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利奈唑胺在烧伤患者中的药代动力学和药效学

Pharmacokinetics and pharmacodynamics of Linezolid in burn patients.

作者信息

Mokline A, Gharsallah L, Rahmani I, Gaies E, Tabelsi S, Messadi A A

机构信息

El Manar Tunis University, Medicine Faculty of Tunis, Tunisia.

Burn Care Department, Burn and Trauma Centre, Tunis, Tunisia.

出版信息

Ann Burns Fire Disasters. 2018 Jun 30;31(2):118-121.

Abstract

Burns induce complex physiological changes such as modification of distribution volume, increased clearance of elements and decrease of protein binding. The pharmacokinetics of many antibiotics may then be modified, which requires dose adjustment. We attempted to evaluate the pharmacokinetics of linezolid in burn patients at a standard dose of 600 mg intravenously thrice a day. A prospective study was conducted in a 20-bed adult burn ICU at a university-affiliated teaching hospital in Tunis. Thirteen adult burned patients with documented and/or suspected multi drug resistant (MDR) gram-positive bacterium-related infections were enrolled in the study. Our study suggests that linezolid dosing at 600mg thrice a day leads to adequate pharmacodynamic/pharmacokinetic exposure to linezolid with a Cmin > 2mg/l in 84.6% of cases, T > MIC in about 87.5% and AUC/MIC > 100 in 61.5% of cases. However, a high variability in linezolid serum concentrations with a substantial percentage of sub-therapeutic levels was observed in a few patients, 15% of cases. Therefore, therapeutic drug monitoring of linezolid might be helpful for adequate dosing of linezolid in burned patients, to avoid the risk of treatment failure or of dose-dependent toxicity.

摘要

烧伤会引发复杂的生理变化,如分布容积改变、元素清除增加以及蛋白结合减少。许多抗生素的药代动力学可能因此发生改变,这就需要调整剂量。我们试图评估静脉注射利奈唑胺标准剂量600毫克、每日三次时在烧伤患者中的药代动力学情况。在突尼斯一所大学附属医院的拥有20张床位的成人烧伤重症监护病房进行了一项前瞻性研究。13例有记录的和/或疑似多重耐药(MDR)革兰氏阳性菌相关感染的成年烧伤患者被纳入研究。我们的研究表明,每日三次给予600毫克利奈唑胺剂量能使患者获得足够的利奈唑胺药效学/药代动力学暴露,84.6%的病例Cmin > 2毫克/升,约87.5%的病例T > MIC,61.5%的病例AUC/MIC > 100。然而,在少数患者(15%的病例)中观察到利奈唑胺血清浓度存在高度变异性,且有相当比例的亚治疗水平。因此,对利奈唑胺进行治疗药物监测可能有助于在烧伤患者中合理给药利奈唑胺,以避免治疗失败或剂量依赖性毒性风险。

相似文献

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Comparison of the pharmacokinetics of linezolid in burn and non-burn rabbits.利奈唑胺在烧伤和非烧伤兔体内的药代动力学比较。
Eur J Drug Metab Pharmacokinet. 2015 Sep;40(3):355-61. doi: 10.1007/s13318-014-0209-6. Epub 2014 Jun 13.

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