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[万古霉素和替考拉宁的比较微生物学及药代动力学活性]

[A comparative microbiological and pharmacokinetic activity of vancomycin and teicoplanin].

作者信息

Cohen R, Barre J, Varon E

机构信息

Service de Microbiologie, Centre Hospitalier Intercommunal, Creteil, France.

出版信息

Pathol Biol (Paris). 1992 Oct;40(8):831-44.

PMID:1484744
Abstract

Vancomycin and teicoplanin are two commercially available glycopeptide antibiotics. They have identical spectra of activity and similar mechanisms of action, and both are complex molecules. In vitro, vancomycin is more active against coagulase-negative staphylococci, while teicoplanin is more active against enterococci and pneumococci. The activity of the two antibiotics against Staphylococcus aureus is similar. The serum pharmacokinetics of vancomycin and teicoplanin are highly different, teicoplanin having a longer elimination half-life (40 hours versus 6-8 hours for vancomycin), but a higher degree of protein binding (90% versus 55%). We compared the two antibiotics on the basis of their inhibitory quotient kinetics, using the MIC90 values for the above bacterial species as the microbiological parameters, and the total and free (non-protein bound) serum concentrations as the pharmacokinetic parameters. The inhibitory quotient kinetics of vancomycin were always more favorable in terms of the free concentrations, even against those bacteria for which the teicoplanin MIC was lower.

摘要

万古霉素和替考拉宁是两种市面上可买到的糖肽类抗生素。它们具有相同的活性谱和相似的作用机制,且都是复杂分子。在体外,万古霉素对凝固酶阴性葡萄球菌的活性更强,而替考拉宁对肠球菌和肺炎球菌的活性更强。这两种抗生素对金黄色葡萄球菌的活性相似。万古霉素和替考拉宁的血清药代动力学有很大差异,替考拉宁的消除半衰期更长(40小时,而万古霉素为6 - 8小时),但蛋白结合程度更高(90%,而万古霉素为55%)。我们以抑制商动力学为基础比较了这两种抗生素,将上述细菌种类的MIC90值作为微生物学参数,将总血清浓度和游离(非蛋白结合)血清浓度作为药代动力学参数。就游离浓度而言,万古霉素的抑制商动力学总是更有利,即使是对替考拉宁MIC较低的那些细菌也是如此。

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