Scheckenbach Vera, Fideler Frank
Department of Anesthesiology and Intensive Care Medicine, University Hospital Tübingen, Eberhard Karls University Tübingen, Hoppe-Seyler Str. 3, 72076, Tübingen, Germany.
Paediatr Drugs. 2025 Mar;27(2):181-189. doi: 10.1007/s40272-024-00659-1. Epub 2024 Nov 1.
Daily, children undergo countless investigations and interventions, which require sedation and immobilization to ensure safety and accuracy. This remains associated with a persistent risk of sedation-induced life-threatening events as children are particularly vulnerable to adverse medical events and complications. Consequently, there is an urgent need to increase the safety of pediatric sedation and anesthesia. An ideal approach involves the use of drugs with fewer intrinsic side effects. In this context, on the basis of their pharmacokinetic properties, remimazolam (RMZ) and dexmedetomidine (DEX) were evaluated for their suitability as ideal sedatives. RMZ and DEX, both of which are currently available in pediatric medicine, have shown great promise in initial publications. To date, only very limited data concerning RMZ in small children are available. RMZ is a novel, ultrashort-acting benzodiazepine that is metabolized by tissue esterase, largely independent of organ function. It has a context-sensitive half-life of approximately 10 min, with minimal accumulation even with prolonged use. Its effects can be completely reversed with flumazenil. DEX, an isomer of medetomidine, is a potent α2-receptor-agonist with multiple indications in anesthesia and intensive care medicine. It has coanalgesic potential, allows for 'arousal sedations' and has a low profile for cardiorespiratory side effects. DEX is metabolized in the liver and is predominantly excreted renally. Both drugs show potential in the prevention and treatment of delirium, with DEX having additional neuroprotective effects. DEX and RMZ possess several properties of an optimal sedative, including clinically insignificant main metabolites and a broad dosage range, indicating their potential to reduce the incidence of sedation-related life-threatening events in children. However, further clinical research is necessary to better evaluate their potential risks.
儿童每天都要接受无数的检查和干预措施，这需要进行镇静和制动以确保安全与准确性。由于儿童特别容易发生不良医疗事件和并发症，这仍然与镇静诱导的危及生命事件的持续风险相关。因此，迫切需要提高儿科镇静和麻醉的安全性。一种理想的方法是使用内在副作用较少的药物。在此背景下，基于其药代动力学特性，对瑞马唑仑（RMZ）和右美托咪定（DEX）作为理想镇静剂的适用性进行了评估。RMZ和DEX目前都已应用于儿科医学，在初步发表的文献中显示出巨大的前景。迄今为止，关于幼儿使用RMZ的可用数据非常有限。RMZ是一种新型超短效苯二氮䓬类药物，通过组织酯酶代谢，很大程度上不依赖器官功能。其上下文敏感半衰期约为10分钟，即使长期使用积累也极少。其作用可用氟马西尼完全逆转。DEX是美托咪定的异构体，是一种强效α2受体激动剂，在麻醉和重症医学中有多种适应症。它具有协同镇痛作用，可实现“唤醒镇静”，且心肺副作用较少。DEX在肝脏中代谢，主要经肾脏排泄。两种药物在预防和治疗谵妄方面均显示出潜力，DEX还具有额外的神经保护作用。DEX和RMZ具有几种理想镇静剂的特性，包括临床意义不大的主要代谢产物和较宽的剂量范围，表明它们有可能降低儿童镇静相关危及生命事件的发生率。然而，需要进一步的临床研究来更好地评估它们的潜在风险。
