Lukas Gorecki , Jaroslav Pejchal , Carilyn Torruellas , Jan Korabecny , Ondrej Soukup
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引用次数: 0
摘要
自 20 世纪 60 年代以来,苯二氮卓类药物地西泮一直是治疗神经毒剂(毒性最强的大规模杀伤性化学武器)引起的癫痫发作的主要解毒剂。然而,它的局限性常常让人质疑其效用。人们投入了大量精力探索替代品,如其他苯二氮卓类药物、抗胆碱能药物或谷氨酸拮抗剂。然而,只有少数药物显示出明显的临床疗效。最终达到临床里程碑的只有两种选择,一种是法国和英国军队采用的地西泮水溶性原药 Avizafone,另一种是美国军队采用的肌肉注射咪达唑仑。最近获得 FDA 批准的咪达唑仑肌肉注射新药具有多种优势,如起效迅速、持续时间短且药代动力学可预测、水溶性注射液的水溶性增加以及储存稳定性延长。在此,我们讨论了在抗惊厥治疗中使用咪达唑仑作为替代品的隐患和前景,尤其侧重于作战伤员护理中的军事用途。我们还考虑并讨论了目前处于实验阶段的其他几种替代品。最近的研究表明,在对中毒伤员进行医疗处理时,咪达唑仑比其他苯二氮卓类药物更有优势。虽然咪达唑仑在急救中的使用简单明了,但由于其镇静作用,在战场条件下对士兵使用的适当剂量却值得商榷。
Midazolam - A diazepam replacement for the management of nerve agent-induced seizures
A benzodiazepine, diazepam, has been the leading antidote for seizures caused by nerve agents, the most toxic chemical weapons of mass destruction, since the 1960s. However, its limitations have often brought questions about its usefulness. Extensive effort has been devoted into exploring alternatives, such as other benzodiazepines, anticholinergics, or glutamate antagonists. However, only few showed clear clinical benefit. The only two options to ultimately reach clinical milestones are Avizafone, a water-soluble prodrug of diazepam adopted by the French and UK armed forces, and intramuscular midazolam, adopted by the US Army. The recently FDA-approved new intramuscular application of midazolam brought several advantages, such as rapid onset of action, short duration with predictable pharmacokinetics, increased water solubility for aqueous injectable solutions, and prolonged storage stability. Herein, we discuss the pitfalls and prospects of using midazolam as a substitute in anticonvulsant therapy with a particular focus on military purposes in combat casualty care. We have also considered and discussed several other alternatives that are currently at the experimental level. Recent studies have shown the superiority of midazolam over other benzodiazepines in the medical management of poisoned casualties. While its use in emergency care is straightforward, the proper dose for soldiers under battlefield conditions is questionable due to its sedative effects.
期刊介绍:
Neuropharmacology publishes high quality, original research and review articles within the discipline of neuroscience, especially articles with a neuropharmacological component. However, papers within any area of neuroscience will be considered. The journal does not usually accept clinical research, although preclinical neuropharmacological studies in humans may be considered. The journal only considers submissions in which the chemical structures and compositions of experimental agents are readily available in the literature or disclosed by the authors in the submitted manuscript. Only in exceptional circumstances will natural products be considered, and then only if the preparation is well defined by scientific means. Neuropharmacology publishes articles of any length (original research and reviews).