selegiline (Rx)

Brand and Other Names:Eldepryl, Zelapar
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

tablet/capsule

  • 1.25mg
  • 5mg
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Parkinson Disease

Conventional

  • 5 mg PO at breakfast & 5 mg at lunch (10 mg/day)
  • After 2-3 days of selegeline therapy, can begin to taper levadopa dose by 10-30% as tolerated; continue to taper based upon patient response
  • Not to exceed 10 mg/day

Orally-disintegrating (with levodopa/carbidopa)

  • Initial 1.25 mg PO qDay, may increase after 6 weeks if inadequate response, no more than 2.5 mg/day
  • Do not take food or liquid for 5 minutes after dose

Renal Impairment

Use caution; safety and efficacy not established

Hepatic Impairment

Use caution; safety and efficacy not established

Safety and efficacy not established

Parkinson Disease

Conventional

- 5 mg PO at breakfast & 5 mg at lunch (10 mg/day)

- <5 mg/day when combined with levodopa

- After 2-3 days of selegeline therapy, can begin to taper levadopa dose by 10-30% as tolerated; continue to taper based upon patient response

- Not to exceed 10 mg/day

Orally-disintegrating (with levodopa/carbidopa)

- Initial 1.25 mg PO qDay, may increase after 6 weeks if inadequate response, no more than 2.5 mg/day

- Do not take food or liquid for 5 minutes after dose

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Interactions

Interaction Checker

and selegiline

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Dyskinesia

            Nausea (20%)

            1-10%

            Abdominal pain

            Dry mouth

            Frequency Not Defined (selected)

            Arrhythmias

            Confusion

            EPS

            Generalized pain

            Hallucinations

            Headache

            HTN

            Insomnia

            Mood changes

            Orthostatic hypotension

            Syncope

            Urinary retention

            Vomiting

            Postmarketing Reports

            Suicidal thoughts and behaviors

            Serotonin syndrome

            Blood pressure elevation

            Activation of mania/hypomania

            External heat

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            Warnings

            Black Box Warnings

            In short-term studies, antidepressants increased the risk of suicidal thinking and behavior in children, adolescents, and young adults (<24 yr of age) taking antidepressants for major depressive disorders and other psychiatric illnesses

            This increase was not seen in patients aged >24 years; a slight decrease in suicidal thinking was seen in adults >65 years

            In children and young adults, risks must be weighed against the benefits of taking antidepressants

            Patients should be monitored closely for changes in behavior, clinical worsening, and suicidal tendencies; this should be done during initial 1-2 months of therapy and dosage adjustments

            The patient’s family should communicate any abrupt changes in behavior to the healthcare provider

            Worsening behavior and suicidal tendencies that are not part of the presenting symptoms may require discontinuation of therapy

            This drug is not approved for use in pediatric patients

            Contraindications

            Hypersensitivity

            Concomitant meperidine, possibly other opioids, many other drugs (check interactions)

            Cautions

            Loses selectivity for MAO-B receptors at higher doses

            Prescriptions should be written for the smallest quantity consistent with good patient care

            May cause exacerbation of hypertension and orthostatic hypotension; use with caution in patients at risk for this effect of those who do not tolerate transient hypotensive episode

            May potentiate dopaminergic side effects of levodopa and cause dyskinesia or exacerbate preexisting dyskinesia, which may in turn require a reduction of lovodopa dose

            Patients with Parkinson disease treated with drugs that increase dopaminergic tone have reported falling asleep while engaged in activities of daily living, including the operation of motor vehicles

            Diminished impulse control; reports of intense urges to gamble, increased sexual urges, intense urges to spend money, binge eating, and/or other intense urges

            In patients with bipolar disorder, treating a depressive episode may precipitate a mixed/manic episode; prior to initiating treatment, screen patients for any personal or family history of bipolar disorder, mania, or hypomania

            Serotonin syndrome reported with use

            Risk of melanoma development increased in Parkinson disease patients; monitor patients closely

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            Pregnancy & Lactation

            Pregnancy

            The available data on use in pregnant women are not sufficient to inform a drug- associated risk of adverse pregnancy-related outcomes; When treating a pregnant woman, the physician should carefully consider both the potential risks of taking an MAOI, particularly the risk of hypertensive crisis during pregnancy, along with the established benefits of treating depression with an antidepressant

            Lactation

            There is no information regarding presence in human milk, or effects on milk production or breastfed infant; because of potential for serious adverse reactions in breastfed infants from therapy, including potential for hypertensive crisis, advise a woman that breastfeeding is not recommended during treatment and for 5 days after final dose

            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

            Selective MAO-B inhibitor; may increase dopaminergic activity by interfering with dopamine reuptake at the synapse.

            Pharmacokinetics

            Peak plasma time: (conventional) 0.5-0.9 hr; (ODT) 15-40 min

            Concentration: (conventional, 5 mg) 0.9-2.7 ng/mL; (ODT, 1.25 /2.5 mg) 3.34/4.47 ng/mL

            Half-life elimination: 10 hr (PO); 18-25hr (TD)

            Onset of action: Within 1 hr

            Duration: 24-72hr (PO)

            Bioavailability: 10%

            Protein Bound: 90%

            Vd: 300 L

            Metabolism: cytochrome P-450 enzymes

            Metabolites: L-amphetamine, L-desmethylselegiline, L-methamphetamine

            Excretion: Urine

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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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