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

Stem definitionDrug idCAS RN
sulpiride derivatives and analogues 2651 51012-32-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • tiapridal
  • tiapride monohydrochloride
  • tiapride hydrochloride
  • tiapride
  • thiapride
  • tiaprizal
  • tiapride HCl
A benzamide derivative that is used as a dopamine antagonist.
  • Molecular weight: 328.43
  • Formula: C15H24N2O4S
  • CLOGP: 1.40
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 1
  • TPSA: 75.71
  • ALOGS: -3.12
  • ROTB: 8

Drug dosage:

DoseUnitRoute
0.40 g O
0.40 g P

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 21.75 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Hosey CM, Chan R, Benet LZ
Vd (Volume of distribution) 1.10 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 4.70 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 3.20 hours Lombardo F, Berellini G, Obach RS
S (Water solubility) 73 mg/mL Bocci G, Oprea TI, Benet LZ

Approvals:

None

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Extrapyramidal disorder 128.54 35.96 36 1782 13248 63473956
Altered state of consciousness 57.45 35.96 23 1795 25207 63461997
Confusional state 55.26 35.96 49 1769 236331 63250873
Somnolence 54.05 35.96 43 1775 178642 63308562
Vertigo 49.32 35.96 27 1791 59860 63427344
Dyskinesia 45.80 35.96 21 1797 31981 63455223
Joint hyperextension 45.11 35.96 8 1810 359 63486845
Fall 42.53 35.96 54 1764 392280 63094924
Hyperaldosteronism 41.33 35.96 7 1811 239 63486965
Hyponatraemic seizure 37.22 35.96 7 1811 436 63486768
Slow response to stimuli 36.86 35.96 8 1810 1024 63486180
Hypoosmolar state 35.99 35.96 6 1812 186 63487018

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Neuroleptic malignant syndrome 90.30 30.67 36 2149 17898 34936848
Hepatic fibrosis 69.47 30.67 21 2164 4586 34950160
Drug-induced liver injury 62.07 30.67 32 2153 28800 34925946
Parkinsonism 57.74 30.67 21 2164 8117 34946629
Hepatic haematoma 55.74 30.67 11 2174 399 34954347
Apathy 53.35 30.67 19 2166 6913 34947833
Altered state of consciousness 50.96 30.67 26 2159 22867 34931879
Coma 50.83 30.67 33 2152 45645 34909101
Rhabdomyolysis 41.08 30.67 34 2151 68129 34886617
Catatonia 32.06 30.67 12 2173 5013 34949733
Pneumonia aspiration 31.89 30.67 24 2161 41879 34912867
Psychomotor skills impaired 31.16 30.67 11 2174 3895 34950851

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Extrapyramidal disorder 136.16 28.53 49 4005 22630 79717704
Neuroleptic malignant syndrome 102.43 28.53 42 4012 27517 79712817
Altered state of consciousness 89.70 28.53 44 4010 43778 79696556
Somnolence 77.86 28.53 77 3977 238904 79501430
Parkinsonism 67.52 28.53 27 4027 16557 79723777
Dyskinesia 65.81 28.53 36 4018 44737 79695597
Coma 64.80 28.53 48 4006 100601 79639733
Confusional state 64.60 28.53 80 3974 317917 79422417
Hepatic fibrosis 64.23 28.53 21 4033 7259 79733075
Fall 62.16 28.53 98 3956 487531 79252803
Pneumonia aspiration 50.09 28.53 35 4019 66932 79673402
Hepatic haematoma 49.85 28.53 11 4043 850 79739484
Behaviour disorder 46.90 28.53 16 4038 6297 79734037
Drug-induced liver injury 43.57 28.53 32 4022 66085 79674249
Wrong patient received product 43.49 28.53 14 4040 4604 79735730
Drug interaction 42.85 28.53 76 3978 415107 79325227
Rhabdomyolysis 42.64 28.53 38 4016 103093 79637241
Joint hyperextension 41.34 28.53 8 4046 323 79740011
Loss of consciousness 40.18 28.53 46 4008 167897 79572437
Apathy 38.93 28.53 17 4037 12960 79727374
Asphyxia 37.27 28.53 16 4038 11704 79728630
Inappropriate affect 33.81 28.53 9 4045 1527 79738807
Dystonia 33.63 28.53 18 4036 21381 79718953
Hyperaldosteronism 32.94 28.53 7 4047 453 79739881
Aggression 32.08 28.53 24 4030 50934 79689400
Vertigo 31.65 28.53 27 4027 69055 79671279
Hyponatraemic seizure 31.63 28.53 7 4047 548 79739786
Psychomotor skills impaired 30.21 28.53 11 4043 5226 79735108
Restlessness 29.49 28.53 22 4032 46470 79693864
Hypoosmolar state 29.00 28.53 6 4048 341 79739993
Delusion 28.83 28.53 16 4038 20407 79719927

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N05AL03 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Benzamides
MeSH PA D014150 Antipsychotic Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D015259 Dopamine Agents
MeSH PA D018492 Dopamine Antagonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D011619 Psychotropic Drugs
MeSH PA D014149 Tranquilizing Agents

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

None




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.58 acidic
pKa2 8.94 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
D(2) dopamine receptor GPCR Ki 7.08 PDSP
Alpha-2A adrenergic receptor GPCR Ki 6.11 DRUG MATRIX
D(3) dopamine receptor GPCR Ki 6.76 PDSP
D(4) dopamine receptor GPCR Ki 7.85 PDSP

External reference:

IDSource
D01522 KEGG_DRUG
51012-33-0 SECONDARY_CAS_RN
C3179399 UMLSCUI
CHEBI:94666 CHEBI
CHEMBL84158 ChEMBL_ID
CHEMBL1256772 ChEMBL_ID
DB13025 DRUGBANK_ID
D063325 MESH_DESCRIPTOR_UI
5467 PUBCHEM_CID
3289 INN_ID
LAH70H9JPH UNII
10588 RXNORM
35065 MMSL
005728 NDDF
005729 NDDF

Pharmaceutical products:

None