Pharmacokinetic/pharmacodynamic evaluation of rasagiline mesylate for Parkinson's disease

Oxidative stress reduction via monoamine oxidase-B (MAO-B) inhibition with rasagiline is under investigation to modify the course of Parkinson's disease (PD) progression. Rasagiline moderately improves motor symptoms and therefore reduces the predominant levodopa-associated wearing-off phenomena.

Following a PubMed database search with the terms rasagiline and selegiline, this review describes the role of rasagiline in the treatment of Parkinson's disease, within a critical discussion of current treatment guidelines. This so-called evidence based research suggests that rasagiline is an alternative to the catechol-O-methyltransferase-inhibitor entacapone, in the treatment of wearing-off phenomena. There is some recent evidence to suggest rasagiline also has monoamine oxidase-A (MAO-A) inhibiting properties, as well as different clinical and pharmacodynamic properties when compared with selegiline, and clinical benefits when used in combination with a dopamine agonist monotherapy.

Rasagiline is well tolerated and safe, however its use has not yet been fully exploited as an alternative to selegiline due to the availability of cheaper generics. When generic rasagiline is available in Europe, more widespread use should focus on the simultaneous administration with entacapone as an approach to delaying the onset of, and improving the severity of, motor complications in levodopa treated patients. The complimentary combination of the pharmacologic principles of rasagiline and entacapone may support the concept of continuous nigrostriatal dopaminergic stimulation.