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西沙比利(cisapride,简称cis)是治疗累及食管到结肠平滑肌的胃肠道动力(motility)疾病的最新促动力(prokinetic)药。促动力药是恢复、正常化并促进胃肠道动力的药物。临床上首次成功应用的多巴胺拮抗剂胃复安(简为met)可改善胃排空,加快小肠转运速度,然而met可通过血脑屏障而对中枢神经系有抗多巴胺作用,有10~20%使用者出现椎体外副作用。多潘立酮(domperidone,简为dom)在一定程度上克服了这些缺点,但cis是促动力药中唯一无抗多巴胺性能,其通过增加肠肌丛节后神经末梢生理性释出乙酰胆碱而发挥作用,改善食管、胃、小肠及大肠推进性运动,无直接抗吐作用。药物动力学及代谢 cis在化学上与met有关。98%与血浆蛋
Cisapride (cis) is the latest prokinetic drug used to treat gastrointestinal motility disorders involving the esophagus to the colon smooth muscle. Propellant drugs are drugs that restore, normalize, and promote gastrointestinal motility. The first successful clinical application of dopamine antagonist metoclopramide (abbreviated met) can improve gastric emptying and speed up the intestinal transit, however met through the blood-brain barrier and the central nervous system has anti-dopamine effect, 10 to 20% Vertebral body users appear side effects. Domperidone (dom), to some extent, overcomes these shortcomings, but cis is the only anti-dopamine-free drug that acts by improving the physiological release of acetylcholine at the nerve endings of the myenteric plexus, Esophageal, stomach, small intestine and colon promote sexual activity, no direct anti-vomiting. Pharmacokinetics and Metabolism cis is chemically related to met. 98% with plasma egg