Class
- Monoamine oxidase type B (MAO-B) inhibitor
Selegiline
Commonly Prescribed for
(FDA approved in bold)
- Parkinson’s disease (PD)
- Major depressive disorder, treatment-refractory (patch only)
- Anxiety disorders
- Alzheimer’s and other dementias
- Migraine
Selegiline
How the Drug Works
- Selectively blocks monoamine oxidase type B (MAO-B) and inhibits metabolism of dopamine, increasing its effectiveness. At higher doses, starts to affect MAO-A as well as -B and inhibits metabolism of norepinephrine, serotonin, and tyramine, as well as dopamine
Selegiline
How Long Until It Works
- PD – weeks
- Depression, anxiety: usually months
Selegiline
If It Works
- PD – may require dose adjustments over time or augmentation with other agents. Most PD patients will eventually require carbidopa-levodopa to manage their symptoms
Selegiline
If It Doesn’t Work
- Bradykinesia, gait, and tremor should improve. If the patient has significantly impaired functioning, add carbidopa-levodopa with or without a dopamine agonist
Selegiline
Best Augmenting Combos for Partial Response or Treatment-Resistance
- For suboptimal effectiveness, add carbidopa-levodopa with or without a COMT inhibitor or a dopamine agonist
- For younger patients with bothersome tremor: anticholinergics may help
- For severe motor fluctuations and/or dyskinesias with good “on” time, functional neurosurgery is an option
- Cognitive impairment/dementia is common in mid-late stage PD and may improve with acetylcholinesterase inhibitors
- For patients with late-stage PD experiencing hallucinations or delusions, consider oral atypical neuroleptics (quetiapine, olanzapine, clozapine). Acute psychosis is a medical emergency that may require hospitalization and short-term use of neuroleptics
Selegiline
Tests
- Monitor for any changes in blood pressure
Adverse Effects (AEs)
Selegiline
How Drug Causes AEs
- Increases concentration of peripheral and CNS dopamine. At higher doses affects serotonin and norepinephrine levels
Selegiline
Notable AEs
- Nausea, hallucinations, confusion, lightheadedness, loss of balance, insomnia, orthostatic hypotension, hypertension, weight gain
Selegiline
Life-Threatening or Dangerous AEs
- Hypertensive crisis, especially at higher doses that prevent breakdown of tyramine. Tyramine-containing foods include aged cheeses, liver, sauerkraut, cured and processed meats, soy, alcohol (especially chianti wine and vermouth), and avocado
Selegiline
Weight Gain
- Common
Selegiline
Sedation
- Unusual
Selegiline
What to Do About AEs
- Lower the dose or change to alternative PD medications
Selegiline
Best Augmenting Agents for AEs
- Orthostatic hypotension: adjust dose or stop antihypertensives, add supplemental salt, and consider fludrocortisone or midodrine
