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中国临床药理学与治疗学 ›› 2021, Vol. 26 ›› Issue (11): 1265-1272.doi: 10.12092/j.issn.1009-2501.2021.11.007

• 临床药理学 • 上一篇    下一篇

替加环素在治疗感染性疾病中的群体药代动力学/药效学研究进展

李文超1,2,白向荣1,李晓玲1,姜德春1   

  1. 1首都医科大学宣武医院药学部,国家老年病医学研究中心,北京 100053;2首都医科大学药学院,北京 100053 
  • 收稿日期:2021-02-02 修回日期:2021-08-17 出版日期:2021-11-26 发布日期:2021-12-03
  • 通讯作者: 李晓玲,女,博士,主任药师,主要从事临床药学方向研究。 E-mail: xiaolingxw@126.com 白向荣,男,硕士,副主任药师,主要从事抗感染临床药学方向。 E-mail: xiangrongbai@163.com
  • 作者简介:李文超,女,硕士研究生,主要从事临床药理学方向研究。 E-mail: 158108215982@163.com
  • 基金资助:
    北京市科学技术委员会“老年人多重用药管理模式的建立与临床应用研究”专项资助课题(D181100000218002);北京市卫生和计划生育委员会“老年重大疾病关键技术研究”(PXM2018_026283_000002);北京市属医院科研培育项目(PX2020038)

Population pharmacokinetics/pharmacodynamics of tigecycline in the treatment of different infectious diseases

LI Wenchao 1,2, BAI Xiangrong 1, LI Xiaoling 1, JIANG Dechun 1   

  1. 1 Department of Pharmacy, Xuanwu Hospital, Capital Medical University, National Clinical Research Center for Geriatric Disorders, Beijing 100053, China; 2 School of Pharmacy, Capital Medical University, Beijing 100053, China
  • Received:2021-02-02 Revised:2021-08-17 Online:2021-11-26 Published:2021-12-03

摘要: 目的:为替加环素的临床应用与未来后续群体药代动力学-药效学研究提供参考。方法:以“替加环素”“群体药代动学”“群体药动学模型”“药效学”或“Tigecycline”“pharmacokinetics”等检索词为中英文关键词,在PubMed、中国知网、万方等数据库中组合检索自建库起至2021年6月1日发表的相关文献,对替加环素群体药动学及药效学的研究进展进行综述。结果与结论:共检索到相关文献73篇,其中有效文献8篇,收集到替加环素群体药动学研究8篇,药动学/药效学研究7篇。目前已有研究在复杂腹腔内感染、皮肤与皮肤软组织感染、社区获得性肺炎、医院获得性肺炎、脓毒性休克及其他重症感染患者等群体中建立了替加环素群体药动学模型,其中二室模型8项。影响替加环素血浆清除率的协变量主要为体质量、肝功能与肾功能指标。体质量也是表观分布容积的重要影响因素。不同疾病类型对替加环素药代动力学的影响是不同的,在临床给药方案制定时需要结合患者的具体情况进行考虑和选择。药效学研究除了需考虑疾病类型、病原菌及患者因素本身情况外,也应考虑替加环素非典型非线性血浆蛋白结合情况的特点,为准确了解不同剂量方案下替加环素的疗效,有必要进行治疗药物监测。

关键词: 替加环素, 群体药代动力学, 药效学, 非典型非线性蛋白结合

Abstract: AIM: To provide reference for the clinical application of tigecycline and subsequent population pharmacokinetic-pharmacodynamics study in the future. METHODS: The Chinese and English keywords of "Tigecycline", "population pharmacokinetics", "population pharmacokinetic model", "pharmacodynamics" or "Tigecycline" pharmacokinetics "were used to search the relevant references published from the time of self-establishment to June 1, 2021 in PubMed, China Knowledge Infrastructure, Wanfang and other databases. The research progress of population pharmacokinetics and pharmacodynamics of tigecycline was reviewed. RESULTS & CONCLUSION: A total of 73 relevant references were retrieved, including 8 tigecycline PPK studies and 7 tigecycline PK/PD studies. At present, tigecycline PPK models had been established in patients with complex intra-abdominal infections, skin and skin and soft tissue infections, community-acquired pneumonia, nosocomial pneumonia, septic shock and other severe infections, including 8 two-compartment models. The main covariates affecting tigecycline plasma clearance were weight-related, liver function and renal function-related parameters. Body weight was also an important factor influencing the apparent volume of distribution. The effect of different disease types on the pharmacokinetics of tigecycline was different, and it needed to be considered and selected in combination with the specific circumstances of patients when formulating clinical dosing regimens. Pharmacodynamics studies should consider not only the type of disease, pathogens and patient factors themselves, but also the characteristics of atypical nonlinear plasma protein binding of tigecycline. In order to accurately understand the efficacy of different dose regimens, it was necessary to monitor the therapeutic drugs of tigecycline.

Key words: tigecycline, population pharmacokinetics, pharmacodynamics, atypical nonlinear plasma protein binding

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