Komoto A, Otsuki M, Nishino T
Department of Microbiology, Kyoto Pharmaceutical University, Japan.
Jpn J Antibiot. 1996 Apr;49(4):352-66.
The in vitro and in vivo antibacterial activities of sulopenem, a new penem, were evaluated in comparison with imipenem (IPM), meropenem (MEPM), ceftazidime (CAZ) and flomoxef (FMOX). Sulopenem had broad and potent antibacterial spectra against Gram-positive and Gram-negative bacteria, including Enterococcus faecalis, Proteus vulgaris, Morganella morganii, Enterobacter spp. and Citrobacter freundii. Sulopenem showed concentration-dependent bactericidal activities against Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae and Acinetobacter calcoaceticus. Morphological observation using phase-contrast microscope revealed that sulopenem induced spherical cell formation with E. coli and K. pneumoniae at lower concentrations and bacteriolysis at higher concentrations. Therapeutic efficacies of sulopenem against systemic infections in mice were almost equal to those of imipenem against Streptococcus pneumoniae. While its therapeutic efficacies were superior to those of meropenem, ceftazidime and flomoxef against S. aureus and S. pneumoniae, they were inferior to those of imipenem/cilastatin against S. aureus, K. pneumoniae and A. calcoaceticus.
将新型青霉烯类药物舒洛培南的体外和体内抗菌活性与亚胺培南(IPM)、美罗培南(MEPM)、头孢他啶(CAZ)和氟氧头孢(FMOX)进行了比较评估。舒洛培南对革兰氏阳性菌和革兰氏阴性菌具有广泛且强效的抗菌谱,包括粪肠球菌、普通变形杆菌、摩根氏摩根菌、肠杆菌属和弗氏柠檬酸杆菌。舒洛培南对金黄色葡萄球菌、大肠杆菌、肺炎克雷伯菌和醋酸钙不动杆菌表现出浓度依赖性杀菌活性。使用相差显微镜进行的形态学观察显示,舒洛培南在较低浓度下可诱导大肠杆菌和肺炎克雷伯菌形成球形细胞,在较高浓度下则导致细菌溶解。舒洛培南对小鼠全身感染的治疗效果与亚胺培南对肺炎链球菌的治疗效果几乎相当。虽然其对金黄色葡萄球菌和肺炎链球菌的治疗效果优于美罗培南、头孢他啶和氟氧头孢,但对金黄色葡萄球菌、肺炎克雷伯菌和醋酸钙不动杆菌的治疗效果不如亚胺培南/西司他丁。