THERAPEUTICS

Brands

• Zelapar, Eldepryl, Emsam

Generic?

• Yes (as oral)

Class

• Antiparkinson agent

Commonly Prescribed for

(FDA approved in bold)

• Parkinson's disease (PD)

• Major depressive disorder, treatmentrefractory (patch only)

• Restless legs syndrome

• Anxiety disorders

• Alzheimer's and other dementias

• Migraine

How the Drug Works

• Selectively and irreversibly blocks monoamine oxidase type B (MAO-B) and increases extrastriatal extracellular dopamine levels. MAO-B is inhibited for at least 24 hours and the activity returns to baseline after 2 weeks. At higher doses, starts to affect MAO-A as well as MAO-B and inhibits metabolism of norepinephrine, serotonin, and tyramine, as well as dopamine

How Long Until It Works

• PD: weeks

• Depression, anxiety: usually months

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

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

Best Augmenting Combos for Partial Response or Treatment-Resistance

• For suboptimal effectiveness, add carbidopa-levodopa with or without a catechol-O-methyl transferase (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

Tests

• Monitor for any changes in blood pressure

ADVERSE EFFECTS (AEs)

How the Drug Causes AEs

• Increases concentration of peripheral and CNS dopamine. At higher doses affects serotonin and norepinephrine levels

Notable AEs

• Nausea, hallucinations, confusion, lightheadedness, loss of balance, insomnia, orthostatic hypotension, hypertension, weight gain

Life-Threatening or Dangerous AEs

• Hypertensive crisis, especially at higher doses that prevent breakdown of tyramine (via MAO-A mostly). Tyramine-containing foods include aged cheeses, liver, sauerkraut, cured and processed meats, soy, alcohol (especially chianti wine and vermouth), and avocado