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Tetrabenazine

 

Tetrabenazine

Tetrabenazine
Systematic (IUPAC) name
(SS,RR)-3-Isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-pyrido[2,1-a]isoquinolin-2-one
Clinical data
Trade names Xenazine
AHFS/Drugs.com
Pregnancy
category
  • C
Legal status
  • ℞-only (US)
Routes of
administration
Oral (tablets, 25 mg)
Pharmacokinetic data
Bioavailability Low, extensive first pass effect
Protein binding 82–85%
Metabolism Hepatic (CYP2D6-mediated)
Excretion Renal and fecal
Identifiers
CAS Registry Number  Y
ATC code N07
PubChem CID:
IUPHAR/BPS
DrugBank  Y
ChemSpider  Y
UNII  Y
KEGG  Y
ChEMBL  Y
Synonyms Ro-1-9569
Chemical data
Formula C19H27NO3
Molecular mass 317.427 g/mol
 Y   

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.

Contents

  • Pharmacology 1
  • Uses 2
  • Side effects 3
  • Warnings 4
  • References 5
  • External links 6

Pharmacology

Tetrabenazine works mainly as a VMAT-inhibitor,[2][3] and as such promotes the early metabolic degradation of monoamines, in particular the neurotransmitter dopamine.

Uses

Tetrabenazine is used as a treatment, but not as a cure, for hyperkinetic disorders[4][5] such as:

Side effects

Some of these include:[7]

  • 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

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.  
  3. ^ Ugolev Y, Segal T, Yaffe D, Gros Y, Schuldiner S (2013). "Identification of conformationally sensitive residues essential for inhibition of vesicular monoamine transport by the noncompetitive inhibitor tetrabenazine". J. Biol. Chem. 288 (45): 32160–71.  
  4. ^ Jankovic J, Beach J (1997). "Long-term effects of tetrabenazine in hyperkinetic movement disorders". Neurology 48 (2): 358–62.  
  5. ^ 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.  
  6. ^ 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.  
  7. ^ Robertson MM (March 2000). "Tourette syndrome, associated conditions and the complexities of treatment". Brain. 123 123 (3): 425–62.  

External links

  • NIMH Repository data sheet
  • "Tetrabenazine" from HOPES: Huntington's Disease Outreach Project for Education at Stanford
  • Detailed monograph on tetrabenazine on rxmed.com
  • Information on tetrabenazine from netdoctor.co.uk
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