Dosing & Uses
Dosage Forms & Strengths
transdermal patch
- 6mg/24hr
- 9mg/24hr
- 12mg/24hr
Depression
1 patch qDay; apply at the same time each day
May increase by 3 mg/24 hr q2Weeks; not to exceed 12 mg/24 hr
Renal Impairment
Mild to moderate impairment: Dose adjustment not necessary
Hepatic Impairment
Mild to moderate impairment: Dose adjustment not necessary
Safety & efficacy not established
Depression
Transdermal: 6 mg
The overall frequency of adverse reactions and of certain types of adverse reactions was increased in elderly patients compared with nonelderly patients
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
>10%
Application site reaction (24%)
1-10%
Hypotension (3-10%)
Diarrhea (9%)
Xerostomia (8%)
Weight loss (5%)
Dyspepsia (4%)
Rash (4%)
Pharyngitis (3%)
Sinusitis (3%)
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 older than 24 years. A slight decrease in suicidal thinking was seen in adults older than 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. Patients should be monitored during initial 1-2 months of therapy and during 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
Contraindicated in patients < 12 years (increased risk of hypertensive crisis)
Contraindications
Hypersensitivity
Concurrency with SSRIs, SNRIs, TCAs, bupropion, meperidine, analgesic agents, dextromethorphan, tramadol, methadone, St. John's wort, mirtazapine, cyclobenzaprine, oral selegiline, other MAOIs, sympathomimetic amines, propoxyphene, cold products, weight-reducing preparations that contain vasoconstrictors, carbamazepine, oxcabazapine, and food supplements containing tyrosine, phenylalanine, tryptophan, or caffeine
<12 years of age
Beginning therapy with contraindicated drug < 2 weeks after stopping transdermal selegiline
General anesthesia
Pheochromocytoma
Cautions
Dietary modifications required for patients using 9 mg/24 hr & 12 mg/24 hr patch
Clinical worsening & suicide ideation may occur despite medication in adolescents & young adults (18-24 years)
Compulsive behavior may occur in patients prescribed dopaminergic agents
Orthostatic hypotension may occur with transdermal product
Use caution in hepatic and renal impairment (safety and efficacy not established)
Avoid exposing selegiline transdermal application site to external sources of direct heat (ie, heating pads, electric blankets, heat lamps, saunas, hot tubs, heated water bed, and prolonged direct sunlight)
Use caution in patients with history of mania; activation of mania/hypomania may occur
Monitor blood pressure when used concomitantly with the drugs buspirone, buspirone, amphetamines, or cold products or weight-reducing preparations that contain sympathomimetic amines (e.g., pseudoephedrine, phenylephrine, phenylpropanolamine, and ephedrine)
Development of a potentially life-threatening serotonin syndrome reported with concomitant use of MAOIs with serotonergic drugs; monitor and discontinue therapy if symptoms occur
Selegiline inhibits catabolism of dietary amines, such as tyramine, and has the potential to produce hypertensive crisis following ingestion oftyramine-rich foods or beverages; discontinue therapy if symptoms occur
Pregnancy & Lactation
Pregnancy Category: C
Lactation: unknown; 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.Pharmacology
Mechanism of Action
Irreversible selective MAO-B inhibitor. The inhibitor causes a decrease in the metabolism of dopamine; selegiline may also increase dopaminergic activity by inhibiting dopamine reuptake at the synapse; transdermal administration can attain higher selegiline blood levels and can effectively inhibit both MAO-A and MAO-B, which in turn blocks catabolism of other centrally active amine neurotransmitters
Pharmacokinetics
Absorption: 25-30%
Distribution: rapid to all body tissues
Protein Bound: 90%
Metabolism: CYP2B6, CYP3A4, CYP2A6, CYP1A2, CYP2C8, CYP2D6
Excretion: Urine (10%), feces (2%)
Images
Patient Handout
Formulary
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