Leppert Wojciech
Chair and Department of Palliative Medicine, Poznan University of Medical Sciences, Poznan, Poland.
Contemp Oncol (Pozn). 2013;17(2):128-33. doi: 10.5114/wo.2013.34614. Epub 2013 Apr 29.
Opioid analgesics are usually effective in the management of severe chronic pain. However, symptoms of opioid-induced bowel dysfunction (OIBD) are common during opioid therapy. Opioid-induced bowel dysfunction is often unsuccessfully managed due to limited effectiveness and numerous adverse effects of traditional laxatives. Newer treatment possibilities directed at the pathomechanism of OIBD comprise combined prolonged-release oxycodone with prolonged-release naloxone (oxycodone/naloxone) tablets. Oxycodone/naloxone provides effective analgesia with limited impact on bowel function as oxycodone displays high oral bioavailability and naloxone act as local antagonist on opioid receptors in the gastrointestinal tract due to nearly complete inactivation in the liver. Oxycodone/naloxone is administered to opioid-naive patients with severe pain and those unsuccessfully treated with weak opioids. Oxycodone/naloxone may be also administered to patients treated with strong opioids who experience intense symptoms of OIBD. Studies conducted to date indicate that oxycodone/naloxone is an important drug in chronic pain management, prevention and treatment of OIBD.
阿片类镇痛药通常对重度慢性疼痛的治疗有效。然而，在阿片类药物治疗期间，阿片类药物引起的肠道功能障碍（OIBD）症状很常见。由于传统泻药效果有限且不良反应众多，阿片类药物引起的肠道功能障碍往往难以得到有效治疗。针对OIBD发病机制的新型治疗方法包括缓释羟考酮与缓释纳洛酮（羟考酮/纳洛酮）联合片剂。羟考酮/纳洛酮能提供有效的镇痛作用，对肠道功能影响有限，因为羟考酮具有较高的口服生物利用度，而纳洛酮由于在肝脏中几乎完全失活，在胃肠道中作为阿片受体的局部拮抗剂发挥作用。羟考酮/纳洛酮适用于未使用过阿片类药物的重度疼痛患者以及使用弱阿片类药物治疗无效的患者。对于使用强阿片类药物治疗且出现严重OIBD症状的患者，也可使用羟考酮/纳洛酮。迄今为止进行的研究表明，羟考酮/纳洛酮是慢性疼痛管理、OIBD预防和治疗中的一种重要药物。
