Washida H, Sakagami H, Awata S, Kan K, Kawai N, Inuzuka K
Washida Clinic.
Jpn J Antibiot. 1996 Mar;49(3):273-8.
The morphological response of urinary Gram-negative bacteria to ceftibuten (CETB) was investigated in four patients with urinary tract infections (one patient: acute uncomplicated cystitis, three patients: chronic complicated urinary tract infection). The daily dose of CETB was 400 mg administered orally and the durations were 3 days for the acute uncomplicated cystitis case and 5 days for the chronic complicated urinary tract infection cases. In the four patients, changes in urinary CETB concentrations, viable bacterial counts, and morphology of the bacteria were studied after the initial administration. The urinary concentrations of CETB were 7.38-60.3 micrograms/ml at one hour after the first administration. The urinary viable cell counts were 1-5 x 10(7) cells/ml before administration, but they were reduced to 1-3 x 10(3) cells/ml at one hour after the first oral administration. Morphological changes of bacteria: Under phase contrast microscopy, filamentous debris and spherical bacteria with severe body damage were observed at 30 minutes after the first administration. By transmission electron microscopy, the cell wall of the filamentous bacteria showed a number of projections with formation of vacuolar structures in the space between the cell wall and the irregularly-shaped cytoplasm. According to the Japanese UTI criteria, the efficacy rate was 100% in the 4 patients. Neither side effect nor abnormal laboratory result was observed in any patient.
The morphological changes of the bacteria suggested that CETB, in vivo, bounds not only penicillin-binding protein (PBP)-3 but also PBP-1.
对4例尿路感染患者(1例:急性单纯性膀胱炎,3例:慢性复杂性尿路感染)研究了尿中革兰氏阴性菌对头孢布烯(CETB)的形态学反应。CETB的日剂量为400mg口服,急性单纯性膀胱炎病例疗程为3天,慢性复杂性尿路感染病例疗程为5天。在这4例患者中,研究了首次给药后尿中CETB浓度、活菌计数及细菌形态的变化。首次给药后1小时尿中CETB浓度为7.38 - 60.3微克/毫升。给药前尿中活菌计数为1 - 5×10⁷个细胞/毫升,但首次口服给药后1小时降至1 - 3×10³个细胞/毫升。细菌的形态学变化:在相差显微镜下,首次给药后30分钟观察到丝状碎片和菌体严重受损的球形细菌。通过透射电子显微镜观察,丝状细菌的细胞壁显示出许多突起,在细胞壁与不规则形状的细胞质之间的空间形成了空泡结构。根据日本尿路感染标准,4例患者的有效率为100%。所有患者均未观察到副作用或实验室检查结果异常。
细菌的形态学变化表明,CETB在体内不仅与青霉素结合蛋白(PBP)-3结合,还与PBP-1结合。