Pharmacology of Amikacin in Humans

ABSTRACT

Amikacin is a new aminoglycoside antibiotic which is active in vitro against most isolates of gram-negative bacilli. A dose of 300 mg/m² intramuscularly produced a highest mean serum concentration of 25.4 μg/ml with a mean serum concentration of 3.1 μg/ml at 8 h. The same dose intravenously produced a highest mean serum concentration of 52.4 μg/ml with a mean serum concentration of 2.1 μg/ml at 8 h. The mean urinary excretion during the first 6 h was 75 and 66%, respectively. When amikacin was administered at a dose of 150 mg/m² every 6 h, there was evidence of some drug accumulation. A loading dose of 150 mg/m² administered intravenously over 30 min followed by 200 mg/m² administered as a continuous infusion every 6 h maintained serum concentrations of 8 μg/ml. No major toxicity was observed with any of these drug regimens.