entacapone

Class




  • Antiparkinson agent




Entacapone


Commonly Prescribed for


(FDA approved in bold)



  • Parkinsonism, including Parkinson’s disease (PD)



Entacapone


How the Drug Works



  • Highly selective peripherally acting inhibitor of catechol-O-methyltransferase (COMT), an important enzyme in dopamine metabolism. Use with levodopa/carbidopa enables more levodopa to enter the brain and prevents the end-of-dose wearing-off seen in PD. Entacapone has less activity on COMT in the brain, meaning the drug is not considered centrally active



Entacapone


How Long Until It Works



  • PD – hours-weeks



Entacapone


If It Works



  • PD – a majority (58%) of patients taking 800 mg or more per day of levodopa will lower levodopa dose, on average by 25% of the total after starting entacapone



Entacapone


If It Doesn’t Work



  • If end-of-dose wearing-off does not improve with entacapone and levodopa, decrease the dosing interval, add a dopamine agonist, monoamine oxidase B (MAO-B) inhibitor or consider neurosurgical options. For sudden, unpredictable wearing–off, consider apomorphine



Entacapone


Best Augmenting Combos for Partial Response or Treatment-Resistance



  • Entacapone is used only as an adjunctive medication in PD with levodopa
  • For dyskinesias, lower dose of levodopa or add a dopamine agonist
  • Younger patients with bothersome tremor: anticholinergics may help
  • For severe motor fluctuations and/or dyskinesias with good “on” time, functional neurosurgery is an option
  • Amantadine may help suppress dyskinesias, although benefit is often short-lived
  • Depression is common in PD and may respond to low dose SSRIs
  • Cognitive impairment/dementia is common in mid-late stage PD and may improve with acetylcholinesterase inhibitors



Entacapone


Tests



  • None required



Adverse Effects (AEs)




Entacapone


How Drug Causes AEs



  • COMT inhibition increases the level and duration of action of levodopa



Entacapone


Notable AEs



  • (Entacapone alone) Diarrhea (usually mild-moderate), dyspnea, weakness. May increase levodopa-related AEs such as dyskinesias, nausea, orthostatic hypotension, and hallucinations



Entacapone


Life-Threatening or Dangerous AEs



  • Rare cases of rhabdomyolysis, unclear if related to entacapone. It is unclear if non-ergot medications such as entacapone that increase dopaminergic activity predispose to the fibrotic complications (i.e., pleural thickening, retroperitoneal fibrosis) seen with ergot agonists



Entacapone


Weight Gain



  • Unusual



Entacapone


Sedation



  • Unusual



Entacapone


What to Do About AEs



  • Many AEs are related to increase in levodopa effect. Reduce levodopa dose. Take after meals to reduce nausea. This may reduce the peak dose and AEs, but delays effect and reduces effectiveness

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

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