Selegiline

Information about Selegiline

Selegiline is an inhibitor of monamine oxidase used in the treatment of depression and as adjunctive therapy in combination with levodopa and carbidopa in the therapy of Parkinson disease. 

Selegiline structure

Liver safety of Selegiline

Selegiline has been associated with a low rate of serum enzyme elevations during treatment, but has not been linked to instances of clinically apparent acute liver injury. 

Mechanism of action of Selegiline

Selegiline (se le' ji leen) is a specific inhibitor of monamine oxidase (MAO) type B, which is a major enzyme in the pathway of dopamine and levodopa metabolism.  As a result, selegiline results in an increase in the bioavailability of levodopa, enhancing and increasing the duration of its effects in Parkinson disease.  Selegiline is also an antidepressant, its mechanism of action being inhibition of dopamine reuptake from the synaptic cleft. 

FDA approval information for Selegiline

Selegiline was approved for use in the United States in 2006, the first MAO-B inhibitor approved for use in the therapy of Parkinson disease as an adjunct to levodopa therapy. 

Dosage and administration for Selegiline

Selegiline is available in capsules and tablets of 5 mg generically and under the brand name Eldepryl, the typical dose being 10 mg daily in two divided doses.  It is also available in oral disintegrating tablets of 1.25 mg under the brand name Zelapar, which is given once or twice daily.  Transdermal patches of selegiline in amounts of 6, 9 and 12 mg/24 hours are available under the brand name Emsam for treatment of depresssion, the usual dose being 6 to 12 mg daily. 

Selegiline 3-D

Side effects of Selegiline

Common side effects include headache, nausea, dizziness, agitation, delusions, insomnia, orthostatic hypotension, dry mouth, headache and gastrointestinal upset – most of which are attributable to enhanced dopaminergic effects.  In higher doses, selegiline can also inhibit MAO-A and, similar to the nonspecific MAO inhibitors, cause increased susceptibility to dietary tyramine inducing hypertensive crises (“cheese effect”).

The following are antidepressant subclasses and drugs

MAO Inhibitors Isocarboxazid, Phenelzine, Tranylcypromine

SNRIs Duloxetine, Levomilnacipran, Venlafaxine

SSRIs Citalopram, Escitalopram, Fluoxetine, Fluvoxamine, Paroxetine, Sertraline, Vilazodone, Vortioxetine

Tricyclics Amitriptyline, Amoxapine, Clomipramine, Desipramine, Doxepin, Imipramine, Nortriptyline, Protriptyline, Trimipramine

Miscellaneous Bupropion, Flibanserin, Mirtazapine, Nefazodone, Trazodone

• Dailymed label info on Selegiline
• FDA Selegiline