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Monoamine Oxidase Inhibitor (MAO-B Selective)

Selegiline | Eldepryl

Clinical Overview

Selegiline is a selective MAO-B inhibitor available in oral and transdermal formulations. At low oral doses, it selectively inhibits MAO-B and is used as adjunctive therapy in Parkinson’s disease. The transdermal patch (Emsam) delivers higher doses that inhibit both MAO-A and MAO-B, making it effective for treatment-resistant depression with potentially fewer dietary restrictions at lower patch strengths.

Primary Clinical Applications

Oral selegiline is indicated as adjunctive therapy in Parkinson’s disease to extend the duration of levodopa effects. The transdermal patch (Emsam) is indicated for major depressive disorder, particularly treatment-resistant cases. The different formulations have distinct indications and dosing requirements.

Mechanism and Clinical Benefits

At low oral doses (≤10 mg daily), selegiline selectively inhibits MAO-B, which metabolizes dopamine, thereby extending dopamine’s action in Parkinson’s disease. At higher doses or with transdermal delivery, it also inhibits MAO-A, providing antidepressant effects by increasing serotonin and norepinephrine levels.

Clinical Considerations

The transdermal formulation bypasses first-pass metabolism, allowing for more predictable dosing and potentially fewer dietary restrictions at lower patch strengths. However, higher patch doses require the same dietary precautions as other MAOIs. The oral formulation has metabolites with amphetamine-like properties that may cause insomnia or agitation.

Prescribing Information

Dosing & Administration

Parkinson’s Disease (Oral):

  • Dose: 5 mg twice daily with breakfast and lunch
  • Maximum: 10 mg daily
  • ODT (Zelapar): 1.25 mg once daily, may increase to 2.5 mg daily

Depression (Transdermal Patch – Emsam):

  • Initial: 6 mg/24 hours patch
  • Range: 6-12 mg/24 hours
  • Maximum: 12 mg/24 hours
  • Dietary restrictions: Required for 9 mg/24 hours and 12 mg/24 hours patches

Administration:

  • Oral: With meals, avoid evening doses
  • Patch: Apply to dry, intact skin on upper torso, thigh, or outer upper arm
  • Patch rotation: Apply to different site each day

Indications

  • Oral: Adjunctive therapy in Parkinson’s disease
  • Transdermal: Major depressive disorder

Contraindications

  • Hypersensitivity to selegiline
  • Transdermal: Use with other MAOIs, SSRIs, SNRIs, tricyclics
  • Transdermal: Use with meperidine, tramadol, methadone
  • Transdermal: Use with dextromethorphan, St. John’s wort
  • Pheochromocytoma

Warnings & Precautions

  • Boxed Warning (Transdermal): Increased risk of suicidal thoughts and behavior in patients under 25 years
  • Dietary restrictions: Required for higher-dose patches (9-12 mg/24 hours)
  • Hypertensive crisis: Risk with tyramine-containing foods (higher patches)
  • Drug interactions: Extensive interactions with transdermal formulation
  • Application site reactions: Common with transdermal patch
  • Insomnia: Due to amphetamine-like metabolites (oral)

Drug Interactions

  • Levodopa: May enhance effects and side effects
  • Antidepressants: Contraindicated with transdermal formulation
  • Sympathomimetics: Risk of hypertensive crisis
  • Meperidine: Contraindicated – risk of serotonin syndrome
  • Tyramine-rich foods: Restrictions needed for higher-dose patches

Adverse Reactions

Oral (Parkinson’s):

  • Nausea, dizziness, abdominal pain, dry mouth
  • Insomnia, hallucinations, confusion

Transdermal (Depression):

  • Application site reactions, headache, insomnia, diarrhea
  • Dry mouth, dyspepsia, rash

Serious:

  • Hypertensive crisis (higher patches), serotonin syndrome

Special Populations

  • Elderly: Start with lower doses, monitor for confusion
  • Hepatic Impairment: Use caution, may require dose reduction
  • Pregnancy: Category C – use only if benefits outweigh risks
  • Patch application: Rotate sites, avoid heat exposure
  • Dietary restrictions: Only required for 9-12 mg/24 hour patches
Medical Disclaimer: This information is for educational purposes only and is not intended as medical advice. Always consult with qualified healthcare professionals before making any treatment decisions. Individual patient circumstances may vary significantly.