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Amoxycillin: A new Semi-synthetic Penicillin

机译:阿莫西林:一种新型的半合成青霉素

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摘要

Amoxycillin (α-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 μg or less of amoxycillin/ml. Strains of Haemophilus influenzae were inhibited by a level of 0·5 μg/ml, and most strains of Escherichia coli, Proteus mirabilis, Shigella sonnei, Salmonella species, and Streptococcus faecalis were sensitive to a concentration of 5 μg 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.
机译:阿莫西林(α-氨基-对羟基苄基青霉素)是一种新型的半合成青霉素,具有与氨苄青霉素相似的广谱抗菌活性。对青霉素敏感的葡萄球菌,链球菌和肺炎球菌菌株对阿莫西林/ ml的浓度为0·1μg或更小。流感嗜血杆菌菌株的抑制水平为0·5μg/ ml,大多数大肠杆菌,米氏变形杆菌,痢疾志贺氏菌,沙门氏菌和粪链球菌菌株对浓度为5μg或更低的阿莫西林/ ml敏感。产生青霉素酶的金黄色葡萄球菌菌株和铜绿假单胞菌,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,新青霉素具有杀菌活性,在存在血清的情况下其抗菌活性不会降低。对志愿者受试者口服给药后,阿莫西林产生的血清浓度是类似剂量的氨苄西林所获得的血清浓度的两倍,并且在尿液中的高浓度下,青霉素的回收率保持不变。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浓度的升高和延长。

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