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西沙必利是最新的通过肠肌层神经丛节后神经末稍生理性增加乙酰胆碱释放而无多巴胺能作用的第三代前动力性药物。用于治疗食管及胃肠道各种运动障碍性疾病,副作用少而轻,病人极易耐受。药代动力学本药98%与血浆蛋白结合,主要代谢物为N-二烷基化合物和芳香族羟基化合物,随尿和粪便排泄。健康自愿者口服单剂或多剂西沙必利后药物半减期约为7～10小时。大鼠喂饲氚标记的西沙必利10mg/kg,在15～30分钟内放射活性物质达最高组织浓度,血浆与组织间的浓度相等,15分钟后雄性大鼠肝组织浓度为血浆的35倍,胃和小肠壁内及肺、肾、软骨和淋巴组织等水平分别比血浆高14～18倍及2～6倍,而脑组织比血浆水平
Cisapride is the newest third-generation antecedent drug that does not have a dopaminergic effect by physiologically increasing acetylcholine release through the myenteric plexus ganglia postganglionic. For the treatment of esophageal and gastrointestinal motility disorders, less side effects and light, the patient easily tolerated. Pharmacokinetics 98% of the drug and plasma protein binding, the main metabolites of N-dialkyl compounds and aromatic hydroxy compounds, excreted with urine and feces. Health volunteers oral single or multiple doses of cisapride drug half-time of about 7 to 10 hours. Rats were fed with tritiated cisapride 10 mg / kg and radioactive substances reached the highest tissue concentration within 15-30 minutes with equal plasma and tissue concentrations. After 15 minutes, the concentration of liver tissue in male rats was 35 times higher than that in plasma , The stomach and small intestine wall and lung, kidney, cartilage and lymphoid tissue levels were 14 to 18 times higher and 2 to 6 times higher plasma levels, while the brain tissue than plasma levels