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Dextromethorphan/levomethorphan issues in a case of opiate overdose

机译:鸦片过量时右美沙芬/左美沙芬的问题

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Dextromethorphan is the c/-isomer of 3-methoxy-N-methylmorphinan (methorphan), a synthetic analogue of codeine. It interacts with the a-opioid receptors with resulting antitussive activity, while it does not show any significant affinity for the i and 8 opioid receptors, which are responsible for analgesic and central nervous system depressant effects. On this basis, d-methorphan is widely used all over the world as an over-the-counter cough suppressant drug. Indeed, there are hundreds of cough and cold preparations containing d-methorphan alone or in combination with analgesic (acetaminophen, acetyl salicylic acid), decongestant (phenylephrine, pseudoephedrine), anthistaminic (chlorpheniramine, brompheniramine, pheniramine), and/or expectorant mucolytic agents. In large doses, d-methorphan and its metabolite dextrorphan antagonize the actions of excitatory amino acids on N-methyl-d-aspartate (NMDA) receptors as do phencyclidine and ketamine.
机译:右美沙芬是可待因的合成类似物3-甲氧基-N-甲基吗啡喃(美沙芬)的顺式异构体。它与α-阿片样物质受体相互作用,产生镇咳活性,但对 i和8类阿片样物质受体没有明显的亲和力,后者负责镇痛和中枢神经系统抑制作用。在此基础上,d-美沙芬在世界范围内广泛用作非处方止咳药。实际上,有数百种咳嗽和感冒药,它们单独或与镇痛药(对乙酰氨基酚,乙酰水杨酸),去充血药(去氧肾上腺素,伪麻黄碱),驱虫药(扑尔敏,氯苯那敏,溴苯那敏,苯那敏)和/或祛痰粘液溶解剂合用。大剂量时,d-美沙芬及其代谢产物右啡烷与苯环利定和氯胺酮一样,拮抗兴奋性氨基酸对N-甲基-d-天冬氨酸(NMDA)受体的作用。

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