a Division of Pharmaceutical and Narcotic Affaire, Vice Chancellor for Food and Drug , Kurdistan University of Medical Sciences , Sanandaj , Iran.
b Department of Pharmacoeconomics and Pharmaceutical Administration, Faculty of Pharmacy and Pharmaceutical Policy Research Center , Tehran University of Medical Sciences , Tehran , Iran.
Expert Opin Pharmacother. 2018 Jul;19(10):1127-1135. doi: 10.1080/14656566.2018.1491549. Epub 2018 Jul 6.
The extensive and alarming use of opioids for pain management in patients with chronic pain receiving palliative care is associated with non-tolerable gastrointestinal (GI) adverse effects. Opioid-induced constipation (OIC) is the most common adverse effect impairing patient quality of life (QOL). In addition, OIC is one of the treatment limiting consequences of opioid analgesics. Management of OIC is becoming a challenge since traditional laxatives have limited efficiency. Peripherally acting mu-opioid receptor antagonists (PAMORA) have been developed for the treatment of OIC with methylnaltrexone bromide being the first approved to treat OIC in adults with advanced illness undergoing palliative care. Areas covered: The authors systematically review the clinical evidence for methylnaltrexone bromide including a review of the pharmacokinetic and pharmacodynamic data along with clinical effectiveness and cost-effectiveness. Though there is a need for further long-term clinical investigation, there is a large body of evidence for both its efficacy and safety in the treatment of OIC. Expert opinion: Methylnaltrexone has both subcutaneous injection and oral dosage forms available in the market. The lack of more evidence in specific populations such as pregnant women, pediatrics and elderly still remains. The global consumption of methylnaltrexone shows a projection of increased use since its approval worldwide in 2008.
阿片类药物在接受姑息治疗的慢性疼痛患者中广泛且令人担忧地用于疼痛管理，这与无法耐受的胃肠道（GI）不良反应有关。阿片类药物引起的便秘（OIC）是最常见的不良反应，会影响患者的生活质量（QOL）。此外，OIC 是阿片类镇痛药治疗受限的后果之一。由于传统的泻药效率有限，OIC 的管理正成为一个挑战。外周作用μ-阿片受体拮抗剂（PAMORA）已被开发用于治疗 OIC，其中甲基纳曲酮溴化物是第一种被批准用于治疗接受姑息治疗的晚期疾病成人 OIC 的药物。涵盖领域：作者系统地回顾了甲基纳曲酮溴化物的临床证据，包括药代动力学和药效学数据以及临床疗效和成本效益的回顾。尽管需要进一步进行长期的临床研究，但在治疗 OIC 方面，它具有大量的疗效和安全性证据。专家意见：甲基纳曲酮既有皮下注射剂型，也有口服剂型在市场上销售。在特定人群（如孕妇、儿科和老年人）中，仍缺乏更多的证据。自 2008 年在全球获得批准以来，全球对甲基纳曲酮的使用预计将增加。
