Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names


Austria: Inspra; Bulgaria: Inspra; Cyprus: Inspra; Czech Republic: Inspra; Denmark: Inspra; Estonia: Inspra; Finland: Inspra; France: Inspra; Germany: Inspra; Greece: Inspra; Hungary: Inspra; Ireland: Inspra; Latvia: Inspra; Lithuania: Inspra; Malta: Inspra; Netherlands: Inspra; Poland: Inspra; Portugal: Inovic, Inspra; Romania: Inspra; Slovakia: Inspra; Slovenia: Inspra; Spain: Elecor, Inspra; Sweden: Inspra; UK: Inspra.

North America

USA: Eplerenone, Inspra.

Latin America

Mexico: Inspra IC.


Japan: Selara.

Drug combinations


Eplerenone: C~24~H~30~O~6~. Mw: 414.49. (1) Pregn-4-ene-7,21-dicarboxylic acid, 9,11-epoxy-17-hydroxy-3-oxo-, γ-lactone, methyl ester, (7α,11α,17α)-; (2) 9,11α-Epoxy-17-hydroxy-3-oxo-17α-pregn-4-ene-7α,21-dicarboxylic acid, γ-lactone, methyl ester. CAS-107724-20-9 (1997).

Pharmacologic Category

Mineralocorticoid (Aldosterone) Receptor Antagonists. Potassium-sparing Diuretics. Selective Aldosterone Blocker. (ATC-Code: C03DA04).

Mechanism of action

A relatively selective competitive mineralocorticoid (aldosterone) receptor antagonist. Binds selectively to mineralocorticoid receptors and has low (less than 1%) affinity for glucocorticoid, progesterone, and androgen receptors. It is a competitive antagonist of aldosterone at mineralocorticoid receptors in the kidney, myocardium, salivary gland, GI tract, brain, and vasculature, and has been shown to inhibit the physiologic effects of aldosterone in these organs. Some of the antihypertensive effects of eplerenone may be related to restoration of endothelial function by increasing the release of nitric oxide, which results in vasodilation. Has been shown to produce sustained increases in plasma renin and serum aldosterone concentrations, reflecting the inhibition of the negative feedback of aldosterone on renin secretion. Appears to have cardioprotective effects in congestive heart failure and left ventricular dysfunction following MI. The cardioprotective action mechanism appears to be related more to the ability of the drug to competitively inhibit the pathophysiologic effects of aldosterone on the myocardium than to its hypotensive effects. Eplerenone reduces coronary vascular inflammation, risk of subsequent development of interstitial myocardial and coronary perivascular fibrosis, cardiac hypertrophy, and/or ventricular remodeling.

Therapeutic use

To reduce the risk of mortality following acute MI in clinically stable patients with left ventricular dysfunction (i.e. LVEF 40% or less) who have demonstrated clinical evidence of CHF. Used orally in the management of hypertension. May be used as monotherapy or in combination with other classes of antihypertensive agents (e.g. ACEIs, angiotensin II receptor antagonists, calcium-channel blocking agents, β-adrenergic blocking agents, thiazide diuretics).

Pregnancy and lactiation implications

No teratogenic effects seen in animal studies; however there are no adequate, well-controlled studies in pregnant women. Use during pregnancy only if potential benefit to the mother outweighs possible risk to the fetus. Not recommended during lactation.

Unlabeled use


Serum potassium concentrations >5.5 mEq/L at initiation of therapy. CrCl ≤30 mL/minute. Concomitant therapy with potent CYP3A4 inhibitors (e.g. ketoconazole, itraconazole, nefazodone, troleandomycin, clarithromycin, ritonavir, nelfinavir). In hypertensive patients with type 2 diabetes mellitus with microalbuminuria. In hypertensive patients with S~cr~>2 or 1.8 mg/dL in males or females, respectively. In hypertensive patients with CrCl <50 mL/minute. In hypertensive patients receiving potassium supplements or potassium-sparing diuretics (e.g. amiloride, spironolactone, triamterene).

Warnings and precautions

Hyperkalemia may cause serious, sometimes fatal, cardiac arrhythmias. Increased risk of hyperkalemia in impaired renal function or diabetes mellitus and in patients receiving concurrent agents affecting the renin-angiotensin-aldosterone system (e.g. ACE inhibitors, angiotensin II receptor antagonists). Use with caution in heart failure patients post-MI with diabetes (especially if patient has proteinuria); risk of hyperkalemia is increased. Use with caution in severe hepatic impairment, and in mild renal impairment; contraindicated with moderate-severe impairment. High potential for CYP interactions (dosage adjustment needed for patients on moderate CYP3A4 inhibitors).



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