Tetrabenazine 12.5mg tablets
A drug formerly used as an antipsychotic but now used primarily in the symptomatic treatment of various hyperkinetic disorders.
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Yellow Card reports
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Suspected adverse reactions reported for Tetrabenazine
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Data from the MHRA Yellow Card scheme. A reported reaction does not necessarily mean the medicine caused it. Contains public sector information licensed under the Open Government Licence v3.0.
EudraVigilance
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Suspected adverse reactions reported for Tetrabenazine
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1 branded products available
WHO defined daily dose (DDD)
100 mg
Not a recommended dose. The DDD is the assumed average maintenance dose per day for a drug used for its main indication in adults. It is a statistical measure used for research and comparison purposes only.
Source: WHO Collaborating Centre for Drug Statistics Methodology, distributed via the NHS dm+d supplementary BNF/ATC mapping files (NHSBSA). Contains public sector information licensed under the Open Government Licence v3.0.
Therapeutically similar medicines
Similarity is based on WHO Anatomical Therapeutic Chemical (ATC) classification and on a factual NHS dm+d therapeutic-grouping code prefix. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
NHS prescribing volume and spending trends
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Codes for healthcare professionals and prescribing systems
These codes are used by healthcare IT systems and prescribers to identify this medicine.
NHS UK identifiers
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SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. BNF code shown is the factual mapping value distributed by NHS Business Services Authority (NHSBSA) in the dm+d supplementary file under OGL v3.0; it is not affiliated with, nor licensed from, the publishers of the British National Formulary. ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
Active and completed clinical studies from ClinicalTrials.gov
Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Academic studies and reviews for this medicine's active substance
Showing the 50 most relevant studies.
Reviews & meta-analyses: 21 · Randomised trials: 2 · 1959–2024
Showing the 50 most relevant studies, sorted by most relevant.
Aman A. Savani, Ivan S. Login
Neurology, 2007
- Anti-Dyskinesia Agents
- Chorea
- Huntington Disease
Stanley N. Caroff, S. Aggarwal, Charles Yonan
Journal of Comparative Effectiveness Research, 2017
- Tardive Dyskinesia
- Clinical Trials as Topic
- Research Design
Connolly A, Wallman P, Dzahini O, et al.
2024
- Antipsychotic Agents
- Psychotic Disorders
- Schizophrenia
RationaleDopamine antagonists induce dopamine receptor supersensitivity. This may manifest in late-appearing movement disorders (tardive dyskinesia (TD). VMAT-2 inhibitors reduce dopaminergic transmission but have limited activity at postsynaptic receptors and so may have antipsychotic activity with lower risk of tardive dyskinesia.MethodsWe conducted a systematic database search from inception to September 2022 for articles describing the use of VMAT-2 inhibitors in psychosis. Inclusion criteria were as follows: Population: adults diagnosed with psychosis or schizophrenia; Intervention: treatment with tetrabenazine, deutetrabenazine or valbenazine; Comparison: comparison with placebo or/and antipsychotic drug; Outcomes: with efficacy outcomes (e.g. Brief Psychiatric Rating Scale (BPRS) change or clinician assessment) and adverse effects ratings (e.g. rating scale or clinician assessment or dropouts); and Studies: in randomised controlled trials and non-randomised studies.ResultsWe identified 4892 records relating to VMAT-2 inhibitor use of which 5 (173 participants) met our a priori meta-analysis inclusion criteria. VMAT-2 inhibitors were more effective than placebo for the outcome 'slight improvement' (risk ratio (RR) = 1.77 (95% CI 1.03, 3.04)) but not for 'moderate improvement' (RR 2.81 (95% CI 0.27, 29.17). VMAT-2 inhibitors were as effective as active comparators on both measures for-'slight improvement' (RR 1.05 (95% CI 0.6, 1.81)) and 'moderate improvement' (RR 1.11 (95% CI 0.51, 2.42). Antipsychotic efficacy was also suggested by a narrative review of 37 studies excluded from the meta-analysis.ConclusionsVMAT-2 inhibitors may have antipsychotic activity and may offer promise for treatment of psychosis with the potential for a reduced risk of TD.
Abstract licence: CC BY
Vadlamani N, Ibrahimli S, Khan FA, et al.
2024
Jack J. Chen, William G. Ondo, Khashayar Dashtipour, et al.
Clinical Therapeutics, 2012
- Chorea
- Dystonia
- Huntington Disease
Samuel Frank, David Stamler, Elise Kayson, et al.
JAMA Neurology, 2017
- Australia
- Chorea
- Tetrabenazine
C. Kenney, Joseph Jankovic
Expert Review of Neurotherapeutics, 2006
- Clinical Trials as Topic
- Drug Tolerance
- Expert Testimony
Joseph Jankovic, Kathleen Clarence‐Smith
Expert Review of Neurotherapeutics, 2011
- Chorea
- Hyperkinesis
- Tetrabenazine
David R.P. Guay
The American journal of geriatric pharmacotherapy, 2010
- Clinical Trials as Topic
- Depression
- Dopamine
Huntington Study Group
Neurology, 2006
- Accidental Falls
- Breast Neoplasms
- Huntington Disease
Sources: aggregated from Europe PMC (EMBL-EBI), OpenAlex, Crossref, PubMed and other open scholarly databases. Retracted articles are excluded. Study information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
None known
Half-life
10 hours
Mechanism
Tetrabenazine is a reversible human vesicular monoamine transporter type 2 inhibitor (Ki = 100 nM).
Food interactions
2 warnings
Human targets
2 targets
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
75%
Half-life
10 hours
[A39004]…
Protein binding
82 - 88%
α-HTBZ = 60 - 68%;
β-HTBZ = 59 - 63%.
Volume of distribution
385L
Metabolism
2 hours
Elimination
75%
Clearance
1.67 L
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
Known interactions with other medications. Always consult a healthcare professional.
Showing 50 of 793 interactions
LD50 oral, mouse: 550 mg/kg
How the body processes this drug — absorption, distribution, metabolism, and elimination
Cmax, oral = 4.8 ng/mL in HD or tardive dyskinesia patients;
Tmax, oral = 69 min in HD or tardive dyskinesia patients
[A39004]
The elimination half-life of tetrabenazine was 10 hours following intravenous bolus administration.
[A251120]
The oral half-lives of its metabolites, α-HTBZ, β-HTBZ and 9-desmethyl-β-DHTBZ, are seven hours, five hours and 12 hours, respectively.
[L42565]
Following a single oral dose of 25 mg tetrabenazine, the elimination half-life was approximately 17.5 hours in subjects with hepatic impairment.
[L42565]
α-HTBZ = 60 - 68%;
β-HTBZ = 59 - 63%.
Tetrabenazine is rapidly distributed to the brain following IV injection. The site with the highest binding is the striatum, while the lowest binding was observed in the cortex.
Urinary excretion of α-HTBZ or β-HTBZ (the major metabolites) accounted for less than 10% of the administered dose.
Proteins and enzymes this drug interacts with in the body
PMID:23363473 PMID:37914936 PMID:38081299 PMID:38517752 PMID:8643547
Regulates the transvesicular monoaminergic gradient that determines the quantal size.
Mediates somatodendritic dopamine release in hippocampal neurons, likely as part of a regulated secretory pathway that integrates retrograde synaptic signals (By similarity). Acts as a primary transporter for striatal dopamine loading ensuring impulse-dependent release of dopamine at the synaptic cleft (By similarity). Responsible for histamine and serotonin storage and subsequent corelease from mast cell granules PMID:8860238
PMID:21645528
Positively regulates postnatal regression of retinal hyaloid vessels via suppression of VEGFR2/KDR activity, downstream of OPN5 (By similarity)
Enzymes involved in drug metabolism — important for understanding drug interactions
ATC N07XX06
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
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Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Tetrabenazine
Additional database identifiers
Drugs Product Database (DPD)
109
ChemSpider
5796
BindingDB
50017701
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10935
GenAtlas
SLC18A2
GeneCards
SLC18A2
GenBank Gene Database
L09118
GenBank Protein Database
292335
Guide to Pharmacology
1012
UniProt Accession
VMAT2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:3023
GenAtlas
DRD2
GeneCards
DRD2
GenBank Gene Database
M30625
GenBank Protein Database
181432
Guide to Pharmacology
215
UniProt Accession
DRD2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:1548
GenAtlas
CBR1
GeneCards
CBR1
GenBank Gene Database
J04056
Guide to Pharmacology
1383
UniProt Accession
CBR1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2625
GenAtlas
CYP2D6
GeneCards
CYP2D6
GenBank Gene Database
M20403
GenBank Protein Database
181350
Guide to Pharmacology
1329
UniProt Accession
CP2D6_HUMAN
DrugBank citations
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Structured knowledge from the free knowledge base
ATC classifications (Wikidata)
Linked open data from Wikidata (Q413050), a free and open knowledge base operated by the Wikimedia Foundation. Data is available under the Creative Commons CC0 1.0 Public Domain Dedication.