Liebers D M, Baltch A L, Smith R P, Hammer M C, Conroy J V, Shayegani M
Department of Medicine, Veterans Administration Medical Center, Albany, New York 12208.
J Antimicrob Chemother. 1988 May;21(5):565-70. doi: 10.1093/jac/21.5.565.
The inhibitory (MIC) and bactericidal (MBC) activities of a new macrolide A-56268 (TE-031) against 306 clinical aerobic bacterial isolates was compared with that of erythromycin. The MIC90/MBC90 ratios for A-56268 were: Campylobacter jejuni 4/16, Haemophilus influenzae 8/8-16, H. parainfluenzae 8/8-16, Legionella pneumophila 0.06/0.5, methicillin-sensitive isolates of Staphylococcus aureus 0.5/1, and coagulase negative staphylococci 1/8, methicillin resistant isolates of Staph. aureus and coagulase negative staphylococci greater than 16/ greater than 16, Streptococcus pneumoniae 0.06/0.125, streptococcus Group A 0.06/2-4, streptococcus Group B 0.06/8- greater than 16, streptococcus Groups C and G 0.125/8 and Str. faecalis 4/64. Compared with erythromycin, A-56268 had greater inhibitory and bactericidal activity against isolates of L. pneumophila, with an MIC90 16-fold less and an MBC90 eight-fold less than that of erythromycin. Except for enterococci, A-56268 showed inhibitory activity equal to or greater than that of penicillin G against isolates of streptococci and an MIC two-fold less than that of erythromycin. For other strains tested, the inhibitory and bactericidal activities of A-56268 and erythromycin were similar. The clinical importance of the differences between these two macrolides will depend on the pharmacokinetic and tissue penetration properties of the new compound.
将新型大环内酯类药物A-56268（TE-031）对306株临床需氧菌分离株的抑菌（MIC）和杀菌（MBC）活性与红霉素进行了比较。A-56268的MIC90/MBC90比值如下：空肠弯曲菌4/16，流感嗜血杆菌8/8 - 16，副流感嗜血杆菌8/8 - 16，嗜肺军团菌0.06/0.5，甲氧西林敏感金黄色葡萄球菌分离株0.5/1，凝固酶阴性葡萄球菌1/8，甲氧西林耐药金黄色葡萄球菌和凝固酶阴性葡萄球菌分离株大于16/大于16，肺炎链球菌0.06/0.125，A组链球菌0.06/2 - 4，B组链球菌0.06/8 - 大于16，C组和G组链球菌0.125/8，粪肠球菌4/64。与红霉素相比，A-56268对嗜肺军团菌分离株具有更强的抑菌和杀菌活性，其MIC90比红霉素低16倍，MBC90比红霉素低8倍。除肠球菌外，A-56268对链球菌分离株的抑菌活性等于或大于青霉素G，且MIC比红霉素低两倍。对于其他受试菌株，A-56268和红霉素的抑菌和杀菌活性相似。这两种大环内酯类药物之间差异的临床重要性将取决于新化合物的药代动力学和组织穿透特性。
