Saad Richard, Chey William D
Division of Gastroenterology, Department of Medicine, University of Michigan Medical Center, Ann Arbor, MI 48109, USA.
Expert Rev Gastroenterol Hepatol. 2008 Aug;2(4):497-508. doi: 10.1586/17474124.2.4.497.
Lubiprostone, a locally acting highly selective type-2 chloride channel activator, has been US FDA approved since January 2006 for the treatment of adults with chronic idiopathic constipation and FDA approved since April 2008 for the treatment of woman aged 18 years or older suffering from irritable bowel syndrome (IBS) with constipation. Through activation of the type-2 chloride channels located on the luminal side of intestinal epithelial cells, it promotes fluid secretion, increasing the liquid content of stool and accelerating small bowel as well as colonic transit. Lubiprostone has demonstrated efficacy with respect to increasing weekly spontaneous bowel movements and improving stool consistency, straining and constipation severity, both in short- and long-term studies. It has also demonstrated efficacy in the treatment of IBS with constipation, with beneficial effects on global symptoms, abdominal pain, constipation-related symptoms and overall quality of life. There is no evidence of a rebound in constipation or IBS symptoms following cessation of lubiprostone. In general, lubiprostone is well tolerated, with the most common side effects including nausea, headache and diarrhea.
鲁比前列酮是一种局部作用的高选择性2型氯离子通道激活剂，自2006年1月起已获得美国食品药品监督管理局（FDA）批准用于治疗成人慢性特发性便秘，自2008年4月起FDA批准其用于治疗18岁及以上患有便秘型肠易激综合征（IBS）的女性。通过激活位于肠上皮细胞腔面的2型氯离子通道，它促进液体分泌，增加粪便的液体含量，并加速小肠和结肠的蠕动。在短期和长期研究中，鲁比前列酮在增加每周自发排便次数、改善粪便稠度、排便费力情况和便秘严重程度方面均显示出疗效。它在治疗便秘型IBS方面也显示出疗效，对整体症状、腹痛、便秘相关症状和总体生活质量均有有益影响。没有证据表明停用鲁比前列酮后便秘或IBS症状会反弹。总体而言，鲁比前列酮耐受性良好，最常见的副作用包括恶心、头痛和腹泻。
