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Rasagiline

    DEA Class;  Rx

    Common Brand Names; Azilect

    • Antiparkinson Agents, MAO Type B Inhibitors

    Second generation, irreversible MAOI-B; for early treatment of Parkinson’s disease as monotherapy and for later disease as adjunct therapy to levodopa; typical MAOI dietary tyramine precautions not required for most foods/beverages when used at manufacturer recommended doses; dopaminergic adverse effects (i.e., hallucinations, dyskinesias) may occur; lower doses required with use of CYP1A2 inhibitors.

    Indicated for the treatment of Parkinson’s disease.

     

    Coadministration with meperidine, tramadol, methadone, and MAOIs, including other selective MAO-B inhibitors increases risk of serotonin syndrome; at least 14 days should elapse between discontinuation of rasagiline and initiation of treatment with these medications

    Coadministration with St. John’s wort and with cyclobenzaprine

    Coadministration with dextromethorphan because of risk of episode of psychosis or bizarre behavior

    • EPS (dyskinesia/dystonia) (18%)
    • Headache (14%)
    • Nausea (10-12%)
    • Postural hypotension (6-9%)
    • Constipation (4-9%)
    • Weight loss (2-9%)
    • Arthralgia (7%)
    • Dyspepsia (7%)
    • Xerostomia (2-6%)
    • Depression (5%)
    • Fall (5%)
    • Flu-like syndrome (5%)
    • Hallucination (4-5%)
    • Conjunctivitis (3%)
    • Fever (3%)
    • Gastroenteritis (3%)
    • Rhinitis (3%)
    • Arthritis (2%)
    • Bruising (2%)
    • Malaise (2%)
    • Neck pain (2%)
    • Parasthesia (2%)
    • Vertigo (2%)

    Rasagiline is a selective inhibitor of MAO-B at the recommended doses of 0.5 or 1 mg daily; selectivity for inhibiting MAO-B diminishes in a dose-related manner as the dose is progressively increased above the recommended daily doses

    May exacerbate hypertension; antihypertensive drugs may require dosage adjustment

    May cause hypotension, especially orthostatic

    May cause or exacerbate dyskinesia; decreasing the levodopa dose may lessen or eliminate this side effect

    Withdrawal-emergent hyperpyrexia and confusion reported with rapid dose reduction of drugs that increase central dopaminergic tone; this is characterized by elevated temperature, muscular rigidity, altered consciousness, and autonomic instability

    Patients with Parkinson disease have a higher risk (2 to 6-fold higher) of developing melanoma than the general population; unclear if this is due to the disease or other factors (eg, drug therapy); monitor for melanomas frequently and on a regular basis

    There are no adequate data on developmental risks associated with use in pregnant women

    There are no data on presence of drug in human milk or effects on breastfed infant; in rats, rasagiline was shown to inhibit prolactin secretion; the clinical relevance in humans is unknown, and there are no data on effects of rasagiline on prolactin secretion in humans

    Adults

    1 mg/day PO.

    Geriatric

    1 mg/day PO.

    Adolescents

    Safety and efficacy have not been established.

    Children

    Safety and efficacy have not been established.

    Infants

    Not indicated.

    Rasagiline mesylate

    tablet

    • 0.5mg
    • 1mg