domperidone Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.01 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.34 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 15 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 3.40 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 9.50 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.08 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 7.50 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1982 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
Drug ineffective 82.08 11.61 227 32585 677611 45975639
Vomiting 79.67 11.61 567 32245 452227 46201023
Neutropenic sepsis 78.78 11.61 67 32745 12257 46640993
Completed suicide 71.79 11.61 9 32803 145911 46507339
Premature labour 71.35 11.61 61 32751 11238 46642012
Hyperprolactinaemia 69.06 11.61 36 32776 2896 46650354
Electrocardiogram QT prolonged 64.07 11.61 123 32689 51202 46602048
Product dose omission issue 61.26 11.61 21 32791 168499 46484751
Gastric pH decreased 54.24 11.61 17 32795 355 46652895
Cestode infection 54.18 11.61 16 32796 271 46652979
Torsade de pointes 43.42 11.61 48 32764 12106 46641144
Akathisia 41.43 11.61 38 32774 7676 46645574
Lip pruritus 41.20 11.61 15 32797 501 46652749
H1N1 influenza 40.12 11.61 20 32792 1464 46651786
Decreased appetite 39.44 11.61 252 32560 193584 46459666
Magnesium deficiency 39.32 11.61 14 32798 438 46652812
Arterial occlusive disease 38.92 11.61 30 32782 4774 46648476
Pituitary tumour benign 37.77 11.61 20 32792 1661 46651589
Premenstrual syndrome 37.33 11.61 15 32797 658 46652592
Hypokalaemia 37.12 11.61 141 32671 87883 46565367
Hyponatraemia 36.87 11.61 155 32657 101177 46552073
Subileus 36.46 11.61 24 32788 2979 46650271
Stoma site erythema 35.43 11.61 17 32795 1145 46652105
Gangrene 35.18 11.61 28 32784 4667 46648583
Derealisation 34.77 11.61 15 32797 788 46652462
On and off phenomenon 34.60 11.61 20 32792 1971 46651279
Pulmonary malformation 34.31 11.61 9 32803 96 46653154
Lichen sclerosus 32.55 11.61 15 32797 922 46652328
Stoma site discharge 32.42 11.61 19 32793 1921 46651329
Dyskinesia 32.08 11.61 66 32746 28859 46624391
Respiratory tract malformation 31.82 11.61 8 32804 71 46653179
Depersonalisation/derealisation disorder 31.47 11.61 15 32797 995 46652255
Cogwheel rigidity 31.43 11.61 17 32795 1473 46651777
Injection site erythema 31.26 11.61 7 32805 74420 46578830
Lung diffusion test decreased 31.03 11.61 13 32799 635 46652615
Drug abuse 30.95 11.61 4 32808 63404 46589846
Forced vital capacity decreased 29.89 11.61 14 32798 893 46652357
Polymenorrhoea 29.43 11.61 15 32797 1151 46652099
Dissociation 27.78 11.61 17 32795 1860 46651390
Menstruation delayed 27.43 11.61 16 32796 1604 46651646
General physical health deterioration 25.06 11.61 153 32659 115616 46537634
Hypomagnesaemia 25.01 11.61 51 32761 22159 46631091
Dystonia 24.97 11.61 35 32777 11222 46642028
Faecaloma 24.95 11.61 29 32783 7723 46645527
Pyrexia 24.86 11.61 363 32449 348439 46304811
Nightmare 24.78 11.61 43 32769 16555 46636695
Febrile neutropenia 24.38 11.61 131 32681 94496 46558754
Lung cyst 24.19 11.61 7 32805 110 46653140
Contraindicated product administered 24.19 11.61 13 32799 79934 46573316
Thyroid stimulating immunoglobulin increased 24.08 11.61 7 32805 112 46653138
Systemic lupus erythematosus 23.87 11.61 8 32804 65172 46588078
Drug hypersensitivity 23.51 11.61 90 32722 243735 46409515
Body temperature fluctuation 23.14 11.61 15 32797 1815 46651435
Oral candidiasis 23.08 11.61 43 32769 17489 46635761
Limbic encephalitis 23.04 11.61 8 32804 232 46653018
Rheumatoid arthritis 22.94 11.61 89 32723 240126 46413124
Duodenal stenosis 22.21 11.61 10 32802 582 46652668
Hypoaesthesia oral 22.20 11.61 32 32780 10527 46642723
Muscle rigidity 22.14 11.61 31 32781 9930 46643320
Vascular encephalopathy 21.93 11.61 9 32803 417 46652833
Maternal exposure during pregnancy 21.72 11.61 24 32788 102525 46550725
Gamma-glutamyltransferase increased 21.69 11.61 60 32752 31680 46621570
Glomerulonephritis chronic 21.57 11.61 7 32805 164 46653086
Nausea 21.22 11.61 632 32180 686822 45966428
Abdominal pain 21.21 11.61 251 32561 229780 46423470
Toxicity to various agents 21.17 11.61 77 32735 211689 46441561
Abdominal discomfort 20.96 11.61 47 32765 151118 46502132
Feeling of despair 20.89 11.61 14 32798 1791 46651459
Sensory loss 20.85 11.61 25 32787 6877 46646373
Respiratory depth decreased 20.46 11.61 5 32807 39 46653211
Constipation 20.23 11.61 199 32613 173898 46479352
Chronic sinusitis 19.95 11.61 21 32791 5012 46648238
Hyperchlorhydria 19.80 11.61 12 32800 1290 46651960
Injection site pain 19.64 11.61 28 32784 107124 46546126
Acute hepatic failure 19.25 11.61 36 32776 14685 46638565
Therapeutic product effect decreased 19 11.61 18 32794 82583 46570667
Hallucination, auditory 18.92 11.61 30 32782 10726 46642524
Arthropathy 18.86 11.61 19 32793 84681 46568569
Cardiac failure congestive 18.85 11.61 22 32790 91728 46561522
Restless legs syndrome 18.58 11.61 37 32775 15806 46637444
Abortion spontaneous 18.54 11.61 4 32808 43642 46609608
Freezing phenomenon 18.41 11.61 12 32800 1465 46651785
Treatment failure 18.41 11.61 23 32789 93064 46560186
Lower respiratory tract infection 18.28 11.61 82 32730 55007 46598243
Therapeutic product effect incomplete 18.01 11.61 17 32795 78136 46575114
Lung disorder 17.94 11.61 69 32743 43235 46610015
Adrenal suppression 17.72 11.61 10 32802 941 46652309
Mucosal inflammation 17.72 11.61 64 32748 38912 46614338
Drooling 17.61 11.61 16 32796 3193 46650057
Cholestasis 17.56 11.61 50 32762 26843 46626407
Maternal exposure during breast feeding 17.49 11.61 15 32797 2774 46650476
Oral cavity fistula 17.39 11.61 9 32803 713 46652537
Injection site reaction 17.30 11.61 6 32806 47843 46605407
Confusional state 17.25 11.61 180 32632 159712 46493538
Muscle disorder 17.19 11.61 18 32794 4268 46648982
Galactorrhoea 17.15 11.61 17 32795 3780 46649470
Bronchopulmonary aspergillosis allergic 17.11 11.61 9 32803 737 46652513
Psoriasis 17.08 11.61 18 32794 78586 46574664
Adverse drug reaction 17.04 11.61 5 32807 44357 46608893
Urinary retention 16.57 11.61 48 32764 26013 46627237
Rash maculo-papular 16.45 11.61 50 32762 27824 46625426
Weight decreased 16.41 11.61 223 32589 210626 46442624
Total lung capacity decreased 16.30 11.61 10 32802 1099 46652151
Infusion site vesicles 16.24 11.61 7 32805 367 46652883
Psoriatic arthropathy 16.15 11.61 3 32809 36376 46616874
Parosmia 16.00 11.61 17 32795 4099 46649151
Mental disorder 15.93 11.61 43 32769 22382 46630868
Rash 15.92 11.61 167 32645 356345 46296905
Menstrual disorder 15.83 11.61 17 32795 4151 46649099
Stoma complication 15.82 11.61 6 32806 225 46653025
Adrenal insufficiency 15.81 11.61 31 32781 13093 46640157
Feeling abnormal 15.66 11.61 41 32771 125019 46528231
Synovitis 15.65 11.61 12 32800 61063 46592187
Unresponsive to stimuli 15.63 11.61 54 32758 32120 46621130
Feeling of body temperature change 15.55 11.61 17 32795 4235 46649015
Hypersensitivity 15.45 11.61 54 32758 150267 46502983
Mydriasis 15.31 11.61 27 32785 10526 46642724
Paranoia 15.23 11.61 27 32785 10570 46642680
Sprue-like enteropathy 15.10 11.61 7 32805 436 46652814
Anti-thyroid antibody positive 15.07 11.61 7 32805 438 46652812
Cardio-respiratory arrest 15.04 11.61 12 32800 59857 46593393
Dysaesthesia pharynx 14.88 11.61 5 32807 131 46653119
Impaired gastric emptying 14.87 11.61 23 32789 8049 46645201
Wrong technique in product usage process 14.85 11.61 10 32802 54412 46598838
Hepatocellular injury 14.74 11.61 50 32762 29472 46623778
Injection site swelling 14.68 11.61 5 32807 40322 46612928
Dermatitis exfoliative generalised 14.56 11.61 14 32798 2999 46650251
Folate deficiency 14.51 11.61 11 32801 1707 46651543
Injection site pruritus 14.34 11.61 5 32807 39738 46613512
Microvillous inclusion disease 14.17 11.61 3 32809 11 46653239
Thyroxine free increased 14.17 11.61 8 32804 754 46652496
Bezoar 14.05 11.61 10 32802 1409 46651841
Stoma site pain 14.02 11.61 9 32803 1071 46652179
Neck pain 14.00 11.61 11 32801 55295 46597955
Overdose 13.89 11.61 32 32780 101947 46551303
Hallucinations, mixed 13.40 11.61 15 32797 3834 46649416
Cerebral calcification 13.33 11.61 5 32807 182 46653068
Repetitive strain injury 13.30 11.61 5 32807 183 46653067
Lung opacity 13.26 11.61 9 32803 1175 46652075
Intention tremor 13.19 11.61 6 32806 358 46652892
Functional residual capacity decreased 13.17 11.61 4 32808 75 46653175
Depressed level of consciousness 13.03 11.61 67 32745 47502 46605748
Stoma site inflammation 13.00 11.61 7 32805 601 46652649
Onychoclasis 12.94 11.61 17 32795 5127 46648123
Dehydration 12.93 11.61 170 32642 159370 46493880
Pseudocholinesterase deficiency 12.88 11.61 4 32808 81 46653169
Blood sodium decreased 12.85 11.61 39 32773 21687 46631563
Drug interaction 12.74 11.61 207 32605 202887 46450363
Infertility 12.64 11.61 7 32805 635 46652615
Gastritis fungal 12.61 11.61 4 32808 87 46653163
Plasma cell myeloma 12.37 11.61 8 32804 44470 46608780
Intestinal perforation 12.31 11.61 25 32787 10826 46642424
Gastric disorder 12.27 11.61 44 32768 26661 46626589
Rhinalgia 12.19 11.61 8 32804 988 46652262
Hospitalisation 12.18 11.61 16 32796 63369 46589881
Injury 12.13 11.61 8 32804 44019 46609231
Gingival pain 12.11 11.61 18 32794 6085 46647165
Serotonin syndrome 12.07 11.61 41 32771 24179 46629071
Altered state of consciousness 12.06 11.61 40 32772 23308 46629942
Delirium 12.04 11.61 55 32757 37173 46616077
Pneumonia aspiration 11.99 11.61 49 32763 31556 46621694
Myopathy 11.96 11.61 22 32790 8859 46644391
Chronic obstructive pulmonary disease 11.64 11.61 14 32798 57619 46595631
Internal haemorrhage 11.63 11.61 15 32797 4440 46648810

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
Vomiting 54.34 12.32 245 15606 219573 29717054
Drug ineffective 40.66 12.32 74 15777 340313 29596314
Aspiration 29.47 12.32 32 15819 10519 29926108
Impaired gastric emptying 28.61 12.32 19 15832 3187 29933440
Completed suicide 27.81 12.32 9 15842 99483 29837144
Neutropenic sepsis 27.43 12.32 32 15819 11377 29925250
Lower respiratory tract infection 27.34 12.32 50 15801 26664 29909963
Urine sodium decreased 27.03 12.32 8 15843 184 29936443
Toxicity to various agents 26.42 12.32 33 15818 177150 29759477
Dyskinesia 26.42 12.32 44 15807 21790 29914837
On and off phenomenon 25.47 12.32 17 15834 2874 29933753
Oesophagitis 24.66 12.32 30 15821 11141 29925486
General physical health deterioration 24.28 12.32 111 15740 99833 29836794
Oesophageal haemorrhage 24.02 12.32 12 15839 1176 29935451
Saliva altered 23.49 12.32 7 15844 165 29936462
Product dose omission issue 22.75 12.32 10 15841 91621 29845006
Nausea 22.56 12.32 248 15603 296709 29639918
Neutrophil count decreased 22.44 12.32 61 15790 42393 29894234
Impulse-control disorder 22.20 12.32 12 15839 1383 29935244
Gastroenteritis 22.08 12.32 31 15820 13235 29923392
Drug abuse 21.94 12.32 8 15843 82064 29854563
Hypomania 21.67 12.32 14 15837 2242 29934385
Hyperkinesia 20.10 12.32 13 15838 2085 29934542
Intentional medical device removal by patient 18.91 12.32 7 15844 328 29936299
Akinesia 18.03 12.32 13 15838 2487 29934140
Dysphagia 17.69 12.32 68 15783 56630 29879997
Pyroglutamic acidosis 17.55 12.32 5 15846 100 29936527
Device dislocation 17.19 12.32 17 15834 5014 29931613
Hepatocellular injury 17.01 12.32 40 15811 25431 29911196
Pneumonia aspiration 16.78 12.32 51 15800 37729 29898898
Gambling disorder 16.65 12.32 11 15840 1829 29934798
Decreased appetite 16.20 12.32 135 15716 149775 29786852
Stoma site discharge 16.13 12.32 10 15841 1491 29935136
Paralysis recurrent laryngeal nerve 15.80 12.32 4 15847 50 29936577
Colitis ischaemic 15.21 12.32 17 15834 5769 29930858
Inappropriate antidiuretic hormone secretion 15.15 12.32 24 15827 11398 29925229
Dyskinesia oesophageal 15.06 12.32 4 15847 61 29936566
Post inflammatory pigmentation change 13.87 12.32 5 15846 217 29936410
Deafness bilateral 13.67 12.32 8 15843 1074 29935553
Drug interaction 13.02 12.32 162 15689 199406 29737221
Shock symptom 13.01 12.32 4 15847 105 29936522
Lumbosacral plexus injury 12.95 12.32 3 15848 25 29936602
Hypocalcaemia 12.60 12.32 32 15819 21344 29915283
Platelet count increased 12.47 12.32 19 15832 8723 29927904
Skin erosion 12.38 12.32 9 15842 1744 29934883
Regurgitation 12.32 12.32 7 15844 889 29935738

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:48561 dopamine blocker
CHEBI has role CHEBI:50919 antiemetico

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
4025225 VUID
N0000171760 NUI
D01745 KEGG_DRUG
83898-65-1 SECONDARY_CAS_RN
4025225 VANDF
C0013015 UMLSCUI
CHEBI:31515 CHEBI
CHEMBL219916 ChEMBL_ID
DB01184 DRUGBANK_ID
D004294 MESH_DESCRIPTOR_UI
3151 PUBCHEM_CID
965 IUPHAR_LIGAND_ID
4110 INN_ID
5587267Z69 UNII
203007 RXNORM
003454 NDDF
005091 NDDF
32955006 SNOMEDCT_US
384972001 SNOMEDCT_US
387181004 SNOMEDCT_US

Pharmaceutical products:

None