EFFECT OF ME 1207, A NEW ORAL CEPHEM ANTIBIOTIC, ON BACTERIAL FLORA IN HUMAN FECES

• Published in: CHEMOTHERAPY Vol. 40; no. Supplement2; pp. 75 - 86
• Main Author: Motohiro, Takashi
• Format: Journal Article
• Language: English; Japanese
• Published: Japanese Society of Chemotherapy 1992; 公益社団法人 日本化学療法学会
• Subjects: ME 1207; ヒト; 糞便内細菌叢; 経口セフェム剤
• ISSN: 0009-3165; 1884-5894
• DOI: 10.11250/chemotherapy1953.40.Supplement2_75

ME 1207, a newly developed oral cephem-antibiotic, was administered to seven healthy male volunteers in a dose of 200 mg, three times a day after meals for seven days, to study the effects of this drug on the fecal bacterial flora and to determine the fecal concentration of ME 1206, which is the main active form of ME 1207, furthermore, the antibacterial activity against organisms chosen at random from feces isolates was determined. The subjects were monitored for adverse reactions and abnormal laboratory findings. The results were as follows. 1. The mean changes in the bacterial flora consisted decreased counts of Enterobacteriaceae among aerobes, and of Lactobacillus, Peptococcaceae, Veillonellaceae, etc., among anaerobes during the treatment. Other remarkable changes in the fecal bacterial flora were also seen in each of the cases with a high fecal concentration of ME 1206. 2. Clostridium di fficile was isolated from five volunteers in counts of 3.0 × 102-2.2 × 108 CFU/g from the first day of treatment to the 30 th day after administration, and D-1 antigen was detected in six cases at levels of 250-2, 000 ng/g from the 5 th day before treatment to the 30 th day after administration. 3. The fecal concentrations of ME 1206 were determined by bioassay, and values of 0.12-1, 730μg/g were detected in all cases on the 2 nd, 4 th and 7 th days of treatment. When assayed by HPLC, values of 210-1, 560 μg/g were detected in three cases on the 2 nd, 4 th and 7 th days. In the other four cases, the fecal concentration was below the limit of detection. 4. The MICs of ME 1206 for some species of Gram-positive cocci were similar to those of cefpodoxime (CPDX) and cefprozil. In case of some species of Enterobacteriaceae, the MICs of ME 1206 were similar to those of cefteram (CFTM), cefpodoxime (CPDX) and cefixime (CFIX). And for Bacteroides fragilis group the MICs of ME 1206 were as high as those of other cephem antibiotics; for C. difficile they were as high as those of CFTM, CPDX, CFIX and cefaclor. 5. As adverse reactions, mild diarrhea occurred during treatment in two cases (Case 5 and 6), and this was thought to have been due to the administration of ME 1207. There were no abnormal laboratory findings.