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比阿培南药动学/药效学和治疗药物监测的研究进展
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陶兴隆 ,张 宇 ,武玺坤 ,马晓松 ,张甜甜 ,吴 瑕 ,董维冲 ,宋 宁 ,张志清 (1.河北医科大学第二医院
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药学部,石家庄 050200;2.河北医科大学第二医院感染性疾病科,石家庄 050200;3.河北医科大学第二医院
预防保健处,石家庄 050200)
中图分类号 R969;R978.1 文献标志码 A 文章编号 1001-0408(2023)15-1915-06
DOI 10.6039/j.issn.1001-0408.2023.15.23
摘 要 比阿培南是一种碳青霉烯类抗菌药物,用于治疗败血症、肺炎、肺脓肿、慢性呼吸道病变继发感染、复杂尿路感染、肾盂肾
炎等疾病。本文对比阿培南药动学、药效学和治疗药物监测(TDM)方面的研究进行了综述,发现该药的药动学参数在健康受试
者中无明显差异,多次给药无蓄积,但在重症患者以及肾功能异常患者中的药动学参数与健康受试者相比存在较大差异,导致常
规治疗方案不能达到预期效果。在药效学方面,可通过增加给药频次、延长滴注时间来提高该药靶目标值的达标率;对于终末期
肾病无尿患者的给药,可以延长间隔时间以避免药物蓄积;但对于重症感染患者,每日1.2 g的剂量仍不能很好地控制鲍曼不动杆
菌、铜绿假单胞菌引起的感染,这限制了其在重症患者中的应用。建议在重症或肾功能异常患者中对该药实施TDM并结合药动
学模型探索最佳的给药方案,以保证该药游离血药浓度保持在最低抑菌浓度以上的时间占给药间隔时间的百分比(%fT>MIC)
在有效范围内,使该药在重症或肾功能异常患者中发挥更大疗效;对于无法进行TDM的医疗机构,可通过增加给药频次和延长滴
注时间来使该药疗效最大化;针对耐药率较高的铜绿假单胞菌、鲍曼不动杆菌及黏质沙雷菌引起的感染,可联合或者更换其他抗
菌药物进行治疗。
关键词 比阿培南;药动学;药效学;治疗药物监测
Research progress in pharmacokinetics/pharmacodynamics and therapeutic drug monitoring of biapenem
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TAO Xinglong ,ZHANG Yu ,WU Xikun ,MA Xiaosong ,ZHANG Tiantian ,WU Xia ,DONG Weichong ,
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SONG Ning ,ZHANG Zhiqing (1. Dept. of Pharmacy, the Second Hospital of Hebei Medical University,
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Shijiazhuang 050200, China;2. Dept. of Infectious Diseases, the Second Hospital of Hebei Medical University,
Shijiazhuang 050200, China;3. Dept. of Preventive Health Care, the Second Hospital of Hebei Medical
University, Shijiazhuang 050200, China)
ABSTRACT Biapenem is a carbapenem antibiotic, and can be used for the treatment of sepsis, pneumonia, lung abscess,
chronic respiratory lesions secondary infection, complex urinary tract infection and pyelonephritis, etc. This article reviewed the
studies on the pharmacokinetics, pharmacodynamics and therapeutic drug monitoring (TDM) of biapenem. The pharmacokinetic
parameters of biapenem are not significantly different in healthy subjects, and there is no accumulation after multiple doses of
biapenem. However, there are large differences in pharmacokinetic parameters in patients with severe disease and patients with
abnormal renal function compared with healthy subjects, which leads to conventional treatment regimens not achieving the desired
outcome. In terms of pharmacodynamics, biapenem can improve the rate of reaching the target value by increasing the frequency of
administration and prolonging the infusion time. For patients with anuria in end-stage renal disease, dosing intervals can be
extended to avoid drug accumulation. However, for patients with severe infection, a daily dose of 1.2 g still can not control
infections caused by Acinetobacter baumannii or Pseudomonas aeruginosa, which limits its use in patients with severe disease. It is
recommended to implement TDM in severe patients and patients with abnormal renal function, and explore the best dosing regimen
for biapenem in combination with pharmacokinetic models to ensure that the time that the free blood concentration of biapenem
remains above minimum inhibitory concentration as a percentage of the time between doses (%fT>MIC) is within the effective
range,so that biapenem can exert a greater efficacy in severe patients and patients with abnormal renal function. For medical
institutions that cannot carry out TDM, the efficacy of biapenem can be maximized by increasing the frequency of administration
and prolonging the infusion time. For infections caused by P.
Δ 基金项目 北京医卫健康公益基金会医学科学研究基金项目 aeruginosa, A. baumannii and Serratia marcescens with high
(No.YWJKJJHKYJJ-ZLTC2301) drug resistance rates, it is recommended to combine or replace
*第一作者 主管药师,硕士。研究方向:临床药学、药动学、药物
other antibiotics.
相互作用。E-mail:long2273985@126.com
# 通信作者 主任药师,硕士生导师,博士。研究方向:临床药学、 KEYWORDS biapenem;pharmacokinetics; pharmacodyna-
药理学、药物新制剂。E-mail:zhangzhq@medmail.com.cn mics; therapeutic drug monitoring
中国药房 2023年第34卷第15期 China Pharmacy 2023 Vol. 34 No. 15 · 1915 ·