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奈替米星的生物活性,一种广谱半合成氨基糖苷类抗生素。

Biological activity of netilmicin, a broad-spectrum semisynthetic aminoglycoside antibiotic.

作者信息

Miller G H, Arcieri G, Weinstein M J, Waitz J A

出版信息

Antimicrob Agents Chemother. 1976 Nov;10(5):827-36. doi: 10.1128/AAC.10.5.827.

Abstract

Netilmicin (Sch 20569) is a new broad-spectrum semisynthetic aminoglycoside derived from sisomicin. Netilmicin was compared to gentamicin, tobramycin, and amikacin in a variety of in vitro test systems as well as in mouse protection tests. Netilmicin was found to be similar in activity to gentamicin against aminoglycoside-susceptible strains in both in vitro and in vivo tests. Netilmicin was also active against many aminoglycoside-resistant strains of gram-negative bacteria, particularly those known to possess adenylating enzymes (ANT 2') or those with a similar resistance pattern. Netilmicin was found to be markedly less toxic than gentamicin in chronic studies in cats, although gentamicin appeared less toxic in acute toxicity tests in mice. The concentrations of netilmicin and gentamicin in serum were compared in dogs after intramuscular dosing, and the pharmacokinetics including peak concentrations in serum were found to be similar.

摘要

奈替米星(Sch 20569)是一种新的广谱半合成氨基糖苷类抗生素,由西索米星衍生而来。在多种体外测试系统以及小鼠保护试验中,将奈替米星与庆大霉素、妥布霉素和阿米卡星进行了比较。发现在体外和体内试验中,奈替米星对氨基糖苷类敏感菌株的活性与庆大霉素相似。奈替米星对许多革兰氏阴性菌的氨基糖苷类耐药菌株也有活性,特别是那些已知具有腺苷化酶(ANT 2')或具有类似耐药模式的菌株。在猫的慢性研究中,发现奈替米星的毒性明显低于庆大霉素,尽管在小鼠的急性毒性试验中庆大霉素的毒性似乎较小。在犬肌肉注射给药后,比较了血清中奈替米星和庆大霉素的浓度,发现包括血清峰浓度在内的药代动力学相似。

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本文引用的文献

1
Aspects of the chronic toxicity of gentamicin sulfate in cats.
J Infect Dis. 1971 Dec;124 Suppl:S125-29. doi: 10.1093/infdis/124.supplement_1.s125.
3
Serum protein binding of the aminoglycoside antibiotics.氨基糖苷类抗生素的血清蛋白结合情况。
Antimicrob Agents Chemother. 1972 Sep;2(3):214-6. doi: 10.1128/AAC.2.3.214.

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