Pharmacokinetics and metabolism of selegiline
Szatmári, I.; Tóth, K.
Acta Pharmaceutica Hungarica 62(5): 243-248
1992
ISSN/ISBN: 0001-6659 PMID: 1488909 Document Number: 398812
As it has been shown is animal experiments, selegiline administered orally is absorbed rapidly. The compound penetrates the blood-brain barrier and the concentration of selegiline and/or its metabolites is high in the brain. Selegiline is eliminated primarily by renal excretion (73%) and 14% of the dose is eliminated with faeces. The main metabolic pathway is N-dealkylation. N-demethyl-selegiline, amphetamine and methamphetamine are the main metabolites. p-Hydroxylated derivatives of amphetamine and methamphetamine could also be identified in rat urine. (-)-Selegiline gives rise to (-) metabolites and does not undergo racemization. Selegiline is bound to macromolecules extensively. The metabolites have lower affinity to plasma proteins than the parent drug do. Selegiline and its metabolites do not accumulate in the organism not even during prolonged administration.