Bergan T, Carlsen I B
Infection. 1980;Suppl 1:103-8. doi: 10.1007/BF01644943.
The responses of bacteria exposed to amoxycillin and ampicillin were studied at continuously decreasing levels with half-life values similar to those which could occur in vivo. For Escherichia coli, the kill-rates were higher with amoxycillin than with ampicillin. The bactericidal response was exponential. With an antibiotic half-life of one hour, the amoxycillin first order inactivation rate was 3.544 h-1 and the viable cell half-life was 0.196 h; the respective values for ampicillin were 2.341 h-1 and 0.296 h. With an antibiotic half-life of five hours, the inactivation rate was 0.704 h-1 corresponding to a viable cell half-life of 0.985 h for amoxycillin compared to 0.358 h-1 and 1.937 h respectively for ampicillin. Comparison of viable counts and photometric monitoring showed that the former is the preferable method for recording the bacterial response to these beta-lactam antibiotics. During the phase of exponential kill, a plateau occurred in the optical density values. This was due in part to an increased biomass per cell. During the recovery phase, the number of viable cells started to increase several hours sooner than did the rise in optical density. For Staphylococcus aureus,the rates of kill were similar with both agents. Amoxycillin had a long bacteriostatic phase which was not seen with ampicillin. This led to a longer lasting antibacterial effect and reduction to a lower total count with amoxycillin. With staphylococci, the viable counts and the photometric responses were parallel.
研究了在体内可能出现的半衰期值持续降低的水平下,细菌对阿莫西林和氨苄西林的反应。对于大肠杆菌,阿莫西林的杀菌率高于氨苄西林。杀菌反应呈指数关系。抗生素半衰期为1小时时,阿莫西林的一级失活率为3.544 h⁻¹,活菌半衰期为0.196 h;氨苄西林的相应值分别为2.341 h⁻¹和0.296 h。抗生素半衰期为5小时时,阿莫西林的失活率为0.704 h⁻¹,对应活菌半衰期为0.985 h,而氨苄西林分别为0.358 h⁻¹和1.937 h。活菌计数与光度监测的比较表明,前者是记录细菌对这些β-内酰胺抗生素反应的更可取方法。在指数杀灭阶段,光密度值出现平台期。这部分是由于每个细胞的生物量增加。在恢复阶段,活菌数量开始增加的时间比光密度升高早几个小时。对于金黄色葡萄球菌,两种药物的杀灭率相似。阿莫西林有一个较长的抑菌期,而氨苄西林没有。这导致阿莫西林的抗菌作用持续时间更长,且总菌数降低到更低水平。对于葡萄球菌,活菌计数和光度反应是平行的。