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 |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.10 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 0 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 45.00 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 5 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 15, 2008 | FDA | VALEANT PHARMS NORTH |
FDA Adverse Event Reporting System (Female)
| 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 | 224.05 | 37.07 | 153 | 2139 | 325226 | 50277606 |
| Off label use | 189.11 | 37.07 | 161 | 2131 | 474265 | 50128567 |
| Parkinsonism | 108.79 | 37.07 | 32 | 2260 | 8815 | 50594017 |
| Hospitalisation | 95.78 | 37.07 | 51 | 2241 | 67886 | 50534946 |
| Dyskinesia | 76.19 | 37.07 | 33 | 2259 | 27828 | 50575004 |
| Tardive dyskinesia | 75.08 | 37.07 | 23 | 2269 | 7256 | 50595576 |
| Prescribed overdose | 73.97 | 37.07 | 27 | 2265 | 14573 | 50588259 |
| Product administration error | 73.03 | 37.07 | 29 | 2263 | 19670 | 50583162 |
| Depression | 64.65 | 37.07 | 56 | 2236 | 165367 | 50437465 |
| Hospice care | 58.51 | 37.07 | 18 | 2274 | 5754 | 50597078 |
| Somnolence | 44.08 | 37.07 | 44 | 2248 | 154941 | 50447891 |
| Product substitution issue | 42.86 | 37.07 | 18 | 2274 | 14039 | 50588793 |
| Akathisia | 40.85 | 37.07 | 15 | 2277 | 8214 | 50594618 |
FDA Adverse Event Reporting System (Male)
| 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 |
|---|---|---|---|---|---|---|
| Off label use | 143.75 | 44.41 | 125 | 1565 | 300675 | 29272162 |
| Prescribed overdose | 106.32 | 44.41 | 33 | 1657 | 8650 | 29564187 |
| Death | 88.13 | 44.41 | 102 | 1588 | 341982 | 29230855 |
| Hospitalisation | 74.71 | 44.41 | 41 | 1649 | 45947 | 29526890 |
| Tic | 59.62 | 44.41 | 15 | 1675 | 1820 | 29571017 |
| Dystonia | 55.90 | 44.41 | 21 | 1669 | 9728 | 29563109 |
| Parkinsonism | 54.13 | 44.41 | 19 | 1671 | 7259 | 29565578 |
| Neuroleptic malignant syndrome | 52.03 | 44.41 | 23 | 1667 | 16125 | 29556712 |
| Tardive dyskinesia | 51.99 | 44.41 | 17 | 1673 | 5241 | 29567596 |
| Anxiety | 49.41 | 44.41 | 40 | 1650 | 85325 | 29487512 |
| Chorea | 47.16 | 44.41 | 11 | 1679 | 970 | 29571867 |
| Depression | 45.30 | 44.41 | 38 | 1652 | 85109 | 29487728 |
FDA Adverse Event Reporting System (Geriatric)
| 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 | 232.47 | 36.01 | 185 | 2809 | 482520 | 64013218 |
| Off label use | 223.98 | 36.01 | 203 | 2791 | 632603 | 63863135 |
| Parkinsonism | 124.67 | 36.01 | 40 | 2954 | 14333 | 64481405 |
| Prescribed overdose | 111.07 | 36.01 | 40 | 2954 | 20291 | 64475447 |
| Tardive dyskinesia | 98.21 | 36.01 | 30 | 2964 | 9148 | 64486590 |
| Hospitalisation | 86.95 | 36.01 | 50 | 2944 | 75157 | 64420581 |
| Dyskinesia | 82.41 | 36.01 | 39 | 2955 | 39349 | 64456389 |
| Tic | 67.16 | 36.01 | 17 | 2977 | 2602 | 64493136 |
| Product administration error | 56.65 | 36.01 | 27 | 2967 | 27616 | 64468122 |
| Dystonia | 56.42 | 36.01 | 24 | 2970 | 18841 | 64476897 |
| Neuroleptic malignant syndrome | 56.11 | 36.01 | 26 | 2968 | 24970 | 64470768 |
| Drug ineffective | 53.84 | 36.01 | 119 | 2875 | 840128 | 63655610 |
| Depression | 47.35 | 36.01 | 50 | 2944 | 183241 | 64312497 |
| Akathisia | 45.90 | 36.01 | 18 | 2976 | 11492 | 64484246 |
| Somnolence | 43.01 | 36.01 | 50 | 2944 | 203595 | 64292143 |
| Impulsive behaviour | 38.52 | 36.01 | 11 | 2983 | 2652 | 64493086 |
| Suicidal ideation | 36.92 | 36.01 | 28 | 2966 | 66514 | 64429224 |
| Drug ineffective for unapproved indication | 36.71 | 36.01 | 21 | 2973 | 31112 | 64464626 |
| Anxiety | 36.64 | 36.01 | 46 | 2948 | 202603 | 64293135 |
| Sedation | 36.06 | 36.01 | 23 | 2971 | 41439 | 64454299 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N07XX06 | NERVOUS SYSTEM OTHER NERVOUS SYSTEM DRUGS OTHER NERVOUS SYSTEM DRUGS Other nervous system drugs |
| 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 |
| CHEBI has role | CHEBI:35476 | neuroleptics |
| CHEBI has role | CHEBI:35640 | adrenergic uptake inhibitors |
| FDA MoA | N0000190855 | Vesicular Monoamine Transporter 2 Inhibitors |
| FDA EPC | N0000190856 | Vesicular Monoamine Transporter 2 Inhibitor |
Drug Use | Suggest Off label Use Form| |View source of the data|
| 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 | |
| Tardive dyskinesia | contraindication | 102449007 | |
| Prolonged QT interval | contraindication | 111975006 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Hyperprolactinemia | contraindication | 237662005 | DOID:12700 |
| Suicidal | contraindication | 267073005 | |
| Akathisia | contraindication | 285145004 | |
| Severe depression | contraindication | 310497006 | |
| Impaired cognition | contraindication | 386806002 | |
| Poor metabolizer due to cytochrome p450 CYP2D6 variant | contraindication | 423629005 | |
| Congenital long QT syndrome | contraindication | 442917000 |
🐶 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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Synaptic vesicular amine transporter | Transporter | INHIBITOR | Ki | 7 | WOMBAT-PK | CHEMBL | |||
| Alpha-2A adrenergic receptor | GPCR | Ki | 6.02 | WOMBAT-PK | |||||
| Alpha-2C adrenergic receptor | GPCR | Ki | 5.89 | WOMBAT-PK | |||||
| Chromaffin granule amine transporter | Transporter | INHIBITOR | Ki | 4.70 | IUPHAR | ||||
| D(2) dopamine receptor | GPCR | Ki | 5.68 | WOMBAT-PK | |||||
| Sodium channel alpha subunits; brain (Types I, II, III) | Ion channel | IC50 | 4.07 | CHEMBL | |||||
| Synaptic vesicular amine transporter | Transporter | Ki | 8.40 | CHEMBL | |||||
| Synaptic vesicular amine transporter | Transporter | Ki | 8.12 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4027903 | VUID |
| N0000177920 | NUI |
| D08575 | KEGG_DRUG |
| 4027903 | VANDF |
| C0039623 | UMLSCUI |
| CHEBI:9467 | CHEBI |
| CHEMBL117785 | ChEMBL_ID |
| DB04844 | DRUGBANK_ID |
| D013747 | MESH_DESCRIPTOR_UI |
| 6018 | PUBCHEM_CID |
| 4834 | IUPHAR_LIGAND_ID |
| 1056 | INN_ID |
| Z9O08YRN8O | UNII |
| 14580381 | PUBCHEM_CID |
| 10390 | RXNORM |
| 16831 | MMSL |
| 63336 | MMSL |
| d04597 | MMSL |
| 003767 | NDDF |
| 323260004 | SNOMEDCT_US |
| 363581004 | SNOMEDCT_US |
Pharmaceutical products:
| 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 |
| Tetrabenazine | Human Prescription Drug Label | 1 | 47335-179 | TABLET | 25 mg | ORAL | ANDA | 31 sections |
| Tetrabenazine | Human Prescription Drug Label | 1 | 47335-277 | TABLET | 12.50 mg | ORAL | ANDA | 31 sections |
| TETRABENAZINE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51224-425 | TABLET | 12.50 mg | ORAL | ANDA | 32 sections |
| TETRABENAZINE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51224-426 | TABLET | 25 mg | ORAL | ANDA | 32 sections |
| Tetrabenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51407-480 | TABLET | 12.50 mg | ORAL | ANDA | 32 sections |
| Tetrabenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51407-481 | TABLET | 25 mg | ORAL | ANDA | 32 sections |
| Tetrabenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60505-3882 | TABLET | 12.50 mg | ORAL | ANDA | 32 sections |
| Tetrabenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60505-3883 | TABLET | 25 mg | ORAL | ANDA | 32 sections |
| Xenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67386-421 | TABLET | 12.50 mg | ORAL | NDA | 31 sections |
| Xenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67386-422 | TABLET | 25 mg | ORAL | NDA | 31 sections |
| Tetrabenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68180-408 | TABLET | 12.50 mg | ORAL | ANDA | 31 sections |
| Tetrabenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68180-409 | TABLET | 25 mg | ORAL | ANDA | 31 sections |
| tetrabenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68682-421 | TABLET | 12.50 mg | ORAL | NDA authorized generic | 31 sections |
| tetrabenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68682-422 | TABLET | 25 mg | ORAL | NDA authorized generic | 31 sections |
| TETRABENAZINE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69452-117 | TABLET | 12.50 mg | ORAL | ANDA | 21 sections |
| TETRABENAZINE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69452-118 | TABLET | 25 mg | ORAL | ANDA | 21 sections |
| tetrabenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70436-101 | TABLET | 12.50 mg | ORAL | ANDA | 31 sections |
| tetrabenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70436-102 | TABLET | 25 mg | ORAL | ANDA | 31 sections |