Selection of a mineralocorticoid receptor antagonist for patients with hypertension or heart failure

Abstract

Clinical trials have demonstrated morbidity and mortality benefits of mineralocorticoid receptor antagonists (MRAs) in patients with heart failure. These studies have used either spironolactone or eplerenone as the MRA. It is generally believed that these two agents have the same effects, and the data from studies using one drug could be extrapolated for the other. National and international guidelines do not generally discriminate between spironolactone and eplerenone, but strongly recommend using an MRA for patients with heart failure due to LV systolic dysfunction and post-infarct LV systolic dysfunction. There are no major clinical trials directly comparing the efficacy of these two drugs. This article aims to compare the pharmacokinetics and pharmacodynamics of spironolactone and eplerenone, and to analyse the available data for their cardiovascular indications and adverse effects. We have also addressed the role of special circumstances including co-morbidities, concomitant drug therapy, cost, and licensing restrictions in choosing an appropriate MRA for a particular patient, thus combining an evidence-based approach with personalized medicine.

Mineralocorticoid Antagonists in the Treatment of Central Serous Chorioretinopathy: A Comparative Analysis

“…These findings corroborate previous clinical data of MR antagonists in other medical conditions, particularly systemic hypertension and heart failure [8,9,10,11]. Eplerenone has been associated with fewer side effects than spironolactone in multiple reports evaluating its use, and this has been attributed to its higher selectivity for the aldosterone receptor [7].…”

“…Studies have suggested a significant increase in side effects with chronic MR antagonist exposure, even with eplerenone (up to 47% in one study), emphasizing its judicious use and need for tapering upon clinical stability [8,9,10,11]…”

Emerging cardiovascular indications of mineralocorticoid receptor antagonists

“…Eplerenone is also a steroidal compound with greater selectivity for MR and minimal binding to progesterone and androgen receptors [3]. Spironolactone and eplerenone differ in their metabolism and half-life [3,4]. There are also a few non-steroidal MR antagonists (e.g., Finerone, BR-4628) at various stages of development [5][6][7].…”

Mineralocorticoid Antagonism: Selectiveness Gives More Opportunities for Heart Failure Management

“…Селективность нового препарата -важное его свойство, позволяющее избегать привыч-ных для спиронолактона негативных эффектов на половую функцию и половую морфологию (гине-комастия, мастодиния) [8]. Более современное срав-нение проведено Iqbal et al [9]. Они отмечают селек-тивность Инспры ® к альдостероновым рецепторам в отличие от неселективного спиронолактона.…”

“…Одна из важнейших проблем -побочные эффекты спиронолактона в сексуальной сфере -фактически отсутствует у Инспры ® . Так, этот препарат стал заменой спироно-лактона при длительной терапии, если развивается гинекомастия у мужчин (либо при отказе принимать препараты при страхе такого побочного эффекта), нарушения менструальной функции и боли в молоч-ных железах (мастодиния) у женщин [9,10].…”