eplerenone Indications/Contra | FAERs | Orange Book | 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

Drug dosage:

DoseUnitRoute
50 mg O

Approvals:

DateAgencyCompanyOrphan
Sept. 27, 2002 FDA GD SEARLE LLC

FDA Adverse Event Reporting System

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
Acute kidney injury 864.82 47.44 243 963 70188 4567598
Hyperkalaemia 540.89 47.44 125 1081 15712 4622074
Hypotension 230.26 47.44 90 1116 67310 4570476
Cardiac failure 219.06 47.44 69 1137 27219 4610567
Cardiac failure chronic 175.45 47.44 32 1174 1190 4636596
Drug interaction 154.50 47.44 67 1139 64441 4573345
Ventricular tachycardia 113.54 47.44 31 1175 7333 4630453
Condition aggravated 102.81 47.44 49 1157 58122 4579664
Renal failure 102.07 47.44 44 1162 41325 4596461
Hyponatraemia 101.61 47.44 38 1168 24692 4613094
Blood potassium increased 95.30 47.44 25 1181 5070 4632716
Dehydration 85.05 47.44 39 1167 42251 4595535
Dyspnoea 81.52 47.44 57 1149 138928 4498858
Oedema peripheral 75.97 47.44 36 1170 41936 4595850
Syncope 67.70 47.44 31 1175 33364 4604422
Dizziness 65.59 47.44 44 1162 99827 4537959
Bradycardia 65.52 47.44 27 1179 22542 4615244
Fall 65.12 47.44 40 1166 78006 4559780
Eosinophilia 61.27 47.44 19 1187 6974 4630812
Gynaecomastia 61.00 47.44 15 1191 2340 4635446
Blood creatinine increased 60.95 47.44 27 1179 26873 4610913
Renal impairment 59.23 47.44 26 1180 25312 4612474
Blood lactic acid 58.41 47.44 8 1198 41 4637745
Diarrhoea 57.83 47.44 48 1158 150137 4487649
Atrial fibrillation 57.10 47.44 27 1179 31188 4606598
Drug ineffective 54.70 47.44 51 1155 186010 4451776
Acute pulmonary oedema 49.40 47.44 13 1193 2656 4635130
Arterial intramural haematoma 48.09 47.44 6 1200 12 4637774

Pharmacologic Action:

SourceCodeDescription
ATC C03DA04 CARDIOVASCULAR SYSTEM
DIURETICS
POTASSIUM-SPARING AGENTS
Aldosterone antagonists
FDA EPC N0000175557 Aldosterone Antagonist
FDA MoA N0000011310 Aldosterone Antagonists
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 agent

Drug Use (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

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

External reference:

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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Inspra HUMAN PRESCRIPTION DRUG LABEL 1 0025-1710 TABLET, FILM COATED 25 mg ORAL NDA 17 sections
Inspra HUMAN PRESCRIPTION DRUG LABEL 1 0025-1720 TABLET, FILM COATED 50 mg ORAL NDA 17 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 0185-5368 TABLET 25 mg ORAL ANDA 16 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 0185-5369 TABLET 50 mg ORAL ANDA 16 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 0378-1030 TABLET, FILM COATED 25 mg ORAL ANDA 16 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 0378-1031 TABLET, FILM COATED 50 mg ORAL ANDA 16 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 0832-0480 TABLET 25 mg ORAL ANDA 16 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 0832-0481 TABLET 50 mg ORAL ANDA 16 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 16729-293 TABLET, FILM COATED 25 mg ORAL ANDA 17 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 16729-294 TABLET, FILM COATED 50 mg ORAL ANDA 17 sections
Inspra HUMAN PRESCRIPTION DRUG LABEL 1 21695-797 TABLET 25 mg ORAL NDA 17 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 42254-011 TABLET 50 mg ORAL ANDA 16 sections
EPLERENONE HUMAN PRESCRIPTION DRUG LABEL 1 51991-877 TABLET, FILM COATED 25 mg ORAL ANDA 17 sections
EPLERENONE HUMAN PRESCRIPTION DRUG LABEL 1 51991-878 TABLET, FILM COATED 50 mg ORAL ANDA 17 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 54868-6065 TABLET 25 mg ORAL ANDA 16 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 59762-1710 TABLET, FILM COATED 25 mg ORAL NDA AUTHORIZED GENERIC 17 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 59762-1720 TABLET, FILM COATED 50 mg ORAL NDA AUTHORIZED GENERIC 17 sections
EPLERENONE HUMAN PRESCRIPTION DRUG LABEL 1 60687-451 TABLET, FILM COATED 25 mg ORAL ANDA 17 sections
Eplerenone HUMAN PRESCRIPTION DRUG LABEL 1 68084-948 TABLET 25 mg ORAL ANDA 17 sections