Ballow C H, Jones R N, Johnson D M, Deinhart J A, Schentag J J
Clinical Pharmacokinetics Laboratory, Millard Fillmore Hospital, Buffalo, New York, USA.
Diagn Microbiol Infect Dis. 1997 Nov;29(3):173-86. doi: 10.1016/s0732-8893(97)81807-x.
Sparfloxacin, a new orally administered fluoroquinolone, was tested against 14,182 clinical strains isolated (generally blood stream and respiratory tract cultures) at nearly 200 hospitals in the United States (USA) and Canada. Sparfloxacin activity was compared with 13 other compounds by Etest (AB BIODISK, Solna, Sweden), broth microdilution, or a standardized disk diffusion method. Using the Food and Drug Administration/product package insert MIC breakpoint for sparfloxacin susceptibility (< or = 0.5 microgram/ml), 94% of Streptococcus pneumoniae (2666 isolates) and 89% of the other streptococci (554 isolates) were susceptible. However, at < or = 1 microgram/ml (the breakpoint for all nonstreptococcal species) sparfloxacin susceptibility rates increased to 100% and 98%, respectively, for the two groups of streptococci. Only 50% and 65% of pneumococci were susceptible to ciprofloxacin (MIC90, 3 micrograms/ml) and penicillin (MIC90, 1.5 micrograms/ml), respectively. Although there were significant differences between regions in the USA in the frequency of penicillin-resistant pneumococcal strains, results indicate that the overall sparfloxacin MIC90 was uniformly at 0.5 microgram/ml. Nearly all (> or = 99%) Haemophilus species and Moraxella catarrhalis, including those harboring beta-lactamases, were susceptible to sparfloxacin, ciprofloxacin, and amoxicillin/clavulanic acid. Only cefprozil and macrolides demonstrated lower potency and spectrum against these two species. Sparfloxacin was active against oxacillin-susceptible Staphylococcus aureus (96 to 97%), Klebsiella spp. (95%), and other tested enteric bacilli (93%). Comparison between broth microdilution MIC and disk diffusion interpretive results for M. catarrhalis, Staphylococcus aureus, and the Enterobacteriaceae showed an absolute intermethod categorical agreement of > 95% using current sparfloxacin breakpoints, in contrast to those of cefpodoxime for S. aureus where a conspicuous discord (98% versus 59%) between methods was discovered. These results demonstrate that sparfloxacin possesses sufficient in vitro activity and spectrum versus pathogens that cause respiratory tract infections (indications), especially strains resistant to other drug classes such as the earlier fluoroquinolones, oral cephalosporins, macrolides, and amoxicillin/clavulanic acid. The sparfloxacin susceptibility breakpoint for streptococci may require modification (< or = 1 microgram/ml) based on the MIC population analysis presented here. A modal MIC (0.38 to 0.5 microgram/ml) was observed at the current breakpoint. Regardless, sparfloxacin inhibited 89% (nonpneumococcal Streptococcus spp.) to 100% (Haemophilus spp., M. catarrhalis) of the isolates tested with a median activity of 97% against indicated species.
司帕沙星是一种新型口服氟喹诺酮类药物,在美国和加拿大近200家医院对从14182株临床分离菌株(主要是血流和呼吸道培养物)进行了测试。通过Etest(AB BIODISK,瑞典索尔纳)、肉汤微量稀释法或标准化纸片扩散法将司帕沙星的活性与其他13种化合物进行了比较。按照美国食品药品监督管理局/产品包装说明书中司帕沙星敏感性的最低抑菌浓度(MIC)界值(≤0.5微克/毫升),94%的肺炎链球菌(2666株分离菌)和89%的其他链球菌(554株分离菌)对其敏感。然而,对于这两组链球菌,当MIC≤1微克/毫升(所有非链球菌属的界值)时,司帕沙星的敏感率分别升至100%和98%。肺炎链球菌对环丙沙星(MIC90为3微克/毫升)和青霉素(MIC90为1.5微克/毫升)的敏感率分别仅为50%和65%。尽管美国不同地区耐青霉素肺炎链球菌菌株的频率存在显著差异,但结果表明司帕沙星的总体MIC90一致为0.5微克/毫升。几乎所有(≥99%)嗜血杆菌属和卡他莫拉菌,包括那些携带β-内酰胺酶的菌株,对司帕沙星、环丙沙星和阿莫西林/克拉维酸敏感。只有头孢丙烯和大环内酯类药物对这两种菌的效力和抗菌谱较低。司帕沙星对苯唑西林敏感的金黄色葡萄球菌(96%至97%)、克雷伯菌属(95%)和其他受试肠杆菌(93%)有活性。对卡他莫拉菌、金黄色葡萄球菌和肠杆菌科细菌的肉汤微量稀释MIC和纸片扩散法解释结果的比较显示,使用当前司帕沙星界值时,方法间的绝对分类一致性>95%,而对于金黄色葡萄球菌,头孢泊肟酯的两种方法间存在明显不一致(98%对59%)。这些结果表明,司帕沙星对引起呼吸道感染的病原体(适应证)具有足够的体外活性和抗菌谱,尤其是对其他药物类别耐药的菌株,如早期氟喹诺酮类、口服头孢菌素类、大环内酯类和阿莫西林/克拉维酸。基于此处给出的MIC群体分析,链球菌的司帕沙星敏感性界值可能需要修改(≤1微克/毫升)。在当前界值下观察到一个模态MIC(0.38至0.5微克/毫升)。无论如何,司帕沙星抑制了89%(非肺炎链球菌属链球菌)至100%(嗜血杆菌属、卡他莫拉菌)的受试分离菌,对指定菌种的中位活性为97%。