Blood level, distribution, metabolite pattern and excretion of [14C]alinidine in mice and rats

Following oral and intravenous administration the absorption, distribution, metabolite pattern and excretion of [14C]alinidine, a drug with specific bradycardic efficacy, was studied in mice and rats. [14C]alinidine was rapidly and extensively absorbed. The distribution of radio-labelled drug over the entire animal body was rapid as indicated by blood level curves as well as by whole body autoradiography. In both species radioactive compounds were eliminated from blood with half-lives ranging from 5.6 h to 7.4 h. More than 50% of the renally excreted radioactivity was a uniform substance behaving in in TLC and HPLC experiments like the drug administered. From rat urine this compound could be identified as [14C]alinidine using mass spectrometry. In mice and rats no definite substance with clonidine-like chromatographic properties was found. Biliary excretion was demonstrated in both species. The renal portion of the total radioactivity elimination was 67.2-70.1% of the dose administered in mice and 68.1-85.1% in rats. Total excretion was 85.1-101.3% of radioactivity given and was complete 3-4 days after [14C]alinidine administration. No significant differences in pharmacokinetic behavior in mice and rats could be found.