(外周作用阿片受体拮抗剂)和阿片受体激动剂与其拮抗剂的组合,即与纳洛酮(OXN)延长释放的羟考酮固定比例为 2:1 的片剂。羟考酮提供镇痛作用,而纳洛酮防止其与位于肠壁的阿片受体结合或取代它。
作者回顾了 OXN 在治疗疼痛和 OIC 患者中的作用。使用 PubMed 数据库中的搜索词“羟考酮/纳洛酮”和“阿片类药物引起的便秘”进行了文献检索,截至 2018 年 10 月。
OXN 提供的镇痛作用与单独使用羟考酮(或优于安慰剂和观察性研究)和其他阿片类药物相当,对肠道功能的干扰有限或减少。每日剂量高达 160mg/80mg 的 OXN 可提供有效的镇痛作用,对肠道功能的负面影响很小。OXN 可成功用于慢性疼痛患者,以预防或治疗 OIC 和 OIBD 症状。