a Clinical Enteric Neuroscience Translational and Epidemiological Research (C.E.N.T.E.R.), Division of Gastroenterology and Hepatology , Mayo Clinic , Rochester , MN , USA.
Expert Rev Clin Pharmacol. 2019 Jul;12(7):579-589. doi: 10.1080/17512433.2019.1620104. Epub 2019 May 23.
: Prucalopride is a selective 5-HT receptor agonist with colonic prokinetic activity. It was recently approved by the FDA for the treatment of chronic idiopathic constipation. Before this approval, there were limited options to improve colonic motility in the treatment of chronic idiopathic constipation. : We systematically searched PubMed, Embase, ClinicalTrials.gov, and international conference presentations, and we reviewed all studies that evaluated prucalopride for the treatment of chronic idiopathic constipation in adults. In this review, we discuss the pharmacokinetics, pharmacodynamics, receptor interactions, phase I-IV clinical trials, and safety outcomes of prucalopride in adults, including the elderly. : Prucalopride is an effective agent to improve colonic motility, decrease colonic transit time, and increase complete spontaneous bowel movements in patients with chronic idiopathic constipation. Unlike previously available 5-HT receptor agonists such as cisapride and tegaserod, prucalopride does not interact with the cardiac hERG potassium channels or other serotonergic receptors in blood vessels and is not associated with an increase in major adverse cardiovascular events. Additionally, prucalopride has demonstrated promise in the treatment of gastroparesis, post-operative ileus, and opioid-induced constipation. Prucalopride directly stimulates colonic motility, differentiating it from all other medications (exclusively osmotic or chloride secretagogues) approved for chronic constipation in the last decade.
普芦卡必利是一种选择性 5-HT 受体激动剂，具有结肠促动力活性。它最近被 FDA 批准用于治疗慢性特发性便秘。在此批准之前，改善慢性特发性便秘结肠动力的选择有限。
我们系统地检索了 PubMed、Embase、ClinicalTrials.gov 和国际会议演讲，并回顾了所有评估普芦卡必利治疗成人慢性特发性便秘的研究。在这篇综述中，我们讨论了普芦卡必利在成人中的药代动力学、药效学、受体相互作用、I-IV 期临床试验和安全性结果，包括老年人。
普芦卡必利是一种有效的药物，可以改善结肠动力，减少结肠转运时间，并增加慢性特发性便秘患者的完全自发性排便。与以前可用的 5-HT 受体激动剂如西沙必利和替加色罗不同，普芦卡必利不会与心脏 hERG 钾通道或血管中的其他 5-羟色胺受体相互作用，也不会增加主要不良心血管事件的风险。此外，普芦卡必利在治疗胃轻瘫、术后肠梗阻和阿片类药物引起的便秘方面也显示出了希望。普芦卡必利直接刺激结肠动力，这使其与过去十年中批准用于慢性便秘的所有其他药物（仅限于渗透或氯化物分泌剂）区分开来。
