[Pharmacokinetic study of eremomycin in an experiment].

Abstract

Pharmacokinetics of eremomycin, a novel original glycopeptide antibiotic was studied. It was shown that after a single intravenous or subcutaneous administration to mice, rabbits and dogs eremomycin concentrations in blood and duration of the antibiotic circulation depended on the dose level and administration route. After subcutaneous or intramuscular administration eremomycin was rapidly absorbed and detected in serum even in 15-30 min. The maximum levels were observed in 2 hours. Absolute bioavailability after subcutaneous administration averaged to 85 per cent. Eremomycin penetrated into organs. The antibiotic concentrations in cerebrospinal fluid were low. The highest concentrations of eremomycin were detected in the kidneys, lungs and spleen. The antibiotic mainly excreted with urine. The renal clearance amounted to 85 per cent of the total clearance. 2-3-month exposure of dogs and rats to eremomycin in doses 4-10 times higher than the approximate single therapeutic doses for humans (250 mg) resulted in cumulation of the antibiotic.