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西沙必利。对其药效学和药代动力学特性以及作为胃肠动力障碍促动力剂的治疗用途的初步综述。

Cisapride. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use as a prokinetic agent in gastrointestinal motility disorders.

作者信息

McCallum R W, Prakash C, Campoli-Richards D M, Goa K L

机构信息

Division of Gastroenterology, University of Virginia School of Medicine, Charlottesville.

出版信息

Drugs. 1988 Dec;36(6):652-81. doi: 10.2165/00003495-198836060-00002.

Abstract

Cisapride, a substituted piperidinyl benzamide chemically related to metoclopramide, is an orally administered prokinetic agent which facilitates or restores motility throughout the length of the gastrointestinal tract. Its novel mechanism of action is thought to involve enhancement of acetylcholine release in the myenteric plexus of the gut. Because of its specificity cisapride is devoid of central depressant or antidopaminergic effects; side effects such as diarrhoea or loose stools, which occur infrequently, are related to its primary pharmacological action. Evidence exists from comparisons with placebo in initial trials to establish the efficacy of cisapride in improving healing rates and symptoms in patients with reflux oesophagitis, in alleviating symptoms in patients with non-ulcer dyspepsia, and in accelerating gastric emptying in gastroparesis. There are less conclusive data regarding the efficacy of cisapride in relieving symptoms in patients with gastroparesis, although preliminary results support a role for cisapride in certain groups such as diabetics. Limited data suggest that patients with chronic constipation due to underlying motility disorders may benefit from cisapride. Unfortunately, there is a paucity of trials comparing the efficacy of cisapride with other therapeutic agents. Thus, the relative position of cisapride in therapy cannot be defined at present. Should future results support preliminary evidence of comparable efficacy to metoclopramide, domperidone and ranitidine (in oesophagitis), cisapride with its favourable tolerability profile should claim a prominent position in the therapy of patients with a variety of gastrointestinal motility disorders.

摘要

西沙必利是一种与甲氧氯普胺化学相关的取代哌啶基苯甲酰胺,是一种口服促动力剂,可促进或恢复整个胃肠道的蠕动。其独特的作用机制被认为涉及增强肠道肌间神经丛中乙酰胆碱的释放。由于其特异性,西沙必利没有中枢抑制或抗多巴胺能作用;腹泻或稀便等副作用很少发生,与它的主要药理作用有关。在最初的试验中,与安慰剂比较有证据表明西沙必利在提高反流性食管炎患者的愈合率和症状改善方面、在缓解非溃疡性消化不良患者的症状方面以及在加速胃轻瘫患者的胃排空方面有效。关于西沙必利在缓解胃轻瘫患者症状方面的疗效数据不太确凿,尽管初步结果支持西沙必利在某些群体(如糖尿病患者)中发挥作用。有限的数据表明,因潜在动力障碍导致慢性便秘的患者可能从西沙必利中获益。不幸的是,比较西沙必利与其他治疗药物疗效的试验很少。因此,目前尚无法确定西沙必利在治疗中的相对地位。如果未来的结果支持其与甲氧氯普胺、多潘立酮和雷尼替丁(在食管炎治疗中)疗效相当的初步证据,那么西沙必利因其良好的耐受性,在治疗各种胃肠道动力障碍患者中应占据重要地位。

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