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File:(RR,SS)-Tetrabenazine Structural Formulae.png
Systematic (IUPAC) name
Clinical data
  • C
Routes of
Oral (tablets, 25 mg)
Legal status
Legal status
Pharmacokinetic data
Bioavailability Low, extensive first pass effect
Protein binding 82–85%
Metabolism Hepatic (CYP2D6-mediated)
Excretion Renal and fecal
CAS Number 58-46-8
ATC code N07XX06 (WHO)
PubChem CID 6018
DrugBank DB04844
ChemSpider 5796
Synonyms Ro-1-9569
Chemical data
Formula C19H27NO3
Molar mass 317.427 g/mol[[Script error: No such module "String".]]
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Tetrabenazine is a drug for the symptomatic treatment of hyperkinetic movement disorder and is marketed under the trade names Nitoman in Canada and Xenazine in New Zealand and some parts of Europe, and is also available in the USA as an orphan drug. On August 15, 2008 the U.S. Food and Drug Administration (FDA) approved the use of tetrabenazine to treat chorea associated with Huntington's disease (HD), the first in the US.[1] The compound has been known since the 1950s.


Tetrabenazine works mainly as a VMAT-inhibitor[2] and as such promotes the early metabolic degradation of monoamines, in particular the neurotransmitter dopamine.


Tetrabenazine is used as a treatment, but not a cure for hyperkinetic disorders[3][4] such as:

Side effects

Because tetrabenazine is closely related to antipsychotics, many of its side effects are similar. Some of these include:[6]

  • Akathisia (aka "restless pacing" – an inability to keep still, with intense anxiety when forced to do so)
  • Depression - the most common side effect, reported in roughly 15% of those who take the medication
  • Dizziness, drowsiness, insomnia, fatigue, nervousness and anxiety
  • Parkinsonism

Unlike many antipsychotics, tetrabenazine is not known to cause tardive dyskinesia.


  • Because of the relatively high incidence of depression, it has been recommended that people with a history of depression avoid taking tetrabenazine.
  • The concomitant intake of MAO inhibitors is contraindicated.


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External links

de:Tetrabenazin it:Tetrabenazina
  1. 1st US drug for Huntington's disease wins approval
  2. Zheng G, Dwoskin LP, Crooks PA (2006). "Vesicular monoamine transporter 2: role as a novel target for drug development". AAPS J. 8 (4): E682–92. doi:10.1208/aapsj080478. PMC 2751365Freely accessible. PMID 17233532. 
  3. Jankovic J, Beach J (1997). "Long-term effects of tetrabenazine in hyperkinetic movement disorders". Neurology. 48 (2): 358–62. PMID 9040721. 
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