Wise R, Rollason T, Logan M, Andrews J M, Bedford K A
Antimicrob Agents Chemother. 1978 Dec;14(6):807-11. doi: 10.1128/AAC.14.6.807.
HR 756, a new parenteral cephalosporin, was compared with cefazolin and carbenicillin for activity against a total of 264 strains of Pseudomonas aeruginosa, Escherichia coli, Klebsiella spp., Proteus mirabilis, Proteus spp. (indole positive), Enterobacter spp., Salmonella typhi, Serratia marcescens, Providencia stuartii, and Staphylococcus aureus. In every comparison, except that with the last organism, HR 756 was clearly more active than cefazolin and carbenicillin. All three compounds had similar activity against penicillin-susceptible staphylococci; against penicillin-resistant strains, HR 756 and cefazolin were equally active and superior to carbenicillin. HR 756 was compared with penicillin for activity against strains of Streptococcus pyogenes, Lancefield group D streptococci, and Neisseria gonorrhoeae; with ampicillin against Haemophilus influenzae; and with cefoxitin against Bacteriodes fragilis. HR 756 was clearly more active than the respective reference compounds in all of these comparisons, except those involving the streptococci. HR 756 and penicillin were essentially equally active against S. pyogenes; against Lancefield group D, penicillin was 32 times as active as HR 756. HR 756 not only compared favorably with the reference compounds with respect to relative activity, but also effected growth inhibition of essentially all test organisms (P. aeruginosa and group D streptococci excepted) at remarkably low concentrations ranging from 0.015 to 2.0 mug/ml. A series of seven transfers of selected strains of E. coli, Klebsiella spp., S. aureus, and P. aeruginosa through medium containing HR 756 led to emergence of strains with significant levels of resistance to the agent. Resistance to HR 756 was retained for at least seven transfers through plain medium.
新型胃肠外头孢菌素HR 756与头孢唑林和羧苄西林进行了比较,以评估其对总共264株铜绿假单胞菌、大肠杆菌、克雷伯菌属、奇异变形杆菌、变形杆菌属(吲哚阳性)、肠杆菌属、伤寒沙门菌、粘质沙雷菌、斯氏普罗威登斯菌和金黄色葡萄球菌的活性。在每一项比较中,除了与最后一种微生物的比较外,HR 756的活性明显高于头孢唑林和羧苄西林。这三种化合物对青霉素敏感葡萄球菌的活性相似;对青霉素耐药菌株,HR 756和头孢唑林活性相当且优于羧苄西林。HR 756与青霉素比较了对化脓性链球菌、D群链球菌和淋病奈瑟菌菌株的活性;与氨苄西林比较了对流感嗜血杆菌的活性;与头孢西丁比较了对脆弱拟杆菌的活性。在所有这些比较中,除了涉及链球菌的比较外,HR 756的活性明显高于相应的对照化合物。HR 756和青霉素对化脓性链球菌的活性基本相同;对D群链球菌,青霉素的活性是HR 756的32倍。HR 756不仅在相对活性方面与对照化合物相比具有优势,而且在0.015至2.0微克/毫升的极低浓度下就能对基本上所有测试微生物(铜绿假单胞菌和D群链球菌除外)产生生长抑制作用。将选定的大肠杆菌、克雷伯菌属、金黄色葡萄球菌和铜绿假单胞菌菌株通过含有HR 756的培养基进行一系列七次传代培养后,出现了对该药物具有显著耐药水平的菌株。对HR 756的耐药性在通过普通培养基进行至少七次传代培养后仍得以保留。