Aoki T, Matsubara Y, Sagara H, Tomizawa I, Takizawa Y, Nitta Y, Seo T, Kamimura M, Masuda G, Negishi M
Kansenshogaku Zasshi. 1989 Jun;63(6):593-605. doi: 10.11150/kansenshogakuzasshi1970.63.593.
For the purpose of evaluation of clinical efficacy, safety and usefulness on acute infectious enteritis (bacillary dysentery, and enteritis caused by Salmonella spp., Campylobacter spp., enteropathogenic E. coli, and so on), T-3262, a newly developed pyridone-carboxylic acid derivative, was administered to a total of 136 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). The daily dose of 450 mg of T-3262 was administered orally three times after meals for 5 days, with the exception of 7 day administration against Salmonella enteritis. A total of 89 cases were evaluated; 23 with Shigella spp., 30 with Salmonella spp., 15 with Campylobacter spp., 6 with enteropathogenic E. coli, and 15 cases with the other pathogens or pathogen-negative. The efficacy on clinical symptoms judging from duration of fever, and duration of diarrhea and abnormal stool character was 100% in all the enteritis except enteropathogenic E. coli enteritis, in which it was 50% (n = 2). Concerning bacteriological response, elimination of the causative organisms from the feces was 100% in Shigella spp. (n = 19), Salmonella spp. (n = 30), and enteropathogenic E. coli (n = 6), although 64.3% in Campylobacter spp. (n = 14). As an adverse effect, epigastric discomfort was observed in one (0.8%) of 130 cases. Deteriorations in laboratory findings were seen in five (6.2%) of 81 cases, consisting of two with elevated GOT and GPT, two with elevated GPT, and one with increased eosinophils count, although they were all slight in degree. MICs of T-3262 which inhibited 90% of the isolates of Shigella spp, Salmonella spp., and Campylobacter spp., were 0.025, 0.05, and 0.78 microgram/ml, respectively. These values were lowest among the quinolone derivatives tested, except that the MIC90 against Campylobacter spp. was the same as that of ofloxacin.
为评估新开发的吡啶酮羧酸衍生物T-3262对急性感染性肠炎（细菌性痢疾以及由沙门氏菌属、弯曲杆菌属、致病性大肠杆菌等引起的肠炎）的临床疗效、安全性和实用性，对总共136例患者和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）的抗菌活性进行了比较。T-3262的日剂量为450mg，饭后口服，每日3次，共给药5天，但沙门氏菌肠炎需给药7天。总共评估了89例病例；其中志贺氏菌属感染23例，沙门氏菌属感染30例，弯曲杆菌属感染15例，致病性大肠杆菌感染6例，其他病原体感染或病原体阴性15例。除致病性大肠杆菌肠炎的疗效为50%（n = 2）外，从发热持续时间、腹泻持续时间和大便性状异常判断，T-3262对所有肠炎的临床症状疗效均为100%。关于细菌学反应，志贺氏菌属（n = 19）、沙门氏菌属（n = 30）和致病性大肠杆菌（n = 6）粪便中病原菌的清除率为100%，而弯曲杆菌属的清除率为64.3%（n = 14）。作为不良反应，130例中有1例（0.8%）出现上腹部不适。81例中有5例（6.2%）实验室检查结果出现恶化，包括2例谷草转氨酶（GOT）和谷丙转氨酶（GPT）升高、2例GPT升高、1例嗜酸性粒细胞计数增加，不过程度均较轻。T-3262对90%的志贺氏菌属、沙门氏菌属和弯曲杆菌属分离菌株的最低抑菌浓度（MIC）分别为0.025、0.05和0.78微克/毫升。在所有测试的喹诺酮类衍生物中，这些值是最低的，但T-3262对弯曲杆菌属的MIC90与氧氟沙星相同。
