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Tetrabenazine

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Tetrabenazine
File:(RR,SS)-Tetrabenazine Structural Formulae.png
File:Tetrabenazine3d.png
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 Consumer Drug Information
  • C
  • ℞-only (US)
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
58-46-8 7pxY
N07XX06
PubChem CID 6018
DrugBank DB04844 7pxY
ChemSpider 5796 7pxY
UNII Z9O08YRN8O 7pxY
KEGG D08575 7pxY
ChEMBL CHEMBL117785 7pxY
Synonyms Ro-1-9569
Chemical data
Formula C19H27NO3
317.427 g/mol
 14pxY (what is this?)  (verify)

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.

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[dead link]
  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. PMC 2751365. PMID 17233532. doi:10.1208/aapsj080478. 
  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. PMC 3820856. PMID 24062308. doi:10.1074/jbc.M113.502971. 
  4. ^ Jankovic J, Beach J (1997). "Long-term effects of tetrabenazine in hyperkinetic movement disorders". Neurology 48 (2): 358–62. PMID 9040721. doi:10.1212/wnl.48.2.358. 
  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. PMID 17133512. doi:10.1002/mds.21222. 
  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. PMID 10450276. 
  7. ^ Robertson MM (March 2000). "Tourette syndrome, associated conditions and the complexities of treatment". Brain. 123 123 (3): 425–62. PMID 10686169. doi:10.1093/brain/123.3.425. 

External links