Tomizawa I, Takizawa Y, Nitta Y, Tsunoda T, Fukuda H, Yamaguchi T, Masuda G, Negishi M, Ajisawa A, Murata M, Ohnishi K, Irimajiri S, Obana M, Sajima Y, Sagara H, Kato H, Hosoda S, Banba T, Sasaki M, Yoshikawa K, Nakagawa M, Ohkubo H, Kim Y, Akao M, Fukuyama M
Department of Infectious Diseases, Minamigaoka Branch of Sapporo City General Hospital.
Kansenshogaku Zasshi. 1996 Jul;70(7):727-45. doi: 10.11150/kansenshogakuzasshi1970.70.727.
Prulifloxacin (PUFX), a new quinolone antimicrobial agent, was administered to a total of 122 patients and carriers to investigate its clinical efficacy, safety and usefulness in infectious enteritis (bacillary dysentery, enteritis caused by Salmonella spp. and enteropathogenic E. coli, cholera and so on). In addition, the minimum inhibitory concentration (MIC) of UFX (active compound) was determined against each clinical isolate, and compared with that of ciprofloxacin (CPFX), ofloxacin (OFLX), tosufloxacin (TFLX) and nalidixic acid (NA). The correlation between the concentration of UFX in feces and the change of the fecal microflora were also investigated when PUFX was administered to the patients with acute infectious enteritis. A daily dose of 400 mg of PUFX was administered orally in two divided doses (morning and evening) for 5 days, with the exception of 7 days administration against salmonella enteritis and 3 days administration against cholera. 84 cases were adapted for evaluating the usefulness. The clinical efficacy was 100% in all the enteritis except salmonella enteritis, in which it was 88.9% (8/9 cases). On the bacteriological efficacy, the elimination rate was 100% in all isolates except Salmonella spp., in which it was 75.0% (12/16 cases). As for the adverse effect, uriticaria in moderate degree was observed in 1 (0.9%) of 109 cases. Abnormal changes in laboratory findings were seen in 3 (3.0%) of 100 cases, consisting of 1 with eosinophilia and 2 with elevated S-GPT, although they were all slight in degree. The usefulness rate was 65.5% (55/84 cases) for "very useful" and 95.2% (80/84 cases) for "very useful" and "useful". MIC90 of UFX against Shigella spp., Salmonella spp., E. coli and V. cholerae, was 0.025, 0.05, 0.025 and 0.05 microgram/ml, respectively. These values were the same as those of CPFX and TFLX, and superior to OFLX and NA. UFX concentrations in feces followed by administration of PUFX in 3 cases with acute infectious enteritis were higher than that of MIC90 of UFX against Shigella spp., Salmonella spp., E. coli and V. cholerae. The changes of the fecal microflora, which influence the efficacy and safety of PUFX, were not observed.
普卢利沙星（PUFX）是一种新型喹诺酮类抗菌药物，共对122例患者及带菌者进行了给药，以研究其在感染性肠炎（细菌性痢疾、沙门氏菌属及致病性大肠杆菌引起的肠炎、霍乱等）中的临床疗效、安全性和实用性。此外，还测定了UFX（活性化合物）对各临床分离株的最低抑菌浓度（MIC），并与环丙沙星（CPFX）、氧氟沙星（OFLX）、妥舒沙星（TFLX）和萘啶酸（NA）进行了比较。在对急性感染性肠炎患者给予PUFX时，还研究了粪便中UFX浓度与粪便微生物群变化之间的相关性。除沙门氏菌肠炎给药7天、霍乱给药3天外，PUFX每日剂量400mg，分两次口服（早晚各一次），共给药5天。84例患者适合评估其有效性。除沙门氏菌肠炎外，所有肠炎的临床有效率均为100%，沙门氏菌肠炎的临床有效率为88.9%（8/9例）。在细菌学疗效方面，除沙门氏菌属外，所有分离株的清除率均为100%，沙门氏菌属的清除率为75.0%（12/16例）。至于不良反应，109例中有1例（0.9%）出现中度荨麻疹。100例中有3例（3.0%）出现实验室检查结果异常，包括1例嗜酸性粒细胞增多和2例谷丙转氨酶升高，不过程度均较轻。“非常有用”的有效率为65.5%（55/84例），“非常有用”和“有用”的总有效率为95.2%（80/84例）。UFX对志贺氏菌属、沙门氏菌属、大肠杆菌和霍乱弧菌的MIC90分别为0.025、0.05、0.025和0.05微克/毫升。这些数值与CPFX和TFLX相同，优于OFLX和NA。3例急性感染性肠炎患者给予PUFX后粪便中的UFX浓度高于UFX对志贺氏菌属、沙门氏菌属、大肠杆菌和霍乱弧菌的MIC90。未观察到影响PUFX疗效和安全性的粪便微生物群变化。
