| 词条 | Tetrabenazine |
| 释义 |
| verifiedrevid = 470603336 | IUPAC_name = (SS,RR)-3-Isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-pyrido[2,1-a]isoquinolin-2-one | image = Tetrabenazine.svg | image2 = Tetrabenazine3d.png | chirality = Racemic mixture | tradename = Xenazine, Nitoman | Drugs.com = {{drugs.com|CDI|tetrabenazine}} | pregnancy_AU = B3 | pregnancy_US = C | legal_AU = S4 | legal_US = ℞-only | routes_of_administration = Oral (tablets) | bioavailability = Low, extensive first pass effect | protein_bound = 82–85% | metabolism = Hepatic (CYP2D6-mediated) | excretion = Renal (~75%) and fecal (7–16%)[1] | IUPHAR_ligand = 4834 | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 58-46-8 | ATC_prefix = N07 | ATC_suffix = XX06 | PubChem = 6018 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = DB04844 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 5796 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = Z9O08YRN8O | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D08575 | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 117785 | C=19 | H=27 | N=1 | O=3 | molecular_weight = 317.427 g/mol | smiles = O=C3C(CC(C)C)CN2C(c1c(cc(OC)c(OC)c1)CC2)C3 | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 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 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = MKJIEFSOBYUXJB-UHFFFAOYSA-N | synonyms = Ro-1-9569 }} Tetrabenazine is a drug for the symptomatic treatment of hyperkinetic movement disorders. It is marketed under the trade names Nitoman in Canada and Xenazine in New Zealand, some parts of Europe, and in the United States as an orphan drug and in Iran as Xentra. 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.[2] The compound has been known since the 1950s. Medical usesTetrabenazine is used as a treatment, but not as a cure, for hyperkinetic disorders[3][4] such as:
Side effectsThe 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.[1] WarningsThere is a boxed warning associated with the use of tetrabenazine:[1]
PharmacologyThe 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.[1] See also
References1. ^1 2 3 {{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|accessdate=9 December 2015}} 2. ^1st US drug for Huntington's disease wins approval {{dead link|date=May 2016|bot=medic}}{{cbignore|bot=medic}} 3. ^{{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}} 4. ^{{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}} 5. ^{{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|url=http://ajp.psychiatryonline.org/cgi/pmidlookup?view=long&pmid=10450276|doi-broken-date=2018-09-04}} External links
8 : Anxiogenics|VMAT inhibitors|Tardive dyskinesia|Orphan drugs|Pyridoisoquinolines|Phenol ethers|Ketones|Huntington's disease |
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