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

Stem definitionDrug idCAS RN
2360 90098-04-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • OPC-12759
  • rebamipide
  • proamipide
  • mucosta
Rebamipide is a mucosal protective agent and is postulated to increase gastric blood flow, prostaglandin biosynthesis and decrease free oxygen radicals.
  • Molecular weight: 370.79
  • Formula: C19H15ClN2O4
  • CLOGP: 1.97
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 3
  • TPSA: 95.50
  • ALOGS: -4.56
  • ROTB: 5

Drug dosage:

DoseUnitRoute
0.30 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 4 Hosey CM, Chan R, Benet LZ
S (Water solubility) 0.03 mg/mL Bocci G, Oprea TI, Benet LZ

Approvals:

DateAgencyCompanyOrphan
Sept. 26, 2011 PMDA

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
Hepatic function abnormal 252.55 18.26 123 10365 37019 63441515
Platelet count decreased 247.96 18.26 182 10306 115940 63362594
Interstitial lung disease 234.74 18.26 139 10349 61769 63416765
Drug eruption 115.38 18.26 67 10421 28627 63449907
Drug ineffective 94.67 18.26 28 10460 1044737 62433797
White blood cell count decreased 91.96 18.26 114 10374 138990 63339544
Malignant neoplasm progression 88.50 18.26 87 10401 82034 63396500
Spinal compression fracture 87.18 18.26 44 10444 14239 63464295
Liver disorder 85.74 18.26 71 10417 53616 63424918
Fatigue 85.64 18.26 21 10467 888007 62590527
Pyrexia 84.47 18.26 217 10271 470261 63008273
Osteonecrosis of jaw 79.16 18.26 57 10431 35066 63443468
Cerebral infarction 75.96 18.26 48 10440 23845 63454689
Neutrophil count decreased 66.86 18.26 63 10425 56343 63422191
Blood bilirubin increased 63.24 18.26 51 10437 37089 63441445
Altered state of consciousness 59.27 18.26 42 10446 25188 63453346
Anaemia 58.44 18.26 141 10347 293289 63185245
Renal impairment 56.07 18.26 71 10417 88284 63390250
Haemorrhage subcutaneous 50.90 18.26 19 10469 2964 63475570
Iron deficiency anaemia 48.66 18.26 34 10454 19935 63458599
Blood pressure decreased 47.31 18.26 56 10432 64966 63413568
Upper respiratory tract inflammation 46.47 18.26 17 10471 2506 63476028
Alanine aminotransferase increased 45.76 18.26 70 10418 103700 63374834
Disseminated intravascular coagulation 45.40 18.26 32 10456 19019 63459515
Aspartate aminotransferase increased 44.25 18.26 64 10424 90213 63388321
Erythema multiforme 44.21 18.26 25 10463 10144 63468390
Decreased appetite 44.02 18.26 115 10373 250937 63227597
Joint swelling 42.58 18.26 3 10485 327663 63150871
Cardiac failure 40.53 18.26 61 10427 89081 63389453
Pain 40.26 18.26 38 10450 740590 62737944
Gastric ulcer haemorrhage 38.63 18.26 18 10470 4890 63473644
Pneumonia bacterial 35.13 18.26 21 10467 9444 63469090
Drug hypersensitivity 34.78 18.26 5 10483 310682 63167852
Drug intolerance 34.48 18.26 5 10483 308656 63169878
Febrile neutropenia 33.91 18.26 66 10422 118383 63360151
Fulminant type 1 diabetes mellitus 33.76 18.26 9 10479 466 63478068
Cancer pain 32.39 18.26 14 10474 3191 63475343
Pancytopenia 31.46 18.26 57 10431 96876 63381658
Concomitant disease aggravated 30.69 18.26 19 10469 9093 63469441
Peritonitis 30.13 18.26 24 10464 17130 63461404
Ileus 28.90 18.26 22 10466 14703 63463831
Enterocolitis 28.04 18.26 17 10471 7841 63470693
Swelling 27.41 18.26 6 10482 275372 63203162
Drug-induced liver injury 26.57 18.26 33 10455 40189 63438345
Duodenal ulcer haemorrhage 25.66 18.26 11 10477 2456 63476078
Gamma-glutamyltransferase increased 24.23 18.26 29 10459 34002 63444532
Enteritis infectious 23.86 18.26 10 10478 2114 63476420
Product dose omission issue 23.53 18.26 5 10483 234308 63244226
Toxicity to various agents 23.39 18.26 6 10482 247244 63231290
Infusion related reaction 23.15 18.26 6 10482 245515 63233019
Compression fracture 23.14 18.26 14 10474 6434 63472100
Cutaneous symptom 22.99 18.26 6 10482 286 63478248
Alopecia 22.50 18.26 14 10474 337522 63141012
Colony stimulating factor therapy 22.32 18.26 6 10482 321 63478213
Colon cancer 22.17 18.26 16 10472 9862 63468672
Hepatitis fulminant 22.10 18.26 11 10477 3453 63475081
Gastrointestinal perforation 22.01 18.26 11 10477 3480 63475054
Blood alkaline phosphatase increased 21.83 18.26 31 10457 42936 63435598
Pharyngitis 21.03 18.26 21 10467 20122 63458412
Adrenocorticotropic hormone deficiency 20.85 18.26 6 10482 413 63478121
Peripheral swelling 20.72 18.26 9 10479 265933 63212601
Infective spondylitis 20.36 18.26 5 10483 186 63478348
Malignant catatonia 20.13 18.26 5 10483 195 63478339
Haemoglobin decreased 19.92 18.26 61 10427 145424 63333110
Glossodynia 19.72 18.26 3 10485 178873 63299661
Tumour haemorrhage 19.40 18.26 8 10480 1623 63476911
Anxiety 19.24 18.26 6 10482 217535 63260999
Pyelonephritis acute 19.07 18.26 11 10477 4630 63473904
Pulmonary alveolar haemorrhage 19.01 18.26 11 10477 4657 63473877
Malignant pleural effusion 18.79 18.26 9 10479 2597 63475937
Sputum retention 18.70 18.26 6 10482 596 63477938
Pneumocystis jirovecii pneumonia 18.34 18.26 18 10470 16896 63461638

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
Interstitial lung disease 249.74 18.47 177 9293 65105 34882356
Hepatic function abnormal 199.52 18.47 133 9337 44230 34903231
Platelet count decreased 90.52 18.47 135 9335 119582 34827879
Disseminated intravascular coagulation 71.50 18.47 54 9416 21762 34925699
Malignant neoplasm progression 70.39 18.47 102 9368 87944 34859517
Cerebral infarction 68.70 18.47 58 9412 27397 34920064
Fatigue 63.34 18.47 12 9458 370641 34576820
Upper respiratory tract inflammation 59.18 18.47 21 9449 1723 34945738
Neutrophil count decreased 52.64 18.47 67 9403 51037 34896424
Decreased appetite 51.03 18.47 128 9342 166264 34781197
Drug eruption 49.69 18.47 42 9428 19856 34927605
Renal impairment 46.45 18.47 88 9382 94425 34853036
Toxicity to various agents 42.73 18.47 3 9467 200359 34747102
Drug ineffective 42.47 18.47 37 9433 456714 34490747
White blood cell count decreased 42.20 18.47 85 9385 95360 34852101
Stomatitis 41.05 18.47 54 9416 42460 34905001
Pyrexia 38.56 18.47 185 9285 332828 34614633
Drug-induced liver injury 36.52 18.47 42 9428 28790 34918671
Liver disorder 35.13 18.47 44 9426 32953 34914508
Gastric ulcer haemorrhage 33.56 18.47 20 9450 5446 34942015
Aspartate aminotransferase increased 29.50 18.47 60 9410 67723 34879738
Hyperuricaemia 28.78 18.47 21 9449 8022 34939439
C-reactive protein increased 28.58 18.47 52 9418 54046 34893415
Non-small cell lung cancer 28.40 18.47 16 9454 3924 34943537
Gastric cancer 28.05 18.47 19 9451 6450 34941011
Eosinophil count increased 27.58 18.47 21 9449 8551 34938910
Cholangitis 27.33 18.47 21 9449 8668 34938793
Pneumonia aspiration 27.02 18.47 44 9426 41859 34905602
Spinal compression fracture 26.42 18.47 19 9451 7097 34940364
Osteonecrosis of jaw 25.99 18.47 28 9442 17861 34929600
Gastric ulcer 25.42 18.47 26 9444 15624 34931837
Altered state of consciousness 25.12 18.47 31 9439 22862 34924599
Confusional state 23.84 18.47 5 9465 144155 34803306
Pneumonia bacterial 23.54 18.47 22 9448 11850 34935611
Blood lactate dehydrogenase increased 23.42 18.47 30 9440 22960 34924501
Lymphangiosis carcinomatosa 23.42 18.47 9 9461 923 34946538
Cancer pain 22.43 18.47 12 9458 2660 34944801
Immune-mediated enterocolitis 21.91 18.47 12 9458 2787 34944674
Erythema multiforme 21.06 18.47 18 9452 8631 34938830
Gamma-glutamyltransferase increased 20.64 18.47 32 9438 29199 34918262
Prescribed underdose 20.55 18.47 18 9452 8915 34938546
Death 20.37 18.47 49 9421 398000 34549461
Fulminant type 1 diabetes mellitus 20.25 18.47 8 9462 883 34946578
Pneumonia 20.10 18.47 167 9303 362460 34585001
Cardiac failure 19.81 18.47 62 9408 91186 34856275
Alanine aminotransferase increased 19.50 18.47 57 9413 80758 34866703
Hypoalbuminaemia 19.36 18.47 20 9450 12154 34935307
Asthenia 19.14 18.47 23 9447 245228 34702233
Rectal cancer 18.77 18.47 10 9460 2197 34945264

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
Interstitial lung disease 465.71 15.69 314 20171 112286 79611617
Hepatic function abnormal 417.26 15.69 250 20235 72857 79651046
Platelet count decreased 312.77 15.69 313 20172 194351 79529552
Malignant neoplasm progression 162.22 15.69 187 20298 135803 79588100
Fatigue 143.56 15.69 32 20453 929695 78794208
Drug eruption 142.93 15.69 106 20379 43829 79680074
Cerebral infarction 134.87 15.69 104 20381 45572 79678331
White blood cell count decreased 132.83 15.69 200 20285 188088 79535815
Drug ineffective 120.87 15.69 64 20421 1080849 78643054
Disseminated intravascular coagulation 115.51 15.69 86 20399 35756 79688147
Neutrophil count decreased 111.62 15.69 129 20356 93830 79630073
Liver disorder 111.50 15.69 114 20371 72303 79651600
Spinal compression fracture 101.80 15.69 60 20425 16898 79707005
Upper respiratory tract inflammation 99.94 15.69 38 20447 3997 79719906
Pyrexia 98.67 15.69 389 20096 678320 79045583
Renal impairment 93.76 15.69 155 20330 157628 79566275
Osteonecrosis of jaw 93.18 15.69 82 20403 43144 79680759
Decreased appetite 92.48 15.69 243 20242 342175 79381728
Toxicity to various agents 79.69 15.69 8 20477 421532 79302371
Altered state of consciousness 69.27 15.69 70 20415 43752 79680151
Blood bilirubin increased 68.86 15.69 85 20400 66147 79657756
Gastric ulcer haemorrhage 67.83 15.69 37 20448 8990 79714913
Aspartate aminotransferase increased 62.78 15.69 121 20364 138520 79585383
Anaemia 60.39 15.69 250 20235 444765 79279138
Confusional state 60.16 15.69 6 20479 317991 79405912
Pain 59.55 15.69 56 20429 703746 79020157
Joint swelling 58.59 15.69 4 20481 288642 79435261
Erythema multiforme 56.06 15.69 42 20443 17609 79706294
Drug hypersensitivity 55.61 15.69 6 20479 298910 79424993
Cancer pain 55.30 15.69 27 20458 5218 79718685
Pneumonia bacterial 54.82 15.69 43 20442 19288 79704615
Haemorrhage subcutaneous 54.47 15.69 26 20459 4783 79719120
Alanine aminotransferase increased 52.88 15.69 124 20361 162446 79561457
Drug-induced liver injury 51.98 15.69 74 20411 66043 79657860
Cardiac failure 51.34 15.69 119 20366 154723 79569180
Fulminant type 1 diabetes mellitus 47.96 15.69 17 20468 1466 79722437
Blood pressure decreased 47.72 15.69 89 20396 99377 79624526
Drug intolerance 47.39 15.69 6 20479 264113 79459790
Gamma-glutamyltransferase increased 42.68 15.69 61 20424 54619 79669284
Iron deficiency anaemia 42.38 15.69 42 20443 25630 79698273
Non-small cell lung cancer 42.14 15.69 24 20461 6336 79717567
Hyperuricaemia 41.82 15.69 30 20455 11769 79712134
Gastric cancer 41.02 15.69 28 20457 10151 79713752
Completed suicide 40.82 15.69 7 20478 245760 79478143
Blood lactate dehydrogenase increased 40.26 15.69 50 20435 39120 79684783
Pneumonia aspiration 40.00 15.69 66 20419 66901 79657002
Cholangitis 39.68 15.69 30 20455 12746 79711157
Anxiety 39.30 15.69 8 20477 248504 79475399
Enterocolitis 38.41 15.69 31 20454 14481 79709422
Peripheral swelling 38.10 15.69 11 20474 269606 79454297
Enteritis infectious 37.66 15.69 18 20467 3320 79720583
Peritonitis 37.54 15.69 41 20444 27995 79695908
Stomatitis 37.32 15.69 102 20383 146655 79577248
Hypotension 37.20 15.69 35 20450 440282 79283621
Product dose omission issue 35.16 15.69 10 20475 247527 79476376
Gastrointestinal perforation 34.96 15.69 21 20464 6116 79717787
Gastric ulcer 34.40 15.69 43 20442 33862 79690041
C-reactive protein increased 34.13 15.69 91 20394 128936 79594967
Pneumonia 33.38 15.69 286 20199 659960 79063943
Swelling 32.21 15.69 8 20477 216703 79507200
Infusion related reaction 31.43 15.69 10 20475 230227 79493676
Blood alkaline phosphatase increased 30.56 15.69 57 20428 63607 79660296
Colon cancer 30.18 15.69 27 20458 14496 79709407
Cerebrovascular accident 29.16 15.69 3 20482 155289 79568614
Herpes zoster 29.15 15.69 70 20415 93013 79630890
Compression fracture 28.99 15.69 19 20466 6441 79717462
Pharyngitis 28.71 15.69 32 20453 22343 79701560
Constipation 28.62 15.69 146 20339 282904 79440999
Febrile neutropenia 28.33 15.69 126 20359 230873 79493030
Eosinophil count increased 28.26 15.69 28 20457 17077 79706826
Hypoalbuminaemia 28.26 15.69 31 20454 21266 79702637
Duodenal ulcer haemorrhage 27.21 15.69 19 20466 7144 79716759
Haemoglobin decreased 27.12 15.69 121 20364 221998 79501905
Dyspnoea 26.97 15.69 121 20364 856904 78866999
Asthenia 26.96 15.69 57 20428 511632 79212271
Radiation pneumonitis 26.48 15.69 15 20470 3918 79719985
Pancytopenia 26.35 15.69 98 20387 165647 79558256
Shock haemorrhagic 26.27 15.69 29 20456 20031 79703872
Post herpetic neuralgia 26.16 15.69 13 20472 2608 79721295
Small intestine ulcer 26.16 15.69 9 20476 710 79723193
Chronic gastritis 26.01 15.69 15 20470 4053 79719850
Weight decreased 25.80 15.69 32 20453 355166 79368737
Hypopituitarism 25.72 15.69 14 20471 3385 79720518
Hypersensitivity 25.67 15.69 18 20467 262221 79461682
Lymphangiosis carcinomatosa 25.48 15.69 12 20473 2142 79721761
Infective spondylitis 24.97 15.69 8 20477 506 79723397
Hepatitis fulminant 24.68 15.69 18 20467 7244 79716659
Concomitant disease aggravated 24.48 15.69 23 20462 13144 79710759
Cerebral haemorrhage 24.46 15.69 49 20436 57624 79666279
Blood urea increased 23.81 15.69 44 20441 48746 79675157
Adrenocorticotropic hormone deficiency 23.72 15.69 10 20475 1375 79722528
Shunt stenosis 23.68 15.69 10 20475 1381 79722522
Immune-mediated enterocolitis 23.63 15.69 15 20470 4815 79719088
Weight increased 23.46 15.69 22 20463 277364 79446539
Pleural effusion 23.18 15.69 86 20399 145176 79578727
Ileus 23.08 15.69 31 20454 26180 79697723
Pyelonephritis acute 22.93 15.69 16 20469 6007 79717896
Sputum retention 22.46 15.69 9 20476 1088 79722815
Death 22.29 15.69 73 20412 566441 79157462
Cholecystitis 22.26 15.69 28 20457 22184 79701719
Cytomegalovirus enterocolitis 22.01 15.69 10 20475 1645 79722258
Thalamus haemorrhage 21.30 15.69 10 20475 1772 79722131
Alopecia 21.20 15.69 17 20468 231338 79492565
Hypocalcaemia 20.67 15.69 42 20443 49882 79674021
Cutaneous symptom 20.56 15.69 7 20478 535 79723368
Idiopathic pulmonary fibrosis 20.36 15.69 13 20472 4215 79719688
Paraesthesia 20.22 15.69 10 20475 176313 79547590
Blood creatine phosphokinase increased 19.94 15.69 49 20436 66041 79657862
Discomfort 19.94 15.69 4 20481 125613 79598290
Lymphocyte count decreased 19.84 15.69 40 20445 47249 79676654
Metastases to liver 19.80 15.69 30 20455 28284 79695619
Pneumothorax 19.79 15.69 30 20455 28293 79695610
General physical health deterioration 19.76 15.69 25 20460 275213 79448690
Cholangitis acute 19.56 15.69 9 20476 1523 79722380
Pulmonary alveolar haemorrhage 19.38 15.69 19 20466 11438 79712465
Pneumocystis jirovecii pneumonia 19.35 15.69 32 20453 32476 79691427
Cerebellar haemorrhage 19.29 15.69 11 20474 2909 79720994
Paronychia 19.24 15.69 16 20469 7792 79716111
White blood cell count increased 19.08 15.69 52 20433 74581 79649322
Brain stem haemorrhage 18.93 15.69 9 20476 1641 79722262
Subdural haematoma 18.79 15.69 31 20454 31403 79692500
Cholecystitis acute 18.58 15.69 20 20465 13431 79710472
Tumour haemorrhage 18.14 15.69 12 20473 4132 79719771
Aortic dissection 18.06 15.69 12 20473 4163 79719740
Cardiac failure chronic 17.98 15.69 18 20467 11117 79712786
Malignant pleural effusion 17.80 15.69 11 20474 3369 79720534
Cellulitis 17.76 15.69 65 20420 108995 79614908
Diabetes mellitus 17.49 15.69 52 20433 78338 79645565
Ocular dysmetria 17.26 15.69 4 20481 73 79723830
Periodontitis 17.25 15.69 12 20473 4484 79719419
Glossodynia 17.02 15.69 3 20482 103334 79620569
Physical deconditioning 16.99 15.69 9 20476 2061 79721842
Colony stimulating factor therapy 16.92 15.69 6 20479 518 79723385
Shunt occlusion 16.63 15.69 8 20477 1496 79722407
Contraindicated product administered 16.51 15.69 10 20475 157528 79566375
Pyelonephritis 16.28 15.69 23 20462 20365 79703538
Immune-mediated hepatic disorder 16.19 15.69 8 20477 1586 79722317
Cardiac failure acute 16.08 15.69 22 20463 18907 79704996
Dyslalia 15.93 15.69 7 20478 1065 79722838
Anaphylactic shock 15.76 15.69 31 20454 35965 79687938

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC A02BX14 ALIMENTARY TRACT AND METABOLISM
DRUGS FOR ACID RELATED DISORDERS
DRUGS FOR PEPTIC ULCER AND GASTRO-OESOPHAGEAL REFLUX DISEASE (GORD)
Other drugs for peptic ulcer and gastro-oesophageal reflux disease (GORD)
MeSH PA D000897 Anti-Ulcer Agents
MeSH PA D000975 Antioxidants
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D005765 Gastrointestinal Agents
MeSH PA D020011 Protective Agents

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Gastritis indication 4556007 DOID:4029
Peptic ulcer indication 13200003 DOID:750




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.32 acidic
pKa2 12.06 acidic
pKa3 13.42 acidic

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
Cholecystokinin receptor type A GPCR AGONIST IC50 4.40 IUPHAR

External reference:

IDSource
D01121 KEGG_DRUG
C0069562 UMLSCUI
CHEBI:32090 CHEBI
CHEMBL1697771 ChEMBL_ID
DB11656 DRUGBANK_ID
C052785 MESH_SUPPLEMENTAL_RECORD_UI
5042 PUBCHEM_CID
871 IUPHAR_LIGAND_ID
6454 INN_ID
LR583V32ZR UNII
1172393005 SNOMEDCT_US
1172878003 SNOMEDCT_US

Pharmaceutical products:

None