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头孢泊肟酯在药代动力学体外模型中的抗菌活性

Antibacterial activity of cefpodoxime proxetil in a pharmacokinetic in-vitro model.

作者信息

Wiedemann B, Jansen A

机构信息

Pharmaceutical Microbiology, Bonn, FRG.

出版信息

J Antimicrob Chemother. 1990 Jul;26(1):71-9. doi: 10.1093/jac/26.1.71.

Abstract

The antibacterial activity of cefpodoxime proxetil was studied in an in-vitro model simulating doses of 100, 200 and 400 mg. Strains of Klebsiella spp. Proteus mirabilis, Escherichia coli, Streptococcus pyogenes, and Haemophilus influenzae were effectively reduced by a dose of 200 mg. While for Esch. coli no dose-activity relationship was observed--the maximal effect was achieved with a simulated dose of 100 mg--Staphylococcus aureus could be reduced effectively only by a simulated dose of 400 mg. The lower doses showed stepwise lower activities. Apart from broad spectrum beta-lactamases like SHV 2 or TEM 5 the presence of plasmid coded beta-lactamases in Esch. coli and H. influenzae did not affect the antibacterial activity of cefpodoxime proxetil. The results show that cefpodoxime was more active against Gram-negative bacteria than amoxycillin, and comparable activity to intramuscular cefotiam in the in-vitro model.

摘要

在一个模拟100、200和400毫克剂量的体外模型中研究了头孢泊肟酯的抗菌活性。200毫克剂量可有效减少肺炎克雷伯菌属、奇异变形杆菌、大肠杆菌、化脓性链球菌和流感嗜血杆菌的菌株数量。虽然对于大肠杆菌未观察到剂量 - 活性关系(模拟剂量为100毫克时达到最大效果),但金黄色葡萄球菌仅在模拟剂量为400毫克时才能有效减少。较低剂量显示出逐步降低的活性。除了SHV-2或TEM-5等广谱β-内酰胺酶外,大肠杆菌和流感嗜血杆菌中质粒编码的β-内酰胺酶的存在并不影响头孢泊肟酯的抗菌活性。结果表明,在体外模型中,头孢泊肟对革兰氏阴性菌的活性比阿莫西林更高,且与肌肉注射头孢替安的活性相当。

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