Distribution and excretion of methamphetamine and its metabolites in rats III. Time-course of concentrations in blood and bile, and distribution after intravenous administration

Publisher Website
Google Scholar
Abstract
1. The time-course of blood total radioactivity after i.v. administration of 3H-methamphetamine to rats showed a biphasic curve. 2. The biological half-life of the α phase (tα1/2) was 6.8 ± 2.0 min, and that of the β phase (tβ1/2) was 11.3±0.8 h. 3. The major metabolite in the blood was unconjugated p-hydroxymethamphetamine. 4. The total radioactivity in bile peaked at 1.5 h after i.v. administration. The major metabolite in the bile was p-hydroxymethamphetamine glucuronide. 5. The major compound excreted in urine was unchanged methamphetamine. 6. Whole-body autoradiography was performed using 14C-methamphetamine, and tissue 3H concn. was determined after i.v. administration of 3H-methamphetamine to rats.