Classes
DEA Class; Rx
Common Brand Names; Azilect
- Antiparkinson Agents, MAO Type B Inhibitors
Description
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.
Indications
Indicated for the treatment of Parkinson’s disease.
Contraindications
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
Adverse Effects
- 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%)
Warnings
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
Pregnancy and Lactation
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
Maximum Dosage
1 mg/day PO.
1 mg/day PO.
Safety and efficacy have not been established.
Safety and efficacy have not been established.
Not indicated.
How supplied
Rasagiline mesylate
tablet
- 0.5mg
- 1mg