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氨苄西林、依匹西林和阿莫西林的体外及体内比较活性

Comparative activities of ampicillin, epicillin and amoxycillin in vitro and in vivo.

作者信息

Basker M J, Gwynn M N, White A R

出版信息

Chemotherapy. 1979;25(3):170-80. doi: 10.1159/000237837.

Abstract

The antibacterial activities of three aminopenicillins ampicillin, epicillin and amoxycillin were compared in vitro and in vivo. The minimum inhibitory concentrations (MIC) of the three penicillins were very similar and the compounds were active against non-beta-lactamase-producing strains of Escherichia coli, Salmonella and Shigella species, Proteus mirabilis, Haemophilus influenzae and Neisseria gonorrhoeae. Streptococci including Streptococcus faecalis, and non-beta-lactamase-producing staphylococci were also sensitive to the compounds but Pseudomonas aeruginosa, Klebsiella aerogenes, Enterobacter and indole-positive Proteus species were resistant. At concentrations close to MIC value epicillin and ampicillin showed similar bactericidal activity against E. coli and against S. typhi and both compounds caused a slower rate of kill than was seen with amoxycillin. Microscopical observation of the cells exposed to ampicillin and epicillin for 1 h showed the presence of filamentous forms which lysed slowly, whereas cells exposed to amoxycillin for the same period rapidly. Epicillin was similar to or slightly less active than ampicillin against experimental mouse infections, and against the majority of infections both compounds were significantly less effective than amoxycillin by the oral and subcutaneous routes of administration.

摘要

对三种氨基青霉素(氨苄西林、依匹西林和阿莫西林)的体外和体内抗菌活性进行了比较。这三种青霉素的最低抑菌浓度(MIC)非常相似,且这些化合物对不产β-内酰胺酶的大肠杆菌、沙门氏菌和志贺氏菌属、奇异变形杆菌、流感嗜血杆菌和淋病奈瑟菌具有活性。包括粪肠球菌在内的链球菌以及不产β-内酰胺酶的葡萄球菌对这些化合物也敏感,但铜绿假单胞菌、产气克雷伯菌、肠杆菌和吲哚阳性变形杆菌属具有抗性。在接近MIC值的浓度下,依匹西林和氨苄西林对大肠杆菌和伤寒沙门氏菌显示出相似的杀菌活性,且这两种化合物的杀菌速度均比阿莫西林慢。对暴露于氨苄西林和依匹西林1小时的细胞进行显微镜观察发现存在丝状形态,其溶解缓慢,而同期暴露于阿莫西林的细胞则迅速溶解。在实验性小鼠感染中,依匹西林的活性与氨苄西林相似或略低于氨苄西林,且对于大多数感染,通过口服和皮下给药途径,这两种化合物的效果均明显低于阿莫西林。

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