部份中文“普卢卡必利”处方（仅供参考）

Resolor（普卢卡必利）2009 年 10 月在欧洲获批后，2010 年 1 月在 德国上市，2010 年 3 月在英国上市。

美国罗切斯特梅奥医院报道，采用普卢卡必利治疗重度慢性便秘短期可显著改善肠道功能，减轻便秘症状。

普卢卡必利（prucalopride）具有高度选择性及特异性的5-HT4受体激动作用。

Camilleri等进行了一项多中心、随机对照研究，对620名重度慢性便秘（大便次数≤2次/周）分别每天服用安慰剂、普卢卡必利2mg或4mg，疗程12周。结果三组排便次数增加的比例分别为25.8%、47.3%和46.6%。普卡必利治疗的两组患者对治疗的满意度和症状严重程度认知都有显著改善，并未发现严重的心血管影响。

普卢卡必利（prucalopride）为苯丙咪唑类药物，是特异性S-HT4受体完全激动剂，具有较高选择性和特异性5- HT4受体作用，增加胆碱能神经递质的释放，刺激肠蠕动反射，增强结肠收缩和近端结肠传输，能够有效地缓解便秘病人的症状，主要用于治疗各种便秘及手术的胃肠道蠕动无力和假性梗阻。

曾用名：4-Amino-5-chloro-2,3-dihydro-N-[1-(3-methoxypropyl)-4-piperidinyl]-7-benzofurancarboxamide 

Resolor(prucalopride)

Resolor launched for chronic constipation

Resolor (prucalopride) is a new treatment for women with chronic laxative-resistant constipation.

PHARMACOLOGY

Prucalopride (Resolor) is a selective, high-affinity 5HT4 agonist.1 It acts on 5HT4 receptors in the gut to accelerate colonic transit; higher doses also seem to enhance gastric emptying and small bowel transit.2

CLINICAL STUDIES

Prucalopride was evaluated in three pivotal trials of identical design, one conducted in Europe and two carried out in the US. Following a two-week run-in phase, investigators randomised males and females with chronic constipation to receive once daily 2mg or 4mg oral doses of prucalopride, or placebo, for 12 weeks. The primary end point in each study was the proportion of patients who experienced a response, defined as an average of three or more spontaneous, complete bowel movements per week.3-5

In the first trial (PRU-INT-6), the intention-to-treat population comprised 713 patients. The proportion of these individuals who experienced a response over the treatment period was significantly greater in the prucalopride 2mg and 4mg groups (19.5% and 23.6%, respectively) than in the placebo group (9.6%; p≤0.01 versus prucalopride 2mg and p≤0.001 versus prucalopride 4mg).3

The second trial (PRU-USA-11) enrolled 628 patients, of whom 620 were included in the intention-to-treat analysis. Compared with the placebo-treated patients, more than twice as many of the patients who received prucalopride responded to treatment (30.9% for the 2mg dose and 28.4% for the 4mg dose versus 12.0% for placebo; p<0.001 for both comparisons).4

A total of 651 patients were enrolled in the third trial (PRU-USA-13); 641 received study medication and qualified for the intention-to-treat analysis. Again, response rates in the prucalopride-treated patients (23.9% and 23.5% at the 2mg and 4mg doses, respectively) were greater than in the placebo-treated patients (12.1%; p≤0.01 for both comparisons).5

The key secondary end point in the pivotal studies was the proportion of patients who experienced an increase in spontaneous, complete bowel movements of at least one per week. In all the studies, this proportion was significantly greater for both prucalopride doses than for placebo (p≤0.001 or p<0.001 for all comparisons).2

Overall, prucalopride was associated with a consistent and significant improvement in patients' satisfaction with their treatment and bowel habits, as assessed by the Patient Assessment of Constipation Quality of Life questionnaire (PAC-QOL). The proportion of participants who had a ≥1-point improvement in the 5-point satisfaction subscale score of the PAC-QOL was 45.3% in those on prucalopride 2mg, compared with 21.3% in those who received placebo.2

Analysis of pooled safety data from the three studies indicated that prucalopride was generally well tolerated; in most cases, adverse effects were mild to moderate and transient. The most common prucalopride-related adverse events were headache, nausea, diarrhoea and abdominal pain. Unlike non-selective gastroprokinetic 5HT4 agonists, prucalopride does not seem to prolong QT interval.2

Although the three pivotal trials of prucalopride recruited both males and females, almost 90% of participants were female. As a result, concerns arose during regulatory assessment that the drug had not been sufficiently evaluated in men; therefore, approval was granted for use only in women. There is no evidence that prucalopride's pharmacokinetics, pharmacodynamics or mechanism of action differ between men and women, although men may require a higher dose. Movetis, the manufacturer of prucalopride, is expected to perform a post-authorisation efficacy study in men.2

Prucalopride is administered as a once daily 1mg or 2mg dose.1 In pivotal trials, the 4mg dose did not provide a significant incremental benefit over the 2mg dose.2

原产地英文商品名:
Resolor 2mg/tab 28tabs/box
原产地英文药品名:
Prucalopride
原产地英文化合物名称:
4-Amino-5-chloro-2,3-dihydro-N-[1-(3-methoxypropyl)-4-piperidinyl]-7-benzofurancarboxamide
中文参考商品译名:
Resolor 2毫克/片 28片/盒
中文参考药品译名:
普卢卡必利
产地国家: 英国
所属类别: 作用于消化系统药物->便秘
处方药:处方药
包装规格: 2毫克/片 28片/盒
销售单价(美元 US$):296美元
销售单价(人民币 RMB): 1948元
计价单位: 盒