Wikipedia:WikiProject Chemicals/Chembox validation/VerifiedDataSandbox and Tetrabenazine: Difference between pages

{{short description|Medication for hyperkinetic movement disorders}}

| verifiedrevid = 470603336

| image = Tetrabenazine.svg

| chirality = [[Racemic mixture]]

| tradename = Xenazine, Xentra, Nitoman, others

| pregnancy_AU = B3

| routes_of_administration = [[By mouth]]

| legal_AU = S4

| legal_AU_comment = <ref>{{cite web|url=https://www.tga.gov.au/resources/prescription-medicines-registrations/tetrabenazine-rantetrabenazine-suntetrabenazine-rbx-sun-pharma-anz-pty-ltd|title=TETRABENAZINE RAN/TETRABENAZINE SUN/TETRABENAZINE RBX (Sun Pharma ANZ Pty Ltd)|website=[[Therapeutic Goods Administration]]}}</ref>

| legal_BR = C1

| legal_BR_comment = <ref>{{Cite web |author=Anvisa |author-link=Brazilian Health Regulatory Agency |date=2023-03-31 |title=RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial |trans-title=Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control|url=https://www.in.gov.br/en/web/dou/-/resolucao-rdc-n-784-de-31-de-marco-de-2023-474904992 |url-status=live |archive-url=https://web.archive.org/web/20230803143925/https://www.in.gov.br/en/web/dou/-/resolucao-rdc-n-784-de-31-de-marco-de-2023-474904992 |archive-date=2023-08-03 |access-date=2023-08-16 |publisher=[[Diário Oficial da União]] |language=pt-BR |publication-date=2023-04-04}}</ref>

| legal_US = Rx-only

| metabolism = [[Liver]] ([[CYP2D6]]-mediated)

| elimination_half-life = 10 hours parent compound (2 to 8 hours active metabolites)<ref name=hl>{{cite journal | vauthors = Yero T, Rey JA | title = Tetrabenazine (Xenazine), An FDA-Approved Treatment Option For Huntington's Disease-Related Chorea | journal = P & T | volume = 33 | issue = 12 | pages = 690–694 | date = December 2008 | pmid = 19750050 | pmc = 2730806 }}</ref>

| excretion = [[Kidney]] (~75%) and fecal (7–16%)<ref name=PI>{{cite web|title=Xenazine (tetrabenazine) Tablets, for Oral Use. Full Prescribing Information. Revised: 6/2015|url=http://www.lundbeck.com/upload/us/files/pdf/Products/Xenazine_PI_US_EN.pdf|publisher=H. Lundbeck A/S|access-date=9 December 2015}}</ref>

| IUPHAR_ligand = 4834

| C=19 | H=27 | N=1 | O=3

'''Tetrabenazine''' is a drug for the symptomatic treatment of [[Hyperkinesia|hyperkinetic]] [[movement disorders]]. It is sold under the brand names '''Nitoman''' and '''Xenazine''' among others. On August 15, 2008, the U.S. [[Food and Drug Administration]] approved the use of tetrabenazine to treat [[Chorea (disease)|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 U.S.<ref>[http://ap.google.com/article/ALeqM5jcxk0L9FfGM69AVQkohaYAUcrVlAD92J09SG0 1st US drug for Huntington's disease wins approval] {{dead link|date=May 2016|bot=medic}}{{cbignore|bot=medic}}</ref> 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:<ref name="JankovicHyperkinectic">{{cite journal|vauthors=Jankovic J, Beach J |title=Long-term effects of tetrabenazine in hyperkinetic movement disorders|journal=Neurology|volume=48|issue=2|pages=358–62|year=1997|pmid=9040721|doi=10.1212/wnl.48.2.358|s2cid=33577525}}</ref><ref name="pmid17133512">{{cite journal|vauthors=Kenney C, Hunter C, Jankovic J |title=Long-term tolerability of tetrabenazine in the treatment of hyperkinetic movement disorders|journal=Movement Disorders|volume=22|issue=2|pages=193–7|date=January 2007|pmid=17133512|doi=10.1002/mds.21222|s2cid=22001960}}</ref>

* [[Huntington's disease]] – specifically, the [[chorea]] associated with it

* [[Tourette syndrome]] and other [[tic disorder]]s

* [[Tardive dyskinesia]],<ref name="pmid10450276">{{cite journal|vauthors=Ondo WG, Hanna PA, Jankovic J |title=Tetrabenazine treatment for tardive dyskinesia: assessment by randomized videotape protocol|journal=American Journal of Psychiatry|volume=156|issue=8|pages=1279–81|date=August 1999|pmid=10450276|doi=10.1176/ajp.156.8.1279|s2cid=40131860 |url=http://ajp.psychiatryonline.org/cgi/pmidlookup?view=long&pmid=10450276}}</ref> a serious and sometimes irreversible side effect of long-term use of many antipsychotics, mainly [[typical antipsychotic]]s

* [[Hemiballismus]], spontaneous flinging limb movements due to contra-lateral [[subthalamic nucleus]] damage

Tetrabenazine has been used as an [[antipsychotic]] in the treatment of [[schizophrenia]], both in the past<ref name="pmid13832091">{{cite journal | vauthors = Smith ME | title = Clinical comparison of tetrabenazine (Ro 1-9569), reserpine and placebo in chronic schizophrenics | journal = Diseases of the Nervous System | volume = 21(3)Suppl | issue = 3 Suppl | pages = 120–123 | date = March 1960 | pmid = 13832091 | doi = }}</ref><ref name="pmid13745210">{{cite journal | vauthors = Sacerdoti G | title = [First clinical experiences with tetrabenazine] | language = Italian | journal = Rassegna di Studi Psichiatrici | volume = 49 | issue = | pages = 450–460 | date = 1960 | pmid = 13745210 | doi = | trans-title = First clinical experiences with tetrabenazine }}</ref><ref name="pmid13748124">{{cite journal | vauthors = Schmitt W | title = [On the pharmacotherapy of psychoses: clinical research on tetrabenazine] | language = German | journal = Psychiatria et Neurologia | volume = 140 | issue = | pages = 23–29 | date = July 1960 | pmid = 13748124 | doi = 10.1159/000131224 | trans-title = On the pharmacotherapy of psychoses: clinical research on tetrabenazine }}</ref><ref name="pmid13684728">{{cite journal | vauthors = Ashcroft GW, Macdougall EJ, Barker PA | title = A comparison of tetrabenazine and chlorpromazine in chronic schizophrenia | journal = The Journal of Mental Science | volume = 107 | issue = 447 | pages = 287–293 | date = March 1961 | pmid = 13684728 | doi = 10.1192/bjp.107.447.287 }}</ref><ref name="pmid13874731">{{cite journal | vauthors = Burckard E, Medhaoui M, Montigneaux P, Pfitzenmeyer J, Pfitzenmeyer H, Schaetzel JC, Singer L, Geissmann P | display-authors = 6 | title = [Clinical, biological and electroencephalographic study of the action of tetrabenazine (Ro 956) in various chronic psychoses] | language = French | journal = Annales Médico-Psychologiques | volume = 120 | issue = 1 | pages = 115–119 | date = January 1962 | pmid = 13874731 | doi = | trans-title = Clinical, biological and electroencephalographic study of the action of tetrabenazine (Ro 956) in various chronic psychoses }}</ref><ref name="pmid14453492">{{cite journal | vauthors = Kammerer T, Singer L, Geissmann P, Wetta JM | title = [Use of a new neuroleptic: tetrabenazine. Clinical, biological and electroencephalographic results] | language = French | journal = Annales Médico-Psychologiques | volume = 120 | issue = 1 | pages = 106–115 | date = January 1962 | pmid = 14453492 | doi = | trans-title = Use of a new neuroleptic: tetrabenazine. Clinical, biological and electroencephalographic results }}</ref><ref name="pmid14081399">{{cite journal | vauthors = Lingjaerde O | title = Tetrabenazine (Nitoman) in the treatment of psychoses. With a discussion on the central mode of action of tetrabenazine and reserpine. | journal = Acta Psychiatrica Scandinavica | volume = 39 | issue = | pages = SUPPL170:1–SUPPL17109 | date = 1963 | pmid = 14081399 | doi = }}</ref><ref name="pmid6007641">{{cite journal | vauthors = Matsumoto Y, Totsuka S, Kato M, Inoue M, Okagami K | title = [Therapy of schizophrenia with tetrabenazine] | language = Japanese | journal = Nihon Rinsho. Japanese Journal of Clinical Medicine | volume = 24 | issue = 7 | pages = 1360–1364 | date = July 1966 | pmid = 6007641 | doi = }}</ref> and in modern times.<ref name="pmid17683910">{{cite journal | vauthors = Malik A, Balkoski V | title = Neurotransmitter depleter tetrabenazine; potential candidate for schizophrenia treatment? | journal = Schizophrenia Research | volume = 96 | issue = 1–3 | pages = 267–268 | date = November 2007 | pmid = 17683910 | doi = 10.1016/j.schres.2007.07.010 | s2cid = 39312847 }}</ref><ref name="pmid22198452">{{cite journal | vauthors = Remington G, Kapur S, Foussias G, Agid O, Mann S, Borlido C, Richards S, Javaid N | display-authors = 6 | title = Tetrabenazine augmentation in treatment-resistant schizophrenia: a 12-week, double-blind, placebo-controlled trial | journal = Journal of Clinical Psychopharmacology | volume = 32 | issue = 1 | pages = 95–99 | date = February 2012 | pmid = 22198452 | doi = 10.1097/JCP.0b013e31823f913e | s2cid = 2649261 }}</ref><ref name="pmid27721587">{{cite journal | vauthors = Kaur N, Kumar P, Jamwal S, Deshmukh R, Gauttam V | title = Tetrabenazine: Spotlight on Drug Review | journal = Annals of Neurosciences | volume = 23 | issue = 3 | pages = 176–185 | date = September 2016 | pmid = 27721587 | pmc = 5043267 | doi = 10.1159/000449184 }}</ref>

==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.<ref name=PI/>

==Warnings==

There is a [[boxed warning]] associated with the use of tetrabenazine:<ref name=PI/>

* 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.<ref name=PI/>

==See also==

* [[Deutetrabenazine]]

{{clear}}

==References==

{{Reflist|2}}

==External links==

*[http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021894s010lbl.pdf Xenazine prescribing information FDA] {{Webarchive|url=https://web.archive.org/web/20170216205253/http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021894s010lbl.pdf |date=2017-02-16 }}

*[https://web.archive.org/web/20070310235952/http://nimh-repository.rti.org/infosheet.asp?rec=200404271700320322 NIMH Repository data sheet]

*[https://archive.today/20100718025247/http://www.stanford.edu/group/hopes/treatmts/tbz/rtbz3.html "Tetrabenazine"] from [[HOPES]]: Huntington's Disease Outreach Project for Education at Stanford

*[http://www.rxmed.com/b.main/b2.pharmaceutical/b2.1.monographs/CPS-%20Monographs/CPS-%20(General%20Monographs-%20N)/NITOMAN.html Detailed monograph on tetrabenazine on rxmed.com]

*[http://www.netdoctor.co.uk/medicines/100004430.html Information on tetrabenazine from netdoctor.co.uk]

{{Antipsychotics}}

{{Other nervous system drugs}}

{{Monoamine reuptake inhibitors}}

[[Category:Anxiogenics]]

[[Category:Huntington's disease]]

[[Category:Ketones]]

[[Category:Orphan drugs]]

[[Category:Phenol ethers]]

[[Category:Tardive dyskinesia]]

[[Category:Tetrahydroisoquinolines]]

[[Category:VMAT inhibitors]]