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蛋白质结合与头孢菌素体内抗菌活性的相关性。

Relevance of protein binding to cephalosporin antimicrobial activity in vivo.

作者信息

Mays B, Short L, Hershman M J, Cheadle W G

机构信息

Department of Surgery, University of Louisville, Ky.

出版信息

Chemotherapy. 1990;36(4):254-8. doi: 10.1159/000238775.

DOI:10.1159/000238775
PMID:2253496
Abstract

Protein binding, serum kinetics and minimum inhibitory concentrations (MICs) for Staphylococcus aureus were determined for cefoxitin, cefazolin, ceftazidime and ceftriaxone in the rabbit. MICs of cefazolin and cefoxitin were also measured for Escherichia coli. Varying concentrations of the bacteria were administered intradermally to create areas of cellulitis, which were quantified as mean erythematous areas (EAs). Despite large differences in protein binding of the antibiotics (range 12-88%) and antibiotic dosing to allow serum concentrations to drop below the respective MICs, there was no statistical difference in the mean EAs of the animals after bacterial challenge. Antibiotic protein binding did not alter the course of cellulitis nor correlate with bacterial MIC in this model.

摘要

在兔体内测定了头孢西丁、头孢唑林、头孢他啶和头孢曲松对金黄色葡萄球菌的蛋白结合率、血清动力学及最低抑菌浓度(MIC)。还测定了头孢唑林和头孢西丁对大肠杆菌的MIC。将不同浓度的细菌皮内注射以造成蜂窝织炎区域,这些区域被量化为平均红斑面积(EA)。尽管抗生素的蛋白结合率差异很大(范围为12%-88%),且给予抗生素剂量以使血清浓度降至各自的MIC以下,但细菌攻击后动物的平均EA没有统计学差异。在该模型中,抗生素蛋白结合并未改变蜂窝织炎的病程,也与细菌MIC无关。

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