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

Stem definitionDrug idCAS RN
1784 14008-44-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • metopimazine hydrochloride
  • metopimazine HCl
  • metopimazine
  • vogalene
  • Molecular weight: 445.60
  • Formula: C22H27N3O3S2
  • CLOGP: 1.30
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 1
  • TPSA: 83.71
  • ALOGS: -4.37
  • ROTB: 6

Drug dosage:

DoseUnitRoute
15 mg O
15 mg P

ADMET properties:

PropertyValueReference
BA (Bioavailability) 20 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
CL (Clearance) 12.14 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 4 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
Acute kidney injury 78.08 36.80 54 1211 263361 63224396
Cholestasis 58.51 36.80 22 1243 29412 63458345
Febrile bone marrow aplasia 50.11 36.80 14 1251 7311 63480446
Drug reaction with eosinophilia and systemic symptoms 48.62 36.80 20 1245 33816 63453941
Hyperkalaemia 45.56 36.80 22 1243 54181 63433576
Poisoning deliberate 40.11 36.80 13 1252 11205 63476552

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
Analgesic drug level increased 52.82 49.92 10 760 846 34955315

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
Acute kidney injury 102.83 34.48 95 2045 519309 79222939
Coma 57.61 34.48 35 2105 100614 79641634
Cholestasis 57.48 34.48 28 2112 52081 79690167
Poisoning deliberate 54.16 34.48 20 2120 18808 79723440
Drug reaction with eosinophilia and systemic symptoms 51.94 34.48 28 2112 64216 79678032
Febrile bone marrow aplasia 41.79 34.48 15 2125 13005 79729243
Hepatitis 41.46 34.48 23 2117 55704 79686544
Hyperkalaemia 39.35 34.48 29 2111 114369 79627879
Analgesic drug level increased 37.75 34.48 10 2130 3168 79739080
Thrombocytopenia 36.42 34.48 40 2100 265219 79477029
Hepatocellular injury 36.38 34.48 20 2120 47573 79694675

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC A04AD05 ALIMENTARY TRACT AND METABOLISM
ANTIEMETICS AND ANTINAUSEANTS
ANTIEMETICS AND ANTINAUSEANTS
Other antiemetics
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|

None




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.41 acidic
pKa2 8.95 Basic
pKa3 3.45 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 10.15 CHEMBL
D(3) dopamine receptor GPCR Ki 9.21 CHEMBL
Histamine H1 receptor GPCR Ki 8.08 CHEMBL

External reference:

IDSource
D05010 KEGG_DRUG
C0066469 UMLSCUI
CHEBI:135726 CHEBI
CHEMBL398615 ChEMBL_ID
DB13591 DRUGBANK_ID
C005260 MESH_SUPPLEMENTAL_RECORD_UI
11140 IUPHAR_LIGAND_ID
2178 INN_ID
238S75V9AV UNII
26388 PUBCHEM_CID
29954 RXNORM
005826 NDDF

Pharmaceutical products:

None