Sivilotti Marco L A
Emergency Medicine and Biomedical and Molecular Sciences, Queen's University, Kingston, Ontario.
Ontario Poison Centre, Hospital for Sick Children, Toronto, Ontario, Canada.
Br J Clin Pharmacol. 2016 Mar;81(3):428-36. doi: 10.1111/bcp.12731. Epub 2015 Sep 21.
Flumazenil and naloxone are considered to be pharmacologically ideal antidotes. By competitive binding at the molecular target receptors, they are highly specific antagonists of two important drug classes, the benzodiazepines and opioids, respectively. Both antidotes enjoy rapid onset and short duration after parenteral administration, are easily titrated and are essentially devoid of agonist effects. Yet only naloxone is widely used as a component of the 'coma cocktail', a sequence of empirical treatments to correct altered mental status, while experts discourage the use of flumazenil for such patients. This review contrasts the history, indications, published evidence and novel applications for each antidote in order to explain this disparity in the clinical use of these 'ideal' antidotes.
氟马西尼和纳洛酮被认为是药理学上理想的解毒剂。通过在分子靶受体上竞争性结合，它们分别是两类重要药物——苯二氮䓬类和阿片类药物的高度特异性拮抗剂。两种解毒剂经肠胃外给药后起效迅速且作用持续时间短，易于滴定，且基本没有激动剂效应。然而，只有纳洛酮被广泛用作“昏迷鸡尾酒”的成分之一，这是一系列用于纠正精神状态改变的经验性治疗措施，而专家不鼓励对这类患者使用氟马西尼。本综述对比了每种解毒剂的历史、适应证、已发表的证据和新应用，以解释这些“理想”解毒剂在临床应用上的这种差异。
