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阿莫西林:一种新型半合成青霉素。

Amoxycillin: a new semi-synthetic penicillin.

作者信息

Sutherland R, Croydon E A, Rolinson G N

出版信息

Br Med J. 1972 Jul 1;3(5817):13-6. doi: 10.1136/bmj.3.5817.13.

DOI:10.1136/bmj.3.5817.13
PMID:4402672
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1788503/
Abstract

Amoxycillin (alpha-amino-p-hydroxybenzylpenicillin) is a new semi-synthetic penicillin with a broad spectrum of antibacterial activity similar to that of ampicillin. Penicillin-sensitive strains of staphylococci, streptococci, and pneumococci were sensitive to concentrations of 0.1 mug or less of amoxycillin/ml. Strains of Haemophilus influenzae were inhibited by a level of 0.5 mug/ml, and most strains of Escherichia coli, Proteus mirabilis, Shigella sonnei, Salmonella species, and Streptococcus faecalis were sensitive to a concentration of 5 mug or less of amoxycillin/ml. Penicillinase-producing strains of Staphylococcus aureus and strains of Pseudomonas aeruginosa, indole-positive Proteus, Klebsiella, and Enterobacter were insensitive to amoxycillin. The new penicillin was bactericidal in activity, as with other penicillins, and its antibacterial activity was not reduced in the presence of serum. After oral administration to volunteer subjects amoxycillin produced serum concentrations twice as high as those obtained with similar doses of ampicillin, and the penicillin was recovered unchanged in high concentrations in the urine. The absorption of amoxycillin was not greatly influenced by food, and administration of probenecid resulted in increased and more prolonged concentrations of amoxycillin in serum.

摘要

阿莫西林(α-氨基-对羟基苄青霉素)是一种新型半合成青霉素,其抗菌谱与氨苄青霉素相似,具有广泛的抗菌活性。对青霉素敏感的葡萄球菌、链球菌和肺炎球菌菌株对浓度为0.1微克/毫升或更低的阿莫西林敏感。流感嗜血杆菌菌株被0.5微克/毫升的浓度所抑制,大多数大肠杆菌、奇异变形杆菌、宋内志贺菌、沙门氏菌属和粪肠球菌菌株对浓度为5微克/毫升或更低的阿莫西林敏感。产青霉素酶的金黄色葡萄球菌菌株以及铜绿假单胞菌、吲哚阳性变形杆菌、克雷伯菌和肠杆菌菌株对阿莫西林不敏感。与其他青霉素一样,这种新型青霉素具有杀菌活性,并且在血清存在的情况下其抗菌活性不会降低。给志愿者口服后,阿莫西林产生的血清浓度是相同剂量氨苄青霉素所产生血清浓度的两倍,并且青霉素在尿液中以高浓度原样回收。食物对阿莫西林的吸收影响不大,丙磺舒的给药导致血清中阿莫西林的浓度升高且持续时间延长。

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本文引用的文献

1
Absorption and excretion of "Penbritin".“青霉素V钾片”的吸收与排泄
Br Med J. 1961 Jul 22;2(5246):198-200. doi: 10.1136/bmj.2.5246.198.
2
Derivatives of 6-aminopenicillanic acid. XI. Alpha-amino-p-hydroxybenzylpenicillin.6-氨基青霉烷酸的衍生物。XI. α-氨基-对羟基苄青霉素。
J Chem Soc Perkin 1. 1971;10:1920-2.
3
The binding of antibiotics to serum proteins.抗生素与血清蛋白的结合。
Br J Pharmacol Chemother. 1965 Dec;25(3):638-50. doi: 10.1111/j.1476-5381.1965.tb01788.x.