Open AccessPharmacokinetics and metabolism of 14C-isepamicin in humans following intravenous administration
Author(s) -
ChinChung Lin,
C.A. Korduba,
Melton B. Affrime,
Elaine Radwanski,
Amin A. Nomeir,
Vishal Batra,
David L. Cutler,
Mitchell N. Cayen
Publication year - 1995
Publication title -
antimicrobial agents and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.07
H-Index - 259
eISSN - 1070-6283
pISSN - 0066-4804
DOI - 10.1128/aac.39.10.2201
Subject(s) - pharmacokinetics , urine , pharmacology , antibacterial agent , bolus (digestion) , intravenous bolus , chemistry , half life , excretion , medicine , antibiotics , biochemistry
Twelve healthy adult male volunteers received 1 g (base equivalent) of 14C-isepamicin (131 microCi) as an intravenous bolus over 5 min. The areas under the plasma concentration-time curves at infinity for isepamicin (196 micrograms*h/ml) and total radioactivity (164 micrograms*h/ml) were similar, indicating no biotransformation of isepamicin. The disappearance of isepamicin from plasma followed a triexponential decline, with half-lives of 0.17, 2.12, and 34 h for the alpha, beta, and gamma phases, respectively. However, the contribution of the gamma phase to the total area under the concentration-time curve was only 2.6%. There were no detectable metabolites in plasma and urine, confirming that isepamicin was not biotransformed. The cumulative levels of isepamicin and total radioactivity excretion in urine from 0 to 120 h were 97.3 and 92.1% of the dose, respectively, indicating that the drug was excreted mainly as unchanged isepamicin in urine.