eplerenone ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
aldosterone antagonists, spironolactone derivates 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 ยตM/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 181.79 20.96 104 4693 75936 50524391
Hyperkalaemia 107.36 20.96 63 4734 48026 50552301
Acute kidney injury 103.15 20.96 117 4680 227941 50372386
Cardiac failure chronic 87.34 20.96 26 4771 3537 50596790
Subclavian vein thrombosis 80.30 20.96 21 4776 1778 50598549
Atrial fibrillation 68.99 20.96 65 4732 101680 50498647
Hypotension 59.70 20.96 91 4706 235378 50364949
Drug interaction 59.07 20.96 83 4714 199538 50400789
Hyponatraemia 53.20 20.96 55 4742 96084 50504243
Hydrothorax 44.82 20.96 11 4786 720 50599607
Cardiomyopathy 44.44 20.96 24 4773 15562 50584765
Femoral neck fracture 44.20 20.96 19 4778 7471 50592856
Embolism venous 43.22 20.96 14 4783 2511 50597816
Cardiac failure acute 42.43 20.96 19 4778 8231 50592096
Degenerative aortic valve disease 40.06 20.96 7 4790 82 50600245
Vascular stent thrombosis 37.64 20.96 10 4787 899 50599428
Oedema peripheral 35.71 20.96 58 4739 157903 50442424
Cardiac ventricular disorder 35.66 20.96 7 4790 160 50600167
Angina pectoris 35.28 20.96 25 4772 26163 50574164
Hypovolaemia 33.93 20.96 17 4780 9448 50590879
Ventricular tachycardia 30.78 20.96 19 4778 15802 50584525
Ejection fraction decreased 30.45 20.96 20 4777 18500 50581827
Subclavian artery thrombosis 29.57 20.96 6 4791 163 50600164
Left ventricular dysfunction 29.45 20.96 16 4781 10490 50589837
Left ventricular dilatation 29.10 20.96 7 4790 421 50599906
Pulmonary arterial pressure increased 28.33 20.96 11 4786 3337 50596990
N-terminal prohormone brain natriuretic peptide increased 27.32 20.96 9 4788 1701 50598626
Stenosis 26.26 20.96 8 4789 1175 50599152
Vascular purpura 26.05 20.96 8 4789 1206 50599121
Labelled drug-drug interaction medication error 24.05 20.96 14 4783 10463 50589864
Subdural haematoma 23.80 20.96 15 4782 12932 50587395
Arrhythmia 22.08 20.96 21 4776 33111 50567216
Therapeutic drug monitoring analysis not performed 21.06 20.96 6 4791 699 50599628

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 525.12 15.98 428 19211 78859 29476029
Cardiac failure chronic 356.07 15.98 141 19498 6326 29548562
Ventricular tachycardia 188.18 15.98 140 19499 22434 29532454
N-terminal prohormone brain natriuretic peptide increased 187.61 15.98 64 19575 1868 29553020
Acute kidney injury 182.77 15.98 483 19156 264784 29290104
Hyperkalaemia 170.82 15.98 207 19432 61185 29493703
Oedema peripheral 162.24 15.98 265 19374 103292 29451596
Hypotension 158.86 15.98 378 19261 193976 29360912
Glomerular filtration rate decreased 149.05 15.98 93 19546 11173 29543715
Dyspnoea 140.74 15.98 505 19134 326227 29228661
Ejection fraction decreased 132.91 15.98 99 19540 15879 29539009
Rales 114.75 15.98 68 19571 7442 29547446
Dyspnoea at rest 113.05 15.98 51 19588 3163 29551725
Mitral valve incompetence 109.73 15.98 82 19557 13211 29541677
Ventricular arrhythmia 104.18 15.98 54 19585 4550 29550338
Cardiac failure acute 97.32 15.98 66 19573 9126 29545762
Computerised tomogram coronary artery abnormal 94.80 15.98 23 19616 185 29554703
Renal impairment 81.60 15.98 172 19467 81161 29473727
Blood potassium increased 70.17 15.98 66 19573 14585 29540303
Liver palpable 68.44 15.98 19 19620 271 29554617
General physical health deterioration 65.01 15.98 182 19457 102675 29452213
Ventricular enlargement 63.78 15.98 20 19619 444 29554444
Electrocardiogram abnormal 62.27 15.98 46 19593 7276 29547612
Atrial fibrillation 61.02 15.98 181 19458 105465 29449423
Exercise tolerance decreased 58.66 15.98 36 19603 4195 29550693
Congestive cardiomyopathy 57.17 15.98 42 19597 6588 29548300
Febrile neutropenia 56.15 15.98 5 19634 112235 29442653
Drug interaction 55.24 15.98 268 19371 197117 29357771
Blood pressure decreased 54.94 15.98 104 19535 45373 29509515
Low cardiac output syndrome 54.18 15.98 18 19621 483 29554405
Hepatic vein dilatation 53.84 15.98 15 19624 217 29554671
Dyspnoea exertional 53.76 15.98 91 19548 36399 29518489
Gynaecomastia 53.34 15.98 44 19595 8173 29546715
Atrial enlargement 52.50 15.98 16 19623 322 29554566
Bradycardia 51.52 15.98 126 19513 65503 29489385
Death 50.68 15.98 94 19545 341990 29212898
Left atrial enlargement 50.62 15.98 19 19620 734 29554154
Dizziness 50.53 15.98 254 19385 189430 29365458
Respiratory tract haemorrhage 49.49 15.98 20 19619 944 29553944
Inferior vena cava dilatation 48.88 15.98 18 19621 659 29554229
Type V hyperlipidaemia 48.36 15.98 18 19621 679 29554209
Venous pressure jugular increased 47.58 15.98 18 19621 711 29554177
Oesophageal perforation 46.96 15.98 18 19621 737 29554151
Blood creatinine increased 46.46 15.98 143 19496 84959 29469929
Soft tissue mass 46.25 15.98 17 19622 619 29554269
Multimorbidity 44.71 15.98 16 19623 539 29554349
Atrial tachycardia 44.58 15.98 23 19616 1918 29552970
Concomitant disease aggravated 43.97 15.98 32 19607 4946 29549942
Jugular vein distension 42.85 15.98 16 19623 609 29554279
Orthopnoea 41.85 15.98 30 19609 4530 29550358
Blood pressure systolic decreased 41.63 15.98 28 19611 3816 29551072
Waist circumference increased 39.98 15.98 16 19623 736 29554152
Hyperuricaemia 38.80 15.98 34 19605 6855 29548033
Cardiogenic shock 38.22 15.98 55 19584 19135 29535753
Pulmonary arterial pressure increased 37.45 15.98 17 19622 1069 29553819
Labelled drug-drug interaction medication error 37.02 15.98 43 19596 12116 29542772
Tricuspid valve incompetence 36.75 15.98 36 19603 8358 29546530
Electrolyte imbalance 36.23 15.98 41 19598 11233 29543655
Ischaemic cardiomyopathy 36.19 15.98 30 19609 5608 29549280
Seizure 35.56 15.98 9 19630 93114 29461774
Mitral valve thickening 34.82 15.98 12 19627 361 29554527
Pulmonary oedema 33.46 15.98 82 19557 42653 29512235
Ventricular dyskinesia 32.64 15.98 10 19629 205 29554683
Blood thyroid stimulating hormone increased 32.16 15.98 22 19617 3083 29551805
White blood cell count decreased 31.94 15.98 8 19631 83354 29471534
Left ventricular enlargement 31.66 15.98 13 19626 639 29554249
Arthralgia 31.30 15.98 28 19611 139589 29415299
Neutropenia 31.25 15.98 25 19614 131686 29423202
Venous pressure jugular decreased 30.92 15.98 7 19632 40 29554848
Breath sounds abnormal 30.86 15.98 27 19612 5430 29549458
Cardiac amyloidosis 30.71 15.98 14 19625 889 29553999
Syncope 30.70 15.98 121 19518 81250 29473638
Hyperthyroidism 30.59 15.98 33 19606 8575 29546313
Superinfection 30.25 15.98 18 19621 1983 29552905
Right ventricular dysfunction 29.99 15.98 14 19625 939 29553949
Arrhythmia 29.93 15.98 65 19574 31248 29523640
Pyrexia 28.50 15.98 97 19542 287525 29267363
Pyonephrosis 28.35 15.98 7 19632 61 29554827
Left ventricular dysfunction 27.97 15.98 32 19607 8870 29546018
Blood pressure inadequately controlled 27.33 15.98 18 19621 2368 29552520
Coronary artery stenosis 27.25 15.98 31 19608 8542 29546346
Cardiac ventricular thrombosis 27.11 15.98 13 19626 926 29553962
Mitral valve calcification 27.10 15.98 11 19628 525 29554363
Glomerular filtration rate abnormal 26.78 15.98 12 19627 732 29554156
Oesophageal carcinoma 26.73 15.98 23 19616 4524 29550364
Transplant failure 26.69 15.98 19 19620 2837 29552051
Malignant neoplasm progression 26.58 15.98 8 19631 73851 29481037
Immunosuppressant drug level increased 25.80 15.98 23 19616 4742 29550146
Product prescribing error 25.36 15.98 44 19595 17932 29536956
Weight increased 24.98 15.98 109 19530 76558 29478330
Myocardial ischaemia 24.96 15.98 41 19598 15987 29538901
N-terminal prohormone brain natriuretic peptide abnormal 24.96 15.98 8 19631 191 29554697
Arterial intramural haematoma 24.76 15.98 6 19633 48 29554840
Rash 24.74 15.98 56 19583 189763 29365125
Brain natriuretic peptide increased 24.06 15.98 21 19618 4209 29550679
Drug ineffective 23.68 15.98 143 19496 363027 29191861
Cardiomyopathy 23.26 15.98 38 19601 14749 29540139
Hypothyroidism 22.53 15.98 39 19600 15867 29539021
Right ventricular failure 22.52 15.98 27 19612 7863 29547025
Cardiomegaly 22.49 15.98 36 19603 13740 29541148
Atrial flutter 22.26 15.98 36 19603 13858 29541030
Cardiac failure congestive 22.05 15.98 105 19534 76476 29478412
Hypotonia 22.01 15.98 25 19614 6877 29548011
Infection 21.65 15.98 12 19627 76739 29478149
Deep vein thrombosis 21.05 15.98 6 19633 57393 29497495
Pulmonary congestion 20.99 15.98 33 19606 12403 29542485
Palpitations 20.84 15.98 58 19581 32546 29522342
Ventricular hypokinesia 20.77 15.98 20 19619 4545 29550343
Non-compaction cardiomyopathy 20.74 15.98 5 19634 39 29554849
Blood lactic acid 20.63 15.98 8 19631 338 29554550
Asthma-chronic obstructive pulmonary disease overlap syndrome 20.59 15.98 10 19629 733 29554155
Atrial thrombosis 20.35 15.98 14 19625 1979 29552909
Adrenocortical insufficiency acute 20.28 15.98 12 19627 1308 29553580
Glycosylated haemoglobin increased 20.22 15.98 28 19611 9398 29545490
Ureteric haemorrhage 20.21 15.98 6 19633 110 29554778
Neuropathy peripheral 20.19 15.98 11 19628 71016 29483872
Leukopenia 19.82 15.98 6 19633 55197 29499691
Pleural effusion 19.56 15.98 97 19542 71811 29483077
Cardiac dysfunction 19.18 15.98 13 19626 1794 29553094
Neutrophil count decreased 19.15 15.98 3 19636 43564 29511324
Chronic kidney disease 18.74 15.98 60 19579 36356 29518532
Abdominal distension 18.71 15.98 70 19569 45841 29509047
Hypertrophy 18.58 15.98 8 19631 443 29554445
Ascites 18.54 15.98 60 19579 36559 29518329
Left ventricular dilatation 18.51 15.98 9 19630 661 29554227
Sinus bradycardia 18.50 15.98 30 19609 11573 29543315
Inflammatory marker increased 18.48 15.98 17 19622 3650 29551238
Cardiac murmur 17.85 15.98 22 19617 6591 29548297
Brain natriuretic peptide abnormal 17.64 15.98 7 19632 315 29554573
Ventricular fibrillation 17.62 15.98 35 19604 15798 29539090
Oedema 17.57 15.98 63 19576 40420 29514468
Skin weeping 17.49 15.98 6 19633 178 29554710
Lung consolidation 17.34 15.98 19 19620 5024 29549864
Cardiovascular insufficiency 17.16 15.98 11 19628 1382 29553506
Dyspnoea paroxysmal nocturnal 17.16 15.98 11 19628 1383 29553505
Heart rate irregular 17.08 15.98 31 19608 13086 29541802
Bronchial hyperreactivity 17.07 15.98 11 19628 1395 29553493
Renal atrophy 17.01 15.98 10 19629 1077 29553811
Back pain 17 15.98 26 19613 102258 29452630
Gastric dilatation 16.88 15.98 8 19631 555 29554333
Coma 16.71 15.98 3 19636 39447 29515441
Conduction disorder 16.64 15.98 12 19627 1828 29553060
Bundle branch block left 16.63 15.98 19 19620 5258 29549630
Sudden cardiac death 16.36 15.98 15 19624 3207 29551681
Hyperaldosteronism 16.34 15.98 5 19634 102 29554786
Alanine aminotransferase increased 16.15 15.98 14 19625 70930 29483958
Pancytopenia 15.99 15.98 19 19620 83149 29471739

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 725.01 16.12 492 21893 131881 64344466
Cardiac failure chronic 472.75 16.12 160 22225 8881 64467466
Acute kidney injury 344.62 16.12 582 21803 448658 64027689
Hyperkalaemia 288.87 16.12 256 22129 100873 64375474
Ventricular tachycardia 229.91 16.12 145 22240 34120 64442227
Hypotension 222.16 16.12 439 21946 380535 64095812
Oedema peripheral 189.70 16.12 294 22091 210023 64266324
Glomerular filtration rate decreased 186.77 16.12 104 22281 19468 64456879
N-terminal prohormone brain natriuretic peptide increased 186.03 16.12 63 22322 3496 64472851
Ejection fraction decreased 161.96 16.12 109 22276 28598 64447749
Cardiac failure acute 150.91 16.12 85 22300 16259 64460088
Atrial fibrillation 141.49 16.12 230 22155 170859 64305488
Dyspnoea 134.79 16.12 548 21837 718126 63758221
Drug interaction 122.11 16.12 337 22048 361746 64114601
Mitral valve incompetence 113.90 16.12 84 22301 25454 64450893
Ventricular arrhythmia 109.96 16.12 53 22332 7362 64468985
Computerised tomogram coronary artery abnormal 109.66 16.12 23 22362 185 64476162
Dyspnoea at rest 108.50 16.12 50 22335 6279 64470068
Rales 106.00 16.12 66 22319 15163 64461184
Renal impairment 104.14 16.12 176 22209 134841 64341506
Exercise tolerance decreased 81.91 16.12 44 22341 7666 64468681
Liver palpable 77.29 16.12 19 22366 328 64476019
Congestive cardiomyopathy 74.95 16.12 46 22339 10298 64466049
Blood potassium increased 74.47 16.12 66 22319 25914 64450433
Bradycardia 74.31 16.12 141 22244 118078 64358269
Ventricular enlargement 69.56 16.12 19 22366 504 64475843
Blood creatinine increased 66.44 16.12 146 22239 135636 64340711
Atrial enlargement 65.18 16.12 19 22366 641 64475706
Cardiomyopathy 64.03 16.12 60 22325 25296 64451051
Electrocardiogram abnormal 63.86 16.12 46 22339 13435 64462912
Blood pressure decreased 63.29 16.12 110 22275 86089 64390258
Hepatic vein dilatation 62.50 16.12 15 22370 233 64476114
General physical health deterioration 61.63 16.12 183 22202 204242 64272105
Labelled drug-drug interaction medication error 61.15 16.12 55 22330 22007 64454340
Respiratory tract haemorrhage 61.13 16.12 22 22363 1462 64474885
Inferior vena cava dilatation 58.43 16.12 18 22367 736 64475611
Low cardiac output syndrome 57.49 16.12 18 22367 777 64475570
Left atrial enlargement 56.82 16.12 19 22366 1013 64475334
Pulmonary arterial pressure increased 56.76 16.12 28 22357 4088 64472259
Left ventricular dysfunction 56.58 16.12 47 22338 16907 64459440
Cardiogenic shock 55.11 16.12 62 22323 32365 64443982
Type V hyperlipidaemia 54.86 16.12 18 22367 904 64475443
Gynaecomastia 54.74 16.12 31 22354 5985 64470362
Orthopnoea 54.67 16.12 36 22349 9098 64467249
Oesophageal perforation 52.72 16.12 18 22367 1023 64475324
Soft tissue mass 51.10 16.12 17 22368 892 64475455
Hyperuricaemia 51.09 16.12 36 22349 10155 64466192
Venous pressure jugular increased 49.32 16.12 18 22367 1245 64475102
Dyspnoea exertional 48.87 16.12 90 22295 73640 64402707
Arthralgia 48.79 16.12 49 22336 442211 64034136
Left ventricular dilatation 46.75 16.12 16 22369 916 64475431
Ischaemic cardiomyopathy 45.98 16.12 29 22356 6809 64469538
Hyponatraemia 45.82 16.12 134 22251 148205 64328142
Multimorbidity 45.46 16.12 16 22369 996 64475351
Rheumatoid arthritis 45.25 16.12 3 22382 164291 64312056
Febrile neutropenia 44.90 16.12 6 22379 187651 64288696
Concomitant disease aggravated 44.89 16.12 35 22350 11507 64464840
Tricuspid valve incompetence 44.41 16.12 41 22344 16962 64459385
Blood pressure systolic decreased 43.85 16.12 31 22354 8789 64467558
Left ventricular enlargement 43.32 16.12 14 22371 670 64475677
Pain 42.31 16.12 80 22305 553431 63922916
Coronary artery stenosis 41.36 16.12 33 22352 11215 64465132
Jugular vein distension 41.29 16.12 16 22369 1306 64475041
Waist circumference increased 40.73 16.12 16 22369 1355 64474992
Dizziness 40.20 16.12 271 22114 429892 64046455
Cardiomegaly 39.76 16.12 45 22340 23639 64452708
Arrhythmia 39.41 16.12 68 22317 52876 64423471
Oesophageal carcinoma 39.31 16.12 23 22362 4720 64471627
Syncope 39.11 16.12 132 22253 157503 64318844
Electrolyte imbalance 39.08 16.12 46 22339 25197 64451150
Renal failure 38.95 16.12 145 22240 181543 64294804
Cardiac failure congestive 37.52 16.12 115 22270 130465 64345882
N-terminal prohormone brain natriuretic peptide abnormal 37.40 16.12 10 22375 244 64476103
Immunosuppressant drug level increased 37.22 16.12 26 22359 7233 64469114
Mitral valve thickening 37.21 16.12 11 22374 390 64475957
Rash 37.05 16.12 64 22321 458485 64017862
Hyperthyroidism 36.56 16.12 38 22347 18141 64458206
Brain natriuretic peptide increased 36.04 16.12 26 22359 7607 64468740
Pulmonary oedema 34.45 16.12 81 22304 78593 64397754
Cardiac ventricular disorder 34.43 16.12 10 22375 333 64476014
Joint swelling 34.16 16.12 16 22369 215366 64260981
Hypovolaemia 34.11 16.12 34 22351 15452 64460895
Ventricular extrasystoles 34.11 16.12 36 22349 17493 64458854
Transplant failure 33.04 16.12 19 22366 3775 64472572
Ventricular dyskinesia 32.72 16.12 10 22375 398 64475949
Drug abuse 32.22 16.12 4 22381 132370 64343977
Breath sounds abnormal 32.15 16.12 29 22356 11640 64464707
Infection 32.11 16.12 12 22373 184868 64291479
Sinusitis 31.89 16.12 6 22379 145922 64330425
Glomerular filtration rate abnormal 31.55 16.12 13 22372 1246 64475101
Ventricular fibrillation 31.30 16.12 40 22345 23820 64452527
Ventricular hypokinesia 31.17 16.12 24 22361 7745 64468602
Venous pressure jugular decreased 30.84 16.12 7 22378 84 64476263
Pyonephrosis 30.54 16.12 7 22378 88 64476259
Hypersensitivity 30.53 16.12 15 22370 196437 64279910
Pleural effusion 30.52 16.12 105 22280 126454 64349893
Stenosis 30.05 16.12 14 22371 1801 64474546
Cardiac ventricular thrombosis 30.04 16.12 13 22372 1407 64474940
Superinfection 30.00 16.12 18 22367 3868 64472479
Angina pectoris 29.82 16.12 55 22330 45026 64431321
Back pain 29.56 16.12 26 22359 250145 64226202
Blood thyroid stimulating hormone increased 29.31 16.12 23 22362 7631 64468716
Degenerative aortic valve disease 28.97 16.12 7 22378 112 64476235
Arthropathy 28.61 16.12 4 22381 120963 64355384
Alopecia 28.36 16.12 11 22374 165679 64310668
Pulmonary congestion 28.17 16.12 38 22347 23842 64452505
Chronic kidney disease 27.97 16.12 62 22323 57857 64418490
Cardiovascular insufficiency 27.94 16.12 15 22370 2609 64473738
Atrial flutter 27.84 16.12 34 22351 19346 64457001
Myocardial ischaemia 27.43 16.12 37 22348 23214 64453133
Product prescribing error 27.17 16.12 46 22339 35223 64441124
Seizure 27.08 16.12 12 22373 166880 64309467
Musculoskeletal stiffness 27.06 16.12 5 22380 123201 64353146
Mitral valve calcification 27.00 16.12 12 22373 1384 64474963
Subclavian vein thrombosis 26.82 16.12 14 22371 2300 64474047
Dehydration 26.82 16.12 147 22238 216616 64259731
Drug ineffective 26.54 16.12 177 22208 840070 63636277
Arterial intramural haematoma 26.28 16.12 6 22379 74 64476273
Subdural haematoma 26.28 16.12 40 22345 28014 64448333
Atrial tachycardia 26.22 16.12 16 22369 3543 64472804
Asthma-chronic obstructive pulmonary disease overlap syndrome 26.12 16.12 11 22374 1114 64475233
Atrial thrombosis 25.87 16.12 15 22370 3027 64473320
Hypotonia 25.41 16.12 25 22360 11187 64465160
Hydrothorax 24.94 16.12 11 22374 1246 64475101
Pain in extremity 24.72 16.12 42 22343 303043 64173304
Right ventricular dysfunction 24.60 16.12 13 22372 2190 64474157
Rash scarlatiniform 24.22 16.12 7 22378 229 64476118
Ascites 24.11 16.12 61 22324 61940 64414407
Non-compaction cardiomyopathy 23.97 16.12 5 22380 39 64476308
Neutropenia 23.68 16.12 29 22356 239595 64236752
Right ventricular failure 23.57 16.12 33 22352 21438 64454909
Blood lactic acid 23.42 16.12 8 22377 455 64475892
Drug hypersensitivity 23.27 16.12 29 22356 237786 64238561
White blood cell count decreased 23.12 16.12 13 22372 157824 64318523
Injection site pain 21.51 16.12 6 22379 111402 64364945
Haematochezia 21.47 16.12 61 22324 66312 64410035
Headache 21.28 16.12 103 22282 529364 63946983
Acute pulmonary oedema 20.92 16.12 24 22361 12785 64463562
Lung consolidation 20.82 16.12 19 22366 7739 64468608
Femoral neck fracture 20.79 16.12 20 22365 8704 64467643
Sinus bradycardia 20.54 16.12 32 22353 22861 64453486
Cardiac dysfunction 20.45 16.12 13 22372 3093 64473254
Bronchial hyperreactivity 20.34 16.12 12 22373 2500 64473847
Adrenocortical insufficiency acute 20.11 16.12 12 22373 2553 64473794
Dyspnoea paroxysmal nocturnal 20.07 16.12 11 22374 1993 64474354
Hepatic enzyme increased 20.06 16.12 10 22375 129933 64346414
Aortic valve incompetence 19.73 16.12 19 22366 8282 64468065
Hypertrophy 19.56 16.12 8 22377 752 64475595
Vascular stent thrombosis 19.50 16.12 13 22372 3351 64472996
Cardiac murmur 19.45 16.12 22 22363 11541 64464806
Drug intolerance 19.37 16.12 22 22363 187970 64288377
Renal atrophy 19.10 16.12 10 22375 1654 64474693
Supraventricular extrasystoles 18.91 16.12 16 22369 5899 64470448
Heart rate irregular 18.83 16.12 34 22351 27379 64448968
Coma 18.31 16.12 4 22381 87611 64388736
Glycosylated haemoglobin increased 18.15 16.12 25 22360 15994 64460353
Hypothyroidism 18.08 16.12 42 22343 40415 64435932
Abdominal discomfort 18.07 16.12 22 22363 182300 64294047
Sudden cardiac death 18.03 16.12 14 22371 4573 64471774
Treatment failure 18.02 16.12 9 22376 116807 64359540
Deep vein thrombosis 17.96 16.12 7 22378 105175 64371172
Product monitoring error 17.95 16.12 15 22370 5439 64470908
Blood cyanide increased 17.94 16.12 4 22381 44 64476303
Urticaria 17.76 16.12 15 22370 147302 64329045
Anaemia 17.68 16.12 205 22180 378475 64097872
Blood potassium abnormal 17.60 16.12 11 22374 2541 64473806
Inflammatory marker increased 17.60 16.12 18 22367 8433 64467914
Limited symptom panic attack 17.47 16.12 4 22381 50 64476297
Heart rate abnormal 16.88 16.12 14 22371 5021 64471326
Brain natriuretic peptide abnormal 16.87 16.12 7 22378 683 64475664
Toxicity to various agents 16.84 16.12 67 22318 363446 64112901
Left atrial dilatation 16.79 16.12 11 22374 2755 64473592
Gastrointestinal haemorrhage 16.53 16.12 90 22295 132222 64344125
Gastric dilatation 16.20 16.12 8 22377 1170 64475177

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




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ 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
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 0025-1720 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 0185-5369 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 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 42291-455 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 59762-1720 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
EPLERENONE HUMAN PRESCRIPTION DRUG LABEL 1 60687-451 TABLET, FILM COATED 25 mg ORAL ANDA 27 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 66993-343 TABLET, FILM COATED 25 mg ORAL ANDA 26 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 66993-344 TABLET, FILM COATED 50 mg ORAL ANDA 26 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 69367-307 TABLET, COATED 25 mg ORAL ANDA 29 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 69367-308 TABLET, COATED 50 mg ORAL ANDA 29 sections
eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 70436-098 TABLET, FILM COATED 25 mg ORAL ANDA 26 sections
eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 70436-099 TABLET, FILM COATED 50 mg ORAL ANDA 26 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 71205-863 TABLET, COATED 25 mg ORAL ANDA 27 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 71205-864 TABLET, COATED 50 mg ORAL ANDA 27 sections