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tetrabenazine

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EntityQ413050· pop 21· linked from 1,644 articles

tetrabenazine

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Also known as Nitoman®, Revocon®, Ro-19569, TBZ, 2-oxo-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-benzoquinolizine, 1,2,4,6,7,11b-hexahydro-3-isobutyl-9,10-dimethoxy-2H-benzo[a]quinolizin-2-one, 2-oxo-3-isobutyl-9,10-dimethoxy-1,2,3,4,6,7-hexahydro-11bH-benzo[a]quinolizine

Tetrabenazine is a drug for the symptomatic treatment of hyperkinetic movement disorders. It is sold under the brand names Nitoman and Xenazine among others. On August 15, 2008, the US Food and Drug Administration (FDA) approved the use of tetrabenazine to treat chorea associated with Huntington's disease. Although other drugs had been used "off-label", tetrabenazine was the first approved treatment for Huntington's disease in the United States. The compound has been known since the 1950s.

Key facts

Drug.synonyms
Ro-1-9569
Drug.verifiedrevid
470603336
Drug.IUPAC_name
(SS,RR)-3-Isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-pyrido[2,1-a]isoquinolin-2-one
Drug.image
Tetrabenazine.svg
Drug.image_class
skin-invert-image
Drug.image2
Tetrabenazine3d.png
Drug.image_class2
bg-transparent
Drug.chirality
Racemic mixture
Drug.tradename
Xenazine, Xentra, Nitoman, others
Drug.pregnancy_AU
B3
Drug.routes_of_administration
By mouth
Drug.legal_AU
S4
Drug.legal_BR
C1
Drug.legal_US
Rx-only
Drug.bioavailability
Low, extensive first pass effect
Drug.protein_bound
82–85%
Drug.metabolism
Liver (CYP2D6-mediated)
Drug.elimination_half life
10 hours parent compound (2 to 8 hours active metabolites)

via Wikipedia infobox

Chemical data

Formula
C19H27NO3
Molecular weight
317.4 g/mol
IUPAC name
9,10-dimethoxy-3-(2-methylpropyl)-1,3,4,6,7,11b-hexahydrobenzo[a]quinolizin-2-one
SMILES
CC(C)CC1CN2CCC3=CC(=C(C=C3C2CC1=O)OC)OC
InChIKey
MKJIEFSOBYUXJB-UHFFFAOYSA-N
XLogP
2.9
Polar surface area
38.8 Ų
H-bond donors
0
H-bond acceptors
4
Formal charge
0

via PubChem

Research

1,887 papers

via PubMed

~6 min read

Encyclopedic overview

10 sections
Contents
  • Medical uses
  • Adverse effects
  • Black box warning
  • Pharmacology
  • Research
  • Animal model of motivational dysfunction
  • Dyskinetic cerebral palsy
  • See also
  • References
  • External links

Tetrabenazine is a drug for the symptomatic treatment of hyperkinetic movement disorders. It is sold under the brand names Nitoman and Xenazine among others. On August 15, 2008, the US Food and Drug Administration (FDA) approved the use of tetrabenazine to treat chorea associated with Huntington's disease. Although other drugs had been used "off-label", tetrabenazine was the first approved treatment for Huntington's disease in the United States. The compound has been known since the 1950s.

==Medical uses== Tetrabenazine is used as a treatment, but not as a cure, for hyperkinetic disorders such as: Huntington's disease – specifically, the chorea associated with it Tourette syndrome and other tic disorders Tardive dyskinesia, a serious and sometimes irreversible side effect of long-term use of many antipsychotics, mainly typical antipsychotics Hemiballismus, spontaneous flinging limb movements due to contra-lateral subthalamic nucleus damage

Excerpted from Wikipedia’s “tetrabenazine” article, available under the CC BY-SA 4.0 licence.