domperidone Indications/Contra | FAERs | Orange Book | BioActivity |

Stem definitionDrug idCAS RN
antipsychotics, risperidone derivatives 945 57808-66-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • domperidone betadex
  • domperidone betacyclodextrin
  • domperidone
  • motilium
  • peridon
  • domperidone maleate
A specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms.
  • Molecular weight: 425.92
  • Formula: C22H24ClN5O2
  • CLOGP: 4.27
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 2
  • TPSA: 67.92
  • ALOGS: -3.66
  • ROTB: 5

Drug dosage:

DoseUnitRoute
30 mg O
30 mg P
0.12 g R

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1982 YEAR INTRODUCED

FDA Adverse Event Reporting System

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
Electrocardiogram QT prolonged 283.81 50.26 73 1039 15222 4622658
Vomiting 172.52 50.26 85 1027 119614 4518266
Premature labour 157.44 50.26 32 1080 2300 4635580
Exposure during pregnancy 156.32 50.26 55 1057 32916 4604964
Intentional overdose 125.12 50.26 42 1070 21724 4616156
Foetal exposure during pregnancy 118.64 50.26 41 1071 23128 4614752
Akathisia 111.64 50.26 26 1086 3517 4634363
Nausea 110.61 50.26 73 1039 177260 4460620
Gastrointestinal disorder 104.26 50.26 34 1078 16027 4621853
Dehydration 97.97 50.26 42 1070 42248 4595632
Suicidal ideation 94.42 50.26 34 1078 21549 4616331
Condition aggravated 91.19 50.26 44 1068 58127 4579753
Drug interaction 86.87 50.26 44 1068 64464 4573416
Torsade de pointes 83.34 50.26 21 1091 3940 4633940
Cholestasis 81.97 50.26 24 1088 7896 4629984
Coma 81.87 50.26 29 1083 17490 4620390
Product use issue 78.77 50.26 31 1081 25005 4612875
Pyrexia 78.52 50.26 49 1063 107095 4530785
Off label use 77.33 50.26 52 1060 129061 4508819
Somnolence 74.34 50.26 35 1077 43625 4594255
Hyperprolactinaemia 74.01 50.26 15 1097 1055 4636825
Pulmonary malformation 74.00 50.26 11 1101 119 4637761
Subileus 72.95 50.26 15 1097 1133 4636747
Premature baby 72.18 50.26 23 1089 10028 4627852
Fatigue 71.69 50.26 52 1060 145514 4492366
Rash maculo-papular 71.63 50.26 22 1090 8507 4629373
Dystonia 70.20 50.26 19 1093 4699 4633181
Mental disorder 69.97 50.26 21 1091 7513 4630367
Abdominal pain 69.40 50.26 37 1075 59987 4577893
Fall 68.17 50.26 40 1072 78006 4559874
Dysphagia 67.82 50.26 28 1084 25503 4612377
Hepatocellular injury 64.73 50.26 20 1092 7880 4630000
Mydriasis 64.62 50.26 17 1095 3771 4634109
Urinary retention 64.43 50.26 21 1091 9826 4628054
Pituitary tumour benign 63.73 50.26 12 1100 574 4637306
Hyponatraemia 61.90 50.26 26 1086 24704 4613176
Hypokalaemia 61.68 50.26 24 1088 18736 4619144
Infusion site vesicles 61.18 50.26 9 1103 90 4637790
Decreased appetite 60.23 50.26 33 1079 56364 4581516
Maternal exposure during breast feeding 58.50 50.26 13 1099 1419 4636461
Vascular encephalopathy 58.26 50.26 9 1103 128 4637752
Faecaloma 56.07 50.26 13 1099 1715 4636165
Diarrhoea 54.88 50.26 45 1067 150140 4487740
Duodenal stenosis 54.38 50.26 9 1103 202 4637678
Respiratory depth decreased 53.95 50.26 7 1105 24 4637856
Loss of consciousness 52.77 50.26 26 1086 35656 4602224
Parkinson's disease 52.60 50.26 14 1098 3242 4634638
Exposure via breast milk 52.41 50.26 11 1101 917 4636963
Cognitive disorder 51.38 50.26 18 1094 10463 4627417
Psychotic disorder 50.86 50.26 18 1094 10777 4627103

Pharmacologic Action:

SourceCodeDescription
ATC A03FA03 ALIMENTARY TRACT AND METABOLISM
DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS
PROPULSIVES
Propulsives
MeSH PA D000932 Antiemetics
MeSH PA D002491 Central Nervous System Agents
MeSH PA D015259 Dopamine Agents
MeSH PA D018492 Dopamine Antagonists
MeSH PA D005765 Gastrointestinal Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018373 Peripheral Nervous System Agents
CHEBI has role CHEBI:50919 antiemetic
CHEBI has role CHEBI:48561 dopaminergic antagonist

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Nausea and vomiting indication 16932000
Acute gastric ulcer with perforation contraindication 19850005
Torsades de pointes contraindication 31722008
Acute nephropathy contraindication 58574008
Acute gastric ulcer with hemorrhage contraindication 89748001
Prolonged QT interval contraindication 111975006
Gastrointestinal obstruction contraindication 126765001
Disease of liver contraindication 235856003 DOID:409
Pregnancy, function contraindication 289908002
Congenital long QT syndrome contraindication 442917000
Pituitary Prolactinoma contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.45 acidic
pKa2 10.04 acidic
pKa3 7.79 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 8.40 IUPHAR IUPHAR
Mu-type opioid receptor GPCR Ki 5.77 DRUG MATRIX
Alpha-2A adrenergic receptor GPCR Ki 5.99 DRUG MATRIX
Sodium-dependent serotonin transporter Transporter Ki 5.79 DRUG MATRIX
Sodium-dependent noradrenaline transporter Transporter Ki 5.59 DRUG MATRIX
5-hydroxytryptamine receptor 2A GPCR Ki 7.96 DRUG MATRIX
5-hydroxytryptamine receptor 2B GPCR Ki 5.78 DRUG MATRIX
5-hydroxytryptamine receptor 2C GPCR Ki 6.16 DRUG MATRIX
Alpha-2B adrenergic receptor GPCR Ki 6.01 DRUG MATRIX
Histamine H1 receptor GPCR Ki 6.81 DRUG MATRIX
Alpha-2C adrenergic receptor GPCR Ki 6.83 DRUG MATRIX
Alpha-1D adrenergic receptor GPCR Ki 6.94 DRUG MATRIX
Kappa-type opioid receptor GPCR Ki 5.55 DRUG MATRIX
Calmodulin Cytosolic other WOMBAT-PK
Alpha-1B adrenergic receptor GPCR Ki 6.28 WOMBAT-PK
Cytochrome P450 2D6 Enzyme Ki 5.10 WOMBAT-PK
Aldehyde oxidase Enzyme IC50 5.52 WOMBAT-PK
Alpha-1A adrenergic receptor GPCR Ki 6.65 WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 6.79 WOMBAT-PK
Solute carrier family 22 member 2 Transporter IC50 5.10 CHEMBL
D(3) dopamine receptor GPCR Ki 8.46 CHEMBL
Multidrug and toxin extrusion protein 2 Transporter IC50 4.83 CHEMBL
Multidrug and toxin extrusion protein 1 Transporter IC50 5.64 CHEMBL
Multidrug resistance protein 1 Transporter WOMBAT-PK
Alpha-1B adrenergic receptor GPCR Ki 7.06 DRUG MATRIX
D(3) dopamine receptor GPCR Ki 7.93 CHEMBL
D(2) dopamine receptor GPCR Ki 9.28 CHEMBL
Alpha-1A adrenergic receptor GPCR IC50 6.55 CHEMBL

External reference:

IDSource
D004294 MESH_DESCRIPTOR_UI
4025225 VUID
N0000171760 NUI
C0013015 UMLSCUI
D01745 KEGG_DRUG
5587267Z69 UNII
4110 INN_ID
32955006 SNOMEDCT_US
3626 RXNORM
387181004 SNOMEDCT_US
4025225 VANDF
003454 NDDF
83898-65-1 SECONDARY_CAS_RN
CHEMBL219916 ChEMBL_ID
DB01184 DRUGBANK_ID
CHEBI:31515 CHEBI
965 IUPHAR_LIGAND_ID
3151 PUBCHEM_CID

Pharmaceutical products:

None