A Prokinetic Agent with a Dual Effect – Itopride – In the Treatment of Dysmotility

P. Dítě, M. Rydlo, M. Dockal, A. Martínek
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Abstract

A wide range of dyspeptic symptoms in clinical practice reflect the high prevalence of functional disorders of the gastrointestinal (GI) tract. Prokinetic agents are the current mainstay in the therapy of functional dyspepsia. One of these drugs is itopride. We evaluated therapeutic efficacy of itopride according to the literature review. The therapeutic potential of itopride is connected with a dual effect: influencing of enzyme acetylcholinesterase activity and blocking dopamine D2 receptors. After the itopride administration, the contractility of smooth muscle in the upper GI tract increases. Itopride is a drug with rapid absorption from the small bowel; its peak serum concentration occurs 35 minutes after oral administration. Itopride does not pass the blood-brain barrier and does not affect the heart rate by influencing the QT segment. Itopride is a safe prokinetic agent with positive influence on the symptoms of functional dyspepsia such as postprandial fullness, bloating, and gastric emptying. Itopride could also be used for the therapy of the mild form of gastro-oesophageal reflux.
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双效促动力剂——依托必利治疗运动障碍
临床实践中广泛的消化不良症状反映了胃肠道功能障碍的高发性。促动力药物是目前治疗功能性消化不良的主要药物。其中一种药物是依托必利。我们根据文献回顾评价依托必利的治疗效果。依托必利的治疗潜力与双重作用有关:影响乙酰胆碱酯酶活性和阻断多巴胺D2受体。依托必利给药后,上消化道平滑肌的收缩力增强。依托必利是一种从小肠迅速吸收的药物;其血清浓度在口服给药后35分钟达到峰值。依托必利不通过血脑屏障,不通过影响QT段影响心率。依托必利是一种安全的促动力学药物,对功能性消化不良的症状如餐后饱腹感、腹胀和胃排空有积极影响。依托必利也可用于治疗轻度胃食管反流。
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