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selegiline hydrochloride

Apo-Selegiline (CA), Dom-Selegiline (CA), Eldepryl, Emsam, Gen-Selegiline (CA), Novo-Selegiline (CA), Nu-Selegiline (CA), PMS-Selegiline, Zelapar

Pharmacologic class: MAO inhibitor (type B)

Therapeutic class: Antidyskinetic Pregnancy risk category C

FDA Box Warning

• Drug may increase risk of suicidal thinking and behavior in children and adolescents with major depressive disorder (MDD) and other psychiatric disorders. Anyone considering using it for MDD in a child or adolescent must balance risk with clinical need, as depression itself increases suicide risk. With patient of any age, observe closely for clinical worsening, suicidality, and unusual behavior changes when therapy begins. Advise family and caregivers to observe patient closely and communicate with prescriber as needed.

• Drug isn't approved for use in pediatric patients.


Unknown. Thought to increase dopaminergic activity by inhibiting MAO type B in nerve cells, increasing dopamine availability to brain cells.


Capsules: 5 mg

Tablets: 5 mg

Tablets (orally disintegrating): 1.25 mg

Transdermal system: 6 mg/24 hours, 9 mg/24 hours, 12 mg/24 hours

Indications and dosages

Adjunctive treatment of Parkinson's disease in patients who don't respond to carbidopa-levodopa alone

Adults: 10 mg P.O. daily in divided doses. After 2 to 3 days, attempt to reduce carbidopa-levodopa dosage (typically by 10% to 30%). Or initially, 1.25 mg (orally disintegrating tablets) P.O. daily for at least 6 weeks. May increase after 6 weeks to 2.5 mg P.O. daily based on effect and tolerability.

Major depressive disorder

Adults: Initially, apply 6 mg/24 hours patch; increase in dose increments of 2 mg/24 hours up to a maximum dose of 12 mg/24 hours at intervals of no less than two weeks, if needed.

Off-label uses

• Initial therapy for Parkinson's disease

• Alzheimer's disease

• Narcolepsy

• Adjunct in schizophrenia


• Hypersensitivity to drug or its components

• Concurrent meperidine therapy


Use cautiously in:

• patients receiving tricyclic antidepressants (TCAs), selective serotonin reuptake inhibitors (SRRIs), or dextromethorphan, carbamazepine, and analgesics such as tramadol, methadone, and propoxyphene

• patients with pheochromocytoma

• elderly patients

• pregnant or breastfeeding patients

• children.


• Give orally disintegrating tablets in the morning before breakfast; don't give food or liquid 5 minutes before and after administration.

• Give capsules or regular tablets with breakfast and lunch, but restrict foods high in tyramine (such as aged cheese, red wine, yogurt, and smoked high-protein foods).

Don't give within 14 days of TCAs or SSRIs (5 weeks for fluoxetine because of its long half-life).

• Apply patch to dry, intact skin on the upper torso (below the neck and above the waist), upper thigh, or the outer surface of the upper arm once every 24 hours.

Adverse reactions

CNS: agitation, anxiety, bradykinesia, chorea, confusion, delusions, depression, dizziness, hallucinations, headache, dyskinesias, increased akinetic involuntary movements, insomnia, lethargy, light-headedness, loss of balance, syncope, vivid dreams

CV: orthostatic hypotension, hypertension, new or increased angina, palpitations, arrhythmias

GI: nausea, diarrhea, abdominal pain, dry mouth, buccal mucosa irritation (with orally disintegrating tablets)

GU: urinary retention

Musculoskeletal: leg pain, low back pain

Other: generalized aches, weight loss


Drug-drug. Adrenergics: increased pressor response

Buspirone: elevated blood pressure

Dextromethorphan: brief episodes of psychosis or bizarre behavior

Levodopa: increased adverse reactions to levodopa

Meperidine and analgesics such as tramadol, methadone, and propoxyphene: stupor, muscle rigidity, severe agitation, fever, death

Other MAO inhibitors: hypertensive crisis

SSRIs, TCAs: severe mental status changes, CNS toxicity (with possible hyperpyrexia and death)

Drug-food. Tyramine-rich foods (such as aged cheese, red wine, yogurt, smoked high-protein foods): hypertensive crisis

Drug-herbs. Cacao: vasopressor effects

Ginseng: headache, tremor, mania

St. John's wort: life-threatening adverse reactions

Patient monitoring

• Monitor vital signs and cardiovascular status.

• Assess neurologic status and motor function. Institute safety measures as needed to prevent injury.

• Monitor weight and fluid intake and output.

• Monitor CBC and liver and kidney function tests.

Patient teaching

• Tell patient to take capsules or regular tablets with or without food, but he should avoid foods and beverages high in tyramine. Provide a list of these foods and beverages.

• Instruct patient (and caregiver as appropriate) to take orally disintegrating tablets in the morning before breakfast and not to push these tablets through the foil backing. Tell patient to peel back the backing of one or two blisters (as prescribed) with dry hands, gently remove the tablet, then immediately place the tablet on top of the tongue where it will disintegrate in seconds. Remind patient to avoid ingesting food or liquids for 5 minutes before and after taking orally disintegrating tablets.

• Inform patient to avoid tyramine-rich foods and beverages beginning on the first day of application of 9mg/24hours-or 12mg/24hours-patch and continue to avoid these foods and beverages for two weeks after a dose reduction to the 6mg/24hours-patch or following the discontinuation of the 9mg/24hours-or 12mg/24hours-patch.

• Instruct patient (and caregiver as appropriate) to monitor neurologic status and motor function and to institute safety precautions as needed to prevent injury.

• Instruct patient to move slowly when sitting up or standing, to avoid dizziness from sudden blood pressure decrease.

• Tell patient (or caregiver) that drug may cause serious interactions with many drugs. Instruct him to tell all prescribers he's taking it.

• Tell patient not to use St. John's wort without consulting with prescriber.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, foods, and herbs mentioned above.

McGraw-Hill Nurse's Drug Handbook, 7th Ed. Copyright © 2013 by The McGraw-Hill Companies, Inc. All rights reserved

selegiline transdermal

(se-le-ji-leen) ,


(trade name)


Therapeutic: antidepressants
Pharmacologic: monoamine oxidase type b inhibitors
Pregnancy Category: C


Major depressive disorder.


Following conversion by MAO to its active form, selegiline inactivates MAO by irreversibly binding to it at type B (brain) sites; this results in higher levels of monoamine neurotransmitters in the brain (dopamine, serotonin, norepinephrine).

Therapeutic effects

Decreased symptoms of depression.


Absorption: 25–30% of patch content is transdermally absorbed, blood levels are higher than those following oral administration because there is less first-pass hepatic metabolism.
Distribution: Rapidly distributes to all body tissues; crosses the blood-brain barrier.
Metabolism and Excretion: Mostly metabolized by the liver, primarily by the CYP2A6, CYP2C9, and CYP3A4/5 enzyme systems. 10% excreted in urine as metabolites, 2% in feces; negligible renal excretion of unchanged drug.
Half-life: 18–25 hr.

Time/action profile

transdermalunknown2 or more wk2 wk (after discontinuation)


Contraindicated in: Hypersensitivity;Pheochromocytoma;Concurrent selective serotonin re-uptake inhibitors (fluoxetine, paroxetine citalopram, escitalopram, and others), nonselective serotonin re-uptake inhibitors (venlafaxine, duloxetine), tricyclic antidepressants (amitriptyline, imipramine, and others), carbamazepine, oxcarbazepine, amphetamines, vasoconstrictors (ephedrine, pseudoephedrine), bupropion, meperidine, tramadol, methadone, propoxyphene, dextromethorphan, mirtazapine cyclobenzaprine, other MAO inhibitors (isocarboxazid, phenelzine, tranylcypromine), oral selegiline, sympathomimetic amines, amphetamines, cocaine, or local anesthetics with vasoconstrictors;St. John's wort;Alcohol.
Use Cautiously in: Elective surgery within 10 days; benzodiazepines, rapacuronium, fentanyl, morphine, and codeine may be used cautiously;May ↑ risk of suicide attempt/ideation especially during early treatment or dose adjustment; risk may be greater in children or adolescents (safe use in children <12 yr not established);History of mania;Dosing at 9 mg/24 hr or 12 mg/24 hr requires dietary modification (avoid foods containing large amounts of tyramine); Geriatric: May be more susceptible to orthostatic hypotension; Obstetric: Use only if benefit outweighs risk to the fetus; Lactation: Safety not established; Pediatric: Safe use in children and adolescents not established.

Adverse Reactions/Side Effects

Central nervous system

  • insomnia (most frequent)
  • abnormal thinking
  • agitation
  • amnesia
  • worsening of mania/hypomania

Ear, Eye, Nose, Throat

  • tinnitus


  • ↑ cough


  • hypertensive crisis (life-threatening)
  • chest pain
  • orthostatic hypotension
  • peripheral edema


  • diarrhea (most frequent)
  • altered taste
  • anorexia
  • constipation
  • flatulence
  • gastroenteritis
  • vomiting


  • dysmenorrhea
  • metrorrhagia
  • urinary frequency


  • application site reactions (most frequent)
  • acne
  • ecchymoses
  • pruritus
  • sweating


  • mylagia
  • neck pain
  • pathologic fracture


  • paresthesia


Drug-Drug interaction

Concurrent selective serotonin re-uptake inhibitors (fluoxetine, paroxetine, citalopram, escitalopram, and others), nonselective serotonin re-uptake inhibitors (venlafaxine, duloxetine ), tricyclic antidepressants (amitriptyline, imipramine, and others), carbamazepine, oxcarbazepine, amphetamines, vasoconstrictors (ephedrine, pseudoephedrine, phenylprolanolamine ), bupropion, meperidine, tramadol, methadone, dextromethorphan, mirtazapine, cyclobenzaprine, other MAO inhibitors (isocarboxazid, phenelzine, tranylcypromine ), oral selegiline, sympathomimetic amines, amphetamines, cocaine, or local anesthetics with vasoconstrictors ; these may all ↑ risk of hypertensive crisis. (Fluoxetine should not be used within 2 wk of initiating therapy).St. John's wort may ↑ risk of hypertensive crisis.


Transdermal (Adults) 6 mg/24 hr, if necessary, may be increased at 2-wk intervals in increments of 3 mg, up to 12 mg/24 hr.


Transdermal patch : 6 mg/24 hr, 9 mg/24 hr, 12 mg/24 hr

Nursing implications

Nursing assessment

  • Assess mental status, mood changes, and anxiety level frequently. Assess for suicidal tendencies, agitation, irritability, and unusual changes in behavior especially during early therapy. Monitor pediatric patients face-to-face weekly during first 4 wk, every other week for 4 wk, at 12 wk, and as clinically indicated during therapy. Restrict amount of drug available to patient.
  • Monitor BP and pulse rate before and frequently during therapy. Report significant changes promptly.
  • Concurrent ingestion of tyramine-rich foods and many medications may result in a life-threatening hypertensive crisis. Signs and symptoms of hypertensive crisis include chest pain, tachycardia or bradycardia, severe headache, neck stiffness or soreness, nausea and vomiting, sweating, photosensitivity, and enlarged pupils. If hypertensive crisis occurs, discontinue selegiline transdermal and administer phentolamine 5 mg or labetalol 20 mg slowly IV to control hypertension. Manage fever with external cooling. Monitor patient closely until symptoms have stabilized.

Potential Nursing Diagnoses

Ineffective coping (Indications)
Noncompliance (Patient/Family Teaching)


  • Transdermal: Apply system to dry, intact skin on the upper torso such as chest, back, upper thigh, or outer surface of the upper arm once every 24 hr at the same time each day. Avoid areas that are hairy, oily, irritated, broken, scarred, or calloused. Wash area gently with soap and warm water, rinse thoroughly. Allow skin to dry completely before application. Apply immediately after removing from package. Do not alter the system (i.e., cut) in any way before application. Remove liner from adhesive layer and press firmly in place with palm of hand for 30 sec, especially around the edges, to make sure contact is complete. Remove used system and fold so that adhesive edges are together. Only 1 selegiline patch should be worn at a time. Dispose away from children and pets. Apply new system to a different site. Wash hands thoroughly with soap and water to remove any medicine that may have gotten on them.

Patient/Family Teaching

  • Instruct patient to apply patch as directed. Advise patients and caregivers to read the Medication Guide about Using Antidepressants in Children and Teenagers. Inform patient that improvement may be noticed after 1 to several weeks of therapy. Advise patient not to discontinue therapy without consulting health care professional.
  • Caution patient to avoid alcohol and CNS depressants during and for at least 2 wk after therapy has been discontinued; they may precipitate a hypertensive crisis. Contact health care professional immediately if symptoms of hypertensive crisis develop. Patients taking 9 mg/24 hr or 12 mg/24 hr must avoid foods or beverages containing tyramine (see ) from the first day of the increased dose through 2 wk after discontinuation of selegiline transdermal therapy.
  • Advise patient to avoid exposing application site to external sources of direct heat such as heating pads, electric blankets, heat lamps, saunas, hot tubs, heated water beds, and prolonged direct sunlight.
  • May cause dizziness or drowsiness. Caution patient to avoid driving and other activities requiring alertness until response to medication is known.
  • Caution patient to change positions slowly to minimize orthostatic hypotension. Geriatric patients are at increased risk for this side effect.
  • Advise patient referred for MRI test to discuss patch with referring health care professional and MRI facility to determine if removal of patch is necessary prior to test and for directions for replacing patch.
  • Advise patients and caregivers to notify health care professional if severe headache, neck stiffness, heart racing or palpitations, anxiety, agitation, panic attacks, insomnia, irritability, hostility, aggressiveness, impulsivity, akathisia, hypomania, mania, change in behavior, worsening of depression, or suicidal ideation occur, especially during initial therapy or during changes in dose.
  • Instruct patient to consult health care professional before taking any Rx, OTC, or herbal products. Caution patient to avoid use of St. John's Wort and the analgesics meperidine, tramadol, or methadone during therapy.
  • Advise patient to notify health care professional of medication regimen before treatment or surgery. If possible, therapy should be discontinued at least 2 wk before surgery.
  • Advise patient to notify health care professional if pregnancy is planned or suspected or if breast feeding.

Evaluation/Desired Outcomes

  • Improved mood in depressed patients.
    • Decreased anxiety.
    • Increased appetite.
    • Improved energy level.
    • Improved sleep. Evaluate effectiveness of therapy periodically.
Drug Guide, © 2015 Farlex and Partners


A trademark for a preparation of the drug selegiline.
The American Heritage® Medical Dictionary Copyright © 2007, 2004 by Houghton Mifflin Company. Published by Houghton Mifflin Company. All rights reserved.


Alternative pharmacology
A prescription drug used to treat Parkinson’s disease, which has acquired currency among some practitioners of alternative medicine as an anti-ageing substance; deprenyl acts on the substantia nigra., a region of the brain that is believed to age more rapidly than others, by blocking the degradation of dopaminergic neurotransmitters.
Segen's Medical Dictionary. © 2012 Farlex, Inc. All rights reserved.
References in periodicals archive ?
Similar concerns about transdermal delivery have been expressed about EMSAM.
* Comment: In two studies of 400 outpatients with major depressive disorder, those treated with the Emsam patch for 68 weeks had significantly more improvement in a depression rating scale than did those on placebo.
However, most of those polled at the meeting indicated they would be unlikely to use transdermal selegiline (Emsam), which is manufactured by Somerset Pharmaceuticals Inc.
The product, which is being marketed under the trade name Emsam, is the first transdermal medication that the FDA has approved for treating major depression.
In three studies lasting 6, 8, or 52 weeks, treatment with 20 mg, 30 mg, and 40 mg of Emsam was significantly more effective than placebo in treating depression, based on different primary end points.