THERAPEUTICS

Brands

• Neupro

Generic?

• No

Class

• Antiparkinson agent

Commonly Prescribed for

(FDA approved in bold)

• Symptoms and signs of Parkinson’s disease (PD)

• Moderate to severe primary restless legs syndrome (RLS)

• Depression

How the Drug Works

• Dopamine agonist, with high affinity for D1, D2, D3 (ratio 1:12:387) receptors. It binds weakly to α2-adrenergic receptors. The antiparkinson action is likely due to D2 agonism within the caudate-putamen. High affinity to D3 receptors might affect impulse control and dyskinesia. The mechanism of action for RLS is probably related to D2 or D3 receptor agonism

How Long Until It Works

• PD: weeks

• RLS: days to weeks

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

• RLS: safe for long-term use with dose adjustments

If It Doesn't Work

• PD: bradykinesia, gait, and tremor should improve. Non-motor symptoms including orthostatic hypotension, depression, and bladder dysfunction do not improve. If the patient has significantly impaired functioning, add carbidopa-levodopa

• RLS: rule out peripheral neuropathy, iron deficiency, thyroid disease. Change to another drug such as a benzodiazepine. Gabapentin enacarbil (not gabapentin) may also be beneficial. In severe cases consider opioids

Best Augmenting Combos for Partial Response or Treatment-Resistance

• For suboptimal effectiveness add carbidopalevodopa with or without a catechol-Omethyltransferase (COMT) inhibitor. Monoamine oxidase (MAO)-B inhibitors may also be beneficial

• For severe motor fluctuations and/or dyskinesias with good “on” time, functional neurosurgery is an option

• For RLS, can change to a different dopamine agonist (pramipexole, ropinirole, carbidopa-levodopa) or add another drug such as a clonazepam or gabapentin enacarbil. In severe cases consider opioids

Tests

• None required

ADVERSE EFFECTS (AEs)

How the Drug Causes AEs

• Direct effect on systemic dopamine receptors