tiapride ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
sulpiride derivatives 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 ยตM/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

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 125.07 39.54 35 1552 11735 50591802
Altered state of consciousness 55.09 39.54 22 1565 21888 50581649
Somnolence 51.71 39.54 41 1546 154944 50448593
Confusional state 47.18 39.54 42 1545 185886 50417651
Joint hyperextension 46.13 39.54 8 1579 287 50603250
Dyskinesia 43.60 39.54 20 1567 27841 50575696
Hyperaldosteronism 40.93 39.54 7 1580 231 50603306

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 84.82 34.02 34 1933 16114 29556446
Hepatic fibrosis 70.85 34.02 20 1947 3232 29569328
Drug-induced liver injury 65.81 34.02 31 1936 21624 29550936
Parkinsonism 58.76 34.02 21 1946 7257 29565303
Hepatic haematoma 55.47 34.02 11 1956 384 29572176
Coma 53.41 34.02 33 1934 39417 29533143
Altered state of consciousness 49.94 34.02 25 1942 19864 29552696
Rhabdomyolysis 42.66 34.02 34 1933 60774 29511786
Apathy 39.44 34.02 15 1952 6156 29566404
Psychomotor skills impaired 34.63 34.02 11 1956 2650 29569910

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 127.23 30.86 46 3573 19506 64475607
Neuroleptic malignant syndrome 95.63 30.86 40 3579 24956 64470157
Altered state of consciousness 88.64 30.86 43 3576 37859 64457254
Somnolence 74.34 30.86 73 3546 203572 64291541
Parkinsonism 68.70 30.86 27 3592 14346 64480767
Coma 66.55 30.86 48 3571 87567 64407546
Dyskinesia 64.04 30.86 35 3584 39353 64455760
Hepatic fibrosis 63.61 30.86 20 3599 5532 64489581
Confusional state 54.55 30.86 70 3549 261074 64234039
Hepatic haematoma 49.20 30.86 11 3608 817 64494296
Drug-induced liver injury 47.76 30.86 31 3588 47612 64447501
Pneumonia aspiration 46.18 30.86 33 3586 59238 64435875
Rhabdomyolysis 43.27 30.86 38 3581 91688 64403425
Joint hyperextension 42.30 30.86 8 3611 258 64494855
Behaviour disorder 38.62 30.86 13 3606 4449 64490664
Fall 37.34 30.86 76 3543 416750 64078363
Wrong patient received product 36.72 30.86 12 3607 3750 64491363
Hyperaldosteronism 33.48 30.86 7 3612 379 64494734
Psychomotor skills impaired 32.48 30.86 11 3608 3834 64491279
Hyponatraemic seizure 31.66 30.86 7 3612 494 64494619
Dystonia 31.29 30.86 17 3602 18848 64476265

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




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ 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