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[磺胺类药物/甲氧苄啶联合用药的协同作用及药代动力学研究。IV. 不同磺胺类药物增强甲氧苄啶效果的比较研究及其给药的关键观察(作者译)]

[Studies on synergistic behaviour and pharmacokinetics of the combination sulfonamide/trimethoprim. IV. A comparative study on potentiating the trimethoprim effect by various sulfonamides and critical observations on its dosing (author's transl)].

作者信息

Seydel J K, Wempe E

出版信息

Arzneimittelforschung. 1977;27(8):1521-32.

PMID:334187
Abstract

The maximum possible inhibitory effect of sulfonamide-(SA)-trimethoprim (TMP) combinations on E. coli is obtained with rather small concentrations of SA according to the results obtained with bacterial growth kinetic studies. In these studies the TMP concentration (significantly below the minimum plasma level) was kept constant and the SA concentration varied. An "antagonistic" effect of high SA concentrations on the synergistic effect of the combination and a reduction of the inhibitory effect of TMP has been observed. According to the results of the bacterial growth kinetics obtained with E. coli and pharmacokinetic studies presented, the suggested dose for the combination 2-sulfa-4,5-dimethyl-oxazole/TMP seems to be sufficient, the dosage regimen is correct, whereas the amount of 3-sulfa-5-methyl-isoxazole (SMZ) in the dose proposed for the combination SMZ/TMP seems to be unreasonably high and the dosage scheme is incorrect.

摘要

根据细菌生长动力学研究结果,使用相当低浓度的磺胺类药物(SA)就能获得磺胺类药物(SA)-甲氧苄啶(TMP)组合对大肠杆菌的最大可能抑制作用。在这些研究中,TMP浓度(显著低于血浆最低水平)保持恒定,SA浓度则有所变化。已观察到高浓度SA对该组合协同效应具有“拮抗”作用,并降低了TMP的抑制作用。根据用大肠杆菌进行的细菌生长动力学结果以及所呈现的药代动力学研究,2-磺胺-4,5-二甲基恶唑/TMP组合的建议剂量似乎足够,给药方案正确,而在磺胺甲恶唑(SMZ)/TMP组合建议剂量中3-磺胺-5-甲基异恶唑(SMZ)的量似乎过高且给药方案不正确。

相似文献

1
[Studies on synergistic behaviour and pharmacokinetics of the combination sulfonamide/trimethoprim. IV. A comparative study on potentiating the trimethoprim effect by various sulfonamides and critical observations on its dosing (author's transl)].[磺胺类药物/甲氧苄啶联合用药的协同作用及药代动力学研究。IV. 不同磺胺类药物增强甲氧苄啶效果的比较研究及其给药的关键观察(作者译)]
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2
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Am J Vet Res. 1994 Oct;55(10):1386-90.
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[Lung tissue diffusion of intravenous trimethoprim-sulfamethoxazole combination (author's transl)].
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Trimethoprim-resistant Enterobacteriaceae in urinary tract infection.尿路感染中对甲氧苄啶耐药的肠杆菌科细菌
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Pharmacokinetics and body fluid and endometrial concentrations of trimethoprim-sulfamethoxazole in mares.甲氧苄啶-磺胺甲恶唑在母马体内的药代动力学、体液及子宫内膜浓度
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[Comparison of pharmacokinetics of the combination trimethoprim and sulfamethoxazole in patients with liver diseases and healthy persons].[肝病患者与健康人联用甲氧苄啶和磺胺甲恶唑的药代动力学比较]
Arzneimittelforschung. 1975 Apr;25(4):656-66.

引用本文的文献

1
Development of sulphonamide-trimethoprim combinations for urinary tract infections. Part I: Comparison of the antibacterial effect of sulphonamides alone and in combination with trimethoprim.用于尿路感染的磺胺类药物-甲氧苄啶组合的研发。第一部分:单独使用磺胺类药物及与甲氧苄啶联合使用时的抗菌效果比较。
Infection. 1979;7 Suppl 4:S359-66. doi: 10.1007/BF01639014.
2
Synergistic antibacterial activity in vitro of trimethoprim and sulphonamides and the importance of pharmacokinetic properties for optimal therapy.
Infection. 1979;7 Suppl 4:S313-20. doi: 10.1007/BF01639006.