A Comparison of the Aldosterone‐blocking Agents Eplerenone and Spironolactone

@article{Struthers2008ACO,
  title={A Comparison of the Aldosterone‐blocking Agents Eplerenone and Spironolactone},
  author={Allan D. Struthers and Henry Krum and Gordon H. Williams},
  journal={Clinical Cardiology},
  year={2008},
  volume={31}
}
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, well‐controlled, clinical trials and comparative studies… 
Selection of a mineralocorticoid receptor antagonist for patients with hypertension or heart failure
TLDR
The pharmacokinetics and pharmacodynamics of spironolactone and eplerenone are compared and the role of special circumstances including co‐morbidities, concomitant drug therapy, cost, and licensing restrictions in choosing an appropriate MRA for a particular patient are addressed, combining an evidence‐based approach with personalized medicine.
Mineralocorticoid receptor antagonists, a class beyond spironolactone--Focus on the special pharmacologic properties of eplerenone.
Comparison of agents that affect aldosterone action.
Safety and Efficacy of Eplerenone in the Management of Essential Hypertension
TLDR
Eplerenone, the selective mineralocorticoid receptor antagonist, is a promising cardiovascular drug licensed for the treatment of heart failure in Europe and heart failure and hypertension in the USA and effectively blocks the mineralocortex receptor without the unpleasant sexual side effect profile of spironolactone.
A double-blind, randomized study comparing the antihypertensive effect of eplerenone and spironolactone in patients with hypertension and evidence of primary aldosteronism
TLDR
The antihypertensive effect of spironolactone was significantly greater than that of eplerenone in hypertension associated with primary aldosteronism.
Mineralocorticoid receptor antagonists lead to increased adenosine bioavailability and modulate contractile cardiac parameters
TLDR
Collectively, MRAs in vivo lead to increased ADO bioavailability and in vitro, the rapid effects of SPI and EPL are mediated by an interaction between ADO receptors A 1 and A 3.
Eplerenone: A Review of Its Use in Patients with Chronic Systolic Heart Failure and Mild Symptoms
TLDR
In the EMPHASIS-HF study, relative to placebo, the addition of eplerenone to optimal background therapy significantly reduced the risk of death from CV causes or hospitalization for HF in patients with chronic systolic HF and mild symptoms.
Spironolactone, but not eplerenone, impairs glucose tolerance in a rat model of metabolic syndrome.
TLDR
It is demonstrated that in comparison with EPL, SPL characteristically impairs glucose tolerance in an animal model of metabolic syndrome, in association with a higher blood level of aldosterone.
SM-368229, a novel selective and potent non-steroidal mineralocorticoid receptor antagonist with strong urinary Na+ excretion activity.
TLDR
SM-368229 dose-dependently increased urinary Na(+)/K(+) ratio with an ED(50) value of 5.6 mg/kg in adrenalectomized rats treated with deoxycorticosterone acetate, and its efficacy was superior to that of SPI or EPL.
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