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Tetrabenazine: Wikis

  

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1 : 1 mixture (racemate)
Systematic (IUPAC) name
(SS,RR)-3-Isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-pyrido[2,1- a]isoquinolin-2-one
Identifiers
CAS number 58-46-8
ATC code N07XX06
PubChem 6018
DrugBank DB04844
ChemSpider 5796
Chemical data
Formula C 19H27NO3  
Mol. mass 317.427 g/mol
Synonyms Ro-1-9569
Pharmacokinetic data
Bioavailability Low, extensive first pass effect
Protein binding 82–85%
Metabolism Hepatic (CYP2D6-mediated)
Half life  ?
Excretion Renal and fecal
Therapeutic considerations
Pregnancy cat. C
Legal status Orphan drug (US)
Routes Oral (tablets, 25 mg)
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Tetrabenazine is a drug for the symptomatical 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.

Contents

Pharmacology

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

Uses

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 the 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 of the antipychotics, tetrabenazine is not known to cause tardive dyskinesia.

Warnings

  • 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.

References

  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. PMID 17233532.  
  3. ^ Jankovic J, Beach J (1997). "Long-term effects of tetrabenazine in hyperkinetic movement disorders". Neurology 48 (2): 358–62. PMID 9040721.  
  4. ^ Kenney C, Hunter C, Jankovic J (January 2007). "Long-term tolerability of tetrabenazine in the treatment of hyperkinetic movement disorders". Mov. Disord. 22 (2): 193–7. doi:10.1002/mds.21222. PMID 17133512.  
  5. ^ Ondo WG, Hanna PA, Jankovic J (August 1999). "Tetrabenazine treatment for tardive dyskinesia: assessment by randomized videotape protocol". Am J Psychiatry 156 (8): 1279–81. PMID 10450276. http://ajp.psychiatryonline.org/cgi/pmidlookup?view=long&pmid=10450276.  
  6. ^ Robertson MM (March 2000). "Tourette syndrome, associated conditions and the complexities of treatment". Brain 123 Pt 3: 425–62. doi:10.1093/brain/123.3.425. PMID 10686169. http://brain.oxfordjournals.org/cgi/pmidlookup?view=long&pmid=10686169.  

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