Neu H C, Labthavikul P
Antimicrob Agents Chemother. 1982 Jun;21(6):906-11. doi: 10.1128/AAC.21.6.906.
Apalcillin, a naphthydridine derivative of ampicillin, was compared with ticarcillin, azlocillin, mezlocillin, piperacillin, cefotaxime, and cefoperazone against gram-negative and gram-positive bacterial isolates and with cefsulodin and tobramycin against Pseudomonas aeruginosa. The minimal concentrations of apalcillin at which 50 and 90% of hospital isolates of Escherichia coli were inhibited were similar to those of mezlocillin and piperacillin (1.6 and 100 micrograms/ml, respectively). Apalcillin had minimal inhibitory concentrations similar to those of piperacillin against Citrobacter freundii and Citrobacter diversus. Against Klebsiella, apalcillin inhibited 50% of organisms at a concentration of 6.3 micrograms/ml, similar to piperacillin. The activity of apalcillin against Enterobacter (E. aerogenes, E. cloacae, and E. agglomerans) was similar to that of mezlocillin and piperacillin and greater than that of ticarcillin. The activity of apalcillin against Proteus mirabilis was similar to that of the other agents, as was its activity against indole-positive Proteus and Providencia. Only 40% of Serratia were inhibited at an apalcillin concentration of 25 micrograms/ml. Apalcillin was as active as piperacillin but twofold less active than cefoxitin or moxalactam against Bacteroides fragilis. It was as active as piperacillin, cefoperazone, and cefsulodin against P. aeruginosa (apalcillin inhibited 90% of organisms at a concentration of 25 mg/ml). There was an inoculum effect and a difference in the minimal inhibitory concentration and minimal bactericidal concentration with beta-lactamase strains. Apalcillin was hydrolyzed by plasmid beta-lactamase but not as well by cephalosporinases.
阿帕西林是氨苄西林的萘啶衍生物,将其与替卡西林、阿洛西林、美洛西林、哌拉西林、头孢噻肟和头孢哌酮针对革兰氏阴性和革兰氏阳性细菌分离株进行了比较,并与头孢磺啶和妥布霉素针对铜绿假单胞菌进行了比较。抑制50%和90%医院分离的大肠杆菌所需的阿帕西林最低浓度与美洛西林和哌拉西林相似(分别为1.6和100微克/毫升)。阿帕西林对弗氏柠檬酸杆菌和差异柠檬酸杆菌的最低抑菌浓度与哌拉西林相似。针对克雷伯菌属,阿帕西林在浓度为6.3微克/毫升时可抑制50%的菌株,与哌拉西林相似。阿帕西林对肠杆菌属(产气肠杆菌、阴沟肠杆菌和聚团肠杆菌)的活性与美洛西林和哌拉西林相似,且大于替卡西林。阿帕西林对奇异变形杆菌的活性与其他药物相似,对吲哚阳性变形杆菌和普罗威登斯菌的活性也相似。在阿帕西林浓度为25微克/毫升时,仅40%的沙雷菌被抑制。阿帕西林对脆弱拟杆菌的活性与哌拉西林相同,但比对头孢西丁或莫拉卡坦的活性低两倍。它对铜绿假单胞菌的活性与哌拉西林、头孢哌酮和头孢磺啶相同(阿帕西林在浓度为25毫克/毫升时可抑制90%的菌株)。对于β-内酰胺酶菌株,存在接种量效应以及最低抑菌浓度和最低杀菌浓度的差异。阿帕西林可被质粒β-内酰胺酶水解,但不能被头孢菌素酶很好地水解。