Details of the Drug

General Information of Drug (ID: DMF0NQR)

Drug Name
Eplerenone
Synonyms
Epoxymexrenone; Inspra; Selara; CGP-30083; Inspra (TN); SC-66110; Eplerenone (JAN/USAN/INN); Inspra, Epoxymexrenone, CGP30083, SC-66110,Eplerenone; 7alpha-methoxycarbonyl-3-oxo-9,11alpha-epoxy-17alpha-pregn-4-ene-21,17-carbolactone
Indication
Disease Entry ICD 11 Status REF
Heart failure BD10-BD13 Approved [1], [2]
Therapeutic Class
Antihypertensive Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 414.5
Topological Polar Surface Area (xlogp) 1.4
Rotatable Bond Count (rotbonds) 2
Hydrogen Bond Donor Count (hbonddonor) 0
Hydrogen Bond Acceptor Count (hbondacc) 6
ADMET Property
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [3]
Bioavailability
69% of drug becomes completely available to its intended biological destination(s) [4]
Elimination
3% of drug is excreted from urine in the unchanged form [3]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 1.723 micromolar/kg/day [5]
Chemical Identifiers
Formula
C24H30O6
IUPAC Name
methyl (1R,2S,9R,10R,11S,14R,15S,17R)-2,15-dimethyl-5,5'-dioxospiro[18-oxapentacyclo[8.8.0.01,17.02,7.011,15]octadec-6-ene-14,2'-oxolane]-9-carboxylate
Canonical SMILES
C[C@]12CCC(=O)C=C1C[C@H]([C@@H]3[C@]24[C@H](O4)C[C@]5([C@H]3CC[C@@]56CCC(=O)O6)C)C(=O)OC
InChI
InChI=1S/C24H30O6/c1-21-7-4-14(25)10-13(21)11-15(20(27)28-3)19-16-5-8-23(9-6-18(26)30-23)22(16,2)12-17-24(19,21)29-17/h10,15-17,19H,4-9,11-12H2,1-3H3/t15-,16+,17-,19+,21+,22+,23-,24-/m1/s1
InChIKey
JUKPWJGBANNWMW-VWBFHTRKSA-N
Cross-matching ID
PubChem CID
443872
ChEBI ID
CHEBI:31547
CAS Number
107724-20-9
DrugBank ID
DB00700
TTD ID
D0Q4SD
INTEDE ID
DR0592
ACDINA ID
D00235

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Mineralocorticoid receptor (MR) TT26PHO MCR_HUMAN Modulator [6]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [7]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Substrate [8]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Heart failure
ICD Disease Classification BD10-BD13
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Mineralocorticoid receptor (MR) DTT NR3C2 7.31E-01 -5.31E-04 -1.53E-03
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 8.58E-01 -3.73E-03 -1.00E-02
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 2.76E-01 -4.64E-01 -9.16E-01
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Eplerenone (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Arn-509 DMT81LZ Minor Increased metabolism of Eplerenone caused by Arn-509 mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [35]
Dronedarone DMA8FS5 Major Decreased metabolism of Eplerenone caused by Dronedarone mediated inhibition of CYP450 enzyme. Angina pectoris [BA40] [36]
Posaconazole DMUL5EW Major Decreased metabolism of Eplerenone caused by Posaconazole mediated inhibition of CYP450 enzyme. Aspergillosis [1F20] [37]
Dalfopristin DM4LTKV Major Decreased metabolism of Eplerenone caused by Dalfopristin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [36]
Clarithromycin DM4M1SG Major Decreased metabolism of Eplerenone caused by Clarithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [37]
Troleandomycin DMUZNIG Major Decreased metabolism of Eplerenone caused by Troleandomycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [37]
Telithromycin DMZ4P3A Major Decreased metabolism of Eplerenone caused by Telithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [37]
Cariprazine DMJYDVK Moderate Additive hypotensive effects by the combination of Eplerenone and Cariprazine. Bipolar disorder [6A60] [38]
Phenylbutazone DMAYL0T Moderate Antagonize the effect of Eplerenone when combined with Phenylbutazone. Chronic pain [MG30] [39]
Ketoprofen DMRKXPT Moderate Increased risk of hyperkalemia by the combination of Eplerenone and Ketoprofen. Chronic pain [MG30] [39]
Mifepristone DMGZQEF Major Decreased metabolism of Eplerenone caused by Mifepristone mediated inhibition of CYP450 enzyme. Cushing syndrome [5A70] [40]
Ivacaftor DMZC1HS Moderate Decreased metabolism of Eplerenone caused by Ivacaftor mediated inhibition of CYP450 enzyme. Cystic fibrosis [CA25] [41]
MK-8228 DMOB58Q Major Decreased metabolism of Eplerenone caused by MK-8228 mediated inhibition of CYP450 enzyme. Cytomegaloviral disease [1D82] [36]
Nefazodone DM4ZS8M Major Decreased metabolism of Eplerenone caused by Nefazodone mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [37]
Selegiline DM6034S Moderate Additive hypotensive effects by the combination of Eplerenone and Selegiline. Depression [6A70-6A7Z] [42]
Isocarboxazid DMAF1NB Moderate Additive hypotensive effects by the combination of Eplerenone and Isocarboxazid. Depression [6A70-6A7Z] [42]
Tranylcypromine DMGB5RE Moderate Additive hypotensive effects by the combination of Eplerenone and Tranylcypromine. Depression [6A70-6A7Z] [42]
OPC-34712 DMHG57U Moderate Additive hypotensive effects by the combination of Eplerenone and OPC-34712. Depression [6A70-6A7Z] [38]
Phenelzine DMHIDUE Moderate Additive hypotensive effects by the combination of Eplerenone and Phenelzine. Depression [6A70-6A7Z] [42]
Primidone DM0WX6I Minor Increased metabolism of Eplerenone caused by Primidone mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [35]
Stiripentol DMMSDOY Major Decreased metabolism of Eplerenone caused by Stiripentol mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [36]
Fosphenytoin DMOX3LB Minor Increased metabolism of Eplerenone caused by Fosphenytoin mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [35]
Rufinamide DMWE60C Moderate Increased metabolism of Eplerenone caused by Rufinamide mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [43]
Phenobarbital DMXZOCG Minor Increased metabolism of Eplerenone caused by Phenobarbital mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [35]
Mefenamic acid DMK7HFI Moderate Antagonize the effect of Eplerenone when combined with Mefenamic acid. Female pelvic pain [GA34] [39]
Itraconazole DMCR1MV Major Decreased metabolism of Eplerenone caused by Itraconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [37]
Miconazole DMPMYE8 Moderate Decreased metabolism of Eplerenone caused by Miconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [44]
Ketoconazole DMPZI3Q Major Decreased metabolism of Eplerenone caused by Ketoconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [37]
Boceprevir DMBSHMF Major Decreased metabolism of Eplerenone caused by Boceprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [37]
Telaprevir DMMRV29 Major Decreased metabolism of Eplerenone caused by Telaprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [37]
Rifampin DMA8J1G Minor Increased metabolism of Eplerenone caused by Rifampin mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [37]
Procarbazine DMIK367 Moderate Additive hypotensive effects by the combination of Eplerenone and Procarbazine. Hodgkin lymphoma [2B30] [42]
Delavirdine DM3NF5G Major Decreased metabolism of Eplerenone caused by Delavirdine mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [37]
Fosamprenavir DM4W9B3 Major Decreased metabolism of Eplerenone caused by Fosamprenavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [37]
Cobicistat DM6L4H2 Major Decreased metabolism of Eplerenone caused by Cobicistat mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [37]
Saquinavir DMG814N Major Decreased metabolism of Eplerenone caused by Saquinavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [37]
Etravirine DMGV8QU Moderate Increased metabolism of Eplerenone caused by Etravirine mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [45]
Amprenavir DMLMXE0 Major Decreased metabolism of Eplerenone caused by Amprenavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [37]
Darunavir DMN3GCH Major Decreased metabolism of Eplerenone caused by Darunavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [36]
Atazanavir DMSYRBX Major Decreased metabolism of Eplerenone caused by Atazanavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [37]
Eprosartan DM07K2I Moderate Increased risk of hyperkalemia by the combination of Eplerenone and Eprosartan. Hypertension [BA00-BA04] [36]
Captopril DM458UM Moderate Increased risk of hyperkalemia by the combination of Eplerenone and Captopril. Hypertension [BA00-BA04] [36]
TAK-491 DMCF6SX Moderate Increased risk of hyperkalemia by the combination of Eplerenone and TAK-491. Hypertension [BA00-BA04] [36]
Perindopril DMOPZDT Moderate Increased risk of hyperkalemia by the combination of Eplerenone and Perindopril. Hypertension [BA00-BA04] [36]
Quinapril DMR8H31 Moderate Increased risk of hyperkalemia by the combination of Eplerenone and Quinapril. Hypertension [BA00-BA04] [36]
Telmisartan DMS3GX2 Moderate Increased risk of hyperkalemia by the combination of Eplerenone and Telmisartan. Hypertension [BA00-BA04] [36]
Irbesartan DMTP1DC Moderate Increased risk of hyperkalemia by the combination of Eplerenone and Irbesartan. Hypertension [BA00-BA04] [36]
Lisinopril DMUOK4C Moderate Increased risk of hyperkalemia by the combination of Eplerenone and Lisinopril. Hypertension [BA00-BA04] [36]
Potassium chloride DMMTAJC Major Increased risk of hyperkalemia by the combination of Eplerenone and Potassium chloride. Hypo-kalaemia [5C77] [46]
Conivaptan DM1V329 Major Decreased metabolism of Eplerenone caused by Conivaptan mediated inhibition of CYP450 enzyme. Hypo-osmolality/hyponatraemia [5C72] [37]
Tolvaptan DMIWFRL Moderate Increased risk of hyperkalemia by the combination of Eplerenone and Tolvaptan. Hypo-osmolality/hyponatraemia [5C72] [47]
Meclofenamic acid DM05FXR Moderate Antagonize the effect of Eplerenone when combined with Meclofenamic acid. Inflammatory spondyloarthritis [FA92] [48]
Berotralstat DMWA2DZ Major Decreased metabolism of Eplerenone caused by Berotralstat mediated inhibition of CYP450 enzyme. Innate/adaptive immunodeficiency [4A00] [36]
Propiomazine DMKY8V1 Moderate Additive hypotensive effects by the combination of Eplerenone and Propiomazine. Insomnia [7A00-7A0Z] [38]
ITI-007 DMUQ1DO Moderate Additive hypotensive effects by the combination of Eplerenone and ITI-007. Insomnia [7A00-7A0Z] [38]
Crizotinib DM4F29C Major Decreased metabolism of Eplerenone caused by Crizotinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [36]
Brigatinib DM7W94S Moderate Increased metabolism of Eplerenone caused by Brigatinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [49]
Ceritinib DMB920Z Major Decreased metabolism of Eplerenone caused by Ceritinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [37]
PF-06463922 DMKM7EW Moderate Increased metabolism of Eplerenone caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [50]
Selpercatinib DMZR15V Moderate Decreased metabolism of Eplerenone caused by Selpercatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [43]
Idelalisib DM602WT Major Decreased metabolism of Eplerenone caused by Idelalisib mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [37]
IPI-145 DMWA24P Major Decreased metabolism of Eplerenone caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [36]
Dabrafenib DMX6OE3 Moderate Increased metabolism of Eplerenone caused by Dabrafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [43]
Exjade DMHPRWG Moderate Decreased metabolism of Eplerenone caused by Exjade mediated inhibition of CYP450 enzyme. Mineral absorption/transport disorder [5C64] [51]
Ozanimod DMT6AM2 Moderate Additive hypotensive effects by the combination of Eplerenone and Ozanimod. Multiple sclerosis [8A40] [42]
Modafinil DMYILBE Minor Increased metabolism of Eplerenone caused by Modafinil mediated induction of CYP450 enzyme. Narcolepsy [7A20] [52]
Promethazine DM6I5GR Moderate Additive hypotensive effects by the combination of Eplerenone and Promethazine. Nausea/vomiting [MD90] [38]
Netupitant DMEKAYI Major Decreased metabolism of Eplerenone caused by Netupitant mediated inhibition of CYP450 enzyme. Nausea/vomiting [MD90] [36]
Naproxen DMZ5RGV Moderate Antagonize the effect of Eplerenone when combined with Naproxen. Osteoarthritis [FA00-FA05] [39]
Aspirin DM672AH Moderate Antagonize the effect of Eplerenone when combined with Aspirin. Pain [MG30-MG3Z] [48]
Etodolac DM6WJO9 Moderate Antagonize the effect of Eplerenone when combined with Etodolac. Pain [MG30-MG3Z] [39]
Diflunisal DM7EN8I Moderate Antagonize the effect of Eplerenone when combined with Diflunisal. Pain [MG30-MG3Z] [39]
Ibuprofen DM8VCBE Moderate Antagonize the effect of Eplerenone when combined with Ibuprofen. Pain [MG30-MG3Z] [39]
Safinamide DM0YWJC Moderate Additive hypotensive effects by the combination of Eplerenone and Safinamide. Parkinsonism [8A00] [42]
Rasagiline DM3WKQ4 Moderate Additive hypotensive effects by the combination of Eplerenone and Rasagiline. Parkinsonism [8A00] [42]
Abametapir DM2RX0I Moderate Decreased metabolism of Eplerenone caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [53]
Lefamulin DME6G97 Moderate Decreased metabolism of Eplerenone caused by Lefamulin mediated inhibition of CYP450 enzyme. Pneumonia [CA40] [54]
Choline salicylate DM8P137 Moderate Antagonize the effect of Eplerenone when combined with Choline salicylate. Postoperative inflammation [1A00-CA43] [39]
Bromfenac DMKB79O Moderate Antagonize the effect of Eplerenone when combined with Bromfenac. Postoperative inflammation [1A00-CA43] [39]
Lonafarnib DMGM2Z6 Major Decreased metabolism of Eplerenone caused by Lonafarnib mediated inhibition of CYP450 enzyme. Premature ageing appearance [LD2B] [37]
Enzalutamide DMGL19D Minor Increased metabolism of Eplerenone caused by Enzalutamide mediated induction of CYP450 enzyme. Prostate cancer [2C82] [35]
Levomepromazine DMIKFEL Moderate Additive hypotensive effects by the combination of Eplerenone and Levomepromazine. Psychotic disorder [6A20-6A25] [38]
Temsirolimus DMS104F Moderate Increased plasma concentrations of Eplerenone and Temsirolimus due to competitive inhibition of the same metabolic pathway. Renal cell carcinoma [2C90] [55]
Salsalate DM13P4C Moderate Antagonize the effect of Eplerenone when combined with Salsalate. Rheumatoid arthritis [FA20] [39]
Meloxicam DM2AR7L Moderate Antagonize the effect of Eplerenone when combined with Meloxicam. Rheumatoid arthritis [FA20] [39]
Oxaprozin DM9UB0P Moderate Antagonize the effect of Eplerenone when combined with Oxaprozin. Rheumatoid arthritis [FA20] [39]
Flurbiprofen DMGN4BY Moderate Antagonize the effect of Eplerenone when combined with Flurbiprofen. Rheumatoid arthritis [FA20] [39]
Quetiapine DM1N62C Moderate Additive hypotensive effects by the combination of Eplerenone and Quetiapine. Schizophrenia [6A20] [38]
Mesoridazine DM2ZGAN Moderate Additive hypotensive effects by the combination of Eplerenone and Mesoridazine. Schizophrenia [6A20] [38]
Aripiprazole DM3NUMH Moderate Additive hypotensive effects by the combination of Eplerenone and Aripiprazole. Schizophrenia [6A20] [38]
Iloperidone DM6AUFY Moderate Additive hypotensive effects by the combination of Eplerenone and Iloperidone. Schizophrenia [6A20] [38]
Paliperidone DM7NPJS Moderate Additive hypotensive effects by the combination of Eplerenone and Paliperidone. Schizophrenia [6A20] [38]
Perphenazine DMA4MRX Moderate Additive hypotensive effects by the combination of Eplerenone and Perphenazine. Schizophrenia [6A20] [38]
Molindone DMAH70G Moderate Additive hypotensive effects by the combination of Eplerenone and Molindone. Schizophrenia [6A20] [38]
Thiothixene DMDINC4 Moderate Additive hypotensive effects by the combination of Eplerenone and Thiothixene. Schizophrenia [6A20] [38]
Trifluoperazine DMKBYWI Moderate Additive hypotensive effects by the combination of Eplerenone and Trifluoperazine. Schizophrenia [6A20] [38]
Risperidone DMN6DXL Moderate Additive hypotensive effects by the combination of Eplerenone and Risperidone. Schizophrenia [6A20] [38]
Amisulpride DMSJVAM Moderate Additive hypotensive effects by the combination of Eplerenone and Amisulpride. Schizophrenia [6A20] [38]
Asenapine DMSQZE2 Moderate Additive hypotensive effects by the combination of Eplerenone and Asenapine. Schizophrenia [6A20] [38]
Salicyclic acid DM2F8XZ Moderate Increased risk of hyperkalemia by the combination of Eplerenone and Salicyclic acid. Seborrhoeic dermatitis [EA81] [48]
Voxelotor DMCS6M5 Major Decreased metabolism of Eplerenone caused by Voxelotor mediated inhibition of CYP450 enzyme. Sickle-cell disorder [3A51] [36]
Telotristat ethyl DMDIYFZ Moderate Increased metabolism of Eplerenone caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [43]
Larotrectinib DM26CQR Moderate Decreased metabolism of Eplerenone caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [37]
Armodafinil DMGB035 Minor Increased metabolism of Eplerenone caused by Armodafinil mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [52]
LEE011 DMMX75K Major Decreased metabolism of Eplerenone caused by LEE011 mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [36]
Pitolisant DM8RFNJ Moderate Increased metabolism of Eplerenone caused by Pitolisant mediated induction of CYP450 enzyme. Somnolence [MG42] [43]
Fostamatinib DM6AUHV Moderate Decreased metabolism of Eplerenone caused by Fostamatinib mediated inhibition of CYP450 enzyme. Thrombocytopenia [3B64] [56]
Sirolimus DMGW1ID Moderate Increased plasma concentrations of Eplerenone and Sirolimus due to competitive inhibition of the same metabolic pathway. Transplant rejection [NE84] [55]
Tacrolimus DMZ7XNQ Moderate Increased plasma concentrations of Eplerenone and Tacrolimus due to competitive inhibition of the same metabolic pathway. Transplant rejection [NE84] [46]
Methdilazine DMAUHQX Moderate Additive hypotensive effects by the combination of Eplerenone and Methdilazine. Vasomotor/allergic rhinitis [CA08] [38]
Trimeprazine DMEMV9D Moderate Additive hypotensive effects by the combination of Eplerenone and Trimeprazine. Vasomotor/allergic rhinitis [CA08] [57]
Amiodarone DMUTEX3 Major Decreased metabolism of Eplerenone caused by Amiodarone mediated inhibition of CYP450 enzyme. Ventricular tachyarrhythmia [BC71] [36]
⏷ Show the Full List of 112 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
Hydrazine yellow E00409 164825 Colorant
Sodium lauryl sulfate E00464 3423265 Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Sunset yellow FCF E00255 17730 Colorant
Beta-D-lactose E00099 6134 Diluent; Dry powder inhaler carrier; Lyophilization aid
Carmellose sodium E00625 Not Available Disintegrant
Eisenoxyd E00585 56841934 Colorant
Ferric hydroxide oxide yellow E00539 23320441 Colorant
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Polysorbate 80 E00665 Not Available Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
Talc E00520 16211421 Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
Triacetin E00080 5541 Humectant; Plasticizing agent; Solvent
Vinylpyrrolidone E00668 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
⏷ Show the Full List of 14 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Eplerenone 25 mg tablet 25 mg Oral Tablet Oral
Eplerenone 50 mg tablet 50 mg Oral Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2876).
2 Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.
3 BDDCS applied to over 900 drugs
4 Critical Evaluation of Human Oral Bioavailability for Pharmaceutical Drugs by Using Various Cheminformatics Approaches
5 Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
6 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
7 Eplerenone: a selective aldosterone receptor antagonist for hypertension and heart failure. Heart Dis. 2003 Sep-Oct;5(5):354-63.
8 The relative role of CYP3A4 and CYP3A5 in eplerenone metabolism. Toxicol Lett. 2019 Oct 15;315:9-13.
9 Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
10 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
11 Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
12 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
13 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
14 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
15 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
16 The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
17 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
18 Drug related genetic polymorphisms affecting adverse reactions to methotrexate, vinblastine, doxorubicin and cisplatin in patients with urothelial cancer. J Urol. 2008 Dec;180(6):2389-95.
19 Human prostate CYP3A5: identification of a unique 5'-untranslated sequence and characterization of purified recombinant protein. Biochem Biophys Res Commun. 1999 Jul 14;260(3):676-81.
20 Polymorphisms in cytochrome P4503A5 (CYP3A5) may be associated with race and tumor characteristics, but not metabolism and side effects of tamoxifen in breast cancer patients. Cancer Lett. 2005 Jan 10;217(1):61-72.
21 Drug Interactions Flockhart Table
22 Induction of hepatic CYP2E1 by a subtoxic dose of acetaminophen in rats: increase in dichloromethane metabolism and carboxyhemoglobin elevation. Drug Metab Dispos. 2007 Oct;35(10):1754-8.
23 Urinary 6 beta-hydroxycortisol excretion in rheumatoid arthritis. Br J Rheumatol. 1997 Jan;36(1):54-8.
24 Clinical pharmacokinetics of imatinib. Clin Pharmacokinet. 2005;44(9):879-94.
25 Kinetics and regulation of cytochrome P450-mediated etoposide metabolism. Drug Metab Dispos. 2004 Sep;32(9):993-1000.
26 Differential mechanism-based inhibition of CYP3A4 and CYP3A5 by verapamil. Drug Metab Dispos. 2005 May;33(5):664-71.
27 Stimulation of testosterone production in rat Leydig cells by aldosterone is mineralocorticoid receptor mediated. Mol Cell Endocrinol. 2005 Nov 24;243(1-2):35-42.
28 Mineralocorticoid receptor-mediated inhibition of the hypothalamic-pituitary-adrenal axis in aged humans. J Gerontol A Biol Sci Med Sci. 2003 Oct;58(10):B900-5.
29 Characterization of rat brain aldosterone receptors reveals high affinity for corticosterone. Endocrinology. 1983 Dec;113(6):2043-51.
30 Biochemical mechanisms of New Molecular Entities (NMEs) approved by United States FDA during 2001-2004: mechanisms leading to optimal efficacy and ... Curr Top Med Chem. 2006;6(5):461-78.
31 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
32 ZK91587: a novel synthetic antimineralocorticoid displays high affinity for corticosterone (type I) receptors in the rat hippocampus. Life Sci. 1988;43(19):1537-43.
33 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 626).
34 Nonsteroidal antagonists of the mineralocorticoid receptor. Curr Opin Nephrol Hypertens. 2015 Sep;24(5):417-24.
35 Agencia Espaola de Medicamentos y Productos Sanitarios Healthcare "Centro de informacion online de medicamentos de la AEMPS - CIMA.".
36 Product Information. Inspra (eplerenone). Searle, Chicago, IL.
37 Cerner Multum, Inc. "Australian Product Information.".
38 Aronowitz JS, Chakos MH, Safferman AZ, Lieberman JA "Syncope associated with the combination of clozapine and enalapril." J Clin Psychopharmacol 14 (1994): 429-30. [PMID: 7884028]
39 Abdel-Haq B, Magagna A, Favilla S, Salvetti A "Hemodynamic and humoral interactions between perindopril and indomethacin in essential hypertensive subjects." J Cardiovasc Pharmacol 18 (1991): s33-6. [PMID: 1725198]
40 He K, Woolf TF, Hollenberg PF "Mechanism-based inactivation of cytochrome P-450-3A4 by mifepristone (RU486)." J Pharmacol Exp Ther 288 (1999): 791-7. [PMID: 9918590]
41 Product Information. Kalydeco (ivacaftor). Vertex Pharmaceuticals, Cambridge, MA.
42 Ban TA "Drug interactions with psychoactive drugs." Dis Nerv Syst 36 (1975): 164-6. [PMID: 1116424]
43 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
44 Product Information. ORAVIG (miconazole). Strativa Pharmaceuticals, a Division of Par Pharmaceuticals, Inc., Woodcliff Lake, NJ.
45 Product Information. Intelence (etravirine). Ortho Biotech Inc, Bridgewater, NJ.
46 Marcy TR, Ripley TL "Aldosterone antagonists in the treatment of heart failure." Am J Health Syst Pharm 63 (2006): 49-58. [PMID: 16373465]
47 Product Information. Samsca (tolvaptan). Otsuka American Pharmaceuticals Inc, Rockville, MD.
48 Radack KL, Deck CC, Bloomfield SS "Ibuprofen interferes with the efficacy of antihypertensive drugs: a randomized, double-blind, placebo-controlled trial of ibuprofen compared with acetaminophen." Ann Intern Med 107 (1987): 628-35. [PMID: 2889416]
49 Product Information. Alunbrig (brigatinib). Ariad Pharmaceuticals Inc, Cambridge, MA.
50 Product Information. Lorbrena (lorlatinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
51 Product Information. Exjade (deferasirox). Novartis Pharmaceuticals, East Hanover, NJ.
52 Doherty MM, Charman WN "The mucosa of the small intestine: how clinically relevant as an organ of drug metabolism?" Clin Pharmacokinet 41 (2002): 235-53. [PMID: 11978143]
53 Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
54 Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
55 Product Information. Prograf (tacrolimus). Fujisawa, Deerfield, IL.
56 Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.
57 Product Information. Clozaril (clozapine). Novartis Pharmaceuticals, East Hanover, NJ.