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tetrabenazine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	2609	58-46-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: choreazine tetrabenazine (+/-)-Tetrabenazine rubigen	A drug formerly used as an antipsychotic and treatment of various movement disorders. Tetrabenazine blocks neurotransmitter uptake into adrenergic storage vesicles and has been used as a high affinity label for the vesicle transport system. Molecular weight: 317.43 Formula: C19H27NO3 CLOGP: 3.27 LIPINSKI: 0 HAC: 4 HDO: 0 TPSA: 38.77 ALOGS: -2.94 ROTB: 4 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

choreazine
tetrabenazine
(+/-)-Tetrabenazine
rubigen

A drug formerly used as an antipsychotic and treatment of various movement disorders. Tetrabenazine blocks neurotransmitter uptake into adrenergic storage vesicles and has been used as a high affinity label for the vesicle transport system.

Molecular weight: 317.43
Formula: C19H27NO3
CLOGP: 3.27
LIPINSKI: 0
HAC: 4
HDO: 0
TPSA: 38.77
ALOGS: -2.94
ROTB: 4

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.10	g	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	5 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
MRTD (Maximum Recommended Therapeutic Daily Dose)	45.00 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Bocci G, Oprea TI, Benet LZ
S (Water solubility)	0.34 mg/mL	Bocci G, Oprea TI, Benet LZ
fu (Fraction unbound in plasma)	0.14 %	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K
EoM (Fraction excreted unchanged in urine)	0 %	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Aug. 15, 2008	FDA	VALEANT PHARMS NORTH

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Death	564.69	30.91	329	3785	374052	63110856
Depression	235.03	30.91	150	3964	196342	63288566
Parkinsonism	166.12	30.91	50	4064	10389	63474519
Dyskinesia	117.92	30.91	52	4062	31950	63452958
Off label use	102.46	30.91	167	3947	674295	62810613
Tardive dyskinesia	98.65	30.91	32	4082	8470	63476438
Somnolence	80.99	30.91	77	4037	178608	63306300
Dysphagia	79.91	30.91	57	4057	88528	63396380
Hospitalisation	79.65	30.91	56	4058	85025	63399883
Product administration error	77.99	30.91	35	4079	22362	63462546

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Death	259.82	34.69	232	2676	397817	34556206
Depression	105.52	34.69	77	2831	97021	34857002
Dystonia	97.83	34.69	36	2872	10809	34943214
Prescribed overdose	87.45	34.69	33	2875	10614	34943409
Tic	85.08	34.69	22	2886	2036	34951987
Off label use	84.29	34.69	135	2773	419389	34534634
Suicidal ideation	78.05	34.69	46	2862	40342	34913681
Chorea	71.40	34.69	17	2891	1120	34952903
Anxiety	67.63	34.69	60	2848	99368	34854655
Hospitalisation	61.35	34.69	45	2863	56857	34897166

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Death	473.96	31.35	307	3533	566207	79174341
Off label use	176.88	31.35	216	3624	906999	78833549
Parkinsonism	153.82	31.35	49	3791	16535	79724013
Tardive dyskinesia	113.74	31.35	35	3805	10536	79730012
Dystonia	86.05	31.35	34	3806	21365	79719183
Prescribed overdose	85.52	31.35	40	3800	37843	79702705
Dyskinesia	85.08	31.35	42	3798	44731	79695817
Hospitalisation	84.59	31.35	54	3786	94182	79646366
Suicidal ideation	79.26	31.35	48	3792	76292	79664256
Depression	76.04	31.35	71	3769	216719	79523829

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N07XX06	NERVOUS SYSTEM OTHER NERVOUS SYSTEM DRUGS OTHER NERVOUS SYSTEM DRUGS Other nervous system drugs
CHEBI has role	CHEBI:35476	neuroleptics
CHEBI has role	CHEBI:35640	adrenergic uptake inhibitors
FDA EPC	N0000190856	Vesicular Monoamine Transporter 2 Inhibitor
FDA MoA	N0000190855	Vesicular Monoamine Transporter 2 Inhibitors
MeSH PA	D018663	Adrenergic Agents
MeSH PA	D018759	Adrenergic Uptake Inhibitors
MeSH PA	D049990	Membrane Transport Modulators
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D014179	Neurotransmitter Uptake Inhibitors

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Huntington's chorea	indication	58756001	DOID:12858
Suicidal thoughts	contraindication	6471006
Mood swings	contraindication	18963009
Feeling agitated	contraindication	24199005
Orthostatic hypotension	contraindication	28651003
Torsades de pointes	contraindication	31722008
Parkinsonism	contraindication	32798002
Depressive disorder	contraindication	35489007
Dysphagia	contraindication	40739000
Low blood pressure	contraindication	45007003

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.01	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Synaptic vesicular amine transporter	Transporter	Q05940	VMAT2_HUMAN	INHIBITOR	Ki	7	WOMBAT-PK	CHEMBL
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	6.02	WOMBAT-PK
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN		Ki	5.89	WOMBAT-PK
Chromaffin granule amine transporter	Transporter	P54219	VMAT1_HUMAN	INHIBITOR	Ki	4.70	IUPHAR
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN		Ki	5.68	WOMBAT-PK
Sodium channel alpha subunits; brain (Types I, II, III)	Ion channel	P35498 Q99250 Q9NY46	SCN1A_HUMAN SCN2A_HUMAN SCN3A_HUMAN		IC50	4.07	CHEMBL
Synaptic vesicular amine transporter	Transporter		VMAT2_BOVIN		Ki	8.40	CHEMBL
Synaptic vesicular amine transporter	Transporter		VMAT2_RAT		Ki	8.12	CHEMBL

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External reference:

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ID	Source
003767	NDDF
10390	RXNORM
1056	INN_ID
14580381	PUBCHEM_CID
16831	MMSL
323260004	SNOMEDCT_US
363581004	SNOMEDCT_US
4027903	VUID
4027903	VANDF
4834	IUPHAR_LIGAND_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Tetrabenazine	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0468	TABLET	12.50 mg	ORAL	ANDA	30 sections
Tetrabenazine	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0469	TABLET	25 mg	ORAL	ANDA	30 sections
Tetrabenazine	Human Prescription Drug Label	1	27241-176	TABLET	12.50 mg	ORAL	ANDA	30 sections
Tetrabenazine	Human Prescription Drug Label	1	27241-177	TABLET	25 mg	ORAL	ANDA	30 sections
Tetrabenazine	Human Prescription Drug Label	1	31722-821	TABLET, COATED	12.50 mg	ORAL	ANDA	31 sections
Tetrabenazine	Human Prescription Drug Label	1	31722-822	TABLET, COATED	25 mg	ORAL	ANDA	31 sections
Tetrabenazine	HUMAN PRESCRIPTION DRUG LABEL	1	42291-806	TABLET	12.50 mg	ORAL	ANDA	33 sections
Tetrabenazine	HUMAN PRESCRIPTION DRUG LABEL	1	42291-807	TABLET	25 mg	ORAL	ANDA	33 sections
Tetrabenazine	HUMAN PRESCRIPTION DRUG LABEL	1	43598-394	TABLET	12.50 mg	ORAL	ANDA	30 sections
Tetrabenazine	HUMAN PRESCRIPTION DRUG LABEL	1	43598-395	TABLET	25 mg	ORAL	ANDA	30 sections

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