Tetrabenazine

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Tetrabenazine
Systematic (IUPAC) name
1,3,4,6,7,11b-Hexahydro- 9,10-dimethoxy-3- (2-methylpropyl)- 2H-benzo[a]quinoline; Ro-1-9569
Identifiers
CAS number 58-46-8
ATC code N07XX
PubChem 6018
Chemical data
Formula C19H27NO3 
Mol. mass 317.427
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

?

Legal status

Orphan drug

Routes tablets: 25 mg

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 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 the neurotransmitter dopamine.

Contents

Common uses

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

Side effects

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

  • 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
  • Parkinsonism

Unlike many of the antipychotics, tetrabenazine is not known to cause Tardive dyskinesia, and in fact can be an effective treatment for the antipsychotic-induced movement disorder.

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 

External links

Wikipedia content modification information:

  • This page was last modified on 19 August 2008, at 18:19.

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