Dosing & Uses
Dosage Forms & Strengths
Monotherapy: 1 mg PO qDay
Adjunct without levodopa: 1 mg PO qDay
Adjunct to levodopa: 0.5 mg PO qDay initially, may increase to 1 mg/day if needed and tolerated; consider reducing levodopa dose
Coadministration with CYP1A2 inhibitors (eg, ciprofloxacin): Not to exceed 0.5 mg/day
Renal impairment: No dosage adjustment required for mild-to-moderate; not studied in severe
- Mild (Child-Pugh A): Not to exceed 0.5 mg/day
- Moderate-to-severe (Child-Pugh B/C): Do not use
Do not exceed recommended doses because of risk for hypertension
<18 years: Safety and efficacy not established
Serious - Use Alternative
Significant - Monitor Closely
EPS (dyskinesia/dystonia) (18%)
Postural hypotension (6-9%)
Weight loss (2-9%)
Flu-like syndrome (5%)
Neck pain (2%)
Bundle branch block
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
May cause hypertension (including severe hypertensive syndromes) at recommended doses
May exacerbate hypertension; antihypertensive drugs may require dosage adjustment
May cause hypotension, especially orthostatic
May cause serotonin syndrome when used with antidepressants
Daytime drowsiness and somnolence reported during activities of daily living
May cause or exacerbate dyskinesia; decreasing the levodopa dose may lessen or eliminate this side effect
Hallucinations and psychotic-like behavior reported
Impulse control/compulsive behaviors reported; case reports describe patients with intense urges to gamble, increased sexual urges, intense urges to spend money, or binge eat
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 & Lactation
Pregnancy Category: C
Lactation: may inhibit lactation; use caution
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Mechanism of Action
Monoamine oxidase inhibitor, selective Type-B; inhibits dopamine depletion in striatal region of the brain, which in turn reduces symptomatic motor deficits of Parkinson's disease
Peak Plasma Time: 1 hr
Onset of action: Within 1 hr
Protein Bound: 88-94%
Vd: 87 L
Via liver, primarily CYP1A2 (in vitro data)
Metabolites: 1-aminoindan, 3-hydroxy-N-propargyl-1-aminoindan, 3-hydroxy-1-aminoindan
Half-life: 1.3-3 hr
Excretion: 62% urine; 7% feces
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.
|1||This drug is available at the lowest co-pay. Most commonly, these are generic drugs.|
|2||This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.|
|3||This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.|
|4||This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.|
|5||This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.|
|6||This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.|
|NC||NOT COVERED – Drugs that are not covered by the plan.|
Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.