[Pharmacologic and clinical differentiation of prokinetic drugs].

Leber, Magen, Darm Pub Date : 1996-07-01
B May, I Greving
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Abstract

In the treatment of gastrointestinal motility disorders 3 prokinetic agents are principally available. They are differentiated from their pharmacological mode of action, their clinical efficacy and tolerability. Metroclopramide is an antidopaminergic benzamide with mainly antiemetic effects and minor prokinetic efficacy in the GI-Tract. Domperidon is a pure dopaminantagonist. It accelerates gastric emptying but has less effect on bowel motility. Cisapride stimulates indirect the secretion of acetylcholine and acts via 5 HT-receptors selective at the plexus myentericus. These pharmacological differences have clinical relevance: metoclopramide and domperidon could not consistently prove efficacy in functional dyspepsia and GORD. In addition the data in other indications are rare. Only cisapride has shown significant responder rates in controlled studies in the treatment of gastrointestinal motility disorders particularly in long term treatment. As concerns tolerability cisapride presents a progress by its selective mode of action in contrast to the agents crossing the blood-brain-barrier.

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[促动力药物的药理与临床辨证]。
在胃肠道运动障碍的治疗中,主要有3种促运动药物。从它们的药理作用方式、临床疗效和耐受性来区分它们。Metroclopramide是一种抗多巴胺能苯甲酰胺,在胃肠道中具有主要的止吐作用和轻微的促动力学作用。Domperidon是一种纯多巴胺拮抗剂。它能加速胃排空,但对肠蠕动的影响较小。西沙比利间接刺激乙酰胆碱的分泌,并通过5个ht受体选择性地作用于肌丛。这些药理学差异具有临床相关性:甲氧氯普胺和冬哌冬不能一致证明对功能性消化不良和GORD的疗效。此外,其他适应症的数据很少。只有西沙必利在治疗胃肠运动障碍的对照研究中显示出显著的应答率,特别是在长期治疗中。就耐受性而言,西沙必利通过其选择性作用方式与穿越血脑屏障的药物相比,呈现出一种进步。
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