利奈唑胺在重症感染患者中的药动学

目的:研究重症感染患者静脉滴注和鼻饲2种不同给药途经下利奈唑胺的药动学特点。方法:本研究为前瞻性研究,2013年8月-2014年3月使用利奈唑胺治疗的6例ICU患者,根据给药途径不同,分为静脉滴注组4例,鼻饲管给药组2例,2组均给予利奈唑胺600 mg/q12h,于给药后第5天的0,0.5,1,2,3,4,6,8,12 h采取静脉血1 mL,监测利奈唑胺的血药浓度。结果:6例患者的C_min变化范围为3.59~19.82 μg·mL^-1,其中2例超过了安全临界值10 μg·mL^-1,AUC_{0-12 h}变化范围为116.7~305.5 μg·h^-1·mL^-1,C_min与AUC_{0-12 h}具有很强的相关性(r=0.997,P=0.001)。结论:重症感染患者利奈唑胺药动学参数个体差异较大,应根据PK/PD相关参数制定合理的给药方案,预防细菌耐药,保证临床治疗效果,减少不良反应。

Pharmacokinetics of linezolid in critically ill patients

OBJECTIVE To compare pharmacokinetics of linezolid by nasogastric and intravenous administration in critically ill patients from intensive care unit.METHODS A prospective study was conducted between August 2013 and March 2014 and 6 patients administered of linezolid were included. The drug was administered in two patients by nasogastric route and four patients by intravenous route. Patients of both groups were all given 600 mg twice daily, blood specimens were collected at zero (prior to dosing), 0.5, 1, 2, 3, 4, 6, 8, 12 after dosing at day 5. Plasma concentrations of linezolid were monitored.RESULTS Trough concentration range of 6 patients was 3.59-19.82 μg·mL^-1, two of them were above the safe value (<10 μg·mL^-1). AUC_{0-12 h} range was 116.7-305.5 μg·h^-1·mL^-1. Trough plasma concentration was positively correlated with AUC_{0-12 h} (r=0.997, P=0.001).CONCLUSION A high variability of linezolid plasma concentrations is observed in intensively cared patients. To prevent bacterial resistance, ensure clinical outcome and reduce adverse reactions, pharmacokinetics/pharmacodynamics of linezolid should be monitored to develop individualized regimen of linezolid in clinical practice.