Jorgensen J H, Maher L A, Howell A W
Department of Pathology, University of Texas Health Science Center, San Antonio 78284-7750.
Antimicrob Agents Chemother. 1991 Jul;35(7):1524-6. doi: 10.1128/AAC.35.7.1524.
Clarithromycin is a new macrolide antibiotic which forms a microbiologically active principal in vivo metabolite, 14-OH-clarithromycin. The in vitro activities of clarithromycin and its metabolite were examined separately and in pharmacokinetically relevant fixed combinations of 4:1 and 2:1 against a group of 50 Haemophilus influenzae isolates. Broth microdilution susceptibility tests indicated that clarithromycin was less active than erythromycin against all but highly erythromycin-susceptible strains, while 14-OH-clarithromycin was generally more active than either antibiotic. An enhancement in activity against the majority of strains was demonstrated when clarithromycin and its metabolite were tested in combination.
克拉霉素是一种新型大环内酯类抗生素，其在体内可形成具有微生物活性的主要代谢产物14-羟基克拉霉素。分别对克拉霉素及其代谢产物的体外活性进行了检测，并以4:1和2:1这两种药代动力学相关的固定组合，对一组50株流感嗜血杆菌分离株进行了检测。肉汤微量稀释药敏试验表明，除对红霉素高度敏感的菌株外，克拉霉素对所有其他菌株的活性均低于红霉素，而14-羟基克拉霉素的活性通常高于这两种抗生素中的任何一种。当克拉霉素及其代谢产物联合检测时，对大多数菌株的活性增强。
