Bouras E P, Camilleri M, Burton D D, McKinzie S
Gastroenterology Research Unit, Mayo Clinic and Mayo Foundation, Rochester, Minnesota 55905, USA.
Gut. 1999 May;44(5):682-6. doi: 10.1136/gut.44.5.682.
Prucalopride (R093877) is a selective and specific 5HT4 agonist, the first of a new chemical class of benzofurans, with gastrointestinal prokinetic activities in vitro.
To evaluate the effects of prucalopride on gastrointestinal and colonic transit.
A validated scintigraphic technique was used to measure gastrointestinal and colonic transit over 48 hours in 50 healthy volunteers. For seven days, each subject received a daily dose of 0. 5, 1, 2, or 4 mg prucalopride, or placebo in a double blind, randomised fashion. The transit test was performed over the last 48 hours.
There were significant accelerations of overall colonic transit at 4, 8, 24, and 48 hours (p<0.05) and proximal colonic emptying t1/2 (p<0.05). The 0.5, 2, and 4 mg doses of prucalopride were almost equally effective and accelerated colonic transit compared with placebo. Prucalopride did not significantly alter gastric emptying (p>0.5) or small bowel transit (overall p=0. 12). The medication appeared to be well tolerated during the seven day treatment of healthy subjects.
Prucalopride accelerates colonic transit, partly by stimulating proximal colonic emptying, but does not alter gastric or small bowel transit in healthy human subjects. Prucalopride deserves further study in patients with constipation.
普芦卡必利（R093877）是一种选择性、特异性的5-羟色胺4（5HT4）激动剂，是新型化学类别苯并呋喃类中的首个药物，在体外具有胃肠促动力活性。
评估普芦卡必利对胃肠及结肠转运的影响。
采用一种经过验证的闪烁扫描技术，对50名健康志愿者48小时内的胃肠及结肠转运情况进行测量。在7天时间里，每位受试者以双盲、随机方式每日服用0.5、1、2或4毫克普芦卡必利，或服用安慰剂。转运测试在最后48小时进行。
在4、8、24和48小时时，结肠整体转运显著加速（p<0.05），近端结肠排空半衰期也显著缩短（p<0.05）。0.5毫克、2毫克和4毫克剂量的普芦卡必利与安慰剂相比，几乎具有同等效果，且能加速结肠转运。普芦卡必利对胃排空（p>0.5）或小肠转运无显著影响（总体p=0.12）。在对健康受试者进行的7天治疗期间，该药物耐受性良好。
普芦卡必利可加速结肠转运，部分原因是刺激近端结肠排空，但对健康受试者的胃或小肠转运无影响。普芦卡必利值得在便秘患者中进一步研究。
