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Cilansetron.

机译:西兰司酮。

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Irritable bowel syndrome is an extremely common disorder affecting approximately 10-20% of the population of North America and Europe. This disorder is characterized by abdominal pain and altered bowel habit. The altered bowel habit can take a number of forms. These include a predominant diarrhea form, a form with constipation and one in which patients alternate between diarrhea and constipated forms of the disorder. Irritable bowel syndrome to date has not been associated with any excess mortality. However, the morbidity associated with irritable bowel syndrome is quite high. This mainly takes on the form of impairment in health-related quality of life, interference with activities of daily living and a considerable degree of human suffering. Likewise, the economic impact of irritable bowel syndrome is not trivial and has been estimated to be between USDollars 20 to 30 billion in the United States alone. In an effort to address this common disabling disorder, a number of new drugs have been developed.One of the latest is cilansetron, which is a competitive type 3 serotonin (5-HT3) receptor antagonist. In phase III trials, cilansetron has been shown to be efficacious for the relief of a wide spectrum of symptoms related to irritable bowel syndrome with diarrhea both in male and female patients. By and large, cilansetron is extremely well tolerated and highly efficacious. The most common side effect of cilansetron is constipation, which is seen in 3-12% of subjects at 6 months. Ischemic colitis, a side effect associated with previous drugs of this class, has been seen in eight subjects (six women and two men) to date. All of these ischemic colitis events have been self-limited and did not require surgery. Because of its high degree of efficacy, the fact that it is well tolerated by the overwhelming majority of patients and that it shows efficacy in both genders, cilansetron represents a major advance in the treatment of irritable bowel syndrome with diarrhea predominance.
机译:肠易激综合症是一种极为普遍的疾病,影响了北美和欧洲约10-20%的人口。这种疾病的特征是腹痛和排便习惯改变。改变的排便习惯可以采取多种形式。这些包括腹泻型,便秘型和腹泻型与便秘型交替的形式。迄今为止,肠易激综合征尚未与任何过量死亡率相关。但是,肠易激综合症的发病率很高。这主要表现为与健康有关的生活质量受损,干扰日常生活活动和相当程度的人类痛苦。同样,肠易激综合症对经济的影响也不是小事,仅在美国,估计就在20至300亿美元之间。为了解决这种常见的致残性疾病,已经开发了许多新药,其中最新的一种是cilansetron,它是一种竞争性3型血清素(5-HT3)受体拮抗剂。在III期临床试验中,西兰司酮已被证明可有效缓解男性和女性患者肠易激综合征和腹泻相关的多种症状。总的来说,香兰司酮具有极好的耐受性和高效性。来兰司酮最常见的副作用是便秘,这在6个月的3-12%的受试者中可见。迄今为止,已经在八名受试者(六名女性和两名男子)中发现了缺血性结肠炎,这是与该类先前药物相关的副作用。所有这些缺血性结肠炎事件都是自限性的,不需要手术。由于其高水平的疗效,绝大多数患者对它的耐受性很强,并且它在两种性别中均显示出疗效,因此,香兰西酮代表了以腹泻为主的肠易激综合征的治疗的重大进展。

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