The pharmacokinetics of isepamicin, a broad-spectrum aminoglycoside an
tibiotic, was studied in man after intramuscular administration. Two g
roups each of 6 volunteers received isepamicin for 10 consecutive days
by intramuscular injection at respective doses of 7.5 mg/kg once dail
y or 7.5 mg/kg twice daily. Plasma and urinary concentrations of isepa
micin were determined using a specific HPLC method. In both groups, th
ere was no drug accumulation following multiple administration. The t(
1/2), which ranged from 2.4 to 2.7 h, was independent of the dosage re
gimen. Isepamicin excreted into (0-24 h) urine accounted for virtually
100% of the dose. The results show that the pharmacokinetics of isepa
micin are similar with these dosage regimens. The drug undergoes no de
tectable biotransformation, does not accumulate upon multiple dosing,
and is cleared solely by urinary excretion.