Eplerenone
A selective mineralocorticoid receptor antagonist used for heart failure after a heart attack and for hypertension, with few hormonal effects.
Drug card
- How it works
- Blocking aldosterone receptors, so sodium is lost and potassium kept
- Used for
- Heart failure with reduced EF after a heart attack
- High blood pressure
- Known for
- High potassium (hyperkalemia)
- Rise in creatinine and worse kidney function
- Its name
- -renone means a mineralocorticoid receptor antagonist
Study it as a flashcard, and it comes back before you forget it.
Mechanism of action
How does eplerenone work?
Binds the mineralocorticoid receptor and blocks aldosterone in the kidney, heart and vessels, binding glucocorticoid, progesterone and androgen receptors much less. Renin and aldosterone rise in response but do not overcome the block. CYP3A4 breaks it down, so strong CYP3A4 inhibitors are contraindicated.
Like other mineralocorticoid receptor antagonists: They bind to mineralocorticoid receptors in the late distal tubule and collecting duct and stop aldosterone from switching them on. Less sodium and water are reabsorbed while potassium is kept, so they are potassium-sparing diuretics. They also block aldosterone in the heart and blood vessels, and in heart failure with reduced ejection fraction they improve survival.
Uses
What is eplerenone used for?
- Heart failure with reduced EF after a heart attack
- High blood pressure
Side effects
Side effects of eplerenone
- High potassium (hyperkalemia)Known forSerious
- Rise in creatinine and worse kidney functionKnown forSerious
- Dizziness
- Headache
- Cough
- Difficulty sleeping
- Nausea and vomiting
- Low blood pressure and dehydration
- Gynecomastia (uncommon)
- Angioedema and rashSerious
Known for marks what an exam expects you to know it for.
Watch for
Cautions and what sets it apart
- Contraindicated if potassium is above 5.5 mmol/L at the start or creatinine clearance is 30 mL/min or less.
- Strong CYP3A4 inhibitors such as ketoconazole, clarithromycin or ritonavir are contraindicated.
- ACE inhibitors, ARBs and NSAIDs raise the risk of hyperkalemia.
- For hypertension it is not used in type 2 diabetes with microalbuminuria or with potassium supplements.
Good to know: More selective than spironolactone, so gynecomastia and menstrual effects are uncommon, but hyperkalemia remains the main risk.
Remember it
A way to remember it
Block aldosterone, keep potassium.
Aldosterone makes the kidney hold on to sodium and let potassium go. Blocking its receptor reverses this, so these diuretics spare potassium, and hyperkalemia is their main danger, above all alongside ACE inhibitors or ARBs.
Written for biofideX
Its name
-renone means mineralocorticoid receptor antagonist
Eplerenone and finerenone block the aldosterone (mineralocorticoid) receptor. Spironolactone, the oldest drug of the class, doesn't carry the stem.
- Every drug name stem
Its class
Mineralocorticoid receptor antagonists
Other mineralocorticoid receptor antagonists with a card:
Easily mixed up with loop diuretics and thiazide and thiazide-like diuretics.
Sources
Checked against
Written for biofideX in plain words, after checking these references:
- Eplerenone tablets: label (DailyMed)
- Eplerenone (NCI Thesaurus)
- About eplerenone (NHS)
- Side effects of eplerenone (NHS)
For learning pharmacology, not for treatment decisions: no doses are given, and a prescriber, pharmacist or the product's own label is the word on any one patient. Spotted a mistake? Tell us and we'll correct it.
Heart failure, rhythm and angina
Eplerenone is one of 10 drugs practiced together here: their classes, how they work, what they treat and what they're known for.
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