Van Landuyt H W, Pyckavet M, Lambert A, Boelaert J
Antimicrob Agents Chemother. 1982 Oct;22(4):535-40. doi: 10.1128/AAC.22.4.535.
The minimal inhibitory concentration of temocillin (BRL 17421) against 476 clinical isolates was determined by an agar dilution method. Temocillin was active against most of the Enterobacteriaceae, Haemophilus, and Neisseria strains tested. The compound showed low activity or was inactive against Bacteroides, Campylobacter, Acinetobacter, Pseudomonas, and Staphylococcus aureus strains. Within each species, individual strains showed a high degree of uniformity in their susceptibility to temocillin; the drug concentrations that inhibited the growth of 90% of organisms were the same or close to those which inhibited the growth of 50% of organisms. In contrast, the same strains showed a very wide range of susceptibility to the other antibiotics tested, including third-generation cephalosporins. Against strains of Enterobacteriaceae highly susceptible to third-generation cephalosporins, temocillin was considerably less active than cefotaxime, ceftazidime, and moxalactam, although it was more active than cefazolin and piperacillin. Against certain strains of Enterobacter and Citrobacter resistant to third-generation cephalosporins, temocillin was more active than cefotaxime and ceftazidime. An increase in the inoculum size did not alter the activity of temocillin, indicating that the compound has high stability to beta-lactamases. The minimal lethal concentration was also very similar to the minimal inhibitory concentration when an inoculum of 10(5) colony-forming units was used.
采用琼脂稀释法测定替莫西林（BRL 17421）对476株临床分离菌的最低抑菌浓度。替莫西林对大多数测试的肠杆菌科细菌、嗜血杆菌和奈瑟菌菌株具有活性。该化合物对拟杆菌、弯曲杆菌、不动杆菌、假单胞菌和金黄色葡萄球菌菌株显示出低活性或无活性。在每个菌种内，各个菌株对替莫西林的敏感性表现出高度一致性；抑制90%菌生长的药物浓度与抑制50%菌生长的浓度相同或接近。相比之下，相同菌株对包括第三代头孢菌素在内的其他测试抗生素表现出非常广泛的敏感性范围。对于对第三代头孢菌素高度敏感的肠杆菌科细菌菌株，替莫西林的活性明显低于头孢噻肟、头孢他啶和拉氧头孢，尽管它比头孢唑林和哌拉西林更具活性。对于某些对第三代头孢菌素耐药的肠杆菌和柠檬酸杆菌菌株，替莫西林比头孢噻肟和头孢他啶更具活性。接种量的增加并未改变替莫西林的活性，表明该化合物对β-内酰胺酶具有高度稳定性。当使用10(5)个菌落形成单位的接种量时，最低致死浓度也与最低抑菌浓度非常相似。
