Springer, Private Bag 65901, Mairangi Bay, 0754, Auckland, New Zealand.
Drugs. 2016 Jan;76(1):99-110. doi: 10.1007/s40265-015-0518-3.
Prucalopride (Resolor®), a highly selective serotonin 5-HT4 receptor agonist, is indicated in the European Economic Area for the treatment of adults with chronic idiopathic constipation (CIC) in whom laxatives have failed to provide adequate relief. This article reviews the pharmacological properties of prucalopride and its clinical efficacy and tolerability in patients with CIC. In five well-designed, 12-week trials in patients with CIC, oral prucalopride 2 mg/day was significantly more effective than placebo at improving bowel function, including the number of bowel movements and a range of other constipation symptoms, as well as health-related quality of life and patient satisfaction; however, no significant differences in bowel function measures were observed between prucalopride and placebo in a 24-week trial. Oral PEG-3350 + electrolytes reconstituted powder was found to be noninferior but not superior to prucalopride according to primary endpoint data from a 4-week, controlled-environment trial. Prucalopride was generally well tolerated in clinical trials; the most common adverse events were headache, diarrhoea, nausea and abdominal pain. No cardiovascular safety issues have arisen with prucalopride treatment. Although further long-term and comparative data would be beneficial, prucalopride provides an additional treatment option for patients with CIC.
普芦卡必利(Resolor®),一种高度选择性的 5-羟色胺 4 受体激动剂,在欧洲经济区被批准用于治疗慢性特发性便秘(CIC)的成年患者,这些患者使用泻药后仍未得到充分缓解。本文综述了普芦卡必利的药理学特性及其在 CIC 患者中的临床疗效和耐受性。在五项针对 CIC 患者的为期 12 周的精心设计的试验中,普芦卡必利 2mg/天口服与安慰剂相比,在改善肠道功能方面更有效,包括排便次数和一系列其他便秘症状,以及健康相关生活质量和患者满意度;然而,在一项为期 24 周的试验中,普芦卡必利与安慰剂在肠道功能测量方面未观察到显著差异。根据为期 4 周的对照环境试验的主要终点数据,PEG-3350+电解质再配制粉末口服与普芦卡必利相比非劣效但不优于普芦卡必利。普芦卡必利在临床试验中总体耐受性良好;最常见的不良反应是头痛、腹泻、恶心和腹痛。普芦卡必利治疗未出现心血管安全性问题。尽管进一步的长期和比较数据将是有益的,但普芦卡必利为 CIC 患者提供了另一种治疗选择。