Treatment of idiopathic Parkinson’s disease (initial monotherapy or as adjunct to levodopa).
藥理
Rasagiline was shown to be a potent, irreversible MAO-B selective inhibitor, which may cause an increase in extracellular levels of dopamine in the striatum.
藥動學
Bioavailability: 36%; Plasma protein binding: 88-94% (albumin 61% to 63%); Metabolism: almost 100% in liver via CYP1A2; Elimination: Renal: 62%, less than 1% unchanged, Fecal: 7%.
禁忌症
Concomitant use of cyclobenzaprine, dextromethorphan, methadone, propoxyphene, St John’s wort, or tramadol; concomitant use of meperidine or an MAO inhibitor (including selective MAO-B inhibitors) within 14 days of rasagiline. Patients with severe hepatic impairment.
Monotherapy: 1mg once daily. Administer without regard to meals
Adjunctive therapy with levodopa: Initial: 0.5 mg once daily; may increase to 1 mg once daily based on response and tolerability.
Dose reduction with concomitant ciprofloxacin or other CYP1A2 inhibitors: 0.5 mg once daily