Tetrabenazine is a drug for the symptomatic treatment of hyperkineticmovement 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 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.[5] The compound has been known since the 1950s.
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]
Warningsedit
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
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]
^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). from the original on 2023-08-03. Retrieved 2023-08-16.
^Yero T, Rey JA (December 2008). "Tetrabenazine (Xenazine), An FDA-Approved Treatment Option For Huntington's Disease-Related Chorea". P & T. 33 (12): 690–694. PMC2730806. PMID 19750050.
^ abcd"Xenazine (tetrabenazine) Tablets, for Oral Use. Full Prescribing Information. Revised: 6/2015" (PDF). H. Lundbeck A/S. Retrieved 9 December 2015.
^1st US drug for Huntington's disease wins approval[dead link]
^Jankovic J, Beach J (1997). "Long-term effects of tetrabenazine in hyperkinetic movement disorders". Neurology. 48 (2): 358–62. doi:10.1212/wnl.48.2.358. PMID 9040721. S2CID 33577525.
^Kenney C, Hunter C, Jankovic J (January 2007). "Long-term tolerability of tetrabenazine in the treatment of hyperkinetic movement disorders". Movement Disorders. 22 (2): 193–7. doi:10.1002/mds.21222. PMID 17133512. S2CID 22001960.
^Ondo WG, Hanna PA, Jankovic J (August 1999). "Tetrabenazine treatment for tardive dyskinesia: assessment by randomized videotape protocol". American Journal of Psychiatry. 156 (8): 1279–81. doi:10.1176/ajp.156.8.1279. PMID 10450276. S2CID 40131860.
^Smith ME (March 1960). "Clinical comparison of tetrabenazine (Ro 1-9569), reserpine and placebo in chronic schizophrenics". Diseases of the Nervous System. 21(3)Suppl (3 Suppl): 120–123. PMID 13832091.
^Sacerdoti G (1960). "[First clinical experiences with tetrabenazine]" [First clinical experiences with tetrabenazine]. Rassegna di Studi Psichiatrici (in Italian). 49: 450–460. PMID 13745210.
^Schmitt W (July 1960). "[On the pharmacotherapy of psychoses: clinical research on tetrabenazine]" [On the pharmacotherapy of psychoses: clinical research on tetrabenazine]. Psychiatria et Neurologia (in German). 140: 23–29. doi:10.1159/000131224. PMID 13748124.
^Ashcroft GW, Macdougall EJ, Barker PA (March 1961). "A comparison of tetrabenazine and chlorpromazine in chronic schizophrenia". The Journal of Mental Science. 107 (447): 287–293. doi:10.1192/bjp.107.447.287. PMID 13684728.
^Burckard E, Medhaoui M, Montigneaux P, Pfitzenmeyer J, Pfitzenmeyer H, Schaetzel JC, et al. (January 1962). "[Clinical, biological and electroencephalographic study of the action of tetrabenazine (Ro 956) in various chronic psychoses]" [Clinical, biological and electroencephalographic study of the action of tetrabenazine (Ro 956) in various chronic psychoses]. Annales Médico-Psychologiques (in French). 120 (1): 115–119. PMID 13874731.
^Kammerer T, Singer L, Geissmann P, Wetta JM (January 1962). "[Use of a new neuroleptic: tetrabenazine. Clinical, biological and electroencephalographic results]" [Use of a new neuroleptic: tetrabenazine. Clinical, biological and electroencephalographic results]. Annales Médico-Psychologiques (in French). 120 (1): 106–115. PMID 14453492.
^Lingjaerde O (1963). "Tetrabenazine (Nitoman) in the treatment of psychoses. With a discussion on the central mode of action of tetrabenazine and reserpine". Acta Psychiatrica Scandinavica. 39: SUPPL170:1–SUPPL17109. PMID 14081399.
^Matsumoto Y, Totsuka S, Kato M, Inoue M, Okagami K (July 1966). "[Therapy of schizophrenia with tetrabenazine]". Nihon Rinsho. Japanese Journal of Clinical Medicine (in Japanese). 24 (7): 1360–1364. PMID 6007641.
^Malik A, Balkoski V (November 2007). "Neurotransmitter depleter tetrabenazine; potential candidate for schizophrenia treatment?". Schizophrenia Research. 96 (1–3): 267–268. doi:10.1016/j.schres.2007.07.010. PMID 17683910. S2CID 39312847.
^Remington G, Kapur S, Foussias G, Agid O, Mann S, Borlido C, et al. (February 2012). "Tetrabenazine augmentation in treatment-resistant schizophrenia: a 12-week, double-blind, placebo-controlled trial". Journal of Clinical Psychopharmacology. 32 (1): 95–99. doi:10.1097/JCP.0b013e31823f913e. PMID 22198452. S2CID 2649261.
^Kaur N, Kumar P, Jamwal S, Deshmukh R, Gauttam V (September 2016). "Tetrabenazine: Spotlight on Drug Review". Annals of Neurosciences. 23 (3): 176–185. doi:10.1159/000449184. PMC5043267. PMID 27721587.
External linksedit
Xenazine prescribing information FDA 2017-02-16 at the Wayback Machine
"Tetrabenazine" from HOPES: Huntington's Disease Outreach Project for Education at Stanford
Detailed monograph on tetrabenazine on rxmed.com
Information on tetrabenazine from netdoctor.co.uk
December 07, 2023
tetrabenazine, drug, symptomatic, treatment, hyperkinetic, movement, disorders, sold, under, brand, names, nitoman, xenazine, among, others, august, 2008, food, drug, administration, approved, tetrabenazine, treat, chorea, associated, with, huntington, disease. 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 U S Food and Drug Administration 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 U S 5 The compound has been known since the 1950s TetrabenazineClinical dataTrade namesXenazine Xentra Nitoman othersOther namesRo 1 9569AHFS Drugs comConsumer Drug InformationPregnancycategoryAU B3Routes ofadministrationBy mouthATC codeN07XX06 WHO Legal statusLegal statusAU S4 Prescription only 1 BR Class C1 Other controlled substances 2 US onlyPharmacokinetic dataBioavailabilityLow extensive first pass effectProtein 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 IdentifiersIUPAC name SS RR 3 Isobutyl 9 10 dimethoxy 1 3 4 6 7 11b hexahydro pyrido 2 1 a isoquinolin 2 oneCAS Number58 46 8 YPubChem CID6018IUPHAR BPS4834DrugBankDB04844 YChemSpider5796 YUNIIZ9O08YRN8OKEGGD08575 YChEMBLChEMBL117785 YCompTox Dashboard EPA DTXSID0042614ECHA InfoCard100 000 348Chemical and physical dataFormulaC 19H 27N O 3Molar mass317 429 g mol 13D model JSmol Interactive imageChiralityRacemic mixtureSMILES O C3C CC C C CN2C c1c cc OC c OC c1 CC2 C3InChI 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 YKey MKJIEFSOBYUXJB UHFFFAOYSA N Y verify Contents 1 Medical uses 2 Side effects 3 Warnings 4 Pharmacology 5 See also 6 References 7 External linksMedical uses editTetrabenazine is used as a treatment but not as a cure for hyperkinetic disorders such as 6 7 Huntington s disease specifically the chorea associated with it Tourette syndrome and other tic disorders Tardive dyskinesia 8 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 damageTetrabenazine 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 editThe 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 editThere 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 depressionPharmacology editSee 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 editDeutetrabenazineReferences edit TETRABENAZINE RAN TETRABENAZINE SUN TETRABENAZINE RBX Sun Pharma ANZ Pty Ltd Therapeutic Goods Administration Anvisa 2023 03 31 RDC Nº 784 Listas de Substancias Entorpecentes Psicotropicas 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 Diario Oficial da Uniao published 2023 04 04 Archived from the original on 2023 08 03 Retrieved 2023 08 16 Yero T Rey JA December 2008 Tetrabenazine Xenazine An FDA Approved Treatment Option For Huntington s Disease Related Chorea P amp T 33 12 690 694 PMC 2730806 PMID 19750050 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 1st US drug for Huntington s disease wins approval dead link Jankovic J Beach J 1997 Long term effects of tetrabenazine in hyperkinetic movement disorders Neurology 48 2 358 62 doi 10 1212 wnl 48 2 358 PMID 9040721 S2CID 33577525 Kenney C Hunter C Jankovic J January 2007 Long term tolerability of tetrabenazine in the treatment of hyperkinetic movement disorders Movement Disorders 22 2 193 7 doi 10 1002 mds 21222 PMID 17133512 S2CID 22001960 Ondo WG Hanna PA Jankovic J August 1999 Tetrabenazine treatment for tardive dyskinesia assessment by randomized videotape protocol American Journal of Psychiatry 156 8 1279 81 doi 10 1176 ajp 156 8 1279 PMID 10450276 S2CID 40131860 Smith ME March 1960 Clinical comparison of tetrabenazine Ro 1 9569 reserpine and placebo in chronic schizophrenics Diseases of the Nervous System 21 3 Suppl 3 Suppl 120 123 PMID 13832091 Sacerdoti G 1960 First clinical experiences with tetrabenazine First clinical experiences with tetrabenazine Rassegna di Studi Psichiatrici in Italian 49 450 460 PMID 13745210 Schmitt W July 1960 On the pharmacotherapy of psychoses clinical research on tetrabenazine On the pharmacotherapy of psychoses clinical research on tetrabenazine Psychiatria et Neurologia in German 140 23 29 doi 10 1159 000131224 PMID 13748124 Ashcroft GW Macdougall EJ Barker PA March 1961 A comparison of tetrabenazine and chlorpromazine in chronic schizophrenia The Journal of Mental Science 107 447 287 293 doi 10 1192 bjp 107 447 287 PMID 13684728 Burckard E Medhaoui M Montigneaux P Pfitzenmeyer J Pfitzenmeyer H Schaetzel JC et al January 1962 Clinical biological and electroencephalographic study of the action of tetrabenazine Ro 956 in various chronic psychoses Clinical biological and electroencephalographic study of the action of tetrabenazine Ro 956 in various chronic psychoses Annales Medico Psychologiques in French 120 1 115 119 PMID 13874731 Kammerer T Singer L Geissmann P Wetta JM January 1962 Use of a new neuroleptic tetrabenazine Clinical biological and electroencephalographic results Use of a new neuroleptic tetrabenazine Clinical biological and electroencephalographic results Annales Medico Psychologiques in French 120 1 106 115 PMID 14453492 Lingjaerde O 1963 Tetrabenazine Nitoman in the treatment of psychoses With a discussion on the central mode of action of tetrabenazine and reserpine Acta Psychiatrica Scandinavica 39 SUPPL170 1 SUPPL17109 PMID 14081399 Matsumoto Y Totsuka S Kato M Inoue M Okagami K July 1966 Therapy of schizophrenia with tetrabenazine Nihon Rinsho Japanese Journal of Clinical Medicine in Japanese 24 7 1360 1364 PMID 6007641 Malik A Balkoski V November 2007 Neurotransmitter depleter tetrabenazine potential candidate for schizophrenia treatment Schizophrenia Research 96 1 3 267 268 doi 10 1016 j schres 2007 07 010 PMID 17683910 S2CID 39312847 Remington G Kapur S Foussias G Agid O Mann S Borlido C et al February 2012 Tetrabenazine augmentation in treatment resistant schizophrenia a 12 week double blind placebo controlled trial Journal of Clinical Psychopharmacology 32 1 95 99 doi 10 1097 JCP 0b013e31823f913e PMID 22198452 S2CID 2649261 Kaur N Kumar P Jamwal S Deshmukh R Gauttam V September 2016 Tetrabenazine Spotlight on Drug Review Annals of Neurosciences 23 3 176 185 doi 10 1159 000449184 PMC 5043267 PMID 27721587 External links editXenazine prescribing information FDA Archived 2017 02 16 at the Wayback Machine NIMH Repository data sheet Tetrabenazine from HOPES Huntington s Disease Outreach Project for Education at Stanford Detailed monograph on tetrabenazine on rxmed com Information on tetrabenazine from netdoctor co uk Retrieved from https en wikipedia org w index php title Tetrabenazine amp oldid 1170641961, wikipedia, wiki, book, books, library,
