RASAGILINE MESYLATE

Rasagiline in the range of 1-6 mg demonstrated a more than proportional increase in AUC, while C max was dose proportional. Rasagiline mean steady-state half life is 3 hours but there is no correlation of pharmacokinetics with its pharmacological effect because of its irreversible inhibition of MAO-B.

AbsorptionRasagiline is rapidly absorbed, reaching peak plasma concentration (Cmax) in approximately 1 hour. The absolute bioavailability of rasagiline is about 36%. Food does not affect the Tmax ...

The effectiveness of rasagiline for the treatment of Parkinson’s disease was established in four 18-to 26-week, randomized, placebo-controlled trials, as initial monotherapy or adjunct therapy. 14.1 Monotherapy Use of rasagiline tablets Study 1 was a double-blind, randomized, fixed-dose parallel group, 26-week study in early Parkinson’s disease patients not receiving any concomitant dopaminergic therapy at the start of the study. The majority of the patients were not treated with medications for Parkinson’s disease before receiving rasagiline. In Study 1,404 patients were randomly assigned to ...

The following adverse reactions are described in more detail in the Warnings and Precautions section of the label:

• Hypertension [see Warnings and Precautions ( 5.1 )]
• Serotonin Syndrome [see Warnings and Precautions ( 5.2 )]
• Falling Asleep During Activities of Daily Living and Somnolence [see Warnings and Precautions ( 5.3 )]
• Hypotension / Orthostatic Hypotension [see Warnings and Precautions ( 5.6 )]
• Dyskinesia [see Warnings and Precautions ( 5.7 )]
• Hallucinations / Psychotic-Like B...

Rasagiline tablets are contraindicated for use with meperidine, tramadol, methadone, propoxyphene and MAO inhibitors (MAOIs), including other selective MAO-B inhibitors, because of risk of serotonin syndrome [see Warnings and Precautions ( 5.2 )]. At least 14 days should elapse between discontinuation of rasagiline tablets and initiation of treatment with these medications. Rasagiline tablets are ...

May cause hypertension (including severe hypertensive syndromes) at recommended doses ( 5.1 ) May cause serotonin syndrome when used with antidepressants ( 5.2 ) May cause falling asleep during activities of daily living, daytime drowsiness, and somnolence ( 5.3 ) May cause hypotension, especially orthostatic ( 5.6 ) May cause or exacerbate dyskinesia. Decreasing the levodopa dose may lessen or eliminate this side effect ( 5.7 ) May cause hallucinations and psychotic-like behavior ( 5.8 ) May ca...

7 DRUG INTERACTIONS Meperidine: Risk of serotonin syndrome ( 4 , 7.1 ) Dextromethorphan: Risk of psychosis or bizarre behavior ( 4 , 7.2 ) MAO inhibitors: Risk of non-selective MAO inhibition and hypertensive crisis ( 4 , 7.3 ) 7.1 Meperidine Serious, sometimes fatal reactions have been precipitated with concomitant use of meperidine (e.g., Demerol and other tradenames) and MAO inhibitors includin...