rasagiline (Rx)

Brand and Other Names:Azilect
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 0.5mg
  • 1mg
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Parkinson Disease

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

Dosage Modifications

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

Hepatic impairment

  • Mild (Child-Pugh A): Not to exceed 0.5 mg/day
  • Moderate-to-severe (Child-Pugh B/C): Do not use

Dosing Considerations

Do not exceed recommended doses because of risk for hypertension

<18 years: Safety and efficacy not established

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Interactions

Interaction Checker

and rasagiline

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            EPS (dyskinesia/dystonia) (18%)

            Headache (14%)

            Nausea (10-12%)

            1-10%

            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%)

            <1%

            CVA

            MI

            Bundle branch block

            Gastrointestinal hemorrhage

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            Warnings

            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

            Cautions

            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

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            Pregnancy & Lactation

            Pregnancy Category: C

            Lactation: may inhibit lactation; use caution

            Pregnancy Categories

            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.

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            Pharmacology

            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

            Absorption

            Peak Plasma Time: 1 hr

            Onset of action: Within 1 hr

            Bioavailability: 36%

            Distribution

            Protein Bound: 88-94%

            Vd: 87 L

            Metabolism

            Via liver, primarily CYP1A2 (in vitro data)

            Metabolites: 1-aminoindan, 3-hydroxy-N-propargyl-1-aminoindan, 3-hydroxy-1-aminoindan

            Elimination

            Half-life: 1.3-3 hr

            Excretion: 62% urine; 7% feces

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            Images

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            Formulary

            FormularyPatient Discounts

            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.

            Tier Description
            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.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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