氟氯西林，一种新型异恶唑基青霉素，与苯唑西林、氯唑西林和双氯西林进行比较。
Flucloxacillin, a new isoxazolyl penicillin, compared with oxacillin, cloxacillin, and dicloxacillin.
作者信息
Sutherland R, Croydon E A, Rolinson G N
出版信息
Br Med J. 1970 Nov 21;4(5733):455-60. doi: 10.1136/bmj.4.5733.455.
Abstract
Flucloxacillin, a new isoxazole penicillin, is active against penicillinase-producing strains of Staphylococcus aureus and is well absorbed in man after oral and intramuscular administration. Compared with isoxazole penicillins in current clinical use-namely, oxacillin, cloxacillin, and dicloxacillin-flucloxacillin has proved as active against Gram-positive cocci, including penicillin-resistant staphylococci. The extent of binding of flucloxacillin to the protein of human serum was similar to that of oxacillin and cloxacillin and less than that of dicloxacillin. In man flucloxacillin given orally produced total and free serum levels higher than those obtained with oxacillin and cloxacillin; total serum levels similar to those of dicloxacillin, and free levels greater than those of dicloxacillin. Similarly, after intramuscular injection the free serum levels of flucloxacillin were higher than those of oxacillin, cloxacillin, and dicloxacillin.
摘要
氟氯西林是一种新型异恶唑青霉素，对产青霉素酶的金黄色葡萄球菌菌株有活性，口服和肌内注射后在人体内吸收良好。与目前临床使用的异恶唑青霉素（即苯唑西林、氯唑西林和双氯西林）相比，氟氯西林已被证明对革兰氏阳性球菌（包括耐青霉素葡萄球菌）具有同等活性。氟氯西林与人血清蛋白的结合程度与苯唑西林和氯唑西林相似，低于双氯西林。在人体内，口服氟氯西林产生的总血清水平和游离血清水平高于苯唑西林和氯唑西林；总血清水平与双氯西林相似，游离水平高于双氯西林。同样，肌内注射后，氟氯西林的游离血清水平高于苯唑西林、氯唑西林和双氯西林。
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Br Med J. 1970 Nov 21;4(5733):455-60. doi: 10.1136/bmj.4.5733.455.
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本文引用的文献
1
CLOXACILLIN: COMPARISON OF ORAL AND PARENTERAL FORMS WITH OXACILLIN AND METHICILLIN.氯唑西林：口服和注射剂型与苯唑西林和甲氧西林的比较。
Antimicrob Agents Chemother (Bethesda). 1963;161:231-6.
2
EFFECT OF SERUM BINDING ON THE DISTRIBUTION OF PENICILLINS IN THE RABBIT.血清结合对青霉素在兔体内分布的影响。
J Lab Clin Med. 1965 Mar;65:406-15.
3
NATURALLY OCCURING METHICILLIN-RESISTANT STAPHYLOCOCCI.天然存在的耐甲氧西林葡萄球菌
J Gen Microbiol. 1964 May;35:183-90. doi: 10.1099/00221287-35-2-183.
4
CHARACTERISTICS OF METHICILLIN-RESISTANT STAPHYLOCOCCI.耐甲氧西林葡萄球菌的特征
J Bacteriol. 1964 Apr;87(4):887-99. doi: 10.1128/jb.87.4.887-899.1964.
5
A new orally effective penicllinase-stable penicillin--BRL. 1621.一种新型口服有效的对青霉素酶稳定的青霉素——BRL. 1621。
Lancet. 1962 Sep 29;2(7257):632-4. doi: 10.1016/s0140-6736(62)92542-4.
6
[The binding of penicillins on the proteins of the blood and tissues].[青霉素与血液及组织中蛋白质的结合]
Arzneimittelforschung. 1962 Aug;12:741-50.
7
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Nature. 1961 Dec 23;192:1183-4. doi: 10.1038/1921183a0.
8
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Antimicrob Agents Chemother (Bethesda). 1965;5:1016-24.
9
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Med J Aust. 1968 Mar 16;1(11):444-6.
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