Selegiline Transdermal

|Selegiline Transdermal

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Selegiline Transdermal

Pronouncation: (se-LEJ-i-leen transdermal)
Class: Antidepressant

Trade Names:
- Transdermal system 6 mg per 24 hr (20 mg per 20 cm 2 )
- Transdermal system 9 mg per 24 hr (30 mg per 30 cm 2 )
- Transdermal system 12 mg per 24 hr (40 mg per 40 cm 2 )

Mechanism of Action


Potentiation of monoamine neurotransmitter activity in the CNS resulting from inhibition of MAO activity is suspected.



Following dermal application, 25% to 30% of the selegiline content is delivered systemically over 24 hr. The degree of absorption may be one-third higher than amounts of 6 to 12 mg per 24 hr. Because extensive first-pass metabolism occurs with oral administration, substantially higher exposure to selegiline and lower exposure to metabolites occur with transdermal dosing.


Plasma protein binding is approximately 90%.


The major enzymes involved with selegiline metabolism appear to be CYP2B6, CYP2C9, and CYP3A4/5, with CYP2A6 having a minor role.


Urine and fecal elimination account for about 10% and 2%, respectively, of a dermal dose. At least 63% of the dose is not absorbed.

Special Populations

Renal Function Impairment

No adjustment of dermal dose is required with renal function impairment.

Hepatic Function Impairment

No adjustment of dermal dose is required with moderate liver function impairment.

Indications and Usage

Treatment of major depressive disorder (MDD).


Coadministration with any of the following: analgesic agents (eg, tramadol, methadone, propoxyphene), bupropion, carbamazepine, cocaine or local anesthetics, cyclobenzaprine, dextromethorphan, dual serotonin and norepinephrine reuptake inhibitors (eg, venlafaxine), meperidine, mirtazapine, oral selegiline or other MAO inhibitors (eg, phenelzine), oxcarbazepine, SSRIs (eg, fluoxetine), St. John"s wort, sympathomimetic amines (eg, amphetamine), tricyclic antidepressants (eg, amitriptyline), vasoconstrictors (eg, pseudoephedrine). Patients with pheochromocytoma; hypersensitivity to any component of the product. Patients should not undergo elective surgery requiring general anesthetics. Discontinue selegiline transdermal at least 10 days prior to elective surgery.

Dosage and Administration


Transdermal Recommended starting and target dose is 6 mg per 24 hr. Based on clinical judgement, the dose may be increased in increments of 3 mg per 24 hr at intervals of no less than 2 wk (max, 12 mg per 24 hr).

General Advice

  • Apply to dry, intact skin on upper torso (below the neck and above the waist), upper thigh, or outer surface of upper arm.
  • Apply to an area that is not hairy, oily, irritated, broken, scared, or calloused.
  • Do not apply to area where clothing is tight, which might cause patch to rub off.
  • Gently wash area with warm water and soap, then dry thoroughly before applying patch.
  • Wash hands thoroughly with soap and water after applying patch.
  • Remove patch after 24 hr.


Store at 68° to 77°F. Do not store outside sealed pouch.

Drug Interactions

Analgesics (eg, methadone, propoxyphene, tramadol), bupropion, carbamazepine, cocaine or local anesthetics, cyclobenzaprine, dextromethorphan, dual serotonin and norepinephrine reuptake inhibitors (eg, venlafaxine), mirtazapine, oral selegiline or other MAO inhibitors (eg, phenelzine), oxcarbazepine, St. John"s wort, SSRIs (eg, fluoxetine), sympathomimetic amines (eg, amphetamine), tricyclic antidepressants (eg, amitriptyline), vasoconstrictors (eg, pseudoephedrine)

Coadministration with selegiline is contraindicated.


Increased BP may occur.

Drugs affecting monoamine activity (eg, amphetamines, meperidine, pentazocine, SSRIs, tricyclic antidepressants)

Severe, life-threatening toxicity, including serotonin syndrome (eg, rigidity, muscle twitching, mental status change, autonomic instability), may occur.

General anesthetics

Patients should not undergo elective surgery requiring general anesthetics; discontinue selegiline transdermal at least 10 days prior to elective surgery.

Oral contraceptives

Selegiline plasma levels may be elevated, increasing the pharmacologic and adverse effects.

Tyramine-containing nutritional supplements

Should be avoided.

Laboratory Test Interactions

None well documented.

Adverse Reactions


Orthostatic hypotension (10%); low systolic BP (3%); hypertension (at least 1%).


Headache (18%); insomnia (12%); abnormal thinking, agitation, amnesia, paresthesia (at least 1%).


Rash (4%); acne, pruritus, sweating (at least 1%).


Pharyngitis (3%); taste perversion, tinnitus (at least 1%).


Diarrhea (9%); dry mouth (8%); dyspepsia (4%); anorexia, constipation, flatulence, gastroenteritis, vomiting (at least 1%).


Abnormal ejaculation (1%); dysmenorrhea, metrorrhagia, urinary frequency, UTI (at least 1%).


Ecchymosis (at least 1%).


Application site reaction (at least 2%).


Weight gain (5%); peripheral edema (at least 1%).


Myalgia, pathological fracture (at least 1%).


Sinusitis (3%); bronchitis, increased cough (at least 1%).


Chest pain, neck pain (at least 1%).



Antidepressants increased the risk of suicidal thinking and behavior in short-term studies in children and adolescents with MDD and other psychiatric disorders. Closely observe patients who are started on therapy for clinical worsening, suicidality, or unusual changes in behavior.


Category C .




Safety and efficacy not established.


No overall differences in efficacy have been noted between elderly and younger patients.

Dietary modifications

Avoid food and beverages rich in tyramine for patients taking selegiline 9 mg per 24 hr and 12 mg per 24 hr.

Hypertensive crisis

May be a risk in patients taking amine-containing medications or tyramine foods if the dose of selegiline is exceeded or if plasma levels are elevated.


Activation may occur; use with caution in patients with history of mania.

Screening for bipolar disorder

Prior to initiating treatment, adequately screen patients with depressive symptoms to determine risk of bipolar disorder.



Agitation, coma, convulsions, cool clammy skin, death, diaphoresis, dizziness, drowsiness, faintness, hallucinations, hyperactivity, hyperpyrexia, hypertension, hypotension, irritability, opisthotonos, precordial pain, rapid and irregular pulse, respiratory depression and failure, severe headache, trismus, vascular collapse.

Patient Information

  • Explain name, dose, action, possible drug interactions, and potential adverse reactions of drug.
  • Obtain patient history, including drug history and any known allergies.
  • Advise patients to read the Medication Guide before starting therapy and each time the prescription is refilled.
  • Encourage patient to discuss contents of the Medication Guide .
  • Caution patient to use the drug exactly as prescribed.
  • Instruct patient to avoid driving or other potentially hazardous activities until effect of medication is determined.
  • Instruct patients to only use 1 selegiline patch at a time.
  • Caution patient to avoid exposing application site to external sources of direct heat (eg, electric blanket, heat lamps, heating pads, hot tubs, prolonged direct sunlight, saunas).
  • Advise patient that if the patch falls off, to apply a new patch at a new site and resume previous schedule.
  • Instruct patients to get up slowly from lying or sitting position and to avoid sudden position changes to prevent postural hypotension.
  • Instruct patient as to the signs and symptoms of hypertensive crisis and to seek immediate medical attention if any signs or symptoms are present.
  • Advise women to notify health care provider if pregnant, planning to become pregnant, or breast-feeding.
  • Caution patient to not take any prescription or OTC medications, herbal preparations, or dietary supplements unless advised by health care provider.
  • Advise patient that follow-up visits may be necessary and to keep appointments.

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