rasagiline

Class




  • Monoamine oxidase type B (MAO-B) inhibitor




Rasagiline


Commonly Prescribed for


(FDA approved in bold)



  • Parkinson’s disease (PD)
  • Alzheimer’s (AD) and other dementias



Rasagiline


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 -B and inhibit metabolism of norepinephrine, serotonin, and tyramine, as well as dopamine



Rasagiline


How Long Until It Works



  • PD – weeks



Rasagiline


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



Rasagiline


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



Rasagiline


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-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



Rasagiline


Tests



  • Monitor for any changes in blood pressure



Adverse Effects (AEs)




Rasagiline


How Drug Causes AEs



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



Rasagiline


Notable AEs



  • In studies, as monotherapy, rasagiline had fewer side effects than placebo. Nausea, hallucinations, confusion, lightheadedness, loss of balance, abdominal pain, orthostatic hypotension, weight loss are uncommon but may occur. Can exacerbate existing dyskinesias



Rasagiline


Life-Threatening or Dangerous AEs



  • Rasagiline currently has a warning regarding possible hypertensive crisis when used in combination with foods containing tyramine. Tyramine-containing foods include aged cheeses, liver, sauerkraut, cured and processed meats, soy, chianti wine, and vermouth. Recent studies however demonstrate that rasagiline has a lower tyramine sensitivity factor than selegiline, which has no tyramine warning. Therefore, it is likely safe to consume tyramine-containing foods while taking rasagiline at therapeutic doses. It is expected that the FDA will withdraw the tyramine warning in light of the tyramine sensitivity studies



Rasagiline


Weight Gain



  • Unusual



Rasagiline


Sedation



  • Unusual



Rasagiline


What to Do About AEs



  • Lower the dose or change to alternative PD medications

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

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