Abstract
The pharmacokinetics and clinical efficacy of ritipenem acoxil, a new oral penem antibiotic, were studied.
1. Pharmacokinetics: the influence of probenecid was investigated in 6 healthy volunteers orally given 200 mg of ritipenem acoxil with or without 1.5 g of probenecid by cross-over method. With probenecid, the T1/2 of ritipenem (the active form of ritipenem acoxil) was prolonged from 0.61 h (without probenecid) to 0.91 h, Cmax and AUC increased from 1.88μg/ml and 2.55 μg·h/ml to 2.87μg/ml and 4.53μg·h/ml, respectively, and renal clearance decreased from 139.7ml/min to 32.6ml/min. These results suggest that tubular excretion was involved in the renal excretion of the drug.
2. Clinical efficacy: ritipenem acoxil was administered in daily doses of 450-1500mg (t. i. d.) to seven patients, 1 with tonsillitis, 2 with acute bronchitis and 4 with pneumonia. The clinical response was excellent in 1 patient, good in 4, fair in 1 and poor in 1. No side effects were found. In one patient we observed an increased transaminase level in blood.
