Rasagiline is a propargylamine and an irreversible monoamine oxidase inhibitor (MAOIs). It is indicated in the treatment of idiopathic Parkinson's disease as initial therapy or as adjunct therapy with levodopa. The monoamine oxidase is an enzyme that catalyzes the oxidative deamination of many amines like serotonin, norepinephrine, epinephrine, and dopamine. There are 2 isoforms of this protein: A and B. The first one is found in cells located in the periphery and breakdown serotonin, norepinephrine, epinephrine, dopamine, and tyramine. The second one, the B isoform, breakdowns phenylethylamine, norepinephrine, epinephrine, dopamine, and tyramine. This isoform is found in the extracellular tissues and mostly in the brain. The mechanism of action of the MAOIs is still not determined, it is thought that they act by increasing free serotonin and norepinephrine concentrations and/or by altering the concentrations of other amines in the CNS. MAO-A inhibition is thought to be more relevant to antidepressant activity than the inhibition caused by MAO B. Selective MAO B inhibitors have no antidepressant effects. The selectivity of rasagiline for inhibiting only MAO-B results in more dopamine in the cytosol and synapse of the neurons in the striatum. The increased dopamine level thus increases the dopaminergic activity. This helps to reduce the symptoms of Parkinson's disease that are caused by low levels of dopamine in the striatum. An overdose of this drug will result in drowsiness, faintness, hyperactivity, hallucinations, respiratory depression, convulsions, and coma. This drug is administered as an oral tablet.

Rasagiline Pathway References