University of Chicago, Department of Anesthesia & Critical Care, Chicago, IL , USA.
Expert Opin Investig Drugs. 2013 Oct;22(10):1225-7. doi: 10.1517/13543784.2013.819341. Epub 2013 Jul 9.
Opioids are potent analgesics for treating moderate to severe pain, but their use is associated with a number of adverse effects, especially opioid-induced constipation (OIC). If the centrally mediated analgesia of opioids could be separated from their peripherally mediated gastrointestinal effects, by a peripherally acting opioid receptor antagonist, opioid-induced bowel dysfunction could be prevented or reversed. There has been considerable interest in peripherally acting opioid antagonists or other compounds to treat OIC. Subcutaneous methylnaltrexone is the first approved therapeutic agent for treatment of OIC, and studies have been conducted using the oral formulation. This editorial contains a brief overview of other selected compounds to treat OIC. Other potential uses of peripherally acting opioid antagonist in clinical practice are also discussed.
阿片类药物是治疗中重度疼痛的有效镇痛药，但它们的使用与许多不良反应有关，特别是阿片类药物引起的便秘（OIC）。如果可以通过外周作用的阿片受体拮抗剂将阿片类药物的中枢介导的镇痛作用与其外周介导的胃肠道作用分开，则可以预防或逆转阿片类药物引起的肠道功能障碍。人们对治疗 OIC 的外周作用阿片受体拮抗剂或其他化合物产生了极大的兴趣。皮下注射美沙酮是治疗 OIC 的第一种获批的治疗药物，并且已经使用口服制剂进行了研究。这篇社论简要概述了其他用于治疗 OIC 的选定化合物。还讨论了外周作用阿片受体拮抗剂在临床实践中的其他潜在用途。
