Chair and Department of Palliative Medicine, Poznan University of Medical Sciences, Osiedle Rusa 25 A, 61 - 245 Poznan, Poland.
Curr Drug Targets. 2014 Jan;15(1):124-35. doi: 10.2174/13894501113149990210.
Common opioids adverse effects include opioid-induced bowel dysfunction (OIBD), which comprises opioid-induced constipation, dry mouth, nausea, vomiting, gastric stasis, bloating, and abdominal pain. Traditional laxatives which are often prescribed for the prevention and treatment of OIBD possess limited efficacy and display adverse effects. A targeted approach to OIBD management is the use of a combination of an opioid agonist with opioid receptor antagonist or administration of purely peripherally acting opioid receptor antagonists.
A literature search with terms "oxycodone/naloxone" in the PubMed and MEDLINE database updated on 31(st) July 2013. All studies of oxycodone/naloxone (randomized, controlled trials and open, uncontrolled studies) were included. In addition, studies on pharmacokinetics and pharmacodynamics of oxycodone/naloxone were included.
A combination of prolonged-release oxycodone with prolonged-release naloxone (OXN) in one tablet with a fixed 2:1 ratio provides effective analgesia with limited disturbing effect on bowel function. Oxycodone is a valued opioid administered either as the first strong opioid or when other strong opioids have been ineffective. Naloxone is an opioid receptor antagonist that displays local antagonist effect on opioid receptors in the gastrointestinal tract and is nearly completely inactivated in the liver after oral administration. As demonstrated in controlled studies conducted in patients with chronic non-malignant and cancer-related pain OXN in daily doses up to 80 mg/40 mg provided equally effective analgesia with an improved bowel function compared to oxycodone administered alone.
OXN is an important drug for chronic pain management, prevention and treatment of OIBD.
常见的阿片类药物不良反应包括阿片类药物引起的肠道功能障碍（OIBD），其包括阿片类药物引起的便秘、口干、恶心、呕吐、胃潴留、腹胀和腹痛。常用于预防和治疗 OIBD 的传统泻药疗效有限，并具有不良反应。针对 OIBD 管理的一种方法是使用阿片类激动剂与阿片受体拮抗剂的组合或给予纯外周作用阿片受体拮抗剂。
检索 2013 年 7 月 31 日更新的 PubMed 和 MEDLINE 数据库中带有“oxycodone/naloxone”的文献。所有包含羟考酮/纳洛酮的研究（随机对照试验和开放、非对照研究）均被纳入。此外，还纳入了羟考酮/纳洛酮的药代动力学和药效学研究。
将延长释放羟考酮与延长释放纳洛酮（OXN）固定为 2:1 的比例制成复方片剂，提供了有效的镇痛作用，对肠道功能的干扰有限。羟考酮是一种有价值的阿片类药物，可作为一线强阿片类药物或在其他强阿片类药物无效时使用。纳洛酮是一种阿片受体拮抗剂，在胃肠道中的阿片受体上显示局部拮抗作用，口服后几乎完全在肝脏中失活。在慢性非恶性和癌症相关疼痛患者中进行的对照研究表明，在每日剂量高达 80mg/40mg 时，与单独给予羟考酮相比，OXN 提供了同样有效的镇痛作用，同时改善了肠道功能。
OXN 是慢性疼痛管理、OIBD 预防和治疗的重要药物。
