Goldstein E J, Citron D M, Warren Y, Tyrrell K, Merriam C V
R. M. Alden Research Laboratory, Santa Monica-University of California at Los Angeles Medical Center, Santa Monica, California 90404, USA.
Antimicrob Agents Chemother. 1999 Sep;43(9):2231-5. doi: 10.1128/AAC.43.9.2231.
Gemifloxacin mesylate (SB 265805), a new fluoronaphthyridone, was tested against 359 recent clinical anaerobic isolates by the National Committee for Clinical Laboratory Standards reference agar dilution method with supplemented brucella blood agar and an inoculum of 10(5) CFU/spot. Comparative antimicrobials tested included trovafloxacin, levofloxacin, grepafloxacin, sparfloxacin, sitafloxacin (DU-6859a), penicillin G, amoxicillin clavulanate, imipenem, cefoxitin, clindamycin, and metronidazole. The MIC(50) and MIC(90) (MICs at which 50 and 90% of the isolates were inhibited) of gemifloxacin against various organisms (with the number of strains tested in parentheses) were as follows (in micrograms per milliliter): for Bacteroides fragilis (28), 0.5 and 2; for Bacteroides thetaiotaomicron (24), 1 and 16; for Bacteroides caccae (12), 1 and 16; for Bacteroides distasonis (12), 8 and >16; for Bacteroides ovatus (12), 4 and >16; for Bacteroides stercoris (12), 0.5 and 0.5; for Bacteroides uniformis (12), 1 and 4; for Bacteroides vulgatus (11), 4 and 4; for Clostridium clostridioforme (15), 0.5 and 0.5; for Clostridium difficile (15), 1 and >16; for Clostridium innocuum (13), 0.125 and 2; for Clostridium perfringens (13), 0.06 and 0.06; for Clostridium ramosum (14), 0.25 and 8; for Fusobacterium nucleatum (12), 0.125 and 0.25; for Fusobacterium necrophorum (11), 0.25 and 0.5; for Fusobacterium varium (13), 0.5 and 1; for Fusobacterium spp. (12), 1 and 2; for Peptostreptococcus anaerobius (13), 0.06 and 0.06; for Peptostreptococcus asaccharolyticus (13), 0.125 and 0.125; for Peptostreptococcus magnus (14), 0.03 and 0.03; for Peptostreptococcus micros (12), 0.06 and 0.06; for Peptostreptococcus prevotii (14), 0.06 and 0.25; for Porphyromonas asaccharolytica (11), 0.125 and 0.125; for Prevotella bivia (10), 8 and 16; for Prevotella buccae (10), 2 and 2; for Prevotella intermedia (10), 0.5 and 0.5; and for Prevotella melaninogenica (11), 1 and 1. Gemifloxacin mesylate (SB 265805) was 1 to 4 dilutions more active than trovafloxacin against fusobacteria and peptostreptococci, and the two drugs were equivalent against clostridia and P. asaccharolytica. Gemifloxacin was equivalent to sitafloxacin (DU 6859a) against peptostreptococci, C. perfringens, and C. ramosum, and sitafloxacin was 2 to 3 dilutions more active against fusobacteria. Sparfloxacin, grepafloxacin, and levofloxacin were generally less active than gemifloxacin against all anaerobes.
甲磺酸吉米沙星(SB 265805),一种新型氟萘啶酮,采用美国国家临床实验室标准委员会的参考琼脂稀释法,在添加了布鲁氏菌血琼脂且接种量为10(5) CFU/点的条件下,对359株近期临床分离的厌氧菌进行了测试。所测试的对照抗菌药物包括曲伐沙星、左氧氟沙星、格帕沙星、司帕沙星、西他沙星(DU-6859a)、青霉素G、阿莫西林克拉维酸、亚胺培南、头孢西丁、克林霉素和甲硝唑。甲磺酸吉米沙星对各种微生物(括号内为测试菌株数量)的MIC(50)和MIC(90)(抑制50%和90%菌株生长所需浓度)如下(以微克/毫升计):脆弱拟杆菌(28株),0.5和2;多形拟杆菌(24株),1和16;粪便拟杆菌(12株),1和16;狄氏拟杆菌(12株),8和>16;卵形拟杆菌(12株),4和>16;硬结拟杆菌(12株),0.5和0.5;单形拟杆菌(12株),1和4;普通拟杆菌(11株),4和4;梭形梭菌(15株),0.5和0.5;艰难梭菌(15株),1和>16;无害梭菌(13株),0.125和2;产气荚膜梭菌(13株),0.06和0.06;多枝梭菌(14株),0.25和8;具核梭杆菌(12株),0.125和0.25;坏死梭杆菌(11株),0.25和0.5;可变梭杆菌(13株),0.5和1;梭杆菌属(12株),1和2;厌氧消化链球菌(13株),0.06和0.06;不解糖消化链球菌(13株),0.125和0.125;大消化链球菌(14株),0.03和0.03;微小消化链球菌(12株),0.06和0.06;普氏消化链球菌(14株),0.06和0.25;不解糖卟啉单胞菌(11株),0.125和0.125;二路普雷沃菌(10株),8和16;颊普雷沃菌(10株),2和2;中间普雷沃菌(10株),0.5和0.5;产黑色素普雷沃菌(11株),1和1。甲磺酸吉米沙星(SB 265805)对梭杆菌属和消化链球菌的活性比曲伐沙星高1至4倍稀释度,对梭菌属和不解糖卟啉单胞菌两种药物活性相当。吉米沙星对消化链球菌、产气荚膜梭菌和多枝梭菌的活性与西他沙星(DU 6859a)相当,西他沙星对梭杆菌属的活性高2至3倍稀释度。司帕沙星、格帕沙星和左氧氟沙星对所有厌氧菌的活性总体上低于吉米沙星。