Tetrabenazine

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Tetrabenazine
Clinical data
Trade namesXenazine, Xentra, Nitoman, others
Other namesRo-1-9569
AHFS/Drugs.comConsumer Drug Information
Pregnancy
category
  • AU: B3
By mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
BioavailabilityLow, extensive first pass effect
Protein binding82–85%
MetabolismLiver (CYP2D6-mediated)
Elimination half-life10 hours parent compound (2 to 8 hours active metabolites)[3]
ExcretionKidney (~75%) and fecal (7–16%)[4]
Identifiers
  • (SS,RR)-3-Isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-pyrido[2,1-a]isoquinolin-2-one
JSmol)
ChiralityRacemic mixture
  • O=C3C(CC(C)C)CN2C(c1c(cc(OC)c(OC)c1)CC2)C3
  • InChI=1S/C19H27NO3/c1-12(2)7-14-11-20-6-5-13-8-18(22-3)19(23-4)9-15(13)16(20)10-17(14)21/h8-9,12,14,16H,5-7,10-11H2,1-4H3 checkY
  • Key:MKJIEFSOBYUXJB-UHFFFAOYSA-N checkY
  (verify)

Tetrabenazine is a drug for the symptomatic treatment of

off label," tetrabenazine was the first approved treatment for Huntington's disease in the U.S.[5]
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:[6][7]

Tetrabenazine has been used as an antipsychotic in the treatment of schizophrenia, both in the past[9][10][11][12][13][14][15][16] and in modern times.[17][18][19]

Side effects

The most common adverse reactions, which have occurred in at least 10% of subjects in studies and at least 5% greater than in subjects who received placebo, have been: sedation or somnolence, fatigue, insomnia, depression, suicidal thoughts, akathisia, anxiety and nausea.[4]

Warnings

There is a boxed warning associated with the use of tetrabenazine:[4]

  • Increases the risk of depression and suicidal thoughts and behavior in patients with Huntington's disease
  • Balance risks of depression and suicidality with the clinical need for control of chorea when considering the use of tetrabenazine
  • Monitor patients for emergence or worsening of depression, suicidality or unusual changes in behavior
  • Inform patients, caregivers and families of the risk of depression and suicidality and instruct to report behaviours of concern promptly to the treating physician
  • Exercise caution when treating patients with a history of depression or prior suicide attempts or ideation
  • Tetrabenazine is contraindicated in patients who are actively suicidal and in patients with untreated or inadequately treated depression

Pharmacology

See also: Monoamine-depleting agent

The precise mechanism of action of tetrabenazine is unknown. Its anti-chorea effect is believed to be due to a reversible depletion of monoamines such as dopamine, serotonin, norepinephrine, and histamine from nerve terminals. Tetrabenazine reversibly inhibits vesicular monoamine transporter 2, resulting in decreased uptake of monoamines into synaptic vesicles, as well as depletion of monoamine storage.[4]

See also

References

  1. ^ "TETRABENAZINE RAN/TETRABENAZINE SUN/TETRABENAZINE RBX (Sun Pharma ANZ Pty Ltd)". Therapeutic Goods Administration.
  2. ^ Anvisa (2023-03-31). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 2023-04-04). Archived from the original on 2023-08-03. Retrieved 2023-08-16.
  3. PMID 19750050
    .
  4. ^ a b c d "Xenazine (tetrabenazine) Tablets, for Oral Use. Full Prescribing Information. Revised: 6/2015" (PDF). H. Lundbeck A/S. Retrieved 9 December 2015.
  5. ^ 1st US drug for Huntington's disease wins approval [dead link]
  6. S2CID 33577525
    .
  7. S2CID 22001960
    .
  8. S2CID 40131860
    .
  9. PMID 13832091
    .
  10. PMID 13745210
    .
  11. PMID 13748124
    .
  12. PMID 13684728
    .
  13. PMID 13874731
    .
  14. PMID 14453492
    .
  15. PMID 14081399
    .
  16. PMID 6007641
    .
  17. S2CID 39312847
    .
  18. S2CID 2649261
    .
  19. PMID 27721587
    .

External links
Retrieved from "https://en.wikipedia.org/w/index.php?title=Tetrabenazine&oldid=1170641961"