Harabe E, Kawai Y, Kanazawa K, Otsuki M, Nishino T
Department of Microbiology, Kyoto Pharmaceutical University, Japan.
Drugs Exp Clin Res. 1992;18(2):37-46.
The in vitro and in vivo antibacterial activities of meropenem were compared with those of imipenem, ceftazidime, flomoxef, cefuzonam and cefotiam. Meropenem showed a broad antibacterial spectrum against clinical isolates of Gram-positive and Gram-negative bacteria. Against Gram-negative bacteria, with the exception of Acinetobacter calcoaceticus, meropenem exhibited the most potent activity among the drugs tested. It inhibited all 330 strains of Enterobacteriaceae at 0.78 mg/l. Meropenem was sensitive against several cephem-resistant strains of Enterobacteriaceae. Against Pseudomonas aeruginosa, meropenem was four-fold more active than imipenem and eight-fold more active than ceftazidime, with an MIC90 of 0.78 mg/l. The therapeutic effect of meropenem on systemic infection in mice was ten to twenty-fold less than that of imipenem against Staphylococcus aureus, Streptococcus pyogenes and Streptococcus pneumoniae. However, meropenem was as effective as imipenem on infections of Escherichia coli, Klebsiella pneumoniae, Serratia marcescens, Acinetobacter calcoaceticus and Pseudomonas aeruginosa. Meropenem was eliminated from mice plasma two-fold faster than imipenem, with a plasma half-life of 7.6 min. From the above results the authors concluded that meropenem is a promising drug for clinical use.
将美罗培南的体外和体内抗菌活性与亚胺培南、头孢他啶、氟氧头孢、头孢唑南和头孢替安进行了比较。美罗培南对革兰氏阳性菌和革兰氏阴性菌的临床分离株显示出广谱抗菌活性。对于革兰氏阴性菌，除醋酸钙不动杆菌外，美罗培南在所测试的药物中表现出最强的活性。它在0.78mg/l时抑制了所有330株肠杆菌科细菌。美罗培南对几种耐头孢菌素的肠杆菌科菌株敏感。对于铜绿假单胞菌，美罗培南的活性比亚胺培南高四倍，比头孢他啶高八倍，MIC₉₀为0.78mg/l。在小鼠中，美罗培南对金黄色葡萄球菌、化脓性链球菌和肺炎链球菌引起的全身感染的治疗效果比亚胺培南低十至二十倍。然而，美罗培南对大肠杆菌、肺炎克雷伯菌、粘质沙雷氏菌、醋酸钙不动杆菌和铜绿假单胞菌感染的疗效与亚胺培南相当。美罗培南从小鼠血浆中消除的速度比亚胺培南快两倍，血浆半衰期为7.6分钟。根据上述结果，作者得出结论，美罗培南是一种有临床应用前景的药物。
