Annales d'Endocrinologie ( IF 2.9 ) Pub Date : 2020-05-27 , DOI: 10.1016/j.ando.2020.03.009 Michel Azizi 1
Blocking the mineralocorticoid receptor (MR) is one of the most effective ways of reducing blood pressure in patients with resistant hypertension and improving cardiovascular prognosis in patients with heart failure with reduced ejection fraction and left ventricular dysfunction after myocardial infarction. Blockade of the biological effects of aldosterone has mostly been achieved with spironolactone and eplerenone, the two steroidal MR antagonists currently on the market. Development of new non-steroidal dihydropyridine-based third- and fourth-generation MR antagonists is ongoing. These antagonists are highly selective for the MR, but have no effect on the glucocorticoid, androgen, progesterone and estrogen receptors, in contrast with spironolactone.
中文翻译:
醛固酮受体拮抗剂
阻断盐皮质激素受体(MR)是降低顽固性高血压患者血压和改善心梗后射血分数降低和左心室功能不全的心力衰竭患者心血管预后的最有效方法之一。目前市场上销售的两种甾体 MR 拮抗剂主要是通过螺内酯和依普利酮来阻断醛固酮的生物学效应。新型非甾体二氢吡啶类第三代和第四代 MR 拮抗剂的开发正在进行中。与螺内酯相比,这些拮抗剂对 MR 具有高度选择性,但对糖皮质激素、雄激素、孕激素和雌激素受体没有影响。