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本文引用的文献

1
Development of a sensitive LC-MS/MS method for quantification of linezolid and its primary metabolites in human serum.建立一种灵敏的 LC-MS/MS 方法,用于定量人血清中的利奈唑胺及其主要代谢物。
J Pharm Biomed Anal. 2020 Jan 30;178:112968. doi: 10.1016/j.jpba.2019.112968. Epub 2019 Nov 5.
2
Therapeutic Drug Monitoring Can Improve Linezolid Dosing Regimens in Current Clinical Practice: A Review of Linezolid Pharmacokinetics and Pharmacodynamics.治疗药物监测可改善当前临床实践中的利奈唑胺给药方案:利奈唑胺药代动力学和药效学综述。
Ther Drug Monit. 2020 Feb;42(1):83-92. doi: 10.1097/FTD.0000000000000710.
3
Linezolid Dosing in Patients With Liver Cirrhosis: Standard Dosing Risk Toxicity.利奈唑胺在肝硬化患者中的剂量:标准剂量有中毒风险。
Ther Drug Monit. 2019 Dec;41(6):732-739. doi: 10.1097/FTD.0000000000000665.
4
Reappraisal of Linezolid Dosing in Renal Impairment To Improve Safety.重新评估肾功能损害患者中利奈唑胺的剂量以提高安全性。
Antimicrob Agents Chemother. 2019 Jul 25;63(8). doi: 10.1128/AAC.00605-19. Print 2019 Aug.
5
Measurement of Linezolid and Its Metabolites PNU-142300 and PNU-142586 in Human Plasma Using Ultra-Performance Liquid Chromatography Method.采用超高效液相色谱法测定人血浆中利奈唑胺及其代谢物PNU - 142300和PNU - 142586。
Chem Pharm Bull (Tokyo). 2019;67(5):439-444. doi: 10.1248/cpb.c18-00840.
6
Evaluation of hematological alterations after therapeutic use of dipyrone in healthy adults: a prospective study.健康成年人治疗性使用安乃近后血液学改变的评估:一项前瞻性研究。
J Basic Clin Physiol Pharmacol. 2018 Jul 26;29(4):385-390. doi: 10.1515/jbcpp-2017-0037.
7
Thrombocytopenia with Tedizolid and Linezolid.替加环素和利奈唑胺相关血小板减少症。
Antimicrob Agents Chemother. 2017 Dec 21;62(1). doi: 10.1128/AAC.01453-17. Print 2018 Jan.
8
Synthesis of Linezolid Metabolites PNU-142300 and PNU-142586 toward the Exploration of Metabolite-Related Events.利奈唑胺代谢物PNU - 142300和PNU - 142586的合成以探索与代谢物相关的事件。
Chem Pharm Bull (Tokyo). 2017;65(2):194-199. doi: 10.1248/cpb.c16-00831.
9
Linezolid: a promising option in the treatment of Gram-positives.利奈唑胺:治疗革兰氏阳性菌的有前途的选择。
J Antimicrob Chemother. 2017 Feb;72(2):354-364. doi: 10.1093/jac/dkw450. Epub 2016 Dec 20.
10
Drug monitoring and individual dose optimization of antimicrobial drugs: oxazolidinones.抗菌药物的药物监测与个体化剂量优化:恶唑烷酮类
Expert Opin Drug Metab Toxicol. 2016 May;12(5):533-44. doi: 10.1517/17425255.2016.1166204. Epub 2016 Mar 28.

肾功能损害患者中主要利奈唑胺代谢物的蓄积。

Accumulation of Major Linezolid Metabolites in Patients with Renal Impairment.

机构信息

Department of Clinical Pharmacy, College of Pharmacy, University of Michigan, Ann Arbor, Michigan, USA.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Michigan, Ann Arbor, Michigan, USA.

出版信息

Antimicrob Agents Chemother. 2020 Apr 21;64(5). doi: 10.1128/AAC.00027-20.

DOI:10.1128/AAC.00027-20
PMID:32152085
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7179609/
Abstract

In patients with renal impairment ( = 22 of 39), the median serum concentrations of linezolid, PNU-142300, and PNU-142586 were 1.6-, 3.3-, 2.8-fold higher, respectively, than in patients without renal impairment. Metabolite concentrations in paired samples were poorly correlated with linezolid concentrations ( = 0.26 for PNU-142300 and 0.06 for PNU-142586). Linezolid and its metabolites share potential toxicophores that deserve characterization to mitigate higher myelosuppression risk in patients with renal impairment.

摘要

在肾功能不全的患者中( = 39 例中的 22 例),与肾功能正常的患者相比,利奈唑胺、PNU-142300 和 PNU-142586 的血清浓度中位数分别高出 1.6 倍、3.3 倍和 2.8 倍。配对样本中的代谢物浓度与利奈唑胺浓度相关性较差(PNU-142300 为 = 0.26,PNU-142586 为 = 0.06)。利奈唑胺及其代谢物具有潜在的毒性作用基团,值得进一步研究以降低肾功能不全患者的骨髓抑制风险。