Bruner Heather C, Atayee Rabia S, Edmonds Kyle P, Buckholz Gary T
Scripps Health and University of California San Diego, Joint Hospice and Palliative Medicine Fellowship, San Diego, CA, USA.
University of California San Diego, Skaggs School of Pharmacy and Pharmaceutical Sciences, La Jolla, CA, USA.
J Pain Res. 2015 Jun 12;8:289-94. doi: 10.2147/JPR.S61326. eCollection 2015.
Opioids are a class of medications frequently used for the treatment of acute and chronic pain, exerting their desired effects at central opioid receptors. Agonism at peripherally located opioid receptors, however, leads to opioid-induced constipation (OIC), one of the most frequent and debilitating side effects of prolonged opioid use. Insufficient relief of OIC with lifestyle modification and traditional laxative treatments may lead to decreased compliance with opioid regimens and undertreated pain. Peripherally acting mu-opioid receptor antagonists (PAMORAs) offer the reversal of OIC without loss of central pain relief. Until recently, PAMORAs were restricted to subcutaneous route or to narrow patient populations. Naloxegol is the first orally dosed PAMORA indicated for the treatment of OIC in noncancer patients. Studies have suggested its efficacy in patients failing traditional constipation treatments; however, insufficient evidence exists to establish its role in primary prevention of OIC at this time.
阿片类药物是一类常用于治疗急慢性疼痛的药物，通过作用于中枢阿片受体发挥预期效果。然而，外周阿片受体激动会导致阿片类药物引起的便秘（OIC），这是长期使用阿片类药物最常见且使人虚弱的副作用之一。生活方式改变和传统泻药治疗对OIC的缓解不足可能导致对阿片类药物治疗方案的依从性降低以及疼痛治疗不足。外周作用的μ-阿片受体拮抗剂（PAMORA）可逆转OIC，同时不丧失中枢性疼痛缓解作用。直到最近，PAMORA还仅限于皮下给药途径或应用于狭窄的患者群体。纳洛西戈是首个用于治疗非癌症患者OIC的口服PAMORA。研究表明其对传统便秘治疗无效的患者有效；然而，目前尚无足够证据确立其在OIC一级预防中的作用。
