Greenwood D, O'Grady F, Baker P
J Antimicrob Chemother. 1979 Sep;5(5):539-47. doi: 10.1093/jac/5.5.539.
The in vitro efficacy of clavulanic acid, a new broad-spectrum inhibitor of enterobacterial beta-lactamases, was investigated. In conventional agar dilution tests, the presence of a sub-inhibitory level of clavulanic acid (8 microgram/ml) lowered the minimum inhibitory concentration of ampicillin for many resistant enterobacteria to therapeutically achievable levels. When tested against dense populations of Escherichia coli and klebsiella strains in a static turbidimetric system and in an in vitro model of the treatment of bacterial cystitis, clavulanic acid plus ampicillin suppressed bacterial growth for periods far exceeding the normal interdose interval at concentrations at which neither agent alone was effective. In addition to its activity as a beta-lactamase inhibitor, clavulanic acid may interact with other beta-lactam antibiotics in a second, distinct way. Because of this synergic interactions may occur with non-beta-lactamase producing organisms, and the overall synergic effect obtained with beta-lactamase producers may be compounded of two separate elements.
研究了新型广谱肠杆菌β-内酰胺酶抑制剂克拉维酸的体外药效。在传统的琼脂稀释试验中,亚抑制水平的克拉维酸(8微克/毫升)可将许多耐药肠杆菌对氨苄西林的最低抑菌浓度降低至治疗可达到的水平。当在静态比浊法系统中以及在细菌性膀胱炎治疗的体外模型中针对大量大肠杆菌和克雷伯菌菌株进行测试时,克拉维酸加氨苄西林在单独使用任何一种药物均无效的浓度下,抑制细菌生长的时间远远超过正常给药间隔时间。除了作为β-内酰胺酶抑制剂的活性外,克拉维酸可能还以另一种独特的方式与其他β-内酰胺类抗生素相互作用。因此,与非β-内酰胺酶产生菌可能会发生协同相互作用,并且与β-内酰胺酶产生菌获得的总体协同效应可能由两个独立的因素组成。