ropinirole

Class




  • Dopamine agonist, non-ergot




Ropinirole


Commonly Prescribed for


(FDA approved in bold)



  • Parkinson’s disease (PD)
  • Restless legs syndrome (RLS)



Ropinirole


How the Drug Works



  • Dopamine agonist, with high affinity for the D2 receptor. This action is likely the main reason for effectiveness in PD. Also binds with high affinity to D3 receptors, but the importance of this is unclear. The mechanism of action for RLS is probably related to D2 receptor agonism



Ropinirole


How Long Until It Works



  • PD – weeks
  • RLS – days to weeks



Ropinirole


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



Ropinirole


If It Doesn’t Work



  • PD – Bradykinesia, gait and tremor should improve. Non-motor symptoms including autonomic symptoms such as postural hypotension, depression, and bladder dysfunction do not improve. If the patient has significantly impaired functioning, add carbidopa-levodopa with or without ropinirole
  • RLS – Rule out peripheral neuropathy, iron deficiency, thyroid disease. Change to another drug such as a benzodiazepine. Antiepileptic drugs (AEDs) such as gabapentin or carbamazepine may also be beneficial. In severe cases consider opioids



Ropinirole


Best Augmenting Combos for Partial Response or Treatment-Resistance



  • For suboptimal effectiveness add carbidopa-levodopa with or without a COMT inhibitor. MAO-B inhibitors may also be beneficial
  • 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
  • Depression is common in PD and may respond to SSRIs
  • 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, withdraw ropinirole and consider oral atypical neuroleptics (quetiapine, olanzapine, clozapine). Acute psychosis is a medical emergency that may require hospitalization
  • For RLS, can change to a different dopamine agonist or add another drug such as a benzodiazepine. AEDs such as gabapentin or carbamazepine may be beneficial. In severe cases consider opioids



Ropinirole


Tests



  • None required



Adverse Effects (AEs)




Ropinirole


How Drug Causes AEs



  • Direct effect on dopamine receptors



Ropinirole


Notable AEs



  • Nausea/vomiting, dizziness, hallucination, constipation, somnolence, abdominal pain/discomfort, diaphoresis, anxiety, viral infection, pharyngitis, dyskinesias, and orthostatic hypotension



Ropinirole


Life-Threatening or Dangerous AEs



  • May cause somnolence or sudden-onset sleep, often without warning. Occurs more often than with ergot agonists or carbidopa-levodopa. Rare syncope or cardiac arrhythmias, most commonly bradycardia



Ropinirole


Weight Gain



  • Unusual



Ropinirole


Sedation



  • Common



Ropinirole


What to Do About AEs



  • Nausea can be problematic when initiating drug – titrate slowly
  • Hallucinations or delusions may require stopping the medication
  • Warn patients about the risks of sleeping while driving

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Feb 16, 2017 | Posted by in PHARMACY | Comments Off on ropinirole

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