Nalbuphine and Addiction: From the Basic Science to Clinical Set

Conter Fs, Oliveira Ar, Weston Ac
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引用次数: 2

Abstract

Opioid drugs are currently the main treatment for acute and chronic pain control. Over the past three decades, misuse of opioids has led to rising worldwide addiction/dependence rates and overdose deaths. In the United States of America, this opiate crisis scenario, which in 2016 alone resulted in the estimated death of over 64,000 people, was characterized as the Opioid Epidemic and declared as a national public health emergency.1 Nalbuphine (C21H27NO4) is a synthetic kappa receptor agonist opioid and partial Mu receptor antagonist,2,3 which has been synthesized in an attempt to provide analgesia without the undesirable side effects of pure agonists.4 Thus, the central analgesic action and lower Nalbuphine addiction/dependence potential would be exerted by the agonist action on kappa receptors, while its Muopioid agonist action would be responsible for its analgesic potential, equivalent to morphine and its lower respiratory depression.5
纳布啡和成瘾:从基础科学到临床设置
阿片类药物是目前控制急性和慢性疼痛的主要治疗方法。在过去三十年中,滥用阿片类药物导致全球成瘾/依赖率和过量死亡人数上升。在美利坚合众国,仅在2016年就造成估计超过64 000人死亡的阿片类药物危机情景被定性为阿片类药物流行病,并被宣布为全国突发公共卫生事件1Nalbuphine (C21H27NO4)是一种合成的kappa受体激动剂阿片和部分Mu受体拮抗剂2,3,它的合成是为了提供镇痛而没有纯激动剂的不良副作用4因此,中枢镇痛作用和较低的纳布啡成瘾/依赖电位将由其对kappa受体的激动剂作用发挥,而其mu阿片激动剂作用将负责其镇痛电位,相当于吗啡及其下呼吸抑制作用
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