A Comparison of the Aldosterone‐blocking Agents Eplerenone and Spironolactone

Abstract

Improved understanding of the adverse pharmacological properties of aldosterone has prompted investigation of the clinical benefits of blocking aldosterone at the receptor level. This article reviews the pharmacology, clinical efficacy, and tolerability of the two available blocking agents, spironolactone and eplerenone. A Medline search identified clinical studies assessing spironolactone and eplerenone. Priority was given to large, wellcontrolled, clinical trials and comparative studies. Pharmacological differences between spironolactone and eplerenone include lower affinity of eplerenone for progesterone, androgen, and glucocorticoid receptors; more consistently demonstrated nongenomic properties for eplerenone; and the presence of long-acting metabolites for spironolactone. Both agents effectively treat hypertension and heart failure but comparisons are complicated by the deficiency of head-to-head trials and differences between patient populations. There are differences in the tolerability profiles; spironolactone is associated with dose-dependent sexual side effects. Both agents produce dose-dependent increases in potassium concentrations, although the effect with spironolactone appears to be greater when both agents are administered at recommended doses. Choice of a specific agent should be based on individual patient issues, such as the nature of heart failure and patient concerns about adverse events.

Clinical effects of eplerenone, a selective aldosterone blocker, in Japanese patients with essential hypertension

“…When we combine these observations with the data from overseas and look at the influence of eplerenone on serum potassium levels at this dose, no dose-dependent changes in potassium levels are ever seen within this range. 21 White et al 17 conducted a placebocontrolled study to determine the antihypertensive effects of eplerenone at 25, 50, 100 and 200 mg per day in 310 patients with essential hypertension. After 12 weeks of treatment, one patient each from the placebo and eplerenone 200 mg groups developed hyperkalemia of X5.5 mEq l À1 , but the authors concluded that the increased dose of eplerenone was not associated with the serum potassium increase.…”

“…Currently, eplerenone is indicated for heart failure in 460 countries based on its anticipated beneficial cardiac effect. 7 It has been reported that eplerenone also has a stable antihypertensive effect, [13][14][15][16][17][18][19][20] with a profile slightly different from that of spironolactone, 21 and fewer adverse reactions, suggesting that it may become a first-line treatment for hypertension. However, clinical data on hypertensive patients in Japan are lacking for eplerenone.…”

A Selective Antagonist of Mineralocorticoid Receptor Eplerenone in Cardiology Practice

“…в 2005 г. описали подобное неренальное негеномное влияние альдостерона на миокард человека [16]. Так-же существуют и другие работы, свидетельствующие о том, что альдостерон ухудшает сократимость и мета-болические функции ишемированного миокарда, по-вышает системное сосудистое сопротивление, а также усиливает вазоконстрикторный эффект ангиотензина II в коронарных артериях [17][18][19].…”

Eplerenone use in primary aldosteronism during pregnancy

“…Unlike spironolactone, it has fewer androgenic effects (gynecomastia, mastalgia, feminization, impotence) 3. Its main side effects include hyperkalemia 3, hypotension, and renal impairment.…”