tiapride 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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
BA (Bioavailability) 75 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 -0.914 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 4.645 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 1.820 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 1.479 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 94.280 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 93.690 % High 1
herg hERG pIC50 4.275 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 1.309 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 2.871 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 94.710 % High 1
kinase-safety-class ACVR2A,ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,JAK2,MAP2K6,MAP3K21,MAP3K7,MAPK7,MAPKAPK2,MTOR,NTRK2,PDK1,PDK2,PIK3CB,PIM2,PLK1,PRKDC,SIK2,SIK3,STK33,SYK,TEK 37
kinase-selectivity-class AXL,BRAF,EPHB4,GRK2,MAPK7,PDK4,SIK2,TEK 8
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 2.685 High 1
mh-clint Mouse hepatocyte intrinsic clearance 3.258 High 1
mppb Mouse plasma protein binding (% unbound) 96.530 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 6.138 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 96.770 % High 1
rh-clint Rat hepatocyte intrinsic clearance 1.603 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 94.140 % High 1
rppb Rat plasma protein binding (% unbound) 94.850 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 891.251 uM High 1

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 157.97 35.20 45 2758 16258 90609386
Somnolence 94.42 35.20 66 2737 209018 90416626
Altered state of consciousness 67.11 35.20 28 2775 31504 90594140
Neuroleptic malignant syndrome 55.68 35.20 20 2783 15076 90610568
Wrong patient 55.36 35.20 11 2792 846 90624798
Vertigo 51.24 35.20 30 2773 69781 90555863
Fall 50.64 35.20 68 2735 481742 90143902
Drug interaction 48.95 35.20 51 2752 276402 90349242
Joint hyperextension 43.70 35.20 8 2795 397 90625247
Hypoosmolar state 41.17 35.20 7 2796 226 90625418
Hyponatraemia 39.86 35.20 33 2770 133505 90492139
Confusional state 39.73 35.20 54 2749 386151 90239493
Hypotension 38.90 35.20 49 2754 325348 90300296
Hyperaldosteronism 38.73 35.20 7 2796 323 90625321
Dyskinesia 38.67 35.20 20 2783 36514 90589130
Choking 37.19 35.20 14 2789 12019 90613625
Asphyxia 36.25 35.20 12 2791 7091 90618553
Slow response to stimuli 35.76 35.20 8 2795 1088 90624556
Hyponatraemic seizure 35.69 35.20 7 2796 503 90625141
Wrong patient received product 35.45 35.20 10 2793 3467 90622177

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 94.66 28.85 40 2819 21432 42597044
Hepatic fibrosis 71.02 28.85 22 2837 4850 42613626
Coma 65.12 28.85 42 2817 53512 42564964
Apathy 59.25 28.85 22 2837 8384 42610092
Parkinsonism 57.71 28.85 23 2836 10600 42607876
Drug-induced liver injury 56.58 28.85 34 2825 38239 42580237
Hepatic haematoma 54.13 28.85 11 2848 431 42618045
Altered state of consciousness 48.50 28.85 28 2831 29231 42589245
Rhabdomyolysis 42.76 28.85 38 2821 77981 42540495
Pneumonia aspiration 39.17 28.85 30 2829 50048 42568428
Thinking abnormal 33.72 28.85 14 2845 7147 42611329
Inappropriate affect 32.55 28.85 8 2851 748 42617728
Heat stroke 29.52 28.85 8 2851 1100 42617376

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 155.92 28.12 58 5673 28809 110554759
Neuroleptic malignant syndrome 139.63 28.12 56 5675 34003 110549565
Somnolence 112.58 28.12 105 5626 297344 110286224
Altered state of consciousness 96.92 28.12 51 5680 57575 110525993
Coma 76.64 28.12 57 5674 117812 110465756
Parkinsonism 72.36 28.12 31 5700 22156 110561412
Fall 69.29 28.12 117 5614 603365 109980203
Drug interaction 66.95 28.12 104 5627 500079 110083489
Hepatic fibrosis 65.65 28.12 22 5709 8044 110575524
Confusional state 57.93 28.12 94 5637 468586 110114982
Dyskinesia 57.87 28.12 35 5696 51411 110532157
Asphyxia 56.93 28.12 23 5708 14192 110569376
Pneumonia aspiration 56.65 28.12 41 5690 81192 110502376
Vertigo 54.19 28.12 41 5690 86829 110496739
Hyponatraemic seizure 51.31 28.12 11 5720 728 110582840
Wrong patient 48.57 28.12 12 5719 1487 110582081
Hepatic haematoma 48.39 28.12 11 5720 954 110582614
Behaviour disorder 47.03 28.12 18 5713 9629 110573939
Loss of consciousness 46.48 28.12 54 5677 196252 110387316
Wrong patient received product 45.72 28.12 16 5715 6658 110576910
Rhabdomyolysis 44.44 28.12 42 5689 120359 110463209
Apathy 44.24 28.12 20 5711 16219 110567349
Drug-induced liver injury 42.63 28.12 41 5690 120026 110463542
Poisoning 41.21 28.12 23 5708 29082 110554486
Joint hyperextension 40.06 28.12 8 5723 373 110583195
Hypotension 39.46 28.12 85 5646 523764 110059804
Intentional overdose 39.23 28.12 41 5690 132460 110451108
Dystonia 38.20 28.12 21 5710 25784 110557784
Inappropriate affect 37.42 28.12 10 5721 1689 110581879
Aggression 37.03 28.12 28 5703 59182 110524386
Hypothermia 35.11 28.12 20 5711 26282 110557286
Delirium 35.09 28.12 39 5692 134986 110448582
Delusion 34.25 28.12 19 5712 23736 110559832
Agitation 33.49 28.12 35 5696 113016 110470552
Hypoosmolar state 33.46 28.12 7 5724 412 110583156
Restlessness 31.68 28.12 25 5706 56234 110527334
Suicide attempt 30.61 28.12 32 5699 103362 110480206
Hyperaldosteronism 30.34 28.12 7 5724 648 110582920
Arthralgia 29.72 28.12 3 5728 779629 109803939
Paradoxical drug reaction 29.65 28.12 13 5718 9804 110573764
Drug abuse 29.58 28.12 41 5690 177370 110406198
Disturbance in attention 29.55 28.12 25 5706 61970 110521598
Avoidant personality disorder 29.22 28.12 5 5726 98 110583470
Electrocardiogram QT prolonged 29.22 28.12 32 5699 108928 110474640
Psychomotor retardation 29.12 28.12 12 5719 7780 110575788
Hyponatraemia 28.65 28.12 45 5686 217608 110365960

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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

Related Drugs by ATC class:

N05AL Benzamides 6 drugs
amisulpridelevosulpirideremoxipridesulpiridesultoprideveralipride

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
LAH70H9JPH INXIGHT DRUGS

Pharmaceutical products:

None