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纳洛酮

Naloxone.

作者信息

Martin W R

出版信息

Ann Intern Med. 1976 Dec;85(6):765-8. doi: 10.7326/0003-4819-85-6-765.

Abstract

Narcotic analgesics and related drugs act as agonists on several receptors that are responsible for their effects on pain perception, mood and feeling state, and respiration, as well as other pharmacologic actions. Naloxone is the first discovered antagonist that is devoid of agonistic activity and appears to be a competitive antagonist at several receptors. The ability of naloxone to displace or prevent the binding of agonistic narcotics is partly responsible for its antagonistic effects. The ability of naloxone to rectify narcotic-depressed homeostats and precipitate abstinence is also related to its antagonistic activity. Certain cautions and principles apply in the use of naloxone in treating narcotic overdose, reversing surgical analgesia, and the treatment of neonates and children. Unapproved uses of naloxine include reversing the psychotomimetic effects of certain agonists-antagonists, terminating narcotic-induced convulsions and coma, reversing non-narcotic depression, diagnosing physical dependence, and treating narcotic addicts.

摘要

麻醉性镇痛药及相关药物作为激动剂作用于多种受体,这些受体决定了它们对痛觉、情绪和感觉状态、呼吸以及其他药理作用的影响。纳洛酮是首个被发现的无激动活性的拮抗剂,它似乎是多种受体的竞争性拮抗剂。纳洛酮取代或阻止激动性麻醉药结合的能力部分地解释了其拮抗作用。纳洛酮纠正麻醉性抑制的内环境稳定并引发戒断反应的能力也与其拮抗活性有关。在使用纳洛酮治疗麻醉药过量、逆转手术镇痛以及治疗新生儿和儿童时,有一些注意事项和原则需要遵循。纳洛酮的未经批准的用途包括逆转某些激动剂 - 拮抗剂的拟精神病效应、终止麻醉药引起的惊厥和昏迷、逆转非麻醉性抑制、诊断身体依赖性以及治疗麻醉药成瘾者。

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