Kasai K, Tsuji A, Miyazaki S, Goto S, Fujimoto K, Masuyoshi S, Arai S
Jpn J Antibiot. 1984 Jul;37(7):1294-305.
The in vitro activity and beta-lactamase stability of cefodizime (HR 221), a new cephalosporin, were compared with those of other cephem antibiotics. HR 221 was highly active against Gram-negative bacteria. The compound inhibited growth of all tested Haemophilus influenzae strains at 0.10 microgram/ml and showed strong activity even against penicillin-resistant Neisseria gonorrhoeae strains, but it was less effective against Pseudomonas aeruginosa than the other antibiotics tested. Against Gram-positive bacteria, HR 221 showed 100% inhibition of growth of Streptococcus pneumoniae at 0.39 microgram/ml, and it was slightly less active against Staphylococcus aureus (MIC90:12.5 micrograms/ml) than other antibiotics such as cefotaxime (CTX). The bactericidal activity of HR 221 against E. coli was dose-related and comparable to that of CTX, cefoperazone and latamoxef. The bactericidal activity of the compound at medium concentrations simulating human serum levels was higher than that of CTX and cefmetazole, and no cell regrowth was noted after beta-lactamase-induced inactivation of the compound. HR 221 was stable to most drug-inactivating enzyme preparations from various bacterial species.
将新型头孢菌素头孢地嗪（HR 221）的体外活性及β-内酰胺酶稳定性与其他头孢烯类抗生素进行了比较。HR 221对革兰氏阴性菌具有高度活性。该化合物在0.10微克/毫升时能抑制所有测试的流感嗜血杆菌菌株生长，甚至对青霉素耐药的淋病奈瑟菌菌株也表现出强活性，但对铜绿假单胞菌的效果不如所测试的其他抗生素。针对革兰氏阳性菌，HR 221在0.39微克/毫升时对肺炎链球菌生长的抑制率达100%，对金黄色葡萄球菌（MIC90：12.5微克/毫升）的活性略低于头孢噻肟（CTX）等其他抗生素。HR 221对大肠杆菌的杀菌活性与剂量相关，且与CTX、头孢哌酮和拉氧头孢相当。该化合物在模拟人体血清水平的中等浓度下的杀菌活性高于CTX和头孢美唑，且该化合物经β-内酰胺酶诱导失活后未见细胞再生长。HR 221对来自各种细菌的大多数药物失活酶制剂稳定。
