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舒芬太尼在儿科临床应用中的药代动力学和药效学方面。

Aspects of pharmacokinetics and pharmacodynamics of sufentanil in pediatric practice.

作者信息

Lundeberg Stefan, Roelofse James A

机构信息

Department of Pediatric Anesthesia and Intensive Care, Pain Treatment Service, Astrid Lindgren Children's Hospital, Stockholm, Sweden.

出版信息

Paediatr Anaesth. 2011 Mar;21(3):274-9. doi: 10.1111/j.1460-9592.2010.03411.x. Epub 2010 Sep 16.

Abstract

Sufentanil is a potent synthetic opioid. Like other opioids, sufentanil creates a stable hemodynamic environment in cardiovascularly compromised pediatric patients. Clearance, expressed as per kilogram, is increased in children compared to adults. The P450 CYP3A4 enzyme is responsible for the major metabolic N-dealkylation pathway. Enzyme activity is reduced in neonates but the maturation of sufentanil clearance is not described. The free active fraction is affected by age because of the reduced α(1) -acid glycoprotein plasma concentrations in neonates. Intranasal administration of sufentanil is a possible option for premedication, procedural sedation and analgesia in children, as this option has been found to be safe and effective. Studies concerning the pharmacokinetics and dynamics of sufentanil administered as a bolus or continuous infusion in children are few.

摘要

舒芬太尼是一种强效合成阿片类药物。与其他阿片类药物一样,舒芬太尼能在心血管功能受损的儿科患者中创造稳定的血流动力学环境。以每千克计算的清除率在儿童中比成人更高。P450 CYP3A4酶负责主要的代谢N-脱烷基途径。新生儿的酶活性降低,但舒芬太尼清除率的成熟情况未作描述。由于新生儿血浆中α(1)-酸性糖蛋白浓度降低,游离活性部分受年龄影响。鼻内给予舒芬太尼是儿童术前用药、程序性镇静和镇痛的一种可能选择,因为已发现这种选择是安全有效的。关于以推注或持续输注方式给予舒芬太尼在儿童中的药代动力学和药效学的研究很少。

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