Eplerenone

Eplerenone Brand Name– Inspra

What is Eplerenone

Eplerenone is a selective aldosterone receptor antagonist (SARA).

While similar in action to spironolactone at the aldosterone receptor, eplerenone has a lower incidence of endocrine related side effects due to its reduced affinity for glucocorticoid, androgen, and progesterone receptors.

Eplerenone is metabolized by CYP3A4 and is subject to many drug interactions that increase the likelihood of developing hyperkalemia, the principal risk associated with eplerenone use.

Eplerenone is used to treat hypertension, and is also used for the management of congestive heart failure.

In the EPHESUS trial, the addition of eplerenone to standard medical therapy has been shown to reduce all-cause mortality (by 15%) for patients with acute myocardial infarction complicated by left ventricular dysfunction and heart failure.

Eplerenone was approved by the FDA in September 2002 for the treatment of hypertension.

The FDA later approved eplerenone for the treatment of heart failure in post-myocardial infarction patients in October 2003

Indications

  1. heart failure
  2. hypertension
  3. reduction of cardiovascular mortality

For the treatment of hypertension, either as monotherapy or in combination with other antihypertensive agents

Side Effects

  1. abdominal pain
  2. amenorrhea
  3. angina
  4. bradycardia
  5. cough
  6. diarrhea
  7. dizziness
  8. edema
  9. elevated hepatic enzymes
  10. fatigue
  11. gynecomastia
  12. headache
  13. hirsutism
  14. hypercholesterolemia
  15. hyperkalemia
  16. hypertriglyceridemia
  17. hyperuricemia
  18. hyponatremia
  19. infertility
  20. mastalgia
  21. menstrual irregularity
  22. muscle paralysis
  23. myocardial infarction
  24. paresthesias
  25. postmenopausal bleeding
  26. rash
  27. vaginal bleeding
  28. weakness

Monitoring Parameters

  • blood pressure
  • serum creatinine/BUN
  • serum electrolytes

Contraindications

  • breast-feeding
  • children
  • diabetes mellitus
  • driving or operating machinery
  • geriatric
  • hepatic disease
  • hyperkalemia
  • infants
  • infertility
  • neonates
  • pregnancy
  • proteinuria
  • renal disease
  • renal failure
  • renal impairment
  • reproductive risk

Interactions

  • Acetaminophen; Dichloralphenazone; Isometheptene
  • Aldesleukin, IL-2
  • Alemtuzumab
  • Alfentanil
  • Aliskiren; Amlodipine
  • Aliskiren; Amlodipine; Hydrochlorothiazide, HCTZ
  • Aliskiren; Valsartan
  • Alprostadil
  • Ambrisentan
  • Amifostine
  • Amiloride
  • Amiloride; Hydrochlorothiazide, HCTZ
  • Amiodarone
  • Amlodipine
  • Amlodipine; Atorvastatin
  • Amlodipine; Benazepril
  • Amlodipine; Celecoxib
  • Amlodipine; Hydrochlorothiazide, HCTZ; Olmesartan
  • Amlodipine; Hydrochlorothiazide, HCTZ; Valsartan
  • Amlodipine; Olmesartan
  • Amlodipine; Telmisartan
  • Amlodipine; Valsartan
  • Amobarbital
  • Amoxicillin; Clarithromycin; Lansoprazole
  • Amoxicillin; Clarithromycin; Omeprazole
  • Amphetamine; Dextroamphetamine Salts
  • Amyl Nitrite
  • Angiotensin II receptor antagonists
  • Angiotensin-converting enzyme inhibitors
  • Apomorphine
  • Apraclonidine
  • Aprepitant, Fosaprepitant
  • Aripiprazole
  • Asenapine
  • Atazanavir
  • Atazanavir; Cobicistat
  • Azilsartan
  • Azilsartan; Chlorthalidone
  • Baclofen
  • Benazepril
  • Benazepril; Hydrochlorothiazide, HCTZ
  • Benzphetamine
  • Boceprevir
  • Bortezomib
  • Bosentan
  • Candesartan
  • Candesartan; Hydrochlorothiazide, HCTZ
  • Captopril
  • Captopril; Hydrochlorothiazide, HCTZ
  • Carbidopa; Levodopa
  • Carbidopa; Levodopa; Entacapone
  • Cariprazine
  • Celecoxib
  • Ceritinib
  • Chloramphenicol
  • Chloroprocaine
  • Ciprofloxacin
  • Citric Acid; Potassium Citrate
  • Citric Acid; Potassium Citrate; Sodium Citrate
  • Clarithromycin
  • Clozapine
  • Co-Enzyme Q10, Ubiquinone
  • Cobicistat
  • Cocaine
  • Conivaptan
  • Crizotinib
  • Cyclosporine
  • Dabrafenib
  • Danazol
  • Darunavir
  • Darunavir; Cobicistat
  • Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Delavirdine
  • Dexmethylphenidate
  • Dextromethorphan; Guaifenesin; Potassium Guaiacolsulfonate
  • Dextromethorphan; Quinidine
  • Diazoxide
  • Diclofenac
  • Diclofenac; Misoprostol
  • Diethylpropion
  • Diflunisal
  • Diltiazem
  • Diphenhydramine; Ibuprofen
  • Diphenhydramine; Naproxen
  • Dronedarone
  • Drospirenone
  • Drospirenone; Estradiol
  • Drospirenone; Ethinyl Estradiol
  • Drospirenone; Ethinyl Estradiol; Levomefolate
  • Duloxetine
  • Duvelisib
  • Efavirenz
  • Efavirenz; Emtricitabine; Tenofovir
  • Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
  • Enalapril, Enalaprilat
  • Enalapril; Felodipine
  • Enalapril; Hydrochlorothiazide, HCTZ
  • Encorafenib
  • Enflurane
  • Ephedrine
  • Epoprostenol
  • Eprosartan
  • Eprosartan; Hydrochlorothiazide, HCTZ
  • Erythromycin
  • Erythromycin; Sulfisoxazole
  • Esomeprazole; Naproxen
  • Etodolac
  • Etomidate
  • Famotidine; Ibuprofen
  • Fedratinib
  • Felodipine
  • Fenoprofen
  • Fish Oil, Omega-3 Fatty Acids (Dietary Supplements)
  • Fluconazole
  • Fluoxetine; Olanzapine
  • Flurbiprofen
  • Fluvoxamine
  • Fosamprenavir
  • Fosinopril
  • Fosinopril; Hydrochlorothiazide, HCTZ
  • Fospropofol
  • General anesthetics
  • grapefruit juice
  • Guaifenesin; Potassium Guaiacolsulfonate
  • Haloperidol
  • Halothane
  • Heparin
  • Hetastarch; Dextrose; Electrolytes
  • Hydralazine; Isosorbide Dinitrate, ISDN
  • Hydrochlorothiazide, HCTZ; Irbesartan
  • Hydrochlorothiazide, HCTZ; Lisinopril
  • Hydrochlorothiazide, HCTZ; Losartan
  • Hydrochlorothiazide, HCTZ; Moexipril
  • Hydrochlorothiazide, HCTZ; Olmesartan
  • Hydrochlorothiazide, HCTZ; Quinapril
  • Hydrochlorothiazide, HCTZ; Spironolactone
  • Hydrochlorothiazide, HCTZ; Telmisartan
  • Hydrochlorothiazide, HCTZ; Triamterene
  • Hydrochlorothiazide, HCTZ; Valsartan
  • Hydrocodone; Ibuprofen
  • Hydrocodone; Potassium Guaiacolsulfonate
  • Hydrocodone; Potassium Guaiacolsulfonate; Pseudoephedrine
  • Ibritumomab Tiuxetan
  • Ibuprofen
  • Ibuprofen; Oxycodone
  • Ibuprofen; Pseudoephedrine
  • Idelalisib
  • Iloperidone
  • Iloprost
  • Imatinib
  • Indinavir
  • Indomethacin
  • Intravenous Lipid Emulsions
  • Iodine; Potassium Iodide, KI
  • Irbesartan
  • Isavuconazonium
  • Isoflurane
  • Isoproterenol
  • Isosorbide Dinitrate, ISDN
  • Isosorbide Mononitrate
  • Isradipine
  • Itraconazole
  • Ketamine
  • Ketoconazole
  • Ketoprofen
  • Ketorolac
  • Lansoprazole; Naproxen
  • Lefamulin
  • Lesinurad
  • Lesinurad; Allopurinol
  • Letermovir
  • Levodopa
  • Lisdexamfetamine
  • Lisinopril
  • Lithium
  • Lopinavir; Ritonavir
  • Losartan
  • Lovastatin; Niacin
  • Lumacaftor; Ivacaftor
  • Lumacaftor; Ivacaftor
  • Lurasidone
  • Meclofenamate Sodium
  • Mefenamic Acid
  • Meloxicam
  • Methamphetamine
  • Methohexital
  • Methylphenidate
  • Mifepristone
  • Milrinone
  • Mitotane
  • Moexipril
  • Monoamine oxidase inhibitors
  • Nabumetone
  • Naproxen
  • Naproxen; Pseudoephedrine
  • Naproxen; Sumatriptan
  • Nebivolol; Valsartan
  • Nefazodone
  • Nelfinavir
  • Nesiritide, BNP
  • Netupitant, Fosnetupitant; Palonosetron
  • Niacin, Niacinamide
  • Niacin; Simvastatin
  • Nicardipine
  • Nifedipine
  • Nilotinib
  • Nimodipine
  • Nisoldipine
  • Nitrates
  • Nitroglycerin
  • Nitroprusside
  • Nonsteroidal antiinflammatory drugs
  • Olanzapine
  • Olmesartan
  • Ombitasvir; Paritaprevir; Ritonavir
  • Oritavancin
  • Oxaprozin
  • Oxymetazoline
  • Paliperidone
  • Penicillin G
  • Pentoxifylline
  • Perindopril
  • Perindopril; Amlodipine
  • Piroxicam
  • Posaconazole
  • Potassium
  • Potassium Acetate
  • Potassium Bicarbonate
  • Potassium Chloride
  • Potassium Citrate
  • Potassium Gluconate
  • Potassium Iodide, KI
  • Potassium Phosphate
  • Potassium Phosphate; Sodium Phosphate
  • Potassium-sparing diuretics
  • Prazosin
  • Procainamide
  • Procaine
  • Propofol
  • Quinapril
  • Quinidine
  • Quinine
  • Ramipril
  • Rasagiline
  • Ribociclib
  • Ribociclib; Letrozole
  • Risperidone
  • Ritonavir
  • Rofecoxib
  • Sacubitril; Valsartan
  • Saquinavir
  • Sevoflurane
  • Silodosin
  • Simeprevir
  • Spironolactone
  • St. John’s Wort, Hypericum perforatum
  • Sulfamethoxazole; Trimethoprim, SMX-TMP, Cotrimoxazole
  • Sulindac
  • Telithromycin
  • Telmisartan
  • Telotristat Ethyl
  • Tetrabenazine
  • Tetracaine
  • Thiopental
  • Thiothixene
  • Tipranavir
  • Tizanidine
  • Tolmetin
  • Trandolapril
  • Trandolapril; Verapamil
  • Trazodone
  • Triamterene
  • Trimethoprim
  • Tucatinib
  • Valdecoxib
  • Valsartan
  • Vemurafenib
  • Verapamil
  • Voriconazole
  • Yohimbine
  • Ziprasidone
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