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Identification
NameEplerenone
Accession NumberDB00700  (APRD00707)
TypeSmall Molecule
GroupsApproved
DescriptionEplerenone, an aldosterone receptor antagonist similar to spironolactone, has been shown to produce sustained increases in plasma renin and serum aldosterone, consistent with inhibition of the negative regulatory feedback of aldosterone on renin secretion. The resulting increased plasma renin activity and aldosterone circulating levels do not overcome the effects of eplerenone. Eplerenone selectively binds to recombinant human mineralocorticoid receptors relative to its binding to recombinant human glucocorticoid, progesterone and androgen receptors.
Structure
Thumb
Synonyms
Epoxymexrenone
Inspra
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
EplerenoneTablet, film coated25 mg/1OralGreenstone LLC2002-09-27Not applicableUs
EplerenoneTablet, film coated25 mg/1OralAvera Mc Kennan Hospital2015-06-17Not applicableUs
EplerenoneTablet, film coated50 mg/1OralGreenstone LLC2002-09-27Not applicableUs
InspraTablet, film coated50 mg/1OralG.D. Searle LLC Division of Pfizer Inc2002-09-27Not applicableUs
InspraTablet25 mg/1OralRebel Distributors Corp2002-09-27Not applicableUs
InspraTablet50 mgOralPfizer Canada Inc2009-05-05Not applicableCanada
InspraTablet, film coated25 mg/1OralG.D. Searle LLC Division of Pfizer Inc2002-09-27Not applicableUs
InspraTablet25 mgOralPfizer Canada Inc2009-05-08Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
EplerenoneTablet25 mg/1OralUpsher Smith Laboratories, Inc.2015-03-16Not applicableUs
EplerenoneTablet50 mg/1OralRebel Distributors Corp.2008-08-01Not applicableUs
EplerenoneTablet25 mg/1OralAmerican Health Packaging2015-09-01Not applicableUs
EplerenoneTablet50 mg/1OralUpsher Smith Laboratories, Inc.2015-03-16Not applicableUs
EplerenoneTablet25 mg/1OralPhysicians Total Care, Inc.2009-09-14Not applicableUs
EplerenoneTablet25 mg/1OralEon Labs, Inc.2008-08-01Not applicableUs
EplerenoneTablet25 mg/1OralApotex Corp2008-07-30Not applicableUs
EplerenoneTablet50 mg/1OralEon Labs, Inc.2008-08-01Not applicableUs
EplerenoneTablet50 mg/1OralApotex Corp2008-07-30Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII6995V82D0B
CAS number107724-20-9
WeightAverage: 414.4914
Monoisotopic: 414.204238692
Chemical FormulaC24H30O6
InChI KeyJUKPWJGBANNWMW-VWBFHTRKSA-N
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
IUPAC Name
methyl (1'R,2R,2'S,9'R,10'R,11'S,15'S,17'R)-2',15'-dimethyl-5,5'-dioxo-18'-oxaspiro[oxolane-2,14'-pentacyclo[8.8.0.0¹,¹⁷.0²,⁷.0¹¹,¹⁵]octadecan]-6'-ene-9'-carboxylate
SMILES
[H][C@@]12CC[C@@]3(CCC(=O)O3)[C@@]1(C)C[[email protected]]1O[C@@]11[C@@]2([H])[C@@H](CC2=CC(=O)CC[C@]12C)C(=O)OC
Pharmacology
IndicationFor improvement of survival of stable patients with left ventricular systolic dysfunction (ejection fraction <40%) and clinical evidence of congestive heart failure after an acute myocardial infarction.
Structured Indications
PharmacodynamicsEplerenone, an aldosterone receptor antagonist similar to spironolactone, has been shown to produce sustained increases in plasma renin and serum aldosterone, consistent with inhibition of the negative regulatory feedback of aldosterone on renin secretion. The resulting increased plasma renin activity and aldosterone circulating levels do not overcome the effects of eplerenone. Eplerenone selectively binds to recombinant human mineralocorticoid receptors relative to its binding to recombinant human glucocorticoid, progesterone and androgen receptors.
Mechanism of actionEplerenone binds to the mineralocorticoid receptor and thereby blocks the binding of aldosterone (component of the renin-angiotensin-aldosterone-system, or RAAS). Aldosterone synthesis, which occurs primarily in the adrenal gland, is modulated by multiple factors, including angiotensin II and non-RAAS mediators such as adrenocorticotropic hormone (ACTH) and potassium. Aldosterone binds to mineralocorticoid receptors in both epithelial (e.g., kidney) and nonepithelial (e.g., heart, blood vessels, and brain) tissues and increases blood pressure through induction of sodium reabsorption and possibly other mechanisms.
TargetKindPharmacological actionActionsOrganismUniProt ID
Mineralocorticoid receptorProteinyes
antagonist
HumanP08235 details
Related Articles
AbsorptionThe absolute bioavailability of eplerenone is unknown.
Volume of distribution
  • 43 to 90 L
Protein binding50%
Metabolism

Eplerenone is metabolized primarily by CYP3A4, however, no active metabolites have been identified in human plasma.

Route of eliminationNot Available
Half life4-6 hours
Clearance
  • Apparent plasma cl=10 L/hr
ToxicityThe most likely symptoms of human overdosage would be anticipated to be hypotension or hyperkalemia. However, no cases of human overdosage with eplerenone have been reported.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Eplerenone Action PathwayDrug actionSMP00135
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AcebutololThe risk or severity of adverse effects can be increased when Eplerenone is combined with Acebutolol.Approved
AceclofenacAceclofenac may decrease the antihypertensive activities of Eplerenone.Approved
AcetazolamideThe risk or severity of adverse effects can be increased when Eplerenone is combined with Acetazolamide.Approved, Vet Approved
AcetovanilloneAcetovanillone may decrease the antihypertensive activities of Eplerenone.Investigational
AcetyldigitoxinThe therapeutic efficacy of Acetyldigitoxin can be decreased when used in combination with Eplerenone.Approved
Acetylsalicylic acidAcetylsalicylic acid may decrease the antihypertensive activities of Eplerenone.Approved, Vet Approved
AdapaleneAdapalene may decrease the antihypertensive activities of Eplerenone.Approved
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Eplerenone.Approved
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Eplerenone.Approved, Illicit
AliskirenThe risk or severity of adverse effects can be increased when Eplerenone is combined with Aliskiren.Approved, Investigational
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Alphacetylmethadol is combined with Eplerenone.Experimental, Illicit
AmifostineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Amifostine.Approved, Investigational
AmilorideEplerenone may increase the hyperkalemic activities of Amiloride.Approved
AmiodaroneThe serum concentration of Eplerenone can be increased when it is combined with Amiodarone.Approved, Investigational
AmlodipineThe risk or severity of adverse effects can be increased when Amlodipine is combined with Eplerenone.Approved
Ammonium chlorideThe risk or severity of adverse effects can be increased when Eplerenone is combined with Ammonium chloride.Approved, Vet Approved
AmobarbitalAmobarbital may increase the hypotensive activities of Eplerenone.Approved, Illicit
Amphotericin BThe risk or severity of adverse effects can be increased when Eplerenone is combined with Amphotericin B.Approved, Investigational
Amyl NitriteThe risk or severity of adverse effects can be increased when Eplerenone is combined with Amyl Nitrite.Approved
AnisodamineAnisodamine may decrease the antihypertensive activities of Eplerenone.Investigational
AntipyrineAntipyrine may decrease the antihypertensive activities of Eplerenone.Approved
AnvirzelThe therapeutic efficacy of Anvirzel can be decreased when used in combination with Eplerenone.Investigational
ApomorphineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Apomorphine.Approved, Investigational
ApraclonidineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Apraclonidine.Approved
ApremilastApremilast may decrease the antihypertensive activities of Eplerenone.Approved, Investigational
AprepitantThe serum concentration of Eplerenone can be increased when it is combined with Aprepitant.Approved, Investigational
ArdeparinArdeparin may increase the hyperkalemic activities of Eplerenone.Approved, Withdrawn
AripiprazoleAripiprazole may increase the hypotensive activities of Eplerenone.Approved, Investigational
ArotinololThe risk or severity of adverse effects can be increased when Eplerenone is combined with Arotinolol.Approved
Arsenic trioxideThe risk or severity of adverse effects can be increased when Eplerenone is combined with Arsenic trioxide.Approved, Investigational
AtazanavirThe serum concentration of Eplerenone can be increased when it is combined with Atazanavir.Approved, Investigational
AtenololThe risk or severity of adverse effects can be increased when Atenolol is combined with Eplerenone.Approved
AtomoxetineThe serum concentration of Eplerenone can be increased when it is combined with Atomoxetine.Approved
AzapropazoneAzapropazone may decrease the antihypertensive activities of Eplerenone.Withdrawn
AzelastineAzelastine may decrease the antihypertensive activities of Eplerenone.Approved
Azilsartan medoxomilEplerenone may increase the hyperkalemic activities of Azilsartan medoxomil.Approved
BalsalazideBalsalazide may decrease the antihypertensive activities of Eplerenone.Approved, Investigational
BarbexacloneBarbexaclone may increase the hypotensive activities of Eplerenone.Experimental
BarbitalBarbital may increase the hypotensive activities of Eplerenone.Illicit
BarnidipineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Barnidipine.Approved
BemiparinBemiparin may increase the hyperkalemic activities of Eplerenone.Approved
BenazeprilEplerenone may increase the hyperkalemic activities of Benazepril.Approved, Investigational
BendroflumethiazideThe risk or severity of adverse effects can be increased when Bendroflumethiazide is combined with Eplerenone.Approved
BenoxaprofenBenoxaprofen may decrease the antihypertensive activities of Eplerenone.Withdrawn
BepridilThe risk or severity of adverse effects can be increased when Eplerenone is combined with Bepridil.Approved, Withdrawn
BetaxololThe risk or severity of adverse effects can be increased when Betaxolol is combined with Eplerenone.Approved
Betulinic AcidBetulinic Acid may decrease the antihypertensive activities of Eplerenone.Investigational
BexaroteneThe serum concentration of Eplerenone can be decreased when it is combined with Bexarotene.Approved, Investigational
BezitramideThe risk or severity of adverse effects can be increased when Bezitramide is combined with Eplerenone.Experimental, Illicit, Withdrawn
BisoprololThe risk or severity of adverse effects can be increased when Bisoprolol is combined with Eplerenone.Approved
BoceprevirThe serum concentration of Eplerenone can be increased when it is combined with Boceprevir.Approved
BortezomibThe serum concentration of Eplerenone can be increased when it is combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Eplerenone can be decreased when it is combined with Bosentan.Approved, Investigational
BretyliumThe risk or severity of adverse effects can be increased when Eplerenone is combined with Bretylium.Approved
BrimonidineThe risk or severity of adverse effects can be increased when Brimonidine is combined with Eplerenone.Approved
BromfenacBromfenac may decrease the antihypertensive activities of Eplerenone.Approved
BromocriptineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Bromocriptine.Approved, Investigational
BucillamineBucillamine may decrease the antihypertensive activities of Eplerenone.Investigational
BumetanideThe risk or severity of adverse effects can be increased when Eplerenone is combined with Bumetanide.Approved
BupivacaineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Bupivacaine.Approved, Investigational
BuprenorphineThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Eplerenone.Approved, Illicit, Investigational, Vet Approved
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Eplerenone.Approved, Illicit, Vet Approved
CanagliflozinCanagliflozin may increase the hyperkalemic activities of Eplerenone.Approved
CandesartanEplerenone may increase the hyperkalemic activities of Candesartan.Approved
CandoxatrilEplerenone may increase the hyperkalemic activities of Candoxatril.Experimental
CaptoprilEplerenone may increase the hyperkalemic activities of Captopril.Approved
CarbamazepineThe metabolism of Eplerenone can be increased when combined with Carbamazepine.Approved, Investigational
CarbetocinThe risk or severity of adverse effects can be increased when Eplerenone is combined with Carbetocin.Approved
CarfentanilThe risk or severity of adverse effects can be increased when Carfentanil is combined with Eplerenone.Illicit, Vet Approved
CarprofenCarprofen may decrease the antihypertensive activities of Eplerenone.Approved, Vet Approved, Withdrawn
CarteololThe risk or severity of adverse effects can be increased when Carteolol is combined with Eplerenone.Approved
CarvedilolThe risk or severity of adverse effects can be increased when Eplerenone is combined with Carvedilol.Approved, Investigational
CastanospermineCastanospermine may decrease the antihypertensive activities of Eplerenone.Experimental
CelecoxibCelecoxib may decrease the antihypertensive activities of Eplerenone.Approved, Investigational
CeritinibThe serum concentration of Eplerenone can be increased when it is combined with Ceritinib.Approved
CertoparinCertoparin may increase the hyperkalemic activities of Eplerenone.Approved
ChloroquineChloroquine may decrease the antihypertensive activities of Eplerenone.Approved, Vet Approved
ChlorothiazideThe risk or severity of adverse effects can be increased when Eplerenone is combined with Chlorothiazide.Approved, Vet Approved
ChlorpromazineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Chlorpromazine.Approved, Vet Approved
ChlorthalidoneThe risk or severity of adverse effects can be increased when Chlorthalidone is combined with Eplerenone.Approved
CilazaprilEplerenone may increase the hyperkalemic activities of Cilazapril.Approved
CilnidipineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Cilnidipine.Approved
ClarithromycinThe serum concentration of Eplerenone can be increased when it is combined with Clarithromycin.Approved
ClemastineThe serum concentration of Eplerenone can be increased when it is combined with Clemastine.Approved
ClevidipineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Clevidipine.Approved
ClofarabineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Clofarabine.Approved, Investigational
ClomipramineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Clomipramine.Approved, Vet Approved
ClonidineThe risk or severity of adverse effects can be increased when Clonidine is combined with Eplerenone.Approved
ClonixinClonixin may decrease the antihypertensive activities of Eplerenone.Approved
ClotrimazoleThe serum concentration of Eplerenone can be increased when it is combined with Clotrimazole.Approved, Vet Approved
ClozapineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Clozapine.Approved
CobicistatThe serum concentration of Eplerenone can be increased when it is combined with Cobicistat.Approved
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Eplerenone.Approved, Illicit
ConivaptanThe serum concentration of Eplerenone can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibThe serum concentration of Eplerenone can be increased when it is combined with Crizotinib.Approved
CurcuminCurcumin may decrease the antihypertensive activities of Eplerenone.Investigational
CyclosporineEplerenone may increase the hyperkalemic activities of Cyclosporine.Approved, Investigational, Vet Approved
CyclosporineThe serum concentration of Eplerenone can be increased when it is combined with Cyclosporine.Approved, Investigational, Vet Approved
D-LimoneneD-Limonene may decrease the antihypertensive activities of Eplerenone.Investigational
DabrafenibThe serum concentration of Eplerenone can be decreased when it is combined with Dabrafenib.Approved
DalteparinDalteparin may increase the hyperkalemic activities of Eplerenone.Approved
DapagliflozinThe risk or severity of adverse effects can be increased when Eplerenone is combined with Dapagliflozin.Approved
DarunavirThe serum concentration of Eplerenone can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Eplerenone can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Eplerenone can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe serum concentration of Eplerenone can be increased when it is combined with Delavirdine.Approved
DesfluraneThe risk or severity of adverse effects can be increased when Eplerenone is combined with Desflurane.Approved
DeslanosideThe therapeutic efficacy of Deslanoside can be decreased when used in combination with Eplerenone.Approved
DexamethasoneThe serum concentration of Eplerenone can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Eplerenone.Approved, Vet Approved
DextromoramideThe risk or severity of adverse effects can be increased when Dextromoramide is combined with Eplerenone.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Eplerenone.Approved, Illicit, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Dezocine is combined with Eplerenone.Approved
DiclofenacDiclofenac may decrease the antihypertensive activities of Eplerenone.Approved, Vet Approved
DiclofenamideThe risk or severity of adverse effects can be increased when Eplerenone is combined with Diclofenamide.Approved
DiflunisalDiflunisal may decrease the antihypertensive activities of Eplerenone.Approved
DigitoxinThe therapeutic efficacy of Digitoxin can be decreased when used in combination with Eplerenone.Approved
DigoxinThe therapeutic efficacy of Digoxin can be decreased when used in combination with Eplerenone.Approved
DihydrocodeineThe risk or severity of adverse effects can be increased when Dihydrocodeine is combined with Eplerenone.Approved, Illicit
DihydroergotamineThe serum concentration of Eplerenone can be increased when it is combined with Dihydroergotamine.Approved
DihydroetorphineThe risk or severity of adverse effects can be increased when Dihydroetorphine is combined with Eplerenone.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Dihydromorphine is combined with Eplerenone.Experimental, Illicit
DiltiazemThe serum concentration of Eplerenone can be increased when it is combined with Diltiazem.Approved
DinutuximabThe risk or severity of adverse effects can be increased when Eplerenone is combined with Dinutuximab.Approved
DiphenoxylateThe risk or severity of adverse effects can be increased when Diphenoxylate is combined with Eplerenone.Approved, Illicit
DipyridamoleThe risk or severity of adverse effects can be increased when Eplerenone is combined with Dipyridamole.Approved
DoxazosinThe risk or severity of adverse effects can be increased when Doxazosin is combined with Eplerenone.Approved
DoxycyclineThe serum concentration of Eplerenone can be increased when it is combined with Doxycycline.Approved, Investigational, Vet Approved
DPDPEThe risk or severity of adverse effects can be increased when DPDPE is combined with Eplerenone.Investigational
DronedaroneThe serum concentration of Eplerenone can be increased when it is combined with Dronedarone.Approved
DrospirenoneDrospirenone may increase the hyperkalemic activities of Eplerenone.Approved
DroxicamDroxicam may decrease the antihypertensive activities of Eplerenone.Approved
DuloxetineEplerenone may increase the orthostatic hypotensive activities of Duloxetine.Approved
DuvelisibDuvelisib may decrease the antihypertensive activities of Eplerenone.Investigational
E6201E6201 may decrease the antihypertensive activities of Eplerenone.Investigational
EbselenEbselen may decrease the antihypertensive activities of Eplerenone.Investigational
EfavirenzThe serum concentration of Eplerenone can be decreased when it is combined with Efavirenz.Approved, Investigational
EfonidipineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Efonidipine.Approved
EmpagliflozinThe risk or severity of adverse effects can be increased when Eplerenone is combined with Empagliflozin.Approved
EnalaprilEplerenone may increase the hyperkalemic activities of Enalapril.Approved, Vet Approved
EnalaprilatEplerenone may increase the hyperkalemic activities of Enalaprilat.Approved
EnoxaparinEnoxaparin may increase the hyperkalemic activities of Eplerenone.Approved
EnzalutamideThe serum concentration of Eplerenone can be decreased when it is combined with Enzalutamide.Approved
EpirizoleEpirizole may decrease the antihypertensive activities of Eplerenone.Approved
EpoprostenolThe risk or severity of adverse effects can be increased when Eplerenone is combined with Epoprostenol.Approved
EprosartanEplerenone may increase the hyperkalemic activities of Eprosartan.Approved
ErythromycinThe serum concentration of Eplerenone can be increased when it is combined with Erythromycin.Approved, Vet Approved
Eslicarbazepine acetateThe serum concentration of Eplerenone can be decreased when it is combined with Eslicarbazepine acetate.Approved
EsmololThe risk or severity of adverse effects can be increased when Esmolol is combined with Eplerenone.Approved
Etacrynic acidThe risk or severity of adverse effects can be increased when Eplerenone is combined with Etacrynic acid.Approved
EtanerceptEtanercept may decrease the antihypertensive activities of Eplerenone.Approved, Investigational
EthylmorphineThe risk or severity of adverse effects can be increased when Ethylmorphine is combined with Eplerenone.Approved, Illicit
EtodolacEtodolac may decrease the antihypertensive activities of Eplerenone.Approved, Investigational, Vet Approved
EtofenamateEtofenamate may decrease the antihypertensive activities of Eplerenone.Approved
EtoricoxibEtoricoxib may decrease the antihypertensive activities of Eplerenone.Approved, Investigational
EtorphineThe risk or severity of adverse effects can be increased when Etorphine is combined with Eplerenone.Illicit, Vet Approved
EtravirineThe serum concentration of Eplerenone can be decreased when it is combined with Etravirine.Approved
Evening primrose oilEvening primrose oil may decrease the antihypertensive activities of Eplerenone.Approved
exisulindexisulind may decrease the antihypertensive activities of Eplerenone.Investigational
FelodipineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Felodipine.Approved, Investigational
FenbufenFenbufen may decrease the antihypertensive activities of Eplerenone.Approved
FenoldopamThe risk or severity of adverse effects can be increased when Eplerenone is combined with Fenoldopam.Approved
FenoprofenFenoprofen may decrease the antihypertensive activities of Eplerenone.Approved
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Eplerenone.Approved, Illicit, Investigational, Vet Approved
FimasartanThe risk or severity of adverse effects can be increased when Eplerenone is combined with Fimasartan.Approved
FloctafenineFloctafenine may decrease the antihypertensive activities of Eplerenone.Approved, Withdrawn
FluconazoleThe serum concentration of Eplerenone can be increased when it is combined with Fluconazole.Approved
FlunixinFlunixin may decrease the antihypertensive activities of Eplerenone.Vet Approved
FlurbiprofenFlurbiprofen may decrease the antihypertensive activities of Eplerenone.Approved, Investigational
FluvoxamineThe serum concentration of Eplerenone can be increased when it is combined with Fluvoxamine.Approved, Investigational
ForasartanEplerenone may increase the hyperkalemic activities of Forasartan.Experimental
FosamprenavirThe serum concentration of Eplerenone can be increased when it is combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Eplerenone can be increased when it is combined with Fosaprepitant.Approved
FosinoprilEplerenone may increase the hyperkalemic activities of Fosinopril.Approved
FosphenytoinThe metabolism of Eplerenone can be increased when combined with Fosphenytoin.Approved
FurosemideThe risk or severity of adverse effects can be increased when Furosemide is combined with Eplerenone.Approved, Vet Approved
Fusidic AcidThe serum concentration of Eplerenone can be increased when it is combined with Fusidic Acid.Approved
GuanfacineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Guanfacine.Approved, Investigational
HalothaneThe risk or severity of adverse effects can be increased when Eplerenone is combined with Halothane.Approved, Vet Approved
HeparinHeparin may increase the hyperkalemic activities of Eplerenone.Approved, Investigational
HeroinThe risk or severity of adverse effects can be increased when Heroin is combined with Eplerenone.Approved, Illicit
HexobarbitalHexobarbital may increase the hypotensive activities of Eplerenone.Approved
HigenamineHigenamine may decrease the antihypertensive activities of Eplerenone.Investigational
HMPL-004HMPL-004 may decrease the antihypertensive activities of Eplerenone.Investigational
HydralazineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Hydralazine.Approved
HydrochlorothiazideThe risk or severity of adverse effects can be increased when Eplerenone is combined with Hydrochlorothiazide.Approved, Vet Approved
HydrocodoneThe risk or severity of adverse effects can be increased when Hydrocodone is combined with Eplerenone.Approved, Illicit
HydroflumethiazideThe risk or severity of adverse effects can be increased when Eplerenone is combined with Hydroflumethiazide.Approved
HydromorphoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Eplerenone.Approved, Illicit
IbuprofenIbuprofen may decrease the antihypertensive activities of Eplerenone.Approved
IbuproxamIbuproxam may decrease the antihypertensive activities of Eplerenone.Withdrawn
IcatibantIcatibant may decrease the antihypertensive activities of Eplerenone.Approved
IdelalisibThe serum concentration of Eplerenone can be increased when it is combined with Idelalisib.Approved
IloprostThe risk or severity of adverse effects can be increased when Eplerenone is combined with Iloprost.Approved, Investigational
ImatinibThe serum concentration of Eplerenone can be increased when it is combined with Imatinib.Approved
ImidaprilEplerenone may increase the hyperkalemic activities of Imidapril.Investigational
ImipramineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Imipramine.Approved
IndapamideThe risk or severity of adverse effects can be increased when Eplerenone is combined with Indapamide.Approved
IndinavirThe serum concentration of Eplerenone can be increased when it is combined with Indinavir.Approved
IndomethacinIndomethacin may decrease the antihypertensive activities of Eplerenone.Approved, Investigational
IndoprofenIndoprofen may decrease the antihypertensive activities of Eplerenone.Withdrawn
IndoraminThe risk or severity of adverse effects can be increased when Eplerenone is combined with Indoramin.Withdrawn
IrbesartanEplerenone may increase the hyperkalemic activities of Irbesartan.Approved, Investigational
IsavuconazoniumThe serum concentration of Eplerenone can be increased when it is combined with Isavuconazonium.Approved, Investigational
IsocarboxazidThe risk or severity of adverse effects can be increased when Eplerenone is combined with Isocarboxazid.Approved
IsofluraneThe risk or severity of adverse effects can be increased when Eplerenone is combined with Isoflurane.Approved, Vet Approved
Isosorbide DinitrateThe risk or severity of adverse effects can be increased when Eplerenone is combined with Isosorbide Dinitrate.Approved
Isosorbide MononitrateThe risk or severity of adverse effects can be increased when Eplerenone is combined with Isosorbide Mononitrate.Approved
IsoxicamIsoxicam may decrease the antihypertensive activities of Eplerenone.Withdrawn
IsoxsuprineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Isoxsuprine.Approved, Withdrawn
IsradipineThe serum concentration of Eplerenone can be increased when it is combined with Isradipine.Approved
ItraconazoleThe serum concentration of Eplerenone can be increased when it is combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Eplerenone can be increased when it is combined with Ivacaftor.Approved
KebuzoneKebuzone may decrease the antihypertensive activities of Eplerenone.Experimental
KetobemidoneThe risk or severity of adverse effects can be increased when Ketobemidone is combined with Eplerenone.Approved
KetoconazoleThe serum concentration of Eplerenone can be increased when it is combined with Ketoconazole.Approved, Investigational
KetoprofenKetoprofen may decrease the antihypertensive activities of Eplerenone.Approved, Vet Approved
KetorolacKetorolac may decrease the antihypertensive activities of Eplerenone.Approved
LabetalolThe risk or severity of adverse effects can be increased when Labetalol is combined with Eplerenone.Approved
LacidipineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Lacidipine.Approved
LeflunomideLeflunomide may decrease the antihypertensive activities of Eplerenone.Approved, Investigational
LercanidipineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Lercanidipine.Approved, Investigational
LevobunololThe risk or severity of adverse effects can be increased when Eplerenone is combined with Levobunolol.Approved
LevobupivacaineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Levobupivacaine.Approved
LevodopaEplerenone may increase the orthostatic hypotensive activities of Levodopa.Approved
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Levomethadyl Acetate is combined with Eplerenone.Approved
LevorphanolThe risk or severity of adverse effects can be increased when Levorphanol is combined with Eplerenone.Approved
LevosimendanThe risk or severity of adverse effects can be increased when Eplerenone is combined with Levosimendan.Approved, Investigational
LisinoprilEplerenone may increase the hyperkalemic activities of Lisinopril.Approved, Investigational
LisofyllineLisofylline may decrease the antihypertensive activities of Eplerenone.Investigational
LithiumThe serum concentration of Lithium can be increased when it is combined with Eplerenone.Approved
LofentanilThe risk or severity of adverse effects can be increased when Lofentanil is combined with Eplerenone.Illicit
LofexidineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Lofexidine.Approved, Investigational
LopinavirThe serum concentration of Eplerenone can be increased when it is combined with Lopinavir.Approved
LornoxicamLornoxicam may decrease the antihypertensive activities of Eplerenone.Approved
LosartanEplerenone may increase the hyperkalemic activities of Losartan.Approved
LovastatinThe serum concentration of Eplerenone can be increased when it is combined with Lovastatin.Approved, Investigational
LoxoprofenLoxoprofen may decrease the antihypertensive activities of Eplerenone.Approved
LuliconazoleThe serum concentration of Eplerenone can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Eplerenone can be increased when combined with Lumacaftor.Approved
LumiracoxibLumiracoxib may decrease the antihypertensive activities of Eplerenone.Approved, Investigational
Magnesium salicylateMagnesium salicylate may decrease the antihypertensive activities of Eplerenone.Approved
MannitolThe risk or severity of adverse effects can be increased when Eplerenone is combined with Mannitol.Approved, Investigational
MasoprocolMasoprocol may decrease the antihypertensive activities of Eplerenone.Approved
MecamylamineThe risk or severity of adverse effects can be increased when Mecamylamine is combined with Eplerenone.Approved
Meclofenamic acidMeclofenamic acid may decrease the antihypertensive activities of Eplerenone.Approved, Vet Approved
Mefenamic acidMefenamic acid may decrease the antihypertensive activities of Eplerenone.Approved
MeloxicamMeloxicam may decrease the antihypertensive activities of Eplerenone.Approved, Vet Approved
MesalazineMesalazine may decrease the antihypertensive activities of Eplerenone.Approved
MetamizoleMetamizole may decrease the antihypertensive activities of Eplerenone.Withdrawn
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Eplerenone.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Methadyl Acetate is combined with Eplerenone.Approved, Illicit
MethazolamideThe risk or severity of adverse effects can be increased when Eplerenone is combined with Methazolamide.Approved
MethohexitalMethohexital may increase the hypotensive activities of Eplerenone.Approved
MethyclothiazideThe risk or severity of adverse effects can be increased when Methyclothiazide is combined with Eplerenone.Approved
MethyldopaThe risk or severity of adverse effects can be increased when Eplerenone is combined with Methyldopa.Approved
MethylphenobarbitalMethylphenobarbital may increase the hypotensive activities of Eplerenone.Approved
MetipranololThe risk or severity of adverse effects can be increased when Eplerenone is combined with Metipranolol.Approved
MetolazoneThe risk or severity of adverse effects can be increased when Metolazone is combined with Eplerenone.Approved
MetoprololThe risk or severity of adverse effects can be increased when Metoprolol is combined with Eplerenone.Approved, Investigational
MifepristoneThe serum concentration of Eplerenone can be increased when it is combined with Mifepristone.Approved, Investigational
MinoxidilThe risk or severity of adverse effects can be increased when Minoxidil is combined with Eplerenone.Approved
MitotaneThe serum concentration of Eplerenone can be decreased when it is combined with Mitotane.Approved
MizoribineMizoribine may decrease the antihypertensive activities of Eplerenone.Investigational
ModafinilThe serum concentration of Eplerenone can be decreased when it is combined with Modafinil.Approved, Investigational
MoexiprilEplerenone may increase the hyperkalemic activities of Moexipril.Approved
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Eplerenone.Approved, Investigational
MoxonidineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Moxonidine.Approved
Mycophenolate mofetilMycophenolate mofetil may decrease the antihypertensive activities of Eplerenone.Approved, Investigational
Mycophenolic acidMycophenolic acid may decrease the antihypertensive activities of Eplerenone.Approved
NabiloneThe risk or severity of adverse effects can be increased when Eplerenone is combined with Nabilone.Approved, Investigational
NabumetoneNabumetone may decrease the antihypertensive activities of Eplerenone.Approved
NadololThe risk or severity of adverse effects can be increased when Eplerenone is combined with Nadolol.Approved
NadroparinNadroparin may increase the hyperkalemic activities of Eplerenone.Approved
NafamostatNafamostat may decrease the antihypertensive activities of Eplerenone.Investigational
NafcillinThe serum concentration of Eplerenone can be decreased when it is combined with Nafcillin.Approved
NaftifineNaftifine may decrease the antihypertensive activities of Eplerenone.Approved
NalbuphineThe risk or severity of adverse effects can be increased when Nalbuphine is combined with Eplerenone.Approved
NaproxenNaproxen may decrease the antihypertensive activities of Eplerenone.Approved, Vet Approved
NCX 4016NCX 4016 may decrease the antihypertensive activities of Eplerenone.Investigational
NebivololThe risk or severity of adverse effects can be increased when Eplerenone is combined with Nebivolol.Approved, Investigational
NefazodoneThe serum concentration of Eplerenone can be increased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Eplerenone can be increased when it is combined with Nelfinavir.Approved
NepafenacNepafenac may decrease the antihypertensive activities of Eplerenone.Approved
NesiritideThe risk or severity of adverse effects can be increased when Eplerenone is combined with Nesiritide.Approved, Investigational
NetupitantThe serum concentration of Eplerenone can be increased when it is combined with Netupitant.Approved
NevirapineThe serum concentration of Eplerenone can be increased when it is combined with Nevirapine.Approved
NicardipineThe risk or severity of adverse effects can be increased when Nicardipine is combined with Eplerenone.Approved
NicorandilNicorandil may increase the hypotensive activities of Eplerenone.Approved
NifedipineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Nifedipine.Approved
Niflumic AcidNiflumic Acid may decrease the antihypertensive activities of Eplerenone.Approved
NilotinibThe serum concentration of Eplerenone can be increased when it is combined with Nilotinib.Approved, Investigational
NilvadipineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Nilvadipine.Approved
NimesulideNimesulide may decrease the antihypertensive activities of Eplerenone.Approved, Withdrawn
NimodipineThe risk or severity of adverse effects can be increased when Nimodipine is combined with Eplerenone.Approved
NisoldipineThe risk or severity of adverse effects can be increased when Nisoldipine is combined with Eplerenone.Approved
NitrendipineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Nitrendipine.Approved
Nitric OxideThe risk or severity of adverse effects can be increased when Eplerenone is combined with Nitric Oxide.Approved
NitroaspirinNitroaspirin may decrease the antihypertensive activities of Eplerenone.Investigational
NitrofurantoinNitrofurantoin may increase the hyperkalemic activities of Eplerenone.Approved, Vet Approved
NitroglycerinThe risk or severity of adverse effects can be increased when Eplerenone is combined with Nitroglycerin.Approved, Investigational
NitroprussideThe risk or severity of adverse effects can be increased when Nitroprusside is combined with Eplerenone.Approved
NormethadoneThe risk or severity of adverse effects can be increased when Normethadone is combined with Eplerenone.Approved, Illicit
ObinutuzumabThe risk or severity of adverse effects can be increased when Eplerenone is combined with Obinutuzumab.Approved
OlaparibThe serum concentration of Eplerenone can be increased when it is combined with Olaparib.Approved
OlmesartanEplerenone may increase the hyperkalemic activities of Olmesartan.Approved, Investigational
OlopatadineOlopatadine may decrease the antihypertensive activities of Eplerenone.Approved
OlsalazineOlsalazine may decrease the antihypertensive activities of Eplerenone.Approved
OmapatrilatEplerenone may increase the hyperkalemic activities of Omapatrilat.Investigational
OpiumThe risk or severity of adverse effects can be increased when Opium is combined with Eplerenone.Approved, Illicit
OrgoteinOrgotein may decrease the antihypertensive activities of Eplerenone.Vet Approved
OsimertinibThe serum concentration of Eplerenone can be increased when it is combined with Osimertinib.Approved
OuabainThe therapeutic efficacy of Ouabain can be decreased when used in combination with Eplerenone.Approved
OxaprozinOxaprozin may decrease the antihypertensive activities of Eplerenone.Approved
OxprenololThe risk or severity of adverse effects can be increased when Eplerenone is combined with Oxprenolol.Approved
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Eplerenone.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Eplerenone.Approved, Investigational, Vet Approved
OxyphenbutazoneOxyphenbutazone may decrease the antihypertensive activities of Eplerenone.Withdrawn
PaclitaxelThe risk or severity of adverse effects can be increased when Eplerenone is combined with Paclitaxel.Approved, Vet Approved
PalbociclibThe serum concentration of Eplerenone can be increased when it is combined with Palbociclib.Approved
PapaverineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Papaverine.Approved
ParecoxibParecoxib may decrease the antihypertensive activities of Eplerenone.Approved
ParnaparinParnaparin may increase the hyperkalemic activities of Eplerenone.Approved
PenbutololThe risk or severity of adverse effects can be increased when Eplerenone is combined with Penbutolol.Approved, Investigational
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Eplerenone.Approved, Vet Approved
PentobarbitalThe metabolism of Eplerenone can be increased when combined with Pentobarbital.Approved, Vet Approved
PerindoprilEplerenone may increase the hyperkalemic activities of Perindopril.Approved
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Eplerenone.Approved
PhenelzineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Phenelzine.Approved
PhenobarbitalThe metabolism of Eplerenone can be increased when combined with Phenobarbital.Approved
PhenoxybenzamineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Phenoxybenzamine.Approved
PhentolamineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Phentolamine.Approved
PhenylbutazonePhenylbutazone may decrease the antihypertensive activities of Eplerenone.Approved, Vet Approved
PhenytoinThe metabolism of Eplerenone can be increased when combined with Phenytoin.Approved, Vet Approved
PimecrolimusPimecrolimus may decrease the antihypertensive activities of Eplerenone.Approved, Investigational
PindololThe risk or severity of adverse effects can be increased when Eplerenone is combined with Pindolol.Approved
PipamperoneThe risk or severity of adverse effects can be increased when Eplerenone is combined with Pipamperone.Approved
PirfenidonePirfenidone may decrease the antihypertensive activities of Eplerenone.Investigational
PiritramideThe risk or severity of adverse effects can be increased when Piritramide is combined with Eplerenone.Investigational
PiroxicamPiroxicam may decrease the antihypertensive activities of Eplerenone.Approved, Investigational
PosaconazoleThe serum concentration of Eplerenone can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PramipexoleThe risk or severity of adverse effects can be increased when Eplerenone is combined with Pramipexole.Approved, Investigational
PrazosinThe risk or severity of adverse effects can be increased when Prazosin is combined with Eplerenone.Approved
PrimidoneThe metabolism of Eplerenone can be increased when combined with Primidone.Approved, Vet Approved
PropacetamolPropacetamol may decrease the antihypertensive activities of Eplerenone.Approved
PropofolThe risk or severity of adverse effects can be increased when Eplerenone is combined with Propofol.Approved, Investigational, Vet Approved
PropranololThe risk or severity of adverse effects can be increased when Propranolol is combined with Eplerenone.Approved, Investigational
PTC299PTC299 may decrease the antihypertensive activities of Eplerenone.Investigational
QuetiapineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Quetiapine.Approved
QuinaprilEplerenone may increase the hyperkalemic activities of Quinapril.Approved, Investigational
QuinidineThe therapeutic efficacy of Quinidine can be decreased when used in combination with Eplerenone.Approved
RamiprilEplerenone may increase the hyperkalemic activities of Ramipril.Approved
RanolazineThe serum concentration of Eplerenone can be increased when it is combined with Ranolazine.Approved, Investigational
RasagilineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Rasagiline.Approved
RemifentanilThe risk or severity of adverse effects can be increased when Remifentanil is combined with Eplerenone.Approved
RescinnamineEplerenone may increase the hyperkalemic activities of Rescinnamine.Approved
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Eplerenone.Approved
ResveratrolResveratrol may decrease the antihypertensive activities of Eplerenone.Experimental, Investigational
ReviparinReviparin may increase the hyperkalemic activities of Eplerenone.Approved
RifabutinThe metabolism of Eplerenone can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Eplerenone can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Eplerenone can be increased when combined with Rifapentine.Approved
RiociguatThe risk or severity of adverse effects can be increased when Eplerenone is combined with Riociguat.Approved
RisperidoneEplerenone may increase the hypotensive activities of Risperidone.Approved, Investigational
RitonavirThe serum concentration of Eplerenone can be increased when it is combined with Ritonavir.Approved, Investigational
RofecoxibRofecoxib may decrease the antihypertensive activities of Eplerenone.Investigational, Withdrawn
RopiniroleThe risk or severity of adverse effects can be increased when Eplerenone is combined with Ropinirole.Approved, Investigational
RopivacaineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Ropivacaine.Approved
RotigotineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Rotigotine.Approved
SacubitrilEplerenone may increase the hyperkalemic activities of Sacubitril.Approved
SalicylamideSalicylamide may decrease the antihypertensive activities of Eplerenone.Approved
Salicylic acidSalicylic acid may decrease the antihypertensive activities of Eplerenone.Approved, Vet Approved
SalsalateSalsalate may decrease the antihypertensive activities of Eplerenone.Approved
SaprisartanEplerenone may increase the hyperkalemic activities of Saprisartan.Experimental
SaquinavirThe serum concentration of Eplerenone can be increased when it is combined with Saquinavir.Approved, Investigational
SaralasinEplerenone may increase the hyperkalemic activities of Saralasin.Investigational
SecobarbitalSecobarbital may increase the hypotensive activities of Eplerenone.Approved, Vet Approved
SelegilineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Selegiline.Approved, Investigational, Vet Approved
SeratrodastSeratrodast may decrease the antihypertensive activities of Eplerenone.Approved, Investigational
SevofluraneThe risk or severity of adverse effects can be increased when Eplerenone is combined with Sevoflurane.Approved, Vet Approved
SildenafilThe serum concentration of Eplerenone can be increased when it is combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Eplerenone can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Eplerenone can be increased when it is combined with Simeprevir.Approved
Sodium NitriteThe risk or severity of adverse effects can be increased when Eplerenone is combined with Sodium Nitrite.Approved
SotalolThe risk or severity of adverse effects can be increased when Sotalol is combined with Eplerenone.Approved
SpiraprilEplerenone may increase the hyperkalemic activities of Spirapril.Approved
SpironolactoneEplerenone may increase the hyperkalemic activities of Spironolactone.Approved
SRT501SRT501 may decrease the antihypertensive activities of Eplerenone.Investigational
St. John's WortThe serum concentration of Eplerenone can be decreased when it is combined with St. John&#39;s Wort.Nutraceutical
StiripentolThe serum concentration of Eplerenone can be increased when it is combined with Stiripentol.Approved
StreptokinaseThe risk or severity of adverse effects can be increased when Eplerenone is combined with Streptokinase.Approved
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with Eplerenone.Approved, Investigational
SulfasalazineSulfasalazine may decrease the antihypertensive activities of Eplerenone.Approved
SulfisoxazoleThe serum concentration of Eplerenone can be increased when it is combined with Sulfisoxazole.Approved, Vet Approved
SulindacSulindac may decrease the antihypertensive activities of Eplerenone.Approved
SuprofenSuprofen may decrease the antihypertensive activities of Eplerenone.Approved, Withdrawn
TacrolimusEplerenone may increase the hyperkalemic activities of Tacrolimus.Approved, Investigational
TamsulosinThe risk or severity of adverse effects can be increased when Eplerenone is combined with Tamsulosin.Approved, Investigational
TapentadolThe risk or severity of adverse effects can be increased when Tapentadol is combined with Eplerenone.Approved
TasosartanEplerenone may increase the hyperkalemic activities of Tasosartan.Approved
TelaprevirThe serum concentration of Eplerenone can be increased when it is combined with Telaprevir.Approved
TelithromycinThe serum concentration of Eplerenone can be increased when it is combined with Telithromycin.Approved
TelmisartanEplerenone may increase the hyperkalemic activities of Telmisartan.Approved, Investigational
TemocaprilEplerenone may increase the hyperkalemic activities of Temocapril.Experimental, Investigational
TenoxicamTenoxicam may decrease the antihypertensive activities of Eplerenone.Approved
TepoxalinTepoxalin may decrease the antihypertensive activities of Eplerenone.Vet Approved
TerazosinThe risk or severity of adverse effects can be increased when Eplerenone is combined with Terazosin.Approved
TeriflunomideTeriflunomide may decrease the antihypertensive activities of Eplerenone.Approved
ThalidomideThe risk or severity of adverse effects can be increased when Eplerenone is combined with Thalidomide.Approved, Investigational, Withdrawn
ThiamylalThiamylal may increase the hypotensive activities of Eplerenone.Approved, Vet Approved
ThiopentalThiopental may increase the hypotensive activities of Eplerenone.Approved, Vet Approved
ThioridazineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Thioridazine.Approved
Tiaprofenic acidTiaprofenic acid may decrease the antihypertensive activities of Eplerenone.Approved
TiclopidineThe serum concentration of Eplerenone can be increased when it is combined with Ticlopidine.Approved
TimololThe risk or severity of adverse effects can be increased when Timolol is combined with Eplerenone.Approved
TinoridineTinoridine may decrease the antihypertensive activities of Eplerenone.Investigational
TinzaparinTinzaparin may increase the hyperkalemic activities of Eplerenone.Approved
TizanidineThe risk or severity of adverse effects can be increased when Tizanidine is combined with Eplerenone.Approved
TocilizumabThe serum concentration of Eplerenone can be decreased when it is combined with Tocilizumab.Approved
TolazolineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Tolazoline.Approved, Vet Approved
TolcaponeThe risk or severity of adverse effects can be increased when Eplerenone is combined with Tolcapone.Approved, Withdrawn
Tolfenamic AcidTolfenamic Acid may decrease the antihypertensive activities of Eplerenone.Approved
TolmetinTolmetin may decrease the antihypertensive activities of Eplerenone.Approved
TolvaptanTolvaptan may increase the hyperkalemic activities of Eplerenone.Approved
TorasemideThe risk or severity of adverse effects can be increased when Torasemide is combined with Eplerenone.Approved
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Eplerenone.Approved, Investigational
TrandolaprilEplerenone may increase the hyperkalemic activities of Trandolapril.Approved
TranilastTranilast may decrease the antihypertensive activities of Eplerenone.Approved, Investigational
TranylcypromineThe risk or severity of adverse effects can be increased when Eplerenone is combined with Tranylcypromine.Approved
TretinoinThe risk or severity of adverse effects can be increased when Eplerenone is combined with Tretinoin.Approved, Investigational, Nutraceutical
TriamtereneEplerenone may increase the hyperkalemic activities of Triamterene.Approved
TrimethoprimTrimethoprim may increase the hyperkalemic activities of Eplerenone.Approved, Vet Approved
Trisalicylate-cholineTrisalicylate-choline may decrease the antihypertensive activities of Eplerenone.Approved
ValdecoxibValdecoxib may decrease the antihypertensive activities of Eplerenone.Investigational, Withdrawn
ValsartanEplerenone may increase the hyperkalemic activities of Valsartan.Approved, Investigational
VenlafaxineThe serum concentration of Eplerenone can be increased when it is combined with Venlafaxine.Approved
VerapamilThe serum concentration of Eplerenone can be increased when it is combined with Verapamil.Approved
VoriconazoleThe serum concentration of Eplerenone can be increased when it is combined with Voriconazole.Approved, Investigational
ZaltoprofenZaltoprofen may decrease the antihypertensive activities of Eplerenone.Approved
ZileutonZileuton may decrease the antihypertensive activities of Eplerenone.Approved, Investigational, Withdrawn
ZiprasidoneThe serum concentration of Eplerenone can be increased when it is combined with Ziprasidone.Approved
ZomepiracZomepirac may decrease the antihypertensive activities of Eplerenone.Withdrawn
Food InteractionsNot Available
References
Synthesis Reference

Bhaskar Reddy Guntoori, Svetoslav S. Bratovanov, Mohamed Ibrahim Zaki, Elena Bejan, Stephen E. Horne, “Process for the preparation and purification of eplerenone.” U.S. Patent US20080234478, issued September 25, 2008.

US20080234478
General ReferencesNot Available
External Links
ATC CodesC03DA04
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (136 KB)
MSDSDownload (68.2 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9839
Blood Brain Barrier+0.8556
Caco-2 permeable+0.5076
P-glycoprotein substrateSubstrate0.7017
P-glycoprotein inhibitor IInhibitor0.8166
P-glycoprotein inhibitor IIInhibitor0.8066
Renal organic cation transporterNon-inhibitor0.7209
CYP450 2C9 substrateNon-substrate0.8229
CYP450 2D6 substrateNon-substrate0.9117
CYP450 3A4 substrateSubstrate0.7407
CYP450 1A2 substrateNon-inhibitor0.6978
CYP450 2C9 inhibitorNon-inhibitor0.7982
CYP450 2D6 inhibitorNon-inhibitor0.931
CYP450 2C19 inhibitorNon-inhibitor0.839
CYP450 3A4 inhibitorNon-inhibitor0.8368
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8902
Ames testNon AMES toxic0.7496
CarcinogenicityNon-carcinogens0.9441
BiodegradationNot ready biodegradable0.9891
Rat acute toxicity2.4761 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9453
hERG inhibition (predictor II)Non-inhibitor0.7742
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Apotex inc
  • Sandoz inc
  • Gd searle llc
Packagers
Dosage forms
FormRouteStrength
TabletOral50 mg/1
Tablet, film coatedOral25 mg/1
Tablet, film coatedOral50 mg/1
TabletOral25 mg/1
TabletOral25 mg
TabletOral50 mg
Prices
Unit descriptionCostUnit
Inspra 25 mg tablet4.87USD tablet
Inspra 50 mg tablet4.87USD tablet
Eplerenone 25 mg tablet4.18USD tablet
Eplerenone 50 mg tablet4.18USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6410054 Yes2000-06-082020-06-08Us
US6410524 Yes2000-05-052020-05-05Us
US6495165 Yes2000-06-082020-06-08Us
US6534093 Yes2000-06-082020-06-08Us
US6558707 Yes2000-06-082020-06-08Us
US6747020 Yes2000-05-052020-05-05Us
US6863902 No2000-10-102020-10-10Us
US7157101 Yes2000-06-082020-06-08Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilitySlightly solubleNot Available
logP1.3Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00903 mg/mLALOGPS
logP1.67ALOGPS
logP2.33ChemAxon
logS-4.7ALOGPS
pKa (Strongest Acidic)15.11ChemAxon
pKa (Strongest Basic)-4.2ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area82.2 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity106.68 m3·mol-1ChemAxon
Polarizability43.79 Å3ChemAxon
Number of Rings6ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as spironolactones and derivatives. These are steroid lactones with a structure based on the spironolactone skeleton.
KingdomOrganic compounds
Super ClassLipids and lipid-like molecules
ClassSteroids and steroid derivatives
Sub ClassSteroid lactones
Direct ParentSpironolactones and derivatives
Alternative Parents
Substituents
  • Spironolactone
  • Oxepane
  • Gamma butyrolactone
  • Dicarboxylic acid or derivatives
  • Methyl ester
  • Oxolane
  • Cyclic ketone
  • Lactone
  • Ketone
  • Carboxylic acid ester
  • Oxacycle
  • Organoheterocyclic compound
  • Ether
  • Oxirane
  • Dialkyl ether
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Carbonyl group
  • Aliphatic heteropolycyclic compound
Molecular FrameworkAliphatic heteropolycyclic compounds
External Descriptors

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Zinc ion binding
Specific Function:
Receptor for both mineralocorticoids (MC) such as aldosterone and glucocorticoids (GC) such as corticosterone or cortisol. Binds to mineralocorticoid response elements (MRE) and transactivates target genes. The effect of MC is to increase ion and water transport and thus raise extracellular fluid volume and blood pressure and lower potassium levels.
Gene Name:
NR3C2
Uniprot ID:
P08235
Molecular Weight:
107066.575 Da
References
  1. Moore TD, Nawarskas JJ, Anderson JR: Eplerenone: a selective aldosterone receptor antagonist for hypertension and heart failure. Heart Dis. 2003 Sep-Oct;5(5):354-63. [PubMed:14503934 ]
  2. Fraccarollo D, Galuppo P, Hildemann S, Christ M, Ertl G, Bauersachs J: Additive improvement of left ventricular remodeling and neurohormonal activation by aldosterone receptor blockade with eplerenone and ACE inhibition in rats with myocardial infarction. J Am Coll Cardiol. 2003 Nov 5;42(9):1666-73. [PubMed:14607457 ]
  3. Rogerson FM, Yao Y, Smith BJ, Fuller PJ: Differences in the determinants of eplerenone, spironolactone and aldosterone binding to the mineralocorticoid receptor. Clin Exp Pharmacol Physiol. 2004 Oct;31(10):704-9. [PubMed:15554912 ]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid 11-beta-monooxygenase activity
Specific Function:
Preferentially catalyzes the conversion of 11-deoxycorticosterone to aldosterone via corticosterone and 18-hydroxycorticosterone.
Gene Name:
CYP11B2
Uniprot ID:
P19099
Molecular Weight:
57559.62 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
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Drug created on June 13, 2005 07:24 / Updated on December 07, 2016 03:54