双重功效镇痛药他喷他多的药理学研究与临床应用

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他喷他多是一种新型双重作用方式的中枢性镇痛药.它既是"阿片受体激动药.又是去甲肾上腺素重吸收抑制药.对急性、炎性和慢性神经病理性疼痛的多种动物模型有镇痛作用,其效能介于吗啡和曲马朵之间,静脉注射或口服均能达到满意的血药浓度,且耐受良好。最常见的静脉注射相关不良反应有嗜睡、眩晕、口干和恶心。药理作用与曲马朵类似,但曲马朵是左旋、右旋对映异构体的外消旋混合物,起μ阿片受体激动和去甲肾上腺素重吸收抑制作用的是不同构型的对映异构体分子及其代谢产物;而他喷他多则不需要中间代谢过程,作为μ阿片受体激动药和去甲肾上腺素重吸收抑制药都是同样的分子在起作用。这就是为什么他喷他多疗效强于曲马朵的原因。 Pentaturone is a new, dual-acting central analgesic that is both an opioid agonist and a norepinephrine reuptake inhibitor. It is indicated for acute, inflammatory, and chronic neuropathic pain A variety of animal models have analgesic effect, the potency between morphine and tramadol, intravenous or oral can reach satisfactory plasma concentrations, and well-tolerated.The most common intravenous adverse reactions associated with lethargy, Dizziness, dry mouth and nausea Pharmacological effects Similar to tramadol, but tramadol is a racemic mixture of levorotatory and dextrorotatory enantiomers that acts as an agonist of μ opioid receptor and norepinephrine reabsorption Is a different configuration of the enantiomeric molecules and their metabolites; and he spray him more does not require intermediate metabolic processes, as mu opioid agonists and norepinephrine reuptake inhibitors are the same molecule At work.This is why he sprayed him more effective than Tramadol effect.
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