Sagara H, Tomizawa I, Takizawa Y, Nitta Y, Tsunoda T, Yamaguchi T, Masuda G, Negishi M, Ajisawa A, Murata M
Department of Infectious Diseases, Tokyo Metropolitan Toshima General Hospital.
Kansenshogaku Zasshi. 1994 Nov;68(11):1390-408. doi: 10.11150/kansenshogakuzasshi1970.68.1390.
A clinical study was conducted on fleroxacin (FLRX) in 143 patients and carriers with infectious enteritis (shigellosis, Salmonella enteritis, Campylobacter enteritis, pathogenic Escherichia coli enteritis, Vibrio parahaemolyticus enteritis, cholera, multiple bacterial infections, pathogen-negative enteritis). Furthermore, its antibacterial activity against clinical isolates, fecal concentration and effect on fecal microflora were conducted. FLRX was administered orally in doses of 200 mg once a day (200 mg group) or 300 mg once a day (300 mg group) for 3 days to cholera, for 7 days to Salmonella enteritis and for 5 days to the other infectious enteritis. The clinical efficacy rates were 100% in both the 200 mg and 300 mg groups. The bacteriological efficacy rates were 100% against Shigella spp., Salmonella spp., pathogenic E. coli, V. parahaemolyticus and V. cholerae O1, and 63.6% against Campylobacter spp. in the 200 mg group. The rates of the 300 mg group were 93.3% against Shigella spp., and 100% against Campylobacter spp. and pathogenic E. coli. As adverse effects, skin rash was observed in 1 case each in both groups (1.1%, 2.1%). Abnormal laboratory findings consisted of 1 case of increased eosinophils and 1 case of elevated GOT and GPT levels in the 200 mg group (2.8%), and 1 case of elevated GPT in the 300 mg group (2.9%). The clinical usefulness rates were 92.9% and 93.3% in the 200 mg and 300 mg groups, respectively. Antibacterial activity was somewhat inferior to that fo ciprofloxacin and equal to or better than that of norfloxacin, demonstrating MIC90 values against Shigella spp., Salmonella spp., pathogenic E. coli, V. parahaemolyticus and Campylobacter spp. of 0.1, 0.2, 0.1, 0.2 and 0.78 micrograms/ml, respectively. Peak fecal concentrations of the drug were 49.0 micrograms/g and 274.4 micrograms/g in the 200 mg group, and 43.3 micrograms/g and below the detection limit (5.0 micrograms/g) in the 300 mg group. With respect to fecal microflora (4 cases), a decrease in Enterobacteriaceae was observed in 3 cases during dosing. But this change showed a tendency to recover after completion of dosing. No effects were observed on anaerobic bacteria.
对143例感染性肠炎（志贺菌病、沙门氏菌肠炎、弯曲菌肠炎、致病性大肠杆菌肠炎、副溶血性弧菌肠炎、霍乱、多重细菌感染、病原体阴性肠炎）患者及带菌者进行了氟罗沙星（FLRX）的临床研究。此外，还研究了其对临床分离株的抗菌活性、粪便浓度及对粪便微生物群的影响。氟罗沙星对霍乱患者口服给药，剂量为每日1次200mg（200mg组）或每日1次300mg（300mg组），疗程3天；对沙门氏菌肠炎患者疗程7天；对其他感染性肠炎患者疗程5天。200mg组和300mg组的临床有效率均为100%。200mg组对志贺菌属、沙门氏菌属、致病性大肠杆菌、副溶血性弧菌和霍乱弧菌O1的细菌学有效率为100%，对弯曲菌属的细菌学有效率为63.6%。300mg组对志贺菌属的细菌学有效率为93.3%，对弯曲菌属和致病性大肠杆菌的细菌学有效率为100%。作为不良反应，两组各有1例出现皮疹（1.1%，2.1%）。200mg组实验室检查异常包括1例嗜酸性粒细胞增多和1例谷草转氨酶（GOT）及谷丙转氨酶（GPT）水平升高（2.8%），300mg组有1例GPT水平升高（2.9%）。200mg组和300mg组的临床有用率分别为92.9%和93.3%。其抗菌活性略低于环丙沙星，与诺氟沙星相当或优于诺氟沙星，对志贺菌属、沙门氏菌属、致病性大肠杆菌、副溶血性弧菌和弯曲菌属的MIC90值分别为0.1、0.2、0.1、0.2和0.78μg/ml。200mg组药物的粪便峰值浓度为49.0μg/g和274.4μg/g，300mg组为43.3μg/g且低于检测限（5.0μg/g）。关于粪便微生物群（4例），给药期间3例观察到肠杆菌科减少。但这种变化在给药结束后有恢复的趋势。对厌氧菌未观察到影响。
