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

Stem definitionDrug idCAS RN
mineralocorticoid receptor (MR, MCR, aldosterone receptor) antagonists 1032 107724-20-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • eplerenone
  • (+)-Eplerenone
  • epoxymexrenone
A spironolactone derivative and selective ALDOSTERONE RECEPTOR antagonist that is used in the management of HYPERTENSION and CONGESTIVE HEART FAILURE, post-MYOCARDIAL INFARCTION.
  • Molecular weight: 414.50
  • Formula: C24H30O6
  • CLOGP: 0.47
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 0
  • TPSA: 82.20
  • ALOGS: -4.66
  • ROTB: 2
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
50 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 3 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 1.72 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 69 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
Sept. 27, 2002 FDA GD SEARLE LLC

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
Cardiac failure 206.27 21.36 119 5843 89023 63394037
Hyperkalaemia 162.77 21.36 86 5876 54117 63428943
Acute kidney injury 157.49 21.36 156 5806 263259 63219801
Cardiac failure chronic 103.22 21.36 31 5931 4387 63478673
Subclavian vein thrombosis 79.46 21.36 21 5941 1869 63481191
Drug interaction 75.67 21.36 100 5862 229031 63254029
Atrial fibrillation 72.96 21.36 71 5891 116565 63366495
Hypotension 69.33 21.36 105 5857 272499 63210561
Cardiomyopathy 52.97 21.36 28 5934 17556 63465504
Hyponatraemia 51.78 21.36 58 5904 111842 63371218
Therapeutic drug monitoring analysis not performed 47.32 21.36 13 5949 1339 63481721
Cardiac failure acute 46.21 21.36 21 5941 9502 63473558
Wound haemorrhage 43.40 21.36 14 5948 2502 63480558
Hypomagnesaemia 42.62 21.36 29 5933 28708 63454352
Hydrothorax 42.28 21.36 11 5951 920 63482140
Femoral neck fracture 42.00 21.36 19 5943 8504 63474556
Bradycardia 40.98 21.36 42 5920 73185 63409875
Embolism venous 40.29 21.36 14 5948 3140 63479920
Oedema peripheral 39.82 21.36 67 5895 189444 63293616
Hypophosphataemia 39.61 21.36 20 5942 11406 63471654
Hypocalcaemia 37.78 21.36 28 5934 31685 63451375
Vascular stent thrombosis 37.01 21.36 10 5952 967 63482093
Degenerative aortic valve disease 36.25 21.36 7 5955 148 63482912
Dyspnoea 35.60 21.36 139 5823 661174 62821886
Cardiac ventricular disorder 35.17 21.36 7 5955 174 63482886
Hypovolaemia 35.01 21.36 18 5944 10655 63472405
Tachypnoea 34.40 21.36 21 5941 17281 63465779
Renal impairment 32.89 21.36 41 5921 88314 63394746
Exercise tolerance decreased 32.74 21.36 14 5948 5483 63477577
Angina pectoris 32.38 21.36 25 5937 30053 63453007
Glomerular filtration rate decreased 31.12 21.36 18 5944 13423 63469637
Therapeutic drug monitoring analysis incorrectly performed 30.69 21.36 7 5955 337 63482723
Ejection fraction decreased 29.51 21.36 21 5941 22311 63460749
Subclavian artery thrombosis 29.29 21.36 6 5956 173 63482887
Glomerular filtration rate increased 28.51 21.36 8 5954 890 63482170
Left ventricular dilatation 28.07 21.36 7 5955 494 63482566
Orthopnoea 27.85 21.36 13 5949 6248 63476812
Pulmonary arterial pressure increased 27.67 21.36 11 5951 3584 63479476
Left ventricular dysfunction 27.61 21.36 16 5946 11972 63471088
Coronary artery occlusion 27.41 21.36 14 5948 8177 63474883
Ventricular tachycardia 26.89 21.36 19 5943 19960 63463100
N-terminal prohormone brain natriuretic peptide increased 25.34 21.36 9 5953 2152 63480908
Stenosis 24.71 21.36 8 5954 1446 63481614
Vascular purpura 24.58 21.36 8 5954 1470 63481590
Hypokalaemia 23.52 21.36 38 5924 103766 63379294
Arrhythmia 23.39 21.36 23 5939 38117 63444943
Electrocardiogram Q wave abnormal 23.39 21.36 5 5957 178 63482882
Fall 23.10 21.36 85 5877 392249 63090811
Subdural haematoma 22.53 21.36 15 5947 14313 63468747
Congestive cardiomyopathy 21.95 21.36 11 5951 6171 63476889

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
Cardiac failure 643.22 15.57 519 23594 90729 34842089
Cardiac failure chronic 380.34 15.57 158 23955 7721 34925097
Rales 257.43 15.57 129 23984 9754 34923064
Ventricular tachycardia 256.93 15.57 183 23930 26396 34906422
Acute kidney injury 232.87 15.57 591 23522 304397 34628421
Ejection fraction decreased 218.34 15.57 146 23967 19008 34913810
Oedema peripheral 213.62 15.57 332 23781 119480 34813338
N-terminal prohormone brain natriuretic peptide increased 203.74 15.57 75 24038 2640 34930178
Hypotension 182.94 15.57 443 23670 221206 34711612
Mitral valve incompetence 182.66 15.57 119 23994 14824 34917994
Hyperkalaemia 181.17 15.57 231 23882 69158 34863660
Dyspnoea 156.73 15.57 591 23522 376191 34556627
Glomerular filtration rate decreased 153.00 15.57 101 24012 12860 34919958
Dyspnoea at rest 123.89 15.57 58 24055 3770 34929048
Exercise tolerance decreased 118.37 15.57 62 24051 5136 34927682
Ventricular enlargement 108.63 15.57 33 24080 631 34932187
Tricuspid valve incompetence 107.82 15.57 73 24040 9687 34923131
Dyspnoea exertional 101.84 15.57 137 23976 43142 34889676
Ventricular arrhythmia 101.03 15.57 57 24056 5471 34927347
Computerised tomogram coronary artery abnormal 98.02 15.57 24 24089 193 34932625
Atrial enlargement 91.43 15.57 29 24084 643 34932175
Renal impairment 90.89 15.57 201 23912 94312 34838506
Congestive cardiomyopathy 89.77 15.57 59 24054 7451 34925367
Cardiac failure acute 88.97 15.57 67 24046 10503 34922315
Soft tissue mass 87.10 15.57 31 24082 988 34931830
Oesophageal perforation 85.83 15.57 32 24081 1167 34931651
Multimorbidity 85.64 15.57 30 24083 912 34931906
Atrial fibrillation 80.39 15.57 225 23888 122168 34810650
Ischaemic cardiomyopathy 75.89 15.57 50 24063 6339 34926479
Low cardiac output syndrome 69.53 15.57 23 24090 585 34932233
Febrile neutropenia 69.35 15.57 7 24106 136842 34795976
Blood pressure decreased 67.93 15.57 125 23988 51390 34881428
Liver palpable 67.34 15.57 19 24094 277 34932541
General physical health deterioration 66.50 15.57 217 23896 128052 34804766
Death 65.44 15.57 109 24004 397940 34534878
Blood potassium increased 65.02 15.57 68 24045 16427 34916391
Bradycardia 64.29 15.57 153 23960 75265 34857553
Superinfection 62.98 15.57 32 24081 2487 34930331
Arrhythmia 57.78 15.57 95 24018 35713 34897105
Electrocardiogram abnormal 55.29 15.57 48 24065 9199 34923619
Labelled drug-drug interaction medication error 54.31 15.57 59 24054 14880 34917938
Drug interaction 54.07 15.57 302 23811 225644 34707174
Left atrial enlargement 53.46 15.57 21 24092 884 34931934
Hepatic vein dilatation 53.27 15.57 15 24098 217 34932601
Transplant failure 52.69 15.57 32 24081 3521 34929297
Electrolyte imbalance 52.53 15.57 57 24056 14355 34918463
Type V hyperlipidaemia 52.27 15.57 20 24093 784 34932034
Myocardial ischaemia 51.84 15.57 62 24051 17346 34915472
Hyperuricaemia 50.63 15.57 43 24070 8000 34924818
Cardiomyopathy 50.27 15.57 60 24053 16748 34916070
Cardiac amyloidosis 50.12 15.57 22 24091 1229 34931589
Blood thyroid stimulating hormone increased 49.81 15.57 33 24080 4222 34928596
Right ventricular dysfunction 48.15 15.57 21 24092 1155 34931663
Immunosuppressant drug level increased 47.91 15.57 37 24076 6018 34926800
Cardiogenic shock 47.57 15.57 74 24039 26544 34906274
Gynaecomastia 47.51 15.57 46 24067 10134 34922684
Syncope 46.70 15.57 154 23959 91297 34841521
Ventricular extrasystoles 46.42 15.57 49 24064 11959 34920859
Inferior vena cava dilatation 46.18 15.57 18 24095 742 34932076
Cardiomegaly 45.99 15.57 55 24058 15383 34917435
Venous pressure jugular increased 45.26 15.57 18 24095 783 34932035
Jugular vein distension 44.85 15.57 17 24096 649 34932169
Product prescribing error 44.16 15.57 66 24047 22861 34909957
Respiratory tract haemorrhage 43.45 15.57 20 24093 1250 34931568
Concomitant disease aggravated 43.29 15.57 34 24079 5667 34927151
Seizure 42.62 15.57 10 24103 104847 34827971
Coronary artery stenosis 42.17 15.57 42 24071 9574 34923244
Orthopnoea 42.17 15.57 32 24081 5071 34927747
Ventricular hypokinesia 41.92 15.57 33 24080 5519 34927299
Breath sounds abnormal 41.71 15.57 36 24077 6845 34925973
Blood creatinine increased 41.60 15.57 152 23961 94824 34837994
Left ventricular dysfunction 40.77 15.57 42 24071 9965 34922853
Hyperthyroidism 40.64 15.57 43 24070 10523 34922295
Inflammatory marker increased 40.38 15.57 31 24082 4997 34927821
Lung consolidation 39.98 15.57 33 24080 5903 34926915
White blood cell count decreased 39.00 15.57 9 24104 95436 34837382
Blood pressure systolic decreased 38.90 15.57 29 24084 4474 34928344
Atrial flutter 37.66 15.57 50 24063 15524 34917294
Dizziness 37.25 15.57 268 23845 218253 34714565
Asthma-chronic obstructive pulmonary disease overlap syndrome 37.06 15.57 18 24095 1269 34931549
Left ventricular enlargement 36.99 15.57 15 24098 687 34932131
Off label use 36.74 15.57 157 23956 419367 34513451
Malignant neoplasm progression 36.58 15.57 8 24105 88038 34844780
Waist circumference increased 36.51 15.57 16 24097 890 34931928
Platelet distribution width increased 36.22 15.57 10 24103 134 34932684
Neutropenia 36.09 15.57 33 24080 156745 34776073
Bundle branch block left 35.67 15.57 31 24082 5948 34926870
Bronchial hyperreactivity 35.00 15.57 19 24094 1690 34931128
Palpitations 34.99 15.57 82 24031 39904 34892914
Pulmonary arterial pressure increased 34.36 15.57 17 24096 1248 34931570
Oesophageal carcinoma 34.26 15.57 37 24076 9267 34923551
Drug ineffective 34.12 15.57 181 23932 456570 34476248
Glomerular filtration rate abnormal 34.00 15.57 15 24098 848 34931970
Mitral valve thickening 33.73 15.57 12 24101 382 34932436
Glomerular filtration rate 33.66 15.57 9 24104 106 34932712
Contraindicated product administered 33.31 15.57 56 24057 21425 34911393
Atrial tachycardia 32.67 15.57 24 24089 3621 34929197
N-terminal prohormone brain natriuretic peptide abnormal 32.54 15.57 10 24103 199 34932619
Left ventricular dilatation 32.39 15.57 14 24099 753 34932065
Aortic valve incompetence 32.01 15.57 29 24084 5875 34926943
Ventricular dyskinesia 30.90 15.57 10 24103 237 34932581
Venous pressure jugular decreased 30.66 15.57 7 24106 40 34932778
Sinus bradycardia 30.40 15.57 41 24072 12922 34919896
Cardiac ventricular thrombosis 29.77 15.57 15 24098 1145 34931673
Stenosis 29.13 15.57 16 24097 1457 34931361
Chronic kidney disease 28.21 15.57 77 24036 41133 34891685
Cardiac failure congestive 28.19 15.57 123 23990 83147 34849671
Atrial thrombosis 27.94 15.57 18 24095 2196 34930622
Pulmonary oedema 27.87 15.57 84 24029 47445 34885373
Pyonephrosis 27.79 15.57 7 24106 64 34932754
Arthralgia 27.41 15.57 47 24066 169994 34762824
Pleural effusion 27.26 15.57 120 23993 81426 34851392
Micturition frequency decreased 27.18 15.57 10 24103 351 34932467
Hypotonia 26.78 15.57 30 24083 7823 34924995
Pyrexia 26.49 15.57 129 23984 332884 34599934
Rash 26.46 15.57 73 24040 222679 34710139
Conduction disorder 26.25 15.57 17 24096 2093 34930725
Mitral valve calcification 25.91 15.57 11 24102 566 34932252
Pulmonary congestion 25.61 15.57 39 24074 13726 34919092
Leukopenia 25.52 15.57 6 24107 62850 34869968
Pulmonary function test abnormal 25.25 15.57 18 24095 2592 34930226
Blood pressure inadequately controlled 25.06 15.57 18 24095 2622 34930196
Neutrophil count decreased 24.88 15.57 3 24110 51101 34881717
Thrombocytopenia 24.44 15.57 44 24069 156203 34776615
Arterial intramural haematoma 23.90 15.57 6 24107 54 34932764
Pericardial fibrosis 23.86 15.57 7 24106 118 34932700
Infusion related reaction 23.77 15.57 4 24109 53053 34879765
Neuropathy peripheral 23.71 15.57 14 24099 83249 34849569
Infection 23.57 15.57 17 24096 90898 34841920
Deep vein thrombosis 23.22 15.57 8 24105 65240 34867578
Heart rate irregular 22.91 15.57 40 24073 15767 34917051
Circulatory collapse 22.77 15.57 47 24066 20991 34911827
Heart valve stenosis 21.76 15.57 6 24107 80 34932738
Pain in extremity 21.28 15.57 34 24079 126479 34806339
Right ventricular failure 20.93 15.57 28 24085 8756 34924062
Ascites 20.75 15.57 75 24038 46496 34886322
Pancytopenia 20.75 15.57 21 24092 95136 34837682
Non-compaction cardiomyopathy 20.55 15.57 5 24108 39 34932779
Blood lactic acid 20.34 15.57 8 24105 338 34932480
Gastric dilatation 20.33 15.57 10 24103 725 34932093
Ureteric haemorrhage 19.98 15.57 6 24107 110 34932708
Brain natriuretic peptide increased 19.95 15.57 22 24091 5637 34927181
Depression 19.43 15.57 23 24090 97075 34835743
Coma 19.27 15.57 4 24109 45674 34887144
Hypokinesia 19.19 15.57 27 24086 8853 34923965
Haemoglobin increased 18.99 15.57 17 24096 3392 34929426
Dyspnoea paroxysmal nocturnal 18.45 15.57 12 24101 1487 34931331
Back pain 18.41 15.57 35 24078 121754 34811064
Renal failure 18.23 15.57 153 23960 130404 34802414
Hypertrophy 18.12 15.57 8 24105 453 34932365
Dehydration 17.98 15.57 152 23961 129817 34803001
Ventricular fibrillation 17.86 15.57 45 24068 22909 34909909
Hypersensitivity 17.75 15.57 10 24103 61025 34871793
Adrenocortical insufficiency acute 17.74 15.57 12 24101 1588 34931230
Hypoglycaemia 17.19 15.57 79 24034 54561 34878257
Angina pectoris 17.05 15.57 54 24059 31309 34901509
Varicose vein 17.00 15.57 11 24102 1352 34931466
Weight increased 16.90 15.57 116 23997 92917 34839901
Glycosylated haemoglobin increased 16.79 15.57 29 24084 11331 34921487
Lower respiratory tract infection 16.77 15.57 54 24059 31583 34901235
Brain natriuretic peptide abnormal 16.44 15.57 7 24106 363 34932455
Scrotal oedema 16.31 15.57 12 24101 1814 34931004
Crepitations 15.97 15.57 15 24098 3181 34929637
Sudden cardiac death 15.92 15.57 16 24097 3685 34929133
Renal atrophy 15.86 15.57 10 24103 1175 34931643
Cardiac dysfunction 15.75 15.57 13 24100 2325 34930493
Haemodynamic test abnormal 15.74 15.57 4 24109 38 34932780
Cardiac resynchronisation therapy 15.74 15.57 4 24109 38 34932780
Intentional product use issue 15.74 15.57 11 24102 59805 34873013
Cardiac murmur 15.72 15.57 23 24090 7814 34925004
Hypervolaemia 15.71 15.57 39 24074 19670 34913148

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
Cardiac failure 889.80 16.54 593 27086 154249 79562460
Cardiac failure chronic 519.66 16.54 181 27498 10954 79705755
Acute kidney injury 466.83 16.54 723 26956 518681 79198028
Hyperkalaemia 349.65 16.54 301 27378 114097 79602612
Ventricular tachycardia 302.98 16.54 186 27493 41749 79674960
Hypotension 265.86 16.54 515 27164 439802 79276907
Rales 261.04 16.54 131 27548 19870 79696839
Oedema peripheral 252.22 16.54 370 27309 251918 79464791
Ejection fraction decreased 236.14 16.54 148 27531 34429 79682280
N-terminal prohormone brain natriuretic peptide increased 209.17 16.54 74 27605 4681 79712028
Glomerular filtration rate decreased 204.05 16.54 116 27563 22586 79694123
Mitral valve incompetence 186.86 16.54 119 27560 28446 79688263
Dyspnoea 179.85 16.54 677 27002 856348 78860361
Atrial fibrillation 178.74 16.54 277 27402 197609 79519100
Cardiac failure acute 149.64 16.54 89 27590 18840 79697869
Renal impairment 139.79 16.54 219 27460 157564 79559145
Drug interaction 139.49 16.54 386 27293 414797 79301912
Exercise tolerance decreased 138.04 16.54 66 27613 9005 79707704
Dyspnoea at rest 123.03 16.54 57 27622 7245 79709464
Ventricular enlargement 123.02 16.54 32 27647 700 79716009
Bradycardia 119.83 16.54 188 27491 135369 79581340
Computerised tomogram coronary artery abnormal 114.31 16.54 24 27655 194 79716515
Tricuspid valve incompetence 113.91 16.54 76 27603 19636 79697073
Atrial enlargement 111.80 16.54 32 27647 1011 79715698
Congestive cardiomyopathy 110.72 16.54 62 27617 11718 79704991
Ventricular arrhythmia 109.76 16.54 56 27623 8784 79707925
Cardiomyopathy 107.10 16.54 85 27594 28689 79688020
Dyspnoea exertional 98.98 16.54 136 27543 86937 79629772
Soft tissue mass 96.65 16.54 30 27649 1258 79715451
Ischaemic cardiomyopathy 96.27 16.54 49 27630 7646 79709063
Oesophageal perforation 94.82 16.54 31 27648 1540 79715169
Multimorbidity 89.30 16.54 29 27650 1410 79715299
Labelled drug-drug interaction medication error 78.76 16.54 70 27609 27580 79689129
Coronary artery stenosis 76.66 16.54 50 27629 12434 79704275
Liver palpable 76.54 16.54 19 27660 342 79716367
Blood pressure decreased 75.73 16.54 129 27550 99337 79617372
Low cardiac output syndrome 72.81 16.54 23 27656 1022 79715687
Cardiogenic shock 72.70 16.54 81 27598 41833 79674876
Completed suicide 72.39 16.54 3 27676 245764 79470945
Left ventricular dysfunction 71.63 16.54 57 27622 19304 79697405
Blood potassium increased 71.49 16.54 68 27611 29207 79687502
Blood creatinine increased 70.55 16.54 162 27517 154895 79561814
Arrhythmia 68.55 16.54 95 27584 61177 79655532
Orthopnoea 68.43 16.54 43 27636 10030 79706679
Cardiomegaly 67.77 16.54 63 27616 26289 79690420
General physical health deterioration 67.06 16.54 229 27450 275009 79441700
Hyperuricaemia 64.60 16.54 44 27635 11755 79704954
Syncope 64.20 16.54 171 27508 179278 79537431
Infusion related reaction 64.04 16.54 4 27675 230233 79486476
Myocardial ischaemia 63.69 16.54 60 27619 25459 79691250
Left ventricular dilatation 63.53 16.54 21 27658 1080 79715629
Hepatic vein dilatation 62.50 16.54 15 27664 233 79716476
Immunosuppressant drug level increased 62.50 16.54 39 27640 8988 79707721
Arthralgia 62.37 16.54 64 27615 571739 79144970
Transplant failure 62.30 16.54 31 27648 4610 79712099
Product prescribing error 61.78 16.54 77 27602 44736 79671973
Superinfection 60.69 16.54 31 27648 4871 79711838
Type V hyperlipidaemia 60.61 16.54 20 27659 1023 79715686
Rheumatoid arthritis 59.90 16.54 3 27676 208467 79508242
Electrocardiogram abnormal 59.21 16.54 48 27631 16689 79700020
Left atrial enlargement 57.81 16.54 20 27659 1183 79715526
Electrolyte imbalance 57.59 16.54 62 27617 30819 79685890
Stenosis 57.29 16.54 24 27655 2398 79714311
Pain 57.17 16.54 98 27581 703704 79013005
Respiratory tract haemorrhage 56.71 16.54 22 27657 1801 79714908
Ventricular hypokinesia 56.57 16.54 37 27642 9242 79707467
Ventricular extrasystoles 56.34 16.54 50 27629 19654 79697055
Inferior vena cava dilatation 55.87 16.54 18 27661 853 79715856
Pulmonary arterial pressure increased 54.07 16.54 28 27651 4527 79712182
Febrile neutropenia 53.84 16.54 8 27671 230991 79485718
Gynaecomastia 52.71 16.54 33 27646 7648 79709061
Renal failure 51.37 16.54 170 27509 200798 79515911
Left ventricular enlargement 50.24 16.54 16 27663 730 79715979
Cardiac failure congestive 50.20 16.54 135 27544 142267 79574442
Joint swelling 49.72 16.54 19 27660 288627 79428082
Oesophageal carcinoma 48.37 16.54 36 27643 11048 79705661
Venous pressure jugular increased 48.28 16.54 18 27661 1322 79715387
Blood thyroid stimulating hormone increased 47.98 16.54 34 27645 9674 79707035
Alopecia 47.52 16.54 11 27668 231344 79485365
Angina pectoris 47.40 16.54 73 27606 51659 79665050
Arthropathy 46.61 16.54 4 27675 177107 79539602
N-terminal prohormone brain natriuretic peptide abnormal 46.11 16.54 12 27667 263 79716446
Lung consolidation 45.76 16.54 32 27647 8915 79707794
Hypersensitivity 45.60 16.54 17 27662 262222 79454487
Rash 45.59 16.54 82 27597 578276 79138433
Concomitant disease aggravated 44.97 16.54 37 27642 13130 79703579
Atrial flutter 44.93 16.54 46 27633 21579 79695130
Atrial thrombosis 44.92 16.54 23 27656 3633 79713076
Hyperthyroidism 43.91 16.54 46 27633 22163 79694546
Pulmonary oedema 43.23 16.54 95 27584 88159 79628550
Platelet distribution width increased 42.97 16.54 10 27669 135 79716574
Chronic kidney disease 42.88 16.54 80 27599 66074 79650635
Pleural effusion 42.72 16.54 129 27550 145133 79571576
Right ventricular dysfunction 42.62 16.54 20 27659 2615 79714094
Breath sounds abnormal 40.69 16.54 38 27641 15946 79700763
Bronchial hyperreactivity 39.90 16.54 20 27659 3020 79713689
Blood pressure systolic decreased 39.67 16.54 32 27647 11044 79705665
Jugular vein distension 39.64 16.54 16 27663 1454 79715255
Drug abuse 39.40 16.54 5 27674 162686 79554023
Inflammatory marker increased 38.40 16.54 31 27648 10709 79706000
Hyponatraemia 38.14 16.54 142 27537 177706 79539003
Drug hypersensitivity 37.89 16.54 29 27650 298887 79417822
Glomerular filtration rate abnormal 37.88 16.54 16 27663 1632 79715077
Headache 37.52 16.54 110 27569 653662 79063047
Waist circumference increased 37.50 16.54 16 27663 1673 79715036
Sinusitis 36.90 16.54 11 27668 195490 79521219
Glomerular filtration rate 36.85 16.54 9 27670 151 79716558
Mitral valve thickening 36.53 16.54 11 27668 416 79716293
Coronary artery occlusion 36.30 16.54 35 27644 15280 79701429
Asthma-chronic obstructive pulmonary disease overlap syndrome 35.95 16.54 19 27660 3202 79713507
Pain in extremity 35.13 16.54 45 27634 364493 79352216
Dizziness 34.78 16.54 306 27373 526135 79190574
Brain natriuretic peptide increased 34.63 16.54 27 27652 8873 79707836
Drug ineffective 34.02 16.54 228 27451 1080685 78636024
Cardiac ventricular disorder 33.79 16.54 10 27669 356 79716353
Cardiac ventricular thrombosis 33.52 16.54 15 27664 1758 79714951
Pulmonary congestion 33.31 16.54 44 27635 27056 79689653
Treatment failure 33.27 16.54 9 27670 170477 79546232
Hepatic enzyme increased 33.17 16.54 11 27668 182599 79534110
Aortic valve incompetence 33.01 16.54 27 27652 9503 79707206
Ventricular dyskinesia 32.72 16.54 10 27669 398 79716311
Infection 32.52 16.54 22 27657 241690 79475019
Dehydration 32.52 16.54 171 27508 248016 79468693
Hypovolaemia 32.07 16.54 35 27644 17656 79699053
Seizure 31.56 16.54 13 27666 188821 79527888
Pulmonary function test abnormal 31.48 16.54 19 27660 4125 79712584
Melaena 31.48 16.54 67 27612 60823 79655886
Back pain 30.93 16.54 36 27643 304144 79412565
Venous pressure jugular decreased 30.84 16.54 7 27672 84 79716625
Bundle branch block left 30.52 16.54 28 27651 11485 79705224
Off label use 30.22 16.54 188 27491 907027 78809682
Gout 30.14 16.54 40 27639 24709 79692000
Ascites 30.07 16.54 75 27604 75487 79641222
Pyonephrosis 29.91 16.54 7 27672 97 79716612
White blood cell count decreased 29.83 16.54 14 27665 188274 79528435
Subclavian vein thrombosis 28.87 16.54 15 27664 2442 79714267
Abdominal discomfort 27.34 16.54 28 27651 250699 79466010
Drug intolerance 27.13 16.54 31 27648 264088 79452621
Conduction disorder 26.99 16.54 16 27663 3363 79713346
Pericardial fibrosis 26.62 16.54 7 27672 160 79716549
Mitral valve calcification 26.38 16.54 12 27667 1461 79715248
Stomatitis 26.37 16.54 9 27670 146748 79569961
Therapeutic drug monitoring analysis not performed 26.19 16.54 13 27666 1923 79714786
Cardiovascular insufficiency 26.15 16.54 15 27664 2966 79713743
Urticaria 26.07 16.54 16 27663 185185 79531524
Hypomagnesaemia 25.86 16.54 53 27626 46858 79669851
Arterial intramural haematoma 25.78 16.54 6 27673 81 79716628
Heart rate irregular 25.66 16.54 43 27636 32636 79684073
Degenerative aortic valve disease 25.65 16.54 7 27672 185 79716524
Scrotal oedema 25.54 16.54 12 27667 1573 79715136
Neutropenia 25.22 16.54 38 27641 287672 79429037
Hypoglycaemia 25.09 16.54 85 27594 101509 79615200
Ventricular fibrillation 25.06 16.54 42 27637 31884 79684825
Circulatory collapse 24.96 16.54 46 27633 37622 79679087
Micturition frequency decreased 24.52 16.54 10 27669 933 79715776
Subdural haematoma 24.20 16.54 41 27638 31393 79685316
Non-compaction cardiomyopathy 23.97 16.54 5 27674 39 79716670
Rash scarlatiniform 23.90 16.54 7 27672 240 79716469
Cardiac amyloidosis 23.84 16.54 12 27667 1828 79714881
Nasopharyngitis 23.76 16.54 32 27647 253849 79462860
Tachypnoea 23.61 16.54 41 27638 32022 79684687
Musculoskeletal stiffness 23.44 16.54 16 27663 174992 79541717
Blood lactic acid 23.42 16.54 8 27671 455 79716254
Hydrothorax 23.31 16.54 11 27668 1457 79715252
Injection site pain 23.26 16.54 8 27671 129830 79586879
Right ventricular failure 22.71 16.54 34 27645 23463 79693246
Hypotonia 22.53 16.54 25 27654 12845 79703864
Coma 22.28 16.54 4 27675 100645 79616064
Sinus bradycardia 22.24 16.54 35 27644 25212 79691497
Abdominal pain upper 22.20 16.54 27 27652 223792 79492917
Left ventricular hypertrophy 21.80 16.54 23 27656 11168 79705541
Dyspnoea paroxysmal nocturnal 21.68 16.54 12 27667 2216 79714493
Wound haemorrhage 21.55 16.54 15 27664 4146 79712563
Heart valve stenosis 21.52 16.54 6 27673 172 79716537
Hypocalcaemia 21.40 16.54 51 27628 49873 79666836
Haematochezia 21.35 16.54 73 27606 87572 79629137
Acute myocardial infarction 21.31 16.54 67 27612 76969 79639740
Gastrointestinal haemorrhage 20.88 16.54 104 27575 147615 79569094
Gastric dilatation 20.72 16.54 10 27669 1392 79715317
Vascular stent thrombosis 20.70 16.54 14 27665 3696 79713013
Acute pulmonary oedema 20.49 16.54 25 27654 14205 79702504
Hypokinesia 20.48 16.54 29 27650 19031 79697678
Osteoarthritis 20.38 16.54 3 27676 87306 79629403
Malignant neoplasm progression 20.20 16.54 11 27668 135979 79580730
Palpitations 19.96 16.54 92 27587 126518 79590191
Benign prostatic hyperplasia 19.37 16.54 22 27657 11590 79705119
Deep vein thrombosis 19.13 16.54 9 27670 120910 79595799
Hypertrophy 19.07 16.54 8 27671 802 79715907
Glomerular filtration rate increased 19.00 16.54 9 27670 1202 79715507
Dyspepsia 18.95 16.54 7 27672 108680 79608029
Intentional product use issue 18.95 16.54 15 27664 152097 79564612
Aortic bruit 18.69 16.54 6 27673 281 79716428
Haemoptysis 18.63 16.54 52 27627 55947 79660762
Anaemia 18.62 16.54 236 27443 444779 79271930
Peripheral artery haematoma 18.55 16.54 5 27674 126 79716583
Femoral neck fracture 18.53 16.54 20 27659 9964 79706745
Sudden cardiac death 18.51 16.54 15 27664 5210 79711499
Haemoglobin increased 18.41 16.54 16 27663 6116 79710593
Neutrophil count decreased 18.25 16.54 5 27674 93954 79622755
Atrial tachycardia 18.23 16.54 17 27662 7116 79709593
Renal atrophy 18.23 16.54 10 27669 1815 79714894
Adrenocortical insufficiency acute 18.22 16.54 12 27667 3031 79713678
Pyrexia 18 16.54 150 27529 678559 79038150
Blood cyanide increased 17.94 16.54 4 27675 44 79716665
Hypervolaemia 17.64 16.54 43 27636 42647 79674062
Epistaxis 17.55 16.54 81 27598 111434 79605275
Injection site erythema 17.55 16.54 3 27676 78194 79638515
Neuropathy peripheral 17.52 16.54 14 27665 141291 79575418
Pemphigoid 17.50 16.54 24 27655 15291 79701418
Limited symptom panic attack 17.47 16.54 4 27675 50 79716659
Activated partial thromboplastin time prolonged 17.33 16.54 23 27656 14205 79702504
Cardiac dysfunction 17.12 16.54 13 27666 4111 79712598
Eosinophilia 16.99 16.54 44 27635 45301 79671408
Suicidal ideation 16.97 16.54 3 27676 76337 79640372
Peripheral coldness 16.72 16.54 24 27655 15946 79700763
Hypokalaemia 16.67 16.54 96 27583 143944 79572765
Supraventricular extrasystoles 16.62 16.54 16 27663 6971 79709738
Therapeutic drug monitoring analysis incorrectly performed 16.62 16.54 7 27672 709 79716000

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C03DA04 CARDIOVASCULAR SYSTEM
DIURETICS
ALDOSTERONE ANTAGONISTS AND OTHER POTASSIUM-SPARING AGENTS
Aldosterone antagonists
FDA MoA N0000011310 Aldosterone Antagonists
FDA EPC N0000175557 Aldosterone Antagonist
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D004232 Diuretics
MeSH PA D006727 Hormone Antagonists
MeSH PA D000451 Mineralocorticoid Receptor Antagonists
MeSH PA D045283 Natriuretic Agents
CHEBI has role CHEBI:35674 antihypertensive drugs

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

DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Chronic Heart Failure Following Myocardial Infarction indication
Hyperkalemia contraindication 14140009
Diabetic renal disease contraindication 127013003
Impaired renal function disorder contraindication 197663003
Disease of liver contraindication 235856003 DOID:409




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

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
Mineralocorticoid receptor Nuclear hormone receptor ANTAGONIST IC50 7 WOMBAT-PK CHEMBL
Glucocorticoid receptor Nuclear hormone receptor IC50 4.74 CHEMBL
Androgen receptor Nuclear hormone receptor IC50 4.77 CHEMBL
Progesterone receptor Nuclear hormone receptor Ki 4.70 CHEMBL
Mineralocorticoid receptor Transcription factor IC50 7.40 CHEMBL

External reference:

IDSource
4021363 VUID
N0000148782 NUI
D01115 KEGG_DRUG
4021363 VANDF
C0961485 UMLSCUI
CHEBI:31547 CHEBI
YNU PDB_CHEM_ID
CHEMBL1095097 ChEMBL_ID
D000077545 MESH_DESCRIPTOR_UI
DB00700 DRUGBANK_ID
C058465 MESH_SUPPLEMENTAL_RECORD_UI
443872 PUBCHEM_CID
2876 IUPHAR_LIGAND_ID
7596 INN_ID
6995V82D0B UNII
298869 RXNORM
147386 MMSL
16969 MMSL
d04815 MMSL
009774 NDDF
398699008 SNOMEDCT_US
407010008 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Inspra HUMAN PRESCRIPTION DRUG LABEL 1 0025-1710 TABLET, FILM COATED 25 mg ORAL NDA 27 sections
Inspra HUMAN PRESCRIPTION DRUG LABEL 1 0025-1710 TABLET, FILM COATED 25 mg ORAL NDA 27 sections
Inspra HUMAN PRESCRIPTION DRUG LABEL 1 0025-1720 TABLET, FILM COATED 50 mg ORAL NDA 27 sections
Inspra HUMAN PRESCRIPTION DRUG LABEL 1 0025-1720 TABLET, FILM COATED 50 mg ORAL NDA 27 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 0185-5368 TABLET 25 mg ORAL ANDA 25 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 0185-5368 TABLET 25 mg ORAL ANDA 25 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 0185-5369 TABLET 50 mg ORAL ANDA 25 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 0185-5369 TABLET 50 mg ORAL ANDA 25 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 0378-1030 TABLET, FILM COATED 25 mg ORAL ANDA 27 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 0378-1030 TABLET, FILM COATED 25 mg ORAL ANDA 27 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 0378-1031 TABLET, FILM COATED 50 mg ORAL ANDA 27 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 0378-1031 TABLET, FILM COATED 50 mg ORAL ANDA 27 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 16729-293 TABLET, FILM COATED 25 mg ORAL ANDA 26 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 16729-294 TABLET, FILM COATED 50 mg ORAL ANDA 26 sections
Inspra HUMAN PRESCRIPTION DRUG LABEL 1 21695-797 TABLET 25 mg ORAL NDA 27 sections
EPLERENONE HUMAN PRESCRIPTION DRUG LABEL 1 31722-049 TABLET, FILM COATED 25 mg ORAL ANDA 23 sections
EPLERENONE HUMAN PRESCRIPTION DRUG LABEL 1 31722-050 TABLET, FILM COATED 50 mg ORAL ANDA 23 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 42254-011 TABLET 50 mg ORAL ANDA 23 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 42291-454 TABLET, COATED 25 mg ORAL ANDA 29 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 42291-454 TABLET, COATED 25 mg ORAL ANDA 29 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 42291-455 TABLET, COATED 50 mg ORAL ANDA 29 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 42291-455 TABLET, COATED 50 mg ORAL ANDA 29 sections
EPLERENONE HUMAN PRESCRIPTION DRUG LABEL 1 51991-877 TABLET, FILM COATED 25 mg ORAL ANDA 27 sections
EPLERENONE HUMAN PRESCRIPTION DRUG LABEL 1 51991-878 TABLET, FILM COATED 50 mg ORAL ANDA 27 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 54868-6065 TABLET 25 mg ORAL ANDA 23 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 59762-1710 TABLET, FILM COATED 25 mg ORAL NDA AUTHORIZED GENERIC 27 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 59762-1710 TABLET, FILM COATED 25 mg ORAL NDA AUTHORIZED GENERIC 27 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 59762-1720 TABLET, FILM COATED 50 mg ORAL NDA AUTHORIZED GENERIC 27 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 59762-1720 TABLET, FILM COATED 50 mg ORAL NDA AUTHORIZED GENERIC 27 sections
EPLERENONE HUMAN PRESCRIPTION DRUG LABEL 1 60687-451 TABLET, FILM COATED 25 mg ORAL ANDA 27 sections