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

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 70.68 31.69 33 2435 38587 63447967
Febrile bone marrow aplasia 65.40 31.69 20 2448 7305 63479249
Hypokalaemia 58.37 31.69 41 2427 103763 63382791
Hypofibrinogenaemia 49.44 31.69 11 2457 1159 63485395
Psychiatric decompensation 47.47 31.69 11 2457 1390 63485164
Bronchospasm 45.25 31.69 19 2449 17261 63469293
Blood phosphorus decreased 43.35 31.69 13 2455 4440 63482114
Clonus 42.84 31.69 13 2455 4623 63481931
Persecutory delusion 39.95 31.69 11 2457 2779 63483775
Polyneuropathy 38.05 31.69 16 2452 14573 63471981
Aplasia 35.35 31.69 11 2457 4248 63482306
Transverse sinus thrombosis 33.47 31.69 7 2461 551 63486003

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 45.15 31.50 46 2006 128223 34826656
Alopecia 39.67 31.50 22 2030 24333 34930546
Thrombocytopenia 32.89 31.50 43 2009 156204 34798675
Nail bed inflammation 32.14 31.50 6 2046 172 34954707

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 85.69 26.21 51 4426 67346 79672565
Polyneuropathy 70.62 26.21 32 4445 24119 79715792
Hypokalaemia 60.71 26.21 56 4421 143984 79595927
Febrile bone marrow aplasia 60.59 26.21 24 4453 12996 79726915
Thrombocytopenia 52.02 26.21 69 4408 265190 79474721
Neutropenia 50.61 26.21 71 4406 287639 79452272
Febrile neutropenia 46.68 26.21 61 4416 230938 79508973
General physical health deterioration 42.67 26.21 64 4413 275174 79464737
Decreased appetite 42.61 26.21 72 4405 342346 79397565
Persecutory delusion 41.29 26.21 14 4463 4895 79735016
Bronchospasm 40.11 26.21 22 4455 24837 79715074
Mucosal inflammation 36.98 26.21 32 4445 75548 79664363
Drug ineffective 36.79 26.21 8 4469 1080905 78659006
Blood phosphorus decreased 33.51 26.21 13 4464 6655 79733256
Clonus 33.19 26.21 13 4464 6827 79733084
Psychiatric decompensation 32.14 26.21 11 4466 3952 79735959
Cholangitis 31.35 26.21 15 4462 12761 79727150
Transverse sinus thrombosis 29.68 26.21 7 4470 658 79739253
Superior sagittal sinus thrombosis 26.42 26.21 7 4470 1056 79738855

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

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:94316 CHEBI
CHEMBL290194 ChEMBL_ID
DB01425 DRUGBANK_ID
C033968 MESH_SUPPLEMENTAL_RECORD_UI
11141 IUPHAR_LIGAND_ID
4823 INN_ID
59338-87-3 SECONDARY_CAS_RN
P55703ZRZY UNII
724156007 SNOMEDCT_US
734457001 SNOMEDCT_US
135497066 PUBCHEM_CID
005228 NDDF
005246 NDDF

Pharmaceutical products:

None