Aoki T, Matsubara Y, Sagara H, Shimizu N, Tomizawa I, Takizawa Y, Nitia Y, Seo T, Kamimura M, Kanehisa N
Kansenshogaku Zasshi. 1989 Jul;63(7):659-75. doi: 10.11150/kansenshogakuzasshi1970.63.659.
For the purpose of evaluation of clinical efficacy, safety and usefulness on Salmonella enteritis, T-3262 (Tosufloxacin tosilate), a newly developed pyridone-carboxylic acid derivative, was administered to a total of 103 patients and carriers. In addition, in vitro antibacterial activity of T-3262 was determined against the clinical isolates, and compared with those of nalidixic acid (NA), pipemidic acid (PPA), enoxacin (ENX), norfloxacin (NFLX) and ofloxacin (OFLX). And when T-3262 was administered to the patients of acute infectious enteritis, fecal drug concentration and their correlation to the changes in the fecal microflora were investigated. The daily dose of 450 mg T-3262 was administered orally three times after meal for 7 days. A total of 63 cases were evaluated (one case of mixed infection caused by Shigella flexneri and Salmonella sp. was included). The clinical efficacy was good in all the enteritis (N = 6). As the bacteriological effect, 60 out of 61 were eradicated, and eradication rate was 98.4%. Adverse effects were observed in four of 102 cases (3.9%), consisting of one with skin rash, one with nausea, headache and stomatitis and two with soft stools. Deteriorations in laboratory findings were seen in 5 of 23 cases (17.4%), consisting of one with elevated GOT, two with elevated GOT and GPT, one with elevated BUN and one with increased eosinophiles count, although they were all slight in degree. MICs of T-3262 which inhibited 90% of the isolates of Salmonella spp. was 0.05 microgram/ml, which was the lowest among the quinolone derivatives tested. The values of the fecal drug concentration of 7 cases of acute infectious enteritis, to which T-3262 administered, were higher than that of MIC90 and recovery rates of T-3262 were distributed from 2.85 to 46.3%. The degrees of changes of the drug concentrations were dependent on individual cases, and did not show the same trend. In addition, changes in the fecal microflora with in 24 hrs after T-3262 administration did not show the same trend.
为评估新型吡啶酮羧酸衍生物T-3262（托氟沙星甲苯磺酸盐）对肠炎沙门氏菌的临床疗效、安全性和实用性，对103例患者及带菌者进行了给药治疗。此外，测定了T-3262对临床分离菌株的体外抗菌活性，并与萘啶酸（NA）、吡哌酸（PPA）、依诺沙星（ENX）、诺氟沙星（NFLX）和氧氟沙星（OFLX）进行了比较。在对急性感染性肠炎患者给予T-3262治疗时，研究了粪便药物浓度及其与粪便微生物群变化的相关性。T-3262的日剂量为450mg，餐后口服，每日3次，共7天。共评估了63例病例（包括1例由福氏志贺菌和沙门氏菌属引起的混合感染病例）。所有肠炎病例（N = 6）的临床疗效均良好。作为细菌学效果，61例中有60例细菌被根除，根除率为98.4%。102例中有4例（3.9%）观察到不良反应，包括1例皮疹、1例恶心、头痛和口腔炎，以及2例软便。23例中有5例（17.4%）实验室检查结果出现恶化，包括1例谷草转氨酶升高、2例谷草转氨酶和谷丙转氨酶升高、1例尿素氮升高和1例嗜酸性粒细胞计数增加，不过程度均较轻。抑制90%肠炎沙门氏菌分离菌株的T-3262的最低抑菌浓度（MIC）为0.05微克/毫升，这在受试喹诺酮类衍生物中是最低的。接受T-3262治疗的7例急性感染性肠炎患者的粪便药物浓度值高于MIC9０，T-3262的回收率在2.85%至46.3%之间。药物浓度的变化程度因个体病例而异，未显示出相同趋势。此外，T-3262给药后24小时内粪便微生物群的变化也未显示出相同趋势。
