首页> 外文期刊>Journal of Endocrinological Investigation: Official Journal of the Italian Society of Endocrinology >Aldosterone receptor antagonists: biology and novel therapeutical applications.
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Aldosterone receptor antagonists: biology and novel therapeutical applications.

机译:醛固酮受体拮抗剂:生物学和新的治疗应用。

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摘要

Recent studies suggest that a dysregulation of the aldosterone system is involved in the pathophysiology of different cardiovascular diseases, including myocardial failure and several cases of essential hypertension. In both rat models and in humans, aldosterone action has been shown to induce heart remodeling and interstitial and perivascular fibrosis of the myocardium. For these reasons, a rationale for the use of aldosterone antagonists (ARAs) of the spirolactone family, which have been available for decades in the treatment of aldosterone excess syndromes, has now emerged. Moreover, the recent validation of their use, in combination with the current therapy, for the treatment of these cardiovascular diseases by trials like the RALES Study has further strenghtened this approach. The development of compounds, like eplerenone, with a greater selectivity for mineralocorticoid receptors, seems promising also in terms of reduction of endocrine side effects. The addition of aldosterone antagonists to the conventional therapy of myocardial failure and of selected cases of hypertension thus appears beneficial, resulting in an improved survival rate and a reduced incidence of cardiac complications. This review article, after a brief recall of the physiology of the aldosterone system, addresses the emerging role of aldosterone in cardiovascular diseases, considers the pharmacology of ARAs and the novel therapeutical applications of these compounds in hypertension and heart failure.
机译:最近的研究表明,醛固酮系统的失调与不同心血管疾病的病理生理学有关,包括心肌衰竭和几例原发性高血压。在大鼠模型和人类中,醛固酮作用已被证明可以诱导心脏重塑以及心肌的间质和血管周围纤维化。由于这些原因,现在已经出现了使用螺内酯家族的醛固酮拮抗剂 (ARA) 的基本原理,这些醛固酮拮抗剂在治疗醛固酮过量综合征方面已有数十年的历史。此外,最近通过RALS研究等试验验证了它们与当前疗法相结合用于治疗这些心血管疾病的用途,进一步加强了这种方法。对盐皮质激素受体具有更大选择性的化合物(如依普利酮)的开发似乎在减少内分泌副作用方面也很有希望。因此,在心肌衰竭和特定高血压病例的常规治疗中加入醛固酮拮抗剂似乎是有益的,从而提高了生存率并降低了心脏并发症的发生率。这篇综述文章在简要回顾了醛固酮系统的生理学之后,讨论了醛固酮在心血管疾病中的新兴作用,考虑了ARA的药理学以及这些化合物在高血压和心力衰竭中的新治疗应用。

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