Basker M J, Edmondson R A, Sutherland R
Infection. 1979;7(2):67-73. doi: 10.1007/BF01641616.
The antibacterial activities of two ureidopenicillins, azlocillin and mezlocillin, were compared with those of the alpha-carboxypenicillins, carbenicillin and ticarcillin, against a large number of gram-positive and gram-negative bacteria. All four penicillins were active against a wide range of bacteria including Pseudomonas aeruginosa, but there were differences in the antibacterial spectra and in the antibacterial effects demonstrated by the two classes of penicillins. In particular, the minimum inhibitory concentrations of azlocillin and mezlocillin against Klebsiella aerogenes and against P. aeruginosa were greatly influenced by the size of bacterial inoculum tested whereas there was no significant inoculum effect with carbenicillin and ticarcillin. In stability tests, the ureidopenicillins were inactivated rapidly by the beta-lactamases of K. aerogenes and P. aeruginosa whereas the alpha-carboxypenicillins were stable. It seems probable that the inoculum effect seen with azlocillin and mezlocillin in antibacterial tests with K. aerogenes and P. aeruginosa is associated with the instability of the compounds to the beta-lactamases of these bacteria.
将两种脲基青霉素阿洛西林和美洛西林的抗菌活性与α-羧基青霉素羧苄西林和替卡西林的抗菌活性进行比较,以对抗大量革兰氏阳性菌和革兰氏阴性菌。所有四种青霉素对包括铜绿假单胞菌在内的多种细菌均有活性,但两类青霉素在抗菌谱和抗菌效果上存在差异。特别是,阿洛西林和美洛西林对产气克雷伯菌和铜绿假单胞菌的最低抑菌浓度受测试细菌接种量大小的影响很大,而羧苄西林和替卡西林则无明显的接种量效应。在稳定性试验中,脲基青霉素被产气克雷伯菌和铜绿假单胞菌的β-内酰胺酶迅速灭活,而α-羧基青霉素则稳定。在产气克雷伯菌和铜绿假单胞菌的抗菌试验中,阿洛西林和美洛西林出现的接种量效应似乎与这些化合物对这些细菌的β-内酰胺酶的不稳定性有关。