Rasagiline [R(+)-N-propargyl-1-aminoindan] mesylate (Azilect®) was approved by the FDA in May of 2006 as monotherapy in early disease and as an adjunct to levodopa in more advanced disease. The recommended doses are 1 mg once a day in early disease and an initial dose of 0.5 mg once a day in advanced disease that can be increased to 1 mg once a day if needed. It produces selective irreversible MAO-B inhibition (93). Platelet MAO-B inhibition is dose-dependent; one hour after ingestion, platelet MAO-B inhibition is 35% with 1 mg rasagiline and 99% with 10 mg rasagiline. By day 6, rasag-iline 2 mg/day inhibits over 99% of platelet MAO-B (93). After discontinuing rasagiline, it takes approximately two weeks for MAO-B activity to return to baseline values (93). The area under the curve (AUC) and maximum concentration (Cmax) increase linearly with rasagiline dosage. The plasma half-lives of rasagiline and its active metabolite 1(R)-aminoindan are 3.5 hours and 11 hours, respectively. As rasagi-line irreversibly inhibits MAO-B, the serum (pharmacokinetic) half-life does not correlate with its functional (pharmacodynamic) half-life.
Rasagiline up to 20 mg/day was well tolerated in healthy male volunteers (93). Dry mouth, headache, nausea, thirst, and abdominal discomfort were the most common adverse effects but tended to be mild. There were no significant effects on vital signs, lab values, physical exam, or EKG.
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