THERAPEUTICS

Brands

• Azilect

Generic?

• Yes

Class

• Antiparkinson agent

Commonly Prescribed for

(FDA approved in bold)

• Parkinson's disease (PD)

How the Drug Works

• Selectively blocks monoamine oxidase type B (MAO-B) and inhibits metabolism of dopamine, increasing its effectiveness. At higher doses, may affect MAO-A as well as MAO-B and inhibit metabolism of norepinephrine, serotonin, and tyramine, as well as dopamine

• It also exerts neuroprotective effects in preclinical studies

How Long Until It Works

• PD: weeks

If It Works

• PD: may require dose adjustments over time or augmentation with other agents. Most PD patients will eventually require carbidopalevodopa to manage their symptoms

If It Doesn't Work

• Bradykinesia, gait, and tremor should improve. If the patient has significantly impaired functioning, consider adding a dopamine agonist and/or carbidopa-levodopa

Best Augmenting Combos for Partial Response or Treatment-Resistance

• For suboptimal effectiveness consider adding a dopamine agonist and/or carbidopa-levodopa with or without a catechol-O-methyl transferase (COMT) inhibitor

• 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- to late-stage PD and may improve with acetylcholinesterase inhibitors

• For patients with late-stage PD experiencing hallucinations or delusions, consider oral atypical neuroleptics (quetiapine, clozapine). Acute psychosis is a medical emergency that may require hospitalization and short-term use of neuroleptics such as low-dose haloperidol

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

• As monotherapy: flu syndrome, arthralgia, depression, dyspepsia, somnolence, hallucination, psychotic-like behavior, impulse control behaviors

• As adjunctive with levodopa: dyskinesia, accidental injury, weight loss, postural hypotension, vomiting, anorexia, arthralgia, abdominal pain, constipation, dry mouth, abnormal dream, and tenosynovitis