Emsam (selegiline transdermal system) represents a significant advancement in the pharmacological management of major depressive disorder (MDD), particularly for patients who have not achieved an adequate response from first-line antidepressant therapies. As a monoamine oxidase inhibitor (MAOI) delivered through a transdermal patch, Emsam offers a unique mechanism of action that bypasses many of the historical limitations and dietary restrictions associated with oral MAOIs. This delivery system provides continuous, controlled delivery of selegiline, enhancing its therapeutic profile while mitigating the risk of tyramine-induced hypertension, a classic concern with this drug class. It is specifically indicated for the treatment of MDD in adults, offering a valuable option within the antidepressant armamentarium.

Features

• Transdermal delivery system (patch) for continuous 24-hour drug administration.
• Available in three dosage strengths: 6 mg/24 hr, 9 mg/24 hr, and 12 mg/24 hr.
• Active ingredient: selegiline, a monoamine oxidase inhibitor (MAOI).
• Specifically inhibits monoamine oxidase type A (MAO-A) and monoamine oxidase type B (MAO-B) in the brain.
• Avoids first-pass hepatic metabolism, potentially reducing metabolite load and some side effects.
• The 6 mg/24 hr dosage does not require dietary modifications for tyramine.

Benefits

• Effective for Treatment-Resistant Cases: Provides a proven therapeutic option for patients who have not responded adequately to other antidepressant classes, such as SSRIs or SNRIs.
• Minimized Dietary Restrictions: At the starting dose of 6 mg/24 hr, patients are not required to follow a tyramine-restricted diet, significantly improving quality of life and adherence compared to traditional oral MAOIs.
• Bypasses GI System: Transdermal administration avoids gastrointestinal side effects like nausea that are common with orally administered antidepressants.
• Continuous Drug Delivery: Maintains stable plasma concentrations over 24 hours, minimizing peak-to-trough fluctuations and associated side effects.
• Dopaminergic Activity: As a metabolite of selegiline includes amphetamines, it may offer benefits for patients with comorbid fatigue, anhedonia, or psychomotor retardation.

Common use

Emsam is indicated for the treatment of major depressive disorder (MDD) in adult patients. It is often considered after an inadequate response to one or more trials of first-line antidepressant agents, such as selective serotonin reuptake inhibitors (SSRIs) or serotonin and norepinephrine reuptake inhibitors (SNRIs). Its unique mechanism and delivery system make it a strategic choice for psychiatrists managing complex or treatment-resistant depressive episodes.

Dosage and direction

• Initial Dose: The recommended starting dose is Emsam 6 mg/24 hr, applied once daily.
• Dose Titration: The dose may be increased in increments of 3 mg/24 hr (e.g., to 9 mg/24 hr or 12 mg/24 hr) at minimum intervals of 2 weeks, based on clinical response and tolerability.
• Maximum Dose: The maximum recommended dose is 12 mg/24 hr.
• Application Instructions:
  • Apply the 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.
  • Do not apply to irritated skin or where cuts are present.
  • Press firmly into place with the palm of the hand for approximately 30 seconds.
  • Rotate the application site with each new patch; do not apply a new patch to the same site for at least 14 days.
  • Avoid exposing the application site to external sources of direct heat (e.g., heating pads, hot tubs, prolonged direct sunlight), as this may increase the amount of drug absorbed.

Precautions

• Hypertension: As with all MAOIs, Emsam can elevate blood pressure. Blood pressure should be monitored regularly, especially following dose increases.
• Serotonin Syndrome: There is a risk of serotonin syndrome, a potentially life-threatening condition, particularly with concomitant use of other serotonergic drugs.
• Activation of Mania/Hypomania: Antidepressants can precipitate a manic or hypomanic episode in patients with bipolar disorder. Emsam should be used with caution in patients with a history of bipolar disorder.
• Suicidality: All antidepressants carry a black box warning for an increased risk of suicidal thinking and behavior in children, adolescents, and young adults. Patients of all ages should be closely monitored for clinical worsening, suicidality, or unusual changes in behavior.
• Orthostatic Hypotension: Can occur, particularly at higher doses. Patients should be advised to rise slowly from a sitting or lying position.
• Pregnancy and Lactation: Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Selegiline is excreted in human milk; caution is advised if used in nursing women.

Contraindications

Emsam is contraindicated in patients with:

• Pheochromocytoma (a tumor of the adrenal gland).
• Concomitant use with other MAOIs or within 14 days of stopping an MAOI.
• Concomitant use with sympathomimetic amines (e.g., amphetamines, cold products containing pseudoephedrine or phenylephrine), methadone, tramadol, propoxyphene, dextromethorphan, St. John’s Wort, or cyclobenzaprine.
• Concomitant use with serotonin precursors (e.g., tryptophan) or other serotonergic drugs (e.g., SSRIs, SNRIs, clomipramine, imipramine, triptans, buspirone).
• A history of hypersensitivity to selegiline or any component of the transdermal system.

Possible side effect

Common adverse reactions (incidence ≥5% and at least twice that of placebo) include:

• Application site reactions (redness, rash, irritation, itching)
• Insomnia
• Dizziness
• Pharyngitis
• Dyspepsia (indigestion)
• Dry mouth
• Diarrhea
• Sinusitis Other less common but serious side effects can include serotonin syndrome, hypertensive crisis (primarily at doses > 9 mg/24 hr), mania/hypomania, and orthostatic hypotension.

Drug interaction

Emsam has numerous significant drug interactions due to its MAOI activity. Key interactions include:

• Serotonergic Drugs: Concomitant use is contraindicated due to the high risk of serotonin syndrome. A sufficient washout period (typically 2-5 weeks depending on the drug’s half-life) is required before initiating Emsam.
• Sympathomimetics: Drugs like amphetamines, methylphenidate, and many over-the-counter decongestants (e.g., pseudoephedrine) can precipitate a hypertensive crisis.
• Meperidine, Tramadol, Methadone, Propoxyphene: Contraindicated; risk of serotonin syndrome or severe opioid toxicity (for meperidine).
• Other MAOIs: Absolute contraindication.
• Tyramine-Rich Foods/Beverages: At doses above 9 mg/24 hr, a tyramine-restricted diet is mandatory to avoid hypertensive crisis.
• TCAs and SSRIs: Contraindicated.
• Bupropion: May increase the risk of hypertension.

Missed dose

• If a dose is missed, the patient should apply the patch as soon as possible.
• However, if it is almost time for the next scheduled dose, the missed dose should be skipped and the regular dosing schedule resumed.
• Patients should not apply two patches at one time to make up for a missed dose.

Overdose

Overdosage with MAOIs, including Emsam, can be severe and potentially fatal. Symptoms may include drowsiness, dizziness, faintness, irritability, hyperactivity, agitation, severe headache, hallucinations, trismus, opisthotonos, seizures, coma, rapid and irregular pulse, hypertension, hypotension, vascular collapse, precordial pain, respiratory depression and failure, hyperpyrexia, diaphoresis, and cool, clammy skin. Management of overdose involves immediate removal of the patch, supportive care, and symptomatic treatment. There is no specific antidote.

Storage

• Store at 25°C (77°F); excursions permitted to 15°–30°C (59°–86°F).
• Keep patches in their sealed pouch until immediately before use.
• Keep out of reach of children and pets.
• Used patches should be folded so the adhesive side sticks to itself and disposed of safely out of reach of children and pets, as the patch still contains active medication.

Disclaimer

This information is for educational and professional medical reference purposes only and is not a substitute for the professional judgment of a healthcare provider in diagnosing and treating patients. The content does not cover all possible uses, directions, precautions, drug interactions, or adverse effects. The reader is advised to consult the full FDA-approved prescribing information and to exercise their own professional judgment in the care and treatment of their patients. Never disregard professional medical advice or delay in seeking it because of something you have read here.

Reviews

• “Emsam has been a game-changer for my patients with truly refractory depression. The transdermal delivery is a major advantage, and the ability to start at 6 mg without diet restrictions removes a significant barrier to MAOI use.” – Psychiatrist, 15 years experience.
• “While application site reactions can be an issue for some, the efficacy profile is impressive. It’s a vital tool in our arsenal for treatment-resistant cases where other options have failed.” – Clinical Researcher, Mood Disorders Center.
• “The need for careful management of drug interactions cannot be overstated. However, for the appropriate, carefully selected patient, Emsam can provide remarkable remission where other agents could not.” – Clinical Pharmacist Specialist in Psychiatry.