About: Tetrabenazine

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An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

Attributes	Values
rdf:type	http://linked.opendata.cz/ontology/drugbank/Drug
http://linked.open...gbank/description	A drug formerly used as an antipsychotic but now used primarily in the symptomatic treatment of various hyperkinetic disorders. It is a monoamine depletor and used as symptomatic treatment of chorea associated with Huntington's disease. FDA approved on August 15, 2008. (en)
http://linked.open...y/drugbank/dosage	http://linked.opendata.cz/resource/drugbank/dosage/271B5936-363D-11E5-9242-09173F13E4C5 http://linked.opendata.cz/resource/drugbank/dosage/271B5937-363D-11E5-9242-09173F13E4C5
http://linked.open...generalReferences	# Jankovic J, Beach J: Long-term effects of tetrabenazine in hyperkinetic movement disorders. Neurology. 1997 Feb;48(2):358-62. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/9040721 # Guay DR: Tetrabenazine, a monoamine-depleting drug used in the treatment of hyperkinetic movement disorders. Am J Geriatr Pharmacother. 2010 Aug;8(4):331-73. doi: 10.1016/j.amjopharm.2010.08.006. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/20869622 (en)
http://linked.open...gy/drugbank/group	approved (en)
http://linked.open...drugbank/halfLife	α-HTBZ = 7 hours; β-HTBZ = 5 hours; 9-desmethyl-β-DHTBZ = 12 hours. (en)
http://linked.open...ugbank/indication	Treatment of hyperkinetic movement disorders like chorea in Huntington's disease, hemiballismus, senile chorea, Tourette syndrome and other tic disorders, and tardive dyskinesia (en)
sameAs	Tetrabenazine
Title	Tetrabenazine (en)
adms:identifier	http://linked.opendata.cz/resource/drugbank/drug/DB04844/identifier/bindingdb/50017701 http://linked.opendata.cz/resource/drugbank/drug/DB04844/identifier/chemspider/5796 http://linked.opendata.cz/resource/drugbank/drug/DB04844/identifier/drugbank/DB04844 http://linked.opendata.cz/resource/drugbank/drug/DB04844/identifier/kegg-compound/C11168 http://linked.opendata.cz/resource/drugbank/drug/DB04844/identifier/national-drug-code-directory/67386-421-01 http://linked.opendata.cz/resource/drugbank/drug/DB04844/identifier/pubchem-compound/6018 http://linked.opendata.cz/resource/drugbank/drug/DB04844/identifier/pubchem-substance/46506426 http://linked.opendata.cz/resource/drugbank/drug/DB04844/identifier/chebi/9467 http://linked.opendata.cz/resource/drugbank/drug/DB04844/identifier/kegg-drug/D08575 http://linked.opendata.cz/resource/drugbank/drug/DB04844/identifier/pharmgkb/PA140222719 http://linked.opendata.cz/resource/drugbank/drug/DB04844/identifier/wikipedia/Tetrabenazine
http://linked.open...mechanismOfAction	Tetrabenazine is a reversible human vesicular monoamine transporter type 2 inhibitor (Ki = 100 nM). It acts within the basal ganglia and promotes depletion of monoamine neurotransmitters serotonin, norepinephrine, and dopamine from stores. It also decreases uptake into synaptic vesicles. Dopamine is required for fine motor movement, so the inhibition of its transmission is efficacious for hyperkinetic movement. Tetrabenazine exhibits weak in vitro binding affinity at the dopamine D2 receptor (Ki = 2100 nM). (en)
http://linked.open...drugbank/packager	Major Pharmaceuticals Lundbeck Inc.
http://linked.open...outeOfElimination	After oral administration, tetrabenazine is extensively hepatically metabolized, and the metabolites are primarily renally eliminated (75%). Tetrabenazine is also cleared fecally (7% to 16%). Unchanged tetrabenazine has not been found in human urine. Urinary excretion of α-HTBZ or β-HTBZ (the major metabolites) accounted for less than 10% of the administered dose. (en)
http://linked.open.../drugbank/synonym	Tetra benazin (en) Tetrabenzaine (en) Tetrabenzine (en) TBZ (en) Tetrabenazina (en) Tetrabenazinum (en) 1,2,4,6,7,11b-hexahydro-3-Isobutyl-9,10-dimethoxy-2H-benzo[a]quinolizin-2-one (en) 2-oxo-3-Isobutyl-9,10-dimethoxy-1,2,3,4,6,7-hexahydro-11bh-benzo[a]quinolizine (en) 2-oxo-3-Isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-benzoquinolizine (en)
http://linked.open...drugbank/toxicity	Dose-limiting adverse effects are sedation, parkinsonism, akathsia, and depression. LD50 oral, mouse: 550 mg/kg (en)
http://linked.open...umeOfDistribution	Steady State, IV, in HD or tardive dyskinesia patients: 385L. 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. (en)
http://linked.open...nk/proteinBinding	Tetrabenazine = 82 - 88%; α-HTBZ = 60 - 68%; β-HTBZ = 59 - 63%. (en)
http://linked.open...ynthesisReference	Michael James Rishel, Kande Kankananamalage Dayarathna Amarasinghe, Sean Richard Dinn, Bruce Fletcher Johnson, "METHOD FOR MAKING TETRABENAZINE COMPOUNDS." U.S. Patent US20080306267, issued December 11, 2008. (en)
foaf:page	http://www.drugs.com/cdi/tetrabenazine.html http://www.rxlist.com/xenazine-drug.htm
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http://linked.open...ugbank/absorption	Following oral administration of tetrabenazine, the extent of absorption is at least 75%. After single oral doses ranging from 12.5 to 50 mg, plasma concentrations of tetrabenazine are generally below the limit of detection because of the rapid and extensive hepatic metabolism of tetrabenazine. Food does not affect the absorption of tetrabenazine. Cmax, oral = 4.8 ng/mL in HD or tardive dyskinesia patients; Tmax, oral = 69 min in HD or tardive dyskinesia patients (en)
http://linked.open.../affectedOrganism	Humans and other mammals (en)
http://linked.open...casRegistryNumber	58-46-8 (en)
http://linked.open...drugbank/category	(en)
http://linked.open...rugbank/clearance	IV, 1.67 L/min in HD or tardive dyskinesia patients (en)
http://linked.open...gbank/containedIn	Fluphenazine HCl 2.5 mg tablet Feosol 45 mg tablet
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