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鲁比前列酮:一种治疗慢性便秘的新型药物。

Lubiprostone: a novel treatment for chronic constipation.

作者信息

Lacy Brian E, Levy L Campbell

机构信息

Section of Gastroenterology & Hepatology, Dartmouth-Hitchcock Medical Center, Lebanon, NH 03756, USA.

出版信息

Clin Interv Aging. 2008;3(2):357-64. doi: 10.2147/cia.s2938.

DOI:10.2147/cia.s2938
PMID:18686757
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2546479/
Abstract

Chronic constipation is highly prevalent, reduces patients' quality of life, and imposes a significant health care burden on society. Lifestyle modifications and over-the-counter agents improve symptoms of constipation in some patients, however many patients have persistent symptoms and require the use of prescription medications. Three prescription medications are currently Food and Drug Administration (FDA) approved and available for the treatment of chronic constipation in adults. This review will focus on lubiprostone, the newest medication available for the treatment of chronic constipation. Lubiprostone is a bicyclic fatty acid metabolite analogue ofprostaglandin E1. It activates specific chloride channels in the gastrointestinal tract to stimulate intestinal fluid secretion, increase gastrointestinal transit, and improve symptoms of constipation. This article will provide a brief overview on chloride channel function in the gastrointestinal tract, describe the structure, function, and pharmacokinetics of lubiprostone, and discuss the safety and efficacy of this new medication.

摘要

慢性便秘非常普遍,会降低患者的生活质量,并给社会带来巨大的医疗负担。生活方式的改变和非处方药物可改善部分患者的便秘症状,然而许多患者症状持续存在,需要使用处方药。目前有三种处方药已获美国食品药品监督管理局(FDA)批准,可用于治疗成人慢性便秘。本综述将聚焦于鲁比前列酮,这是治疗慢性便秘的最新药物。鲁比前列酮是前列腺素E1的双环脂肪酸代谢物类似物。它激活胃肠道中的特定氯离子通道,以刺激肠道液体分泌,增加胃肠道蠕动,并改善便秘症状。本文将简要概述胃肠道中氯离子通道的功能,描述鲁比前列酮的结构、功能和药代动力学,并讨论这种新药的安全性和有效性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/45f3/2546479/30d028757d59/cia0302-357-01.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/45f3/2546479/30d028757d59/cia0302-357-01.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/45f3/2546479/30d028757d59/cia0302-357-01.jpg

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本文引用的文献

1
Systematic Review: FDA-Approved Prescription Medications for Adults With Constipation.系统评价:美国食品药品监督管理局批准的用于成人便秘的处方药
Gastroenterol Hepatol (N Y). 2006 Oct;2(10):736-749.
2
Multicenter, 4-week, double-blind, randomized, placebo-controlled trial of lubiprostone, a locally-acting type-2 chloride channel activator, in patients with chronic constipation.多中心、为期4周的双盲随机安慰剂对照试验,研究局部作用的2型氯离子通道激活剂鲁比前列酮治疗慢性便秘患者的疗效。
Am J Gastroenterol. 2008 Jan;103(1):170-7. doi: 10.1111/j.1572-0241.2007.01524.x. Epub 2007 Oct 4.
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Lubiprostone, a locally acting chloride channel activator, in adult patients with chronic constipation: a double-blind, placebo-controlled, dose-ranging study to evaluate efficacy and safety.
Children (Basel). 2025 Jun 28;12(7):857. doi: 10.3390/children12070857.
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Raising Expectations in IBS-C Management.提高IBS-C管理的期望。
Gastroenterol Hepatol (N Y). 2025 Apr;21(4):218-231.
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Sex-specific transcriptome similarity networks elucidate comorbidity relationships.性别特异性转录组相似性网络阐明了共病关系。
bioRxiv. 2025 Jan 24:2025.01.22.634077. doi: 10.1101/2025.01.22.634077.
6
Lubiprostone Reduces Fat Content on MRI-PDFF in Patients With MASLD: A 48-Week Randomised Controlled Trial.鲁比前列酮可降低非酒精性脂肪性肝病患者MRI-PDFF的脂肪含量:一项48周的随机对照试验。
Aliment Pharmacol Ther. 2025 Feb;61(4):628-635. doi: 10.1111/apt.18478. Epub 2025 Jan 2.
7
Lubiprostone Improves Distal Segment-Specific Colonic Contractions through TRPC4 Activation Stimulated by EP3 Prostanoid Receptor.鲁比前列酮通过EP3前列腺素受体刺激的TRPC4激活改善特定结肠远端节段的收缩。
Pharmaceuticals (Basel). 2024 Oct 4;17(10):1327. doi: 10.3390/ph17101327.
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A Case Study in the IBS-C Management Continuum: Assessing Patient Response and Tailoring Treatment.肠易激综合征便秘型管理连续统一体的案例研究:评估患者反应并调整治疗方案
Gastroenterol Hepatol (N Y). 2024 Jul;20(7):383-427.
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Leaky Gut Syndrome: Myths and Management.肠漏综合征:误解与应对
Gastroenterol Hepatol (N Y). 2024 Aug;20(5):264-272.
10
Effectiveness and safety of lubiprostone after switching from stimulant laxatives in elderly patients with chronic constipation.老年慢性便秘患者从刺激性泻药转换为鲁比前列酮后的有效性和安全性。
JGH Open. 2023 Aug 11;7(9):610-617. doi: 10.1002/jgh3.12956. eCollection 2023 Sep.
鲁比前列酮,一种局部作用的氯离子通道激活剂,用于成年慢性便秘患者:一项评估疗效和安全性的双盲、安慰剂对照、剂量范围研究。
Aliment Pharmacol Ther. 2007 Jun 1;25(11):1351-61. doi: 10.1111/j.1365-2036.2007.03320.x.
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A randomized, multicenter, placebo-controlled trial of polyethylene glycol laxative for chronic treatment of chronic constipation.一项关于聚乙二醇泻药用于慢性便秘长期治疗的随机、多中心、安慰剂对照试验。
Am J Gastroenterol. 2007 Jul;102(7):1436-41. doi: 10.1111/j.1572-0241.2007.01199.x. Epub 2007 Mar 31.
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Functional bowel disorders.功能性肠病
Gastroenterology. 2006 Apr;130(5):1480-91. doi: 10.1053/j.gastro.2005.11.061.
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Effect of a selective chloride channel activator, lubiprostone, on gastrointestinal transit, gastric sensory, and motor functions in healthy volunteers.选择性氯离子通道激活剂鲁比前列酮对健康志愿者胃肠转运、胃感觉及运动功能的影响。
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