1992 Volume 40 Issue Supplement2 Pages 344-351
We studied the pharmacokinetics and clinical efficacy of ME 1207, a new oral cephem, and obtained the following results.
1. Pharmacokinetics
The influence of probenecid was investigated in 6 healthy volunteers orally administered 200mg of ME 1207 with or without 1.5g of probenecid in the fasting state. With probenecid, T1/2 of ME 1206 (the active form of ME 1207) was prolonged from 1.09 hours (without probenecid) to 2.11 hours, Cmax and AUC increased from 1.99μg/ml and 5.12μg·h/ml to 3.16μg/ml and 15.7μg·h/ml, respectively, and Clr decreased from 4.64 l/h to 0.882 l/h. These results suggest that tubular excretion was involved in the renal excretion of the drug.
2. Clinical efficacy
ME 1207 was administered to 8 patients with lacunar tonsillitis (1), pneumonia (1), acute bronchitis (4), chronic pyelonephritis (1) and acute cystitis (1) at a dose of 100-200mg three times a day for 6-14 days. The clinical efficacy was excellent or good in 6 cases, and poor or fair in 2 cases. Side effects were observed in 2 cases (diarrhea in one, and diarrhea and nausea in the other). As to laboratory findings, an increase of eosinophils was observed in one case.
