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Drugs. 2013 Nov;73(17):1935-50. doi: 10.1007/s40265-013-0140-1.
The highly selective serotonin 5-HT4 receptor agonist prucalopride (Resolor(®), Resotran(®), Resotrans(®)) is indicated for the treatment of chronic constipation. In four randomized, double-blind, multicentre, 12-week trials in patients (predominantly women) with chronic constipation, oral prucalopride 2 mg once daily improved bowel function to a significantly greater extent than placebo, with a significantly greater proportion of prucalopride than placebo recipients achieving an average of ≥3 spontaneous, complete bowel movements per week (primary endpoint). Significantly greater improvements in health-related quality of life, patient satisfaction with treatment and bowel habit, and a range of constipation-related symptoms were also seen with prucalopride than with placebo. Satisfaction with treatment and bowel habit was maintained with prucalopride in the longer term. Prucalopride was generally well tolerated in patients with chronic constipation, with the most commonly reported adverse events (headache, nausea, abdominal pain, diarrhoea) primarily occurring on the first day of treatment. During the clinical trials, no cardiovascular safety issues have arisen in patients with chronic constipation receiving prucalopride. In conclusion, prucalopride is an important option for use in patients with chronic constipation who have not experienced adequate relief with laxatives.
高度选择性 5-羟色胺 4 受体激动剂普芦卡必利(Resolor(®)、Resotran(®)、Resotrans(®))适用于治疗慢性便秘。在四项针对慢性便秘患者(主要为女性)的随机、双盲、多中心、为期 12 周的试验中,每日口服普芦卡必利 2mg 可显著改善肠道功能,优于安慰剂,普芦卡必利组较安慰剂组有更多患者达到每周平均≥3 次自发完全排便的主要终点。普芦卡必利还显著改善了与健康相关的生活质量、患者对治疗的满意度和排便习惯,以及一系列与便秘相关的症状。长期使用普芦卡必利也能维持对治疗和排便习惯的满意度。普芦卡必利在慢性便秘患者中总体耐受性良好,最常见的不良反应(头痛、恶心、腹痛、腹泻)主要发生在治疗的第 1 天。在临床试验中,接受普芦卡必利治疗的慢性便秘患者未出现心血管安全性问题。总之,普芦卡必利是治疗未通过泻药充分缓解的慢性便秘患者的重要选择。