O'Kane Aislinn, Quinney Sara K, Kinney Emily, Bergstrom Richard F, Tillman Emma M
Division of Clinical Pharmacology, Department of Medicine, Indiana University School of Medicine, Indianapolis, Indiana, USA.
Riley Hospital for Children, Indianapolis, Indiana, USA.
Clin Transl Sci. 2024 Dec;17(12):e70020. doi: 10.1111/cts.70020.
Dexmedetomidine is a centrally acting alpha-2 agonist used for initiation and maintenance of procedural sedation and mechanical ventilation in adult and pediatric settings. It is commonly used in both pediatric and neonatal intensive care units. Dexmedetomidine requires extensive titration, and patients can be over or under-sedated during titration, leading to adverse events such as hypotension and bradycardia, or inadequate sedation, which can result in self-extubation. There is a critical need to identify factors that contribute to variation in metabolism, clearance, and downstream targets of dexmedetomidine so that individualized pediatric dosing regimens can be developed. This review is focused on dexmedetomidine pharmacokinetics and pharmacodynamics in the pediatric population and dexmedetomidine-related pharmacogenes in both adults and children. We found that the strongest predictors of dexmedetomidine pharmacokinetics were age and size. Multiple pharmacogenes of significance have been identified, including ADRA2A, UGT2B10, UGT1A4, CYP1A2, CYP2A6, and CYP2D6. Evidence is weak for the correlation of these individual polymorphic genes with dexmedetomidine pharmacokinetics/dynamics, though there may be a polygenetic influence on pharmacologic response. This review provides a comprehensive overview of the genomic data gathered to date. We aim to summarize current pharmacologic studies regarding dexmedetomidine use and pharmacology in pediatric patients.
右美托咪定是一种中枢作用的α-2激动剂,用于成人和儿童患者的程序性镇静及机械通气的诱导和维持。它常用于儿科和新生儿重症监护病房。右美托咪定需要进行广泛的滴定,在滴定过程中患者可能镇静过度或不足,从而导致低血压、心动过缓等不良事件,或镇静不足,进而可能导致自行拔管。迫切需要确定导致右美托咪定代谢、清除及下游靶点变异的因素,以便制定个体化的儿科给药方案。本综述聚焦于右美托咪定在儿科人群中的药代动力学和药效学,以及成人和儿童中与右美托咪定相关的药物基因。我们发现,右美托咪定药代动力学的最强预测因素是年龄和体型。已确定多个具有重要意义的药物基因,包括ADRA2A、UGT2B10、UGT1A4、CYP1A2、CYP2A6和CYP2D6。虽然这些单个多态性基因与右美托咪定药代动力学/药效学之间的相关性证据不足,但可能存在多基因对药理反应的影响。本综述全面概述了迄今为止收集的基因组数据。我们旨在总结目前关于右美托咪定在儿科患者中的使用及药理学的研究。