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克拉维酸增强型阿莫西林:犬体内的体外活性和生物利用度

Clavulanate-potentiated amoxycillin: activity in vitro and bioavailability in the dog.

作者信息

Bywater R J, Palmer G H, Buswell J F, Stanton A

出版信息

Vet Rec. 1985 Jan 12;116(2):33-6. doi: 10.1136/vr.116.2.33.

Abstract

Clavulanic acid is an inhibitor of beta-lactamase (penicillinase) and when used with amoxycillin the resulting combination becomes active against most bacteria resistant to amoxycillin through production of beta-lactamase. A total of 551 bacterial isolates from dogs and cats were examined by disc sensitivity testing, which showed that there was amoxycillin resistance particularly among staphylococci (50 per cent), Klebsiella species (97 per cent) and Escherichia coli (28 per cent). A combination of potassium clavulanate and amoxycillin reduced the incidence of resistance to 0.3, 3 and 7 per cent, respectively. Minimum inhibitory concentrations were determined for a number of the isolates and showed marked reductions in the presence of potassium clavulanate. A formulation containing amoxycillin trihydrate and potassium clavulanate (4:1) was dosed to beagles at 12.5 mg/kg. Concentrations of the drugs in blood, tissue fluid and skin showed that both drugs were sufficiently well absorbed and distributed to allow a prediction of efficacy against infections caused by beta-lactamase producing bacteria.

摘要

克拉维酸是一种β-内酰胺酶(青霉素酶)抑制剂,与阿莫西林合用时,所形成的组合对大多数因产生β-内酰胺酶而对阿莫西林耐药的细菌具有活性。通过纸片扩散法药敏试验对总共551株来自犬猫的细菌分离株进行了检测,结果显示存在阿莫西林耐药情况,尤其是在葡萄球菌(50%)、克雷伯菌属(97%)和大肠杆菌(28%)中。克拉维酸钾与阿莫西林的组合分别将耐药发生率降低至0.3%、3%和7%。对一些分离株测定了最低抑菌浓度,结果显示在有克拉维酸钾存在时显著降低。一种含有三水合阿莫西林和克拉维酸钾(4:1)的制剂以12.5mg/kg的剂量给予比格犬。血液、组织液和皮肤中的药物浓度表明,两种药物均吸收和分布良好,从而可以预测对由产β-内酰胺酶细菌引起的感染的疗效。

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