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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.

DOI:10.1159/000237837
PMID:256524
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。

相似文献

1
Comparative activities of ampicillin, epicillin and amoxycillin in vitro and in vivo.氨苄西林、依匹西林和阿莫西林的体外及体内比较活性
Chemotherapy. 1979;25(3):170-80. doi: 10.1159/000237837.
2
Amoxycillin: a new semi-synthetic penicillin.阿莫西林:一种新型半合成青霉素。
Br Med J. 1972 Jul 1;3(5817):13-6. doi: 10.1136/bmj.3.5817.13.
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Comparative effects of amoxycillin and ampicillin in the treatment of experimental mouse infections.阿莫西林与氨苄西林治疗实验性小鼠感染的对比效果
Antimicrob Agents Chemother. 1975 Feb;7(2):179-85. doi: 10.1128/AAC.7.2.179.
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Comparative effects of amoxycillin and ampicillin on the morphology of Escherichia coli in vivo and correlation with activity.阿莫西林和氨苄西林对体内大肠杆菌形态的比较作用及其与活性的相关性
Antimicrob Agents Chemother. 1977 Dec;12(6):736-44. doi: 10.1128/AAC.12.6.736.
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Augmentin: laboratory studies.阿莫西林克拉维酸钾:实验室研究。
Scott Med J. 1982;27 Spec No.:S21-3. doi: 10.1177/00369330820270S105.
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Comparative in vivo activity of bacampicillin and amoxycillin.巴卡西林与阿莫西林的体内活性比较
Infection. 1979;7 Suppl 5:S438-42. doi: 10.1007/BF01659766.
7
Comparative activity of amoxycillin and ampicillin in an experimental bacterial infection in mice.阿莫西林与氨苄西林在小鼠实验性细菌感染中的活性比较
Antimicrob Agents Chemother. 1973 Sep;4(3):285-93. doi: 10.1128/AAC.4.3.285.
8
Evaluation of amino penicillins in experimental infections in mice.氨基青霉素在小鼠实验性感染中的评估。
Scand J Infect Dis Suppl. 1978(14):207-13.
9
Epicillin: in vitro laboratory studies.埃匹西林:体外实验室研究。
Infect Immun. 1971 Jul;4(1):44-9. doi: 10.1128/iai.4.1.44-49.1971.
10
Antibacterial activity and synergy, in vitro and in vivo, of a combination of amoxycillin and flucloxacillin.
Chemotherapy. 1979;25(1):30-9. doi: 10.1159/000237819.

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J Clin Microbiol. 2014 Feb;52(2):624-6. doi: 10.1128/JCM.02374-13. Epub 2013 Nov 13.
2
Simultaneous pharmacodynamic analysis of the lag and bactericidal phases exhibited by beta-lactams against Escherichia coli.β-内酰胺类药物对大肠杆菌的迟滞期和杀菌期的同步药效学分析
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Bacterial kill rates of amoxycillin and ampicillin at exponentially diminishing concentrations simulating in vivo conditions.
在模拟体内条件下,阿莫西林和氨苄西林在指数递减浓度时的细菌杀灭率。
Infection. 1980;Suppl 1:103-8. doi: 10.1007/BF01644943.
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An in vitro model for monitoring bacterial responses to antibiotic agents under simulated in vivo conditions.一种用于在模拟体内条件下监测细菌对抗生素药物反应的体外模型。
Infection. 1980;Suppl 1:096-10. doi: 10.1007/BF01644942.
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The in vitro activity of ampicillin, amoxicillin, cephalexin, nitrofurantoin, sulphadiazine and trimethoprim against Streptococcus agalactiae isolated from urinary and other infections.氨苄西林、阿莫西林、头孢氨苄、呋喃妥因、磺胺嘧啶和甲氧苄啶对从泌尿系统及其他感染中分离出的无乳链球菌的体外活性。
Infection. 1982 Sep-Oct;10(5):299-302. doi: 10.1007/BF01640879.