Esposito S, Noviello S, Ianniello F
Infectious Diseases Clinic, II University of Naples, Italy.
J Chemother. 2000 Dec;12(6):475-81. doi: 10.1179/joc.2000.12.6.475.
The aim of the present investigation was to study and compare the killing activity of two new fluoroquinolone compounds, moxifloxacin and grepafloxacin, and a new generation macrolide, clarithromycin, against three clinical isolates of Streptococcus pneumoniae (penicillin-susceptible, -intermediate and -resistant) and two Streptococcus pyogenes (erythromycin-susceptible and -resistant) strains by simulating their human pharmacokinetics in a pharmacodynamic model. Results were achieved by measuring the reduction in viable bacterial count during the 24-h experimental period. All three antimicrobials led to a continuous reduction in the bacterial counts of penicillin-susceptible S. pneumoniae and erythromycin-susceptible S. pyogenes strains, the maximal reduction observed after 8-10 hours being 5-6 logs for moxifloxacin and 3 logs for grepafloxacin; clarithromycin exhibited a similar reduction of 5 logs only after 24 h. No regrowth was observed for any strain after 24 h with any of the antibiotics. The bactericidal activity of both the fluoroquinolones was not affected by penicillin resistance of S. pneumoniae and erythromycin resistance of S. pyogenes. In contrast, clarithromycin was not able to reduce the bacterial count of penicillin-resistant S. pneumoniae and erythromycin-resistant S. pyogenes strains. Moxifloxacin exhibited, within 24 h, higher and faster bactericidal activity than grepafloxacin and clarithromycin against S. pneumoniae, and was not affected by penicillin resistance. These results suggest that moxifloxacin is a promising new agent for treatment of streptococcal infections.
本研究的目的是通过在药效学模型中模拟两种新型氟喹诺酮类化合物莫西沙星和格帕沙星以及新一代大环内酯类药物克拉霉素在人体中的药代动力学,研究并比较它们对三株肺炎链球菌临床分离株(青霉素敏感、中介和耐药)和两株化脓性链球菌(红霉素敏感和耐药)菌株的杀菌活性。通过测量24小时实验期内活菌数的减少来得出结果。所有三种抗菌药物均使青霉素敏感的肺炎链球菌和红霉素敏感的化脓性链球菌菌株的细菌数持续减少,莫西沙星在8 - 10小时后观察到的最大减少量为5 - 6个对数,格帕沙星为3个对数;克拉霉素仅在24小时后才出现类似的5个对数的减少。24小时后,使用任何一种抗生素均未观察到任何菌株再生长。两种氟喹诺酮类药物的杀菌活性不受肺炎链球菌青霉素耐药性和化脓性链球菌红霉素耐药性的影响。相比之下,克拉霉素不能降低青霉素耐药的肺炎链球菌和红霉素耐药的化脓性链球菌菌株的细菌数。在24小时内,莫西沙星对肺炎链球菌的杀菌活性高于格帕沙星和克拉霉素,且起效更快,并且不受青霉素耐药性的影响。这些结果表明,莫西沙星是一种有前景的治疗链球菌感染的新型药物。