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To compare the simplicity and tolerability of two human models used for evaluation of anti-emetic drugs for severe vomiting

机译:比较两种用于评估严重呕吐止吐药的人类模型的简单性和耐受性

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  ABSTRACT For evaluation of the antiemetic effects of the drugs animal models (Ferret,cat dog etc) are used. Although good guidelines may be established through the animal experiments, they may not give accurate indication of the antiemetic effect of the antiemetic drugs in patients due to species differences in pharmacokinetic and pharmacodynamic responses. Therefore, Ipecacuanha-induced emesis and flare models are used to predict more accurately the antiemetic effect of the antiemetic drugs. In ipecacuanha-induced emesis model in 10 healthy human volunteers slow intravenous injection of ondanserton -2 ml. (4 mg) was given over 5 minutes.Thirty minutes after inj. ondanserton, 30 ml. oral syrup of tincture ipecac was given with glassful of water. Then the parameters like time, number and duration of emesis were noted over 6 hour’s period. In flare model in 6 healthy human volunteers Injection Serotonin 0.05 ml of 12.98 µM was given intradermally on the flexor aspect of forearm. Resulting flare response was measured over 5 minutes. At the end of half an hour, injection ondansetron and same dose of injection serotonin was given intradermally. Resulting flare response was measured in the similar way. Out of these two models, ipecac model is technically easy and clinically relevant but its tolerability is less. Flare model has excellent tolerability but it is technically not very easy. Thus one can choose the effective model accordingly. Key words: Antiemetic, Ipecacuanha, Ondansetron, Serotonin
机译:摘要为了评估药物的止吐作用,使用了动物模型(鼬,猫狗等)。尽管可以通过动物实验建立良好的指导原则,但由于药代动力学和药效学反应的物种差异,它们可能无法准确指示止吐药对患者的止吐作用。因此,Ipecacuanha诱导的呕吐和耀斑模型可用于更准确地预测止吐药的止吐作用。在ipecacuanha诱导的呕吐模型中,有10位健康的人类志愿者缓慢静脉注射ondanserton -2 ml。注射30分钟后(5毫克)(4毫克)。昂丹瑟顿30毫升。酒吐根口服糖浆加一杯水。然后记录6小时内的呕吐时间,次数和持续时间等参数。在6名健康人类志愿者的耀斑模型中,在前臂屈肌方面皮内注射0.05 ml的12.98 µM血清素。在5分钟内测量了产生的耀斑响应。在半小时结束时,皮内注射恩丹西酮和相同剂量的5-羟色胺。以相似的方式测量了产生的耀斑响应。在这两个模型中,吐根模型在技术上很容易且在临床上具有相关性,但其耐受性较低。 Flare模型具有出色的耐受性,但从技术上讲并不容易。因此,人们可以据此选择有效的模型。关键词:止吐药,Ipecacuanha,恩丹西酮,5-羟色胺

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