Name the category.
Antiparkinson Agents
Name the main drug.
Selegiline
Describe the mechanism of action.
Nonselective inhibition of monoamine oxidase → ↓ breakdown of epinephrine, norepinephrine, serotonin, and dopamine → ↑ levels of epinephrine, norepinephrine, serotonin, and dopamine
Selegiline: selective MAO-B inhibitor → mainly ↓ breakdown of dopamine → ↑ levels of dopamine
List the indications.
Major depressive disorder (third- or fourth-line therapy): particularly effective treatment for atypical depression
Parkinson disease: selegiline (as an adjunct to carbidopa-levodopa)
Anxiety
List side effects.
CNS stimulation
Sexual dysfunction
Orthostatic hypotension
Weight gain
Hypertensive crisis with ingestion of foods containing tyramine
Examples: aged cheeses, smoked/cured meats, alcoholic beverages (especially beer and red wine), dried fruits, fava beans, chocolate
Tyramine stimulates the sympathetic nervous system by releasing other neurotransmitters, such as noradrenaline, from vesicles into the synaptic cleft.
List drug interactions.
risk of serotonin syndrome if used concomitantly with other serotonergic drugs, including linezolid, SSRIs, TCAs, meperidine, dextromethorphan, and St. John’s wort
Describe additional important considerations.
Before starting new serotonergic drugs or ceasing dietary restrictions (e.g., foods containing tyramine), MAOI therapy has to be stopped for at least 2 weeks.
Rarely used due to poor side-effect profile
For the treatment of depression, selegiline is available as a transdermal patch (the oral form is only used for Parkinson disease).
Last changed2 years ago