Davis Peter J, Cladis Franklyn P
Department of Anesthesiology, University of Pittsburgh School of Medicine, Children's Hospital of Pittsburgh, 3705 Fifth Avenue, Pittsburgh, PA 15213, USA.
Clin Pharmacokinet. 2005;44(8):787-96. doi: 10.2165/00003088-200544080-00002.
Remifentanil is a synthetic opioid that was developed in the early 1990s and introduced into clinical use in 1996. It is a methyl ester and is metabolised by nonspecific tissue and plasma esterases. Consequently, it is a drug that undergoes rapid elimination and has a reported terminal elimination half-life of between 10 and 35 minutes. Because there is no drug accumulation, the context-sensitive half-time remains constant; thus the pharmacokinetics of the drug do not change regardless of the duration of infusion. The organ-independent elimination of remifentanil, coupled with the fact that its clearance is greater in infants and neonates compared with older age groups, make its pharmacokinetic profile different from any other opioid. In addition, its unique metabolism confers predictability in its clinical use. Like other opioid mu receptor agonists, remifentanil provides dose-dependent analgesia, while the adverse effects of this drug, e.g. respiratory depression, are also thought to be dose related. The incidence of nausea and vomiting appear similar to other opioids. Its rapid and consistent metabolism regardless of duration of infusion has made remifentanil an attractive analgesic/anaesthetic option for paediatric care providers.
瑞芬太尼是一种合成阿片类药物，于20世纪90年代初研发，并于1996年引入临床使用。它是一种甲酯，由非特异性组织和血浆酯酶代谢。因此，它是一种消除迅速的药物，据报道其终末消除半衰期在10至35分钟之间。由于没有药物蓄积，其上下文敏感半衰期保持恒定；因此，无论输注持续时间如何，该药物的药代动力学都不会改变。瑞芬太尼不依赖器官的消除，再加上其在婴儿和新生儿中的清除率高于年龄较大的群体，使其药代动力学特征不同于任何其他阿片类药物。此外，其独特的代谢方式使其临床应用具有可预测性。与其他阿片类μ受体激动剂一样，瑞芬太尼提供剂量依赖性镇痛，而该药物的不良反应，如呼吸抑制，也被认为与剂量有关。恶心和呕吐的发生率与其他阿片类药物相似。无论输注持续时间如何，瑞芬太尼都能快速且持续地代谢，这使其成为儿科护理人员有吸引力的镇痛/麻醉选择。
