Selegiline oral (ELDEPRYL)
Selegiline oral (ELDEPRYL)
Oral selegiline, approved for Parkinson’s disease, does not inhibit MAO-A to the extent needed for antidepressant effect.
Selegiline transdermal (EMSAM)
Oral selegiline, at doses used for treatment of Parkinson’s disease, is a selective inhibitor of MAO-B, which breaks down dopamine (DA). Oral selegiline at recommended doses does not inhibit MAO-A, making it ineffective for depression. It is necessary to block MAO-A to keep norepinephrine and serotonin from being broken down (oxidized).
The transdermal formulation of selegiline (EMSAM) allows the drug to achieve higher levels in the brain (where MAO-A breaks down serotonin) than in the gut (where MAO-A breaks down dietary tyramine).
Transdermal selegiline is the only MAOI available in the US for the treatment of depression that does not require dietary tyramine restriction at the clinically effective daily dose of 6 mg However, at higher doses, dietary restriction of tyramine is recommended.
Metabolism of selegiline produces a tiny amount of methamphetamine, which blocks dopamine reuptake and may contribute to the antidepressant benefit. The methamphetamine metabolite may produce a false positive on drug screens. Selegiline is not a controlled substance.
Transdermal selegiline is the only MAOI available in the US for the treatment of depression that does not require dietary tyramine restriction at the clinically effective daily dose of 6 mg However, at higher doses, dietary restriction of tyramine is recommended.
Metabolism of selegiline produces a tiny amount of methamphetamine, which blocks dopamine reuptake and may contribute to the antidepressant benefit. The methamphetamine metabolite may produce a false positive on drug screens. Selegiline is not a controlled substance.