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比沙可啶:药理学和临床证据综述,以指导便秘患者临床实践中的应用。

Bisacodyl: A review of pharmacology and clinical evidence to guide use in clinical practice in patients with constipation.

机构信息

NIHR Nottingham Biomedical Research Centre (BRC),, Nottingham University Hospitals NHS Trust, University of Nottingham, Nottingham, UK.

Nottingham Digestive Diseases Centre, School of Medicine, University of Nottingham, Nottingham, UK.

出版信息

Neurogastroenterol Motil. 2021 Oct;33(10):e14123. doi: 10.1111/nmo.14123. Epub 2021 Mar 9.

DOI:10.1111/nmo.14123
PMID:33751780
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8596401/
Abstract

BACKGROUND

Bisacodyl is a member of the diphenylmethane family and is considered to be a stimulant laxative. It has a dual prokinetic and secretory action and needs to be converted into the active metabolite bis-(p-hydroxyphenyl)-pyridyl-2-methane (BHPM) in the gut to achieve the desired laxative effect. Bisacodyl acts locally in the large bowel by directly enhancing the motility, reducing transit time, and increasing the water content of the stool. A recent network meta-analysis concluded that bisacodyl showed similar efficacy to prucalopride, lubiprostone, linaclotide, tegaserod, velusetrag, elobixibat, and sodium picosulfate for the primary endpoint of ≥3 complete spontaneous bowel movements (CSBM)/week and an increase of ≥1 CSBM/week over baseline. The meta-analysis also found that bisacodyl may be superior to the other laxatives for the secondary endpoint of change from baseline in the number of spontaneous bowel movements per week in patients with chronic constipation. This observation stimulated the authors to review the available literature on bisacodyl, which has been available on the market since the 1950 s.

PURPOSE

The aim of the current review was to provide an overview of the historic background, structure, function, and mechanism of action of bisacodyl. Additionally, we discuss the important features and studies for bisacodyl to understand its peculiar characteristics and guide its use in clinical practice, but also stimulate research on open questions.

摘要

背景

比沙可啶属于二苯甲烷家族,被认为是一种刺激性泻药。它具有双重促动力和分泌作用,需要在肠道内转化为活性代谢物双-(对羟苯基)-吡啶-2-甲烷(BHPM),才能达到预期的通便效果。比沙可啶在大肠中局部起作用,通过直接增强运动、减少传输时间和增加粪便中的水分含量来起作用。最近的一项网络荟萃分析得出结论,比沙可啶在主要终点(每周≥3 次完全自发的排便(CSBM)和每周基线增加≥1 次 CSBM)方面与普芦卡必利、鲁比前列酮、利那洛肽、替加色罗、维鲁司他、依洛西班和聚乙二醇 4000 硫酸钠相似,疗效相似。荟萃分析还发现,对于慢性便秘患者每周自发排便次数从基线的变化这一次要终点,比沙可啶可能优于其他泻药。这一观察结果促使作者回顾了自 20 世纪 50 年代以来一直在市场上销售的比沙可啶的现有文献。

目的

本综述的目的是概述比沙可啶的历史背景、结构、功能和作用机制。此外,我们还讨论了比沙可啶的重要特征和研究,以了解其独特的特点,并指导其在临床实践中的应用,同时也激发对开放性问题的研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/34f3/8596401/f9f8dfaf53b8/NMO-33-e14123-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/34f3/8596401/3fb398eff084/NMO-33-e14123-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/34f3/8596401/203ce91de7e0/NMO-33-e14123-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/34f3/8596401/fb616a8d492e/NMO-33-e14123-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/34f3/8596401/5deba0c02966/NMO-33-e14123-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/34f3/8596401/f9f8dfaf53b8/NMO-33-e14123-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/34f3/8596401/3fb398eff084/NMO-33-e14123-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/34f3/8596401/203ce91de7e0/NMO-33-e14123-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/34f3/8596401/fb616a8d492e/NMO-33-e14123-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/34f3/8596401/5deba0c02966/NMO-33-e14123-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/34f3/8596401/f9f8dfaf53b8/NMO-33-e14123-g005.jpg

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