Pharmacology of selegiline

Neurology
M GerlachP Riederer

Abstract

The acetylenic selective monoamine oxidase (MAO) type B suicide inhibitor selegiline (previously called L-deprenyl) has proved to be a useful adjuvant to levodopa therapy and monotherapy of Parkinson's disease (PD). Selegiline is readily absorbed from the gastrointestinal tract and rapidly enters the brain and spinal cord following oral administration. The drug binds to brain regions with a high MAO-B content, such as the thalamus, the striatum, the cortex, and the brainstem. It is extensively metabolized in humans, mainly in the liver, to form desmethylselegiline and methamphetamine, which are further metabolized to amphetamine. Eighty-six percent of the 10-mg dose was recovered in the urine within 24 hours. These data suggest that accumulation of metabolites does not occur. Although not all features of its anti-PD action are known, studies using brain obtained at autopsy from patients who had been treated with 10 mg of selegiline showed that selective inhibition of MAO-B, with the concomitant increase of phenylethylamine and dopamine (DA) but not of serotonin or noradrenaline, in the basal ganglia may be regarded as its mode of action. The protective effects afforded by selegiline in PD, resulting in a delayed need for levodo...Continue Reading

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