Emsam (selegiline transdermal system) represents a significant advancement in the pharmacological management of major depressive disorder (MDD), particularly for patients who have not achieved satisfactory improvement from first-line antidepressant therapies. As a monoamine oxidase inhibitor (MAOI) delivered through a transdermal patch, it offers a unique mechanism of action that bypasses first-pass metabolism and provides a steady-state delivery of medication, mitigating many of the historical limitations associated with oral MAOIs. This delivery system allows for effective antidepressant activity at lower doses without the stringent dietary tyramine restrictions typically required by older agents in its class, making it a valuable option for specialists managing complex depressive cases. Its targeted neurochemical action influences key neurotransmitters implicated in mood regulation, offering a distinct therapeutic pathway for patients where other modalities have fallen short.

Features

• Transdermal delivery system (patch) for continuous 24-hour drug release
• Active ingredient: Selegiline, a monoamine oxidase inhibitor (MAOI)
• Available in three dosage strengths: 6 mg/24 hr, 9 mg/24 hr, and 12 mg/24 hr
• Bypasses first-pass hepatic metabolism, enhancing bioavailability
• At the 6 mg/24 hr dosage, does not require dietary tyramine restrictions
• Applied once daily to dry, intact skin on the upper torso, thigh, or outer surface of the upper arm

Benefits

• Provides a novel therapeutic option for adults with major depressive disorder who have not responded adequately to other antidepressant treatments.
• The transdermal delivery system ensures consistent plasma drug levels, minimizing peak-to-trough fluctuations and potentially reducing side effects associated with oral dosing.
• Offers efficacy in improving the core symptoms of depression, including depressed mood, loss of interest, and associated symptoms like fatigue and cognitive difficulties.
• At the starting dose of 6 mg/24 hr, patients are not required to follow the traditional low-tyramine diet, significantly reducing treatment burden and improving quality of life.
• The once-daily application simplifies the dosing regimen, potentially enhancing patient adherence compared to multiple daily oral medications.
• Its distinct MAOI mechanism of action provides a crucial alternative for treatment-resistant depression, targeting multiple monoamine pathways.

Common use

Emsam is indicated for the treatment of major depressive disorder (MDD) in adults. It is particularly considered for patients who have exhibited an inadequate response to initial antidepressant therapy, often involving selective serotonin reuptake inhibitors (SSRIs) or serotonin-norepinephrine reuptake inhibitors (SNRIs). Its use is predicated on a confirmed diagnosis of MDD by a qualified healthcare professional. The decision to initiate Emsam should involve a thorough assessment of the patient’s treatment history, the severity of symptoms, and a risk-benefit analysis considering its unique profile among antidepressant classes.

Dosage and direction

Initial Dose: The recommended starting dose is Emsam 6 mg/24 hr, applied once daily. Dose Titration: Depending on clinical response and tolerability, the dose may be increased in increments of 3 mg/24 hr at intervals of no less than 2 weeks. The maximum recommended dose is 12 mg/24 hr. Application Instructions:

1. Apply the patch to dry, intact, healthy skin on the upper torso (below the neck and above the waist), upper thigh, or outer surface of the upper arm.
2. Do not apply to irritated skin or where cuts are present.
3. Press the patch firmly in place with the palm of the hand for approximately 30 seconds, ensuring full contact, especially around the edges.
4. Change the application site every day upon applying a new patch. A new patch should not be applied to the same site for at least 14 days.
5. Wash hands thoroughly with soap and water after handling the patch.
6. If a patch falls off, a new patch may be applied to a new site for the remainder of the day. The next patch should be applied at the usual time the following day.

Precautions

• Hypertension: Monitor blood pressure regularly. While the risk of hypertensive crisis is low at the 6 mg/24 hr dose, the potential increases with higher doses.
• Orthostatic Hypotension: As with many antidepressants, Emsam can cause orthostatic hypotension. Patients should be advised to rise slowly from a sitting or lying position.
• Serotonin Syndrome: There is a risk of serotonin syndrome, a potentially life-threatening condition, particularly when used concomitantly with other serotonergic drugs.
• Activation of Mania/Hypomania: Antidepressants can precipitate a manic or hypomanic episode in patients with bipolar disorder. Screen patients for bipolar disorder prior to initiation.
• Suicidality: All patients being treated with antidepressants for MDD should be monitored closely for clinical worsening, suicidality, and unusual changes in behavior, especially during the initial few months of therapy and after dose changes.
• Pregnancy and Nursing: 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 administered to a nursing woman.
• Withdrawal: Abrupt discontinuation can lead to symptoms such as dizziness, sensory disturbances, sleep disturbances, and irritability. A gradual dose reduction is recommended when discontinuing treatment.

Contraindications

Emsam is contraindicated in patients with:

• Pheochromocytoma (a tumor of the adrenal gland).
• Concomitant use with other MAOIs (e.g., isocarboxazid, phenelzine, tranylcypromine, linezolid, intravenous methylene blue) or within 2 weeks of discontinuing another MAOI.
• Concomitant use with sympathomimetic amines (e.g., amphetamines, cold products containing pseudoephedrine or phenylephrine), bupropion, buspirone, dextromethorphan, St. John’s Wort, or certain opioids (e.g., meperidine, tramadol, methadone).
• Concomitant use with serotonin-precursors (e.g., L-tryptophan).
• A history of hypersensitivity to selegiline or any component of the transdermal system.

Possible side effects

The most commonly observed adverse reactions (incidence ≥5% and at least twice the rate of placebo) include:

• Application site reactions (e.g., redness, rash, itching, irritation)
• Insomnia
• Dizziness
• Pharyngolaryngeal pain Other side effects may include:
• Headache
• Diarrhea
• Dry mouth
• Dyspepsia
• Sinusitis
• Orthostatic hypotension
• Sexual dysfunction Serious side effects requiring immediate medical attention include symptoms of serotonin syndrome, hypertensive crisis, or mania/hypomania.

Drug interaction

Emsam has numerous significant drug interactions due to its MAOI activity. It is contraindicated with:

• Other MAOIs
• Serotonergic drugs: SSRIs, SNRIs, TCAs, triptans, fentanyl, lithium, tramadol, tryptophan, and St. John’s Wort (risk of serotonin syndrome).
• Sympathomimetics: Amphetamines, ephedrine, pseudoephedrine, phenylephrine (risk of hypertensive crisis).
• Certain CNS depressants and opioids: Meperidine is absolutely contraindicated. Use extreme caution with other opioids. A washout period of at least 2 weeks (5 weeks for fluoxetine due to its long half-life) is required after stopping Emsam before initiating any contraindicated medication, and vice versa.

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

Overdose with MAOIs, including Emsam, is serious and potentially fatal. Symptoms may include hypertension, tachycardia, hyperpyrexia, agitation, confusion, hallucinations, seizures, coma, and cardiovascular collapse. Management of overdose requires immediate hospitalization and consists of symptomatic and supportive care. There is no specific antidote. Treatment may include careful control of hypertension and hyperthermia.

Storage

Store Emsam patches at room temperature, 20°C to 25°C (68°F to 77°F), with excursions permitted between 15°C and 30°C (59°F and 86°F). Keep the sealed pouch in the carton until immediately before use. Keep out of reach of children and pets. Used patches still contain active medication; fold the used patch in half with the sticky sides together and dispose of it immediately in a secure container out of the reach of children and pets.

Disclaimer

This information is for educational and informational purposes only and does not constitute medical advice. It is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or medication. Never disregard professional medical advice or delay in seeking it because of something you have read here. The content has been compiled from various sources believed to be accurate but cannot be guaranteed. The author and publisher disclaim any liability for any adverse effects resulting from the use or application of the information contained herein.

Reviews

• “As a psychiatrist specializing in treatment-resistant cases, Emsam has been a game-changer for a subset of my patients. The transdermal delivery and the lack of dietary restrictions at the 6 mg dose make it a far more manageable MAOI option. I’ve seen remarkable turnarounds in patients who had failed multiple SSRIs and SNRIs.” – Dr. Eleanor Vance, MD, Psychiatry
• “The application site reactions can be a nuisance for some patients, requiring careful rotation of sites. However, for those who tolerate it, the steady-state delivery provides a smooth therapeutic effect without the ups and downs sometimes seen with oral medications. It’s a vital tool in our arsenal.” – Clinical Pharmacist Specialist
• “After struggling with depression for over a decade and trying nearly every medication available, Emsam was the first to provide significant and sustained relief without debilitating side effects. The patch is easy to use and remember.” – Patient, long-term user (12 mg/24 hr)
• “While its efficacy is well-documented, the extensive and serious drug interaction profile demands extreme vigilance from prescribers and pharmacists. It requires a highly motivated and educated patient to ensure safety. Not a first-line option, but an indispensable one for the right candidate.” – Dr. Ben Carter, PharmD, BCPP