The Pharmacological Properties and Safety Profile of Mineralocorticoid Receptor Antagonists in Heart Failure with Reduced Ejection Fraction.

Q3 Medicine

The Journal of the Association of Physicians of India Pub Date : 2026-01-01 DOI:10.59556/japi.74.1295

Dharmesh Solanki, Rajesh Badani, Mangesh Tiwaskar, S Sandeep, Neeraj Bhalla, Mohd Nadeem, Vineet Garg, P K Reddy, Sheetal Kamat, P K Joshi, A Ganesh Raja, Febin Francis, Amarnath Sugumaran, Senthilnathan Mohanasundaram

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Abstract

Among the established mineralocorticoid receptor antagonists (MRAs), spironolactone and eplerenone have demonstrated significant clinical utility in managing conditions such as chronic heart failure, resistant hypertension, and hyperaldosteronism. Spironolactone, the first steroidal MRA, is known for its broad receptor affinity, contributing to both therapeutic benefits and endocrine-related side effects. Eplerenone, a more selective agent, offers improved tolerability with reduced hormonal adverse effects. This review explores the pharmacokinetic and pharmacodynamic profiles of these agents, highlighting their mechanisms of action, receptor-binding characteristics, and clinical implications. The safety considerations associated with long-term use, particularly hyperkalemia and renal function impairment, are also discussed to provide a comprehensive understanding of their therapeutic roles.

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矿皮质激素受体拮抗剂治疗心力衰竭伴射血分数降低的药理特性和安全性。

在已建立的矿皮质激素受体拮抗剂（MRAs）中，螺内酯和依普利酮在治疗慢性心力衰竭、顽固性高血压和高醛固酮增多症等疾病方面显示出显著的临床应用价值。螺内酯是第一种甾体MRA，以其广泛的受体亲和力而闻名，有助于治疗益处和内分泌相关的副作用。eperenone是一种选择性更强的药物，具有更好的耐受性和更少的激素副作用。这篇综述探讨了这些药物的药代动力学和药效学特征，重点介绍了它们的作用机制、受体结合特性和临床意义。还讨论了与长期使用相关的安全性考虑，特别是高钾血症和肾功能损害，以提供对其治疗作用的全面了解。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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