alizapride 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
sulpiride derivatives and analogues 120 59338-93-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • alizapride
  • alizapride hydrochloride
  • alizapride HCl
a dopamine antagonist with prokinetic and antiemetic effects used in the treatment of nausea and vomiting, including postoperative nausea and vomiting. Its effect is due to its antagonist activity at D2 receptors in the chemoreceptor trigger zone (CTZ) in the central nervous system (CNS), this action prevents nausea and vomiting triggered by most stimuli.
  • Molecular weight: 315.38
  • Formula: C16H21N5O2
  • CLOGP: 2.53
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 2
  • TPSA: 83.14
  • ALOGS: -2.84
  • ROTB: 6

Drug dosage:

DoseUnitRoute
0.15 g O
0.15 g P

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 28.42 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 84 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 1.60 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 6.60 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 2.80 hours Lombardo F, Berellini G, Obach RS
S (Water solubility) 70 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,AURKA,AXL,BRAF,CAMK2D,CDK5,CDK9,DYRK1B,EGFR,EIF2AK3,ERBB2,GRK1,GRK2,GRK3,ITK,MAP3K21,MAPK1,MAPK7,PDK1,PDK2,PDK4,PRKDC,SIK2,TEK 24
kinase-selectivity-class CAMK2D,EGFR,EIF2AK3,GAK,GRK2,IRAK1,MAP3K7,PDK1,SIK2,SIK3,STK33 11
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1981 YEAR INTRODUCED

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
Encephalopathy 93.93 35.30 41 3074 46403 90578929
Febrile bone marrow aplasia 74.71 35.30 23 3092 9715 90615617
Bronchospasm 61.23 35.30 24 3091 20685 90604647
Hypokalaemia 61.02 35.30 44 3071 131072 90494260
Neutropenia 49.49 35.30 49 3066 224855 90400477
Hypofibrinogenaemia 49.06 35.30 11 3104 1359 90623973
Psychiatric decompensation 45.23 35.30 11 3104 1932 90623400
Febrile neutropenia 43.43 35.30 39 3076 158310 90467022
Blood phosphorus decreased 43.35 35.30 13 3102 5021 90620311
Polyneuropathy 42.09 35.30 18 3097 19323 90606009
Clonus 41.65 35.30 13 3102 5737 90619595
Persecutory delusion 39.76 35.30 11 3104 3197 90622135
Aplasia 37.38 35.30 11 3104 3980 90621352
Thrombocytopenia 36.08 35.30 40 3075 208685 90416647

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
General physical health deterioration 48.55 27.88 53 2589 151193 42467500
Alopecia 34.78 27.88 22 2620 29254 42589439
Nail bed inflammation 31.68 27.88 6 2636 176 42618517
Thrombocytopenia 31.42 27.88 48 2594 190231 42428462
Neutropenia 29.72 27.88 48 2594 199383 42419310
Periodontitis 28.81 27.88 9 2633 2202 42616491
Drug ineffective 28.61 27.88 3 2639 630194 41988499

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
Encephalopathy 105.33 27.29 60 5539 80995 110502705
Neutropenia 80.82 27.29 97 5502 374523 110209177
Polyneuropathy 71.19 27.29 34 5565 31978 110551722
Febrile bone marrow aplasia 66.26 27.29 27 5572 17438 110566262
Hypokalaemia 65.53 27.29 62 5537 182386 110401314
Thrombocytopenia 65.04 27.29 84 5515 348801 110234899
Bronchospasm 54.97 27.29 28 5571 30211 110553489
Febrile neutropenia 49.45 27.29 70 5529 316697 110267003
Decreased appetite 41.60 27.29 81 5518 475765 110107935
General physical health deterioration 40.39 27.29 75 5524 425220 110158480
Persecutory delusion 39.30 27.29 14 5585 6277 110577423
Mucosal inflammation 37.03 27.29 34 5565 96107 110487593
Drug ineffective 36.18 27.29 16 5583 1520524 109063176
Anaemia 34.96 27.29 82 5517 547004 110036696
Blood phosphorus decreased 33.05 27.29 13 5586 7652 110576048
Clonus 31.44 27.29 13 5586 8703 110574997
Acute kidney injury 30.01 27.29 85 5514 635345 109948355
Leukopenia 29.50 27.29 37 5562 148754 110434946
Cholangitis 29.32 27.29 15 5584 16320 110567380
Transverse sinus thrombosis 29.31 27.29 7 5592 771 110582929
Psychiatric decompensation 29.23 27.29 11 5588 5754 110577946
Hyperthermia 28.27 27.29 16 5583 21256 110562444
Proteinuria 27.85 27.29 20 5579 39998 110543702

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC A03FA05 ALIMENTARY TRACT AND METABOLISM
DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS
PROPULSIVES
Propulsives
MeSH PA D000932 Antiemetics
MeSH PA D002491 Central Nervous System Agents
MeSH PA D005765 Gastrointestinal Agents
MeSH PA D018373 Peripheral Nervous System Agents

Related Drugs by ATC class:

A03FA Propulsives 9 drugs
acotiamidebromopridecinitapridecisaprideclebopridedomperidoneitopridemetoclopramidemosapride

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

DiseaseRelationSNOMED_IDDOID
Postoperative nausea and vomiting indication 1488000
Nausea and vomiting indication 16932000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.11 acidic
pKa2 13.45 acidic
pKa3 8.72 Basic
pKa4 0.34 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 ANTAGONIST Ki 7.15 WOMBAT-PK DRUGBANK
Alpha-2C adrenergic receptor GPCR Ki 7 WOMBAT-PK
D(2) dopamine receptor GPCR IC50 6.70 CHEMBL

External reference:

IDSource
D07102 KEGG_DRUG
17311 RXNORM
C0051162 UMLSCUI
CHEBI:748164 CHEBI
CHEMBL290194 ChEMBL_ID
DB01425 DRUGBANK_ID
C033968 MESH_SUPPLEMENTAL_RECORD_UI
135413504 PUBCHEM_CID
11141 IUPHAR_LIGAND_ID
4823 INN_ID
59338-87-3 SECONDARY_CAS_RN
P55703ZRZY UNII
005228 NDDF
005246 NDDF
724156007 SNOMEDCT_US
734457001 SNOMEDCT_US

Pharmaceutical products:

None