We performed basic and clinical studies on ME1207, a new oral cephalosporin antibiotic, with the following results. 1) Antimicrobial activity The MICs of ME1206, the active substance of ME1207, were determined with an inoculum size of 106 cells/ml. Its antimicrobial activity against granvnegative rods, except Pseudomonas aeruginosa was as good as that of cefixime and cefteram. Especially, the MIC90 of ME1206 was 0.39 ~1.56 μg/ml for Escherichia coli, Klebsiella pneumoniae and Proteus spp. Moreover, its activity against Staphylococcus aureus was 2 ~3 times higher than that of cefaclor and cephalexin. 2) Absorption and urinary excretion The mean serum concentrations of ME1206 reached a peak of 1.81μg/ml 3 hours after the administration of ME1207. Its half life was 1.77 hours and the mean urinary excretion rate was 16.13%. Probenecid interfered with the urinary excretion of ME1206, therefore, its peak level became higher and its half life was prolonged. Dried aluminium hydroxide gel had little influenced on the absorption and excretion of ME1207, but cimetidine delayed the absorption and therefore its peak level was lower. 3) Clinical efficacy Three patients with pneumonia, 5 with bronchitis, 1 with pharyngitis, 3 with cystitis, 1 with epididymitis and cystitis, and 1 with appendicitis were treated with ME1207. The patients were administered a daily dose of 300 mg or 400 mg for 3-15 days. The clinical response was excellent in 4, good in 7, fair in 1, poor in 1, and unknown in one patient. The efficacy rate was 84.6%. As adverse reactions, abdominal pain, vomiting and diarrhea were seen in a patient, and elevation of GOT, GPT and ALP was observed in another patient.
|出版ステータス||出版済み - 1994|
All Science Journal Classification (ASJC) codes
- Pharmacology (medical)
- Infectious Diseases
- Drug Discovery