domperidone indications/contra

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

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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 192.31 42.52 48 657 10747 3374407
Vomiting 126.40 42.52 59 646 89472 3295682
Intentional overdose 108.37 42.52 33 672 15192 3369962
Pyrexia 85.67 42.52 44 661 81071 3304083
Dehydration 82.75 42.52 33 672 33616 3351538
Fatigue 76.80 42.52 45 660 107195 3277959
Exposure during pregnancy 74.62 42.52 29 676 27534 3357620
Somnolence 70.24 42.52 29 676 32175 3352979
Fall 67.99 42.52 34 671 58849 3326305
Hypokalaemia 65.42 42.52 22 683 13783 3371371
Infusion site vesicles 65.17 42.52 9 696 68 3385086
Dystonia 63.01 42.52 16 689 3751 3381403
Diarrhoea 62.23 42.52 39 666 104309 3280845
Mydriasis 61.82 42.52 15 690 2919 3382235
Nausea 61.60 42.52 42 663 129603 3255551
Urinary retention 60.56 42.52 18 687 7554 3377600
Duodenal stenosis 58.20 42.52 9 696 158 3384996
Decreased appetite 56.94 42.52 27 678 41463 3343691
Renal failure 56.37 42.52 25 680 32915 3352239
Respiratory depth decreased 56.25 42.52 7 698 20 3385134
Hyponatraemia 55.63 42.52 21 684 18338 3366816
Drug interaction 53.84 42.52 27 678 46785 3338369
Psychotic disorder 53.83 42.52 17 688 8717 3376437
Infusion site pruritus 53.36 42.52 9 696 277 3384877
Sopor 53.27 42.52 14 691 3750 3381404
Constipation 51.46 42.52 23 682 30789 3354365
Cognitive disorder 51.33 42.52 16 689 7858 3377296
Torsade de pointes 51.30 42.52 13 692 3016 3382138
Hepatocellular injury 51.12 42.52 14 691 4381 3380773
Peripheral swelling 50.84 42.52 19 686 16113 3369041

Pharmacologic Action:

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SourceCodeDescription
ATC A03FA03 ALIMENTARY TRACT AND METABOLISM
DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS
PROPULSIVES
Propulsives
MeSH PA D000932 Antiemetics
MeSH PA D001337 Autonomic Agents
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)

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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

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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:

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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:

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IDSource
965 IUPHAR_LIGAND_ID
4025225 VUID
N0000171760 NUI
C0013015 UMLSCUI
D01745 KEGG_DRUG
5587267Z69 UNII
4110 INN_ID
3626 RXNORM
32955006 SNOMEDCT_US
387181004 SNOMEDCT_US
4025225 VANDF
N0000167200 NDFRT
N0000171760 NDFRT
003454 NDDF
83898-65-1 SECONDARY_CAS_RN
CHEMBL219916 ChEMBL_ID
3151 PUBCHEM_CID
D004294 MESH_DESCRIPTOR_UI
DB01184 DRUGBANK_ID
CHEBI:31515 CHEBI

Pharmaceutical products:

None