tetrabenazine

Class




  • Antiadrenergic, antidopaminergic, synaptic vesicle blocker, antimonoaminergic




Tetrabenazine


Commonly Prescribed for


(FDA approved in bold)



  • Chorea in Huntington’s disease (HD)
  • Dyskinesias in HD
  • Psychosis
  • Hemiballism
  • Dystonia (especially tardive)
  • Myoclonus
  • Gilles de la Tourette syndrome (GTS) or tics
  • Hypertension



Tetrabenazine


How the Drug Works



  • Depleting agent that reversibly depletes stores of monoamines (dopamine, norepinephrine, serotonin, and histamine) from nerve terminals and blocks post-synaptic dopamine receptors. Effectiveness is likely related to dopamine depletion



Tetrabenazine


How Long Until It Works



  • Usually less than 1 week



Tetrabenazine


If It Works



  • In neurologic conditions, continue to assess effect of the medication, determine if still needed and adjust to optimal dose



Tetrabenazine


If It Doesn’t Work



  • Chorea: Consider benzodiazepines and anticonvulsants (valproate). Neuroleptics are usually effective. Reserpine is an alternative depleting agent
  • Generalized dystonia: Anticholinergics, baclofen, or benzodiazepines may be effective. Surgical treatments (including pallidotomy, thalamotomy, deep brain stimulation, myotomy, rhizotomy, or peripheral denervation) are reserved for refractory cases
  • GTS/tics – Neuroleptics and alpha-2 adrenergic agonists are often effective



Tetrabenazine


Best Augmenting Combos for Partial Response or Treatment-Resistance



  • Chorea – combine with anticonvulsants, neuroleptics, or benzodiazepines
  • Dystonia – combine with anticholinergics or benzodiazepines
  • GTS/tics – Combine with neuroleptics for refractory cases



Tetrabenazine


Tests



  • At doses of 50 mg or greater, test patients for the CYP-450 2D6 gene to determine if they are poor, intermediate, or extensive metabolizers



Adverse Effects (AEs)




Tetrabenazine


How Drug Causes AEs



  • Related to monoamine depletion



Tetrabenazine


Notable AEs



  • Drowsiness, fatigue, dizziness, depression, anxiety, insomnia
  • Parkinsonism, akathisia, orthostatic hypotension, nausea
  • Upper respiratory tract infection, dyspnea, dysuria



Tetrabenazine


Life-Threatening or Dangerous AEs



  • Falls and resulting trauma
  • Neuroleptic malignant syndrome
  • Parkinsonism and extrapyramidal tract dysfunction (less common than neuroleptics)
  • QTc prolongation (usually mild)
  • Dysphagia



Tetrabenazine


Weight Gain



  • Common



Tetrabenazine


Sedation



  • Common



Tetrabenazine


What to Do About AEs

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

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