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头孢他啶和拉氧头孢的比较药代动力学

Comparative pharmacokinetics of ceftazidime and moxalactam.

作者信息

Tjandramaga T B, Van Hecken A, Mullie A, Verbesselt R, De Schepper P J, Verbist L

出版信息

Antimicrob Agents Chemother. 1982 Aug;22(2):237-41. doi: 10.1128/AAC.22.2.237.

DOI:10.1128/AAC.22.2.237
PMID:6765416
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC183718/
Abstract

The pharmacokinetics of ceftazidime and moxalactam were compared after intravenous and intramuscular administration of single 1-g doses to eight healthy volunteers in a crossover study. The bioavailability of the antibiotics after administration by either route was almost complete. Both drugs had similar areas under the serum curves. Significant differences between ceftazidime and moxalactam were observed with respect to the apparent volume of distribution (18.4 and 24.1 liters, respectively), to the terminal half-life (1.6 versus 2.0 h), and to urinary recovery of the active compound (96 versus 79%). Ceftazidime was almost completely eliminated by renal excretion (greater than 96%), whereas about 20% of the moxalactam was eliminated by nonrenal mechanisms. The concentrations of ceftazidime and moxalactam in serum after a 1-g dose exceeded the concentrations required to inhibit 90% of the Enterobacteriaceae for about 8 and 10 h, respectively. The levels of ceftazidime and moxalactam in serum exceeded the 90% minimal inhibitory concentration of Pseudomonas aeruginosa for about 6 and 1 h, respectively.

摘要

在一项交叉研究中,对8名健康志愿者单次静脉注射和肌肉注射1克剂量的头孢他啶和拉氧头孢的药代动力学进行了比较。两种给药途径后抗生素的生物利用度几乎是完全的。两种药物的血清曲线下面积相似。在表观分布容积(分别为18.4升和24.1升)、终末半衰期(1.6小时对2.0小时)以及活性化合物的尿回收率(96%对79%)方面,观察到头孢他啶和拉氧头孢之间存在显著差异。头孢他啶几乎完全通过肾脏排泄消除(超过96%),而约20%的拉氧头孢通过非肾脏机制消除。1克剂量后血清中头孢他啶和拉氧头孢的浓度分别超过抑制90%肠杆菌科细菌所需浓度约8小时和10小时。血清中头孢他啶和拉氧头孢的水平分别超过铜绿假单胞菌90%最小抑菌浓度约6小时和1小时。

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本文引用的文献

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GR 20263, a new broad-spectrum cephalosporin with anti-pseudomonal activity.GR 20263,一种具有抗假单胞菌活性的新型广谱头孢菌素。
Antimicrob Agents Chemother. 1980 May;17(5):876-83. doi: 10.1128/AAC.17.5.876.
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GR-20263: a new aminothiazolyl cephalosporin with high activity against Pseudomonas and Enterobacteriaceae.GR - 20263:一种对假单胞菌属和肠杆菌科具有高活性的新型氨基噻唑基头孢菌素。
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Moxalactam and cefazolin: comparative pharmacokinetics in normal subjects.羟羧氧酰胺菌素和头孢唑林:正常受试者体内的比较药代动力学
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Comparison of cefotaxime and moxalactam pharmacokinetics and tissue levels.头孢噻肟与拉氧头孢的药代动力学及组织浓度比较。
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Assessment of pharmacokinetic constants from postinfusion blood curves obtained after I.V. infusion.通过静脉输注后获得的输注后血药浓度曲线评估药代动力学常数。
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Piperacillin: human pharmacokinetics after intravenous and intramuscular administration.哌拉西林:静脉注射和肌肉注射后的人体药代动力学
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