Department of Internal Medicine, International University of Health and Welfare Mita Hospital, Minato-ku, Tokyo, Japan.
Hypertens Res. 2013 Mar;36(3):185-90. doi: 10.1038/hr.2012.182. Epub 2012 Nov 22.
In the presence of salt, aldosterone causes hypertension and organ damage via the mineralocorticoid receptor (MR) through various mechanisms. MR antagonists are considered to be potassium-sparing diuretics that exert their effect by blocking MR in the kidney, and they are not the first choice for treating hypertension. However, the importance and usefulness of inhibiting aldosterone in the management of hypertension have recently been revealed in both the basic and clinical fields. In Japan, both the selective MR antagonist eplerenone and the non-selective MR antagonist spironolactone are indicated for the treatment of hypertension. Although these drugs are generally used in the same manner, in some cases they require differentiation. This differentiation is divided into two types due to the differences in their features and differences in their contraindications in Japan. Based on a number of studies on MR antagonists that have been recently published, the diseases and clinical conditions targeted by MR antagonists appear to be likely to increase in the future. In Japan, we consider it necessary to carefully differentiate spironolactone from eplerenone in regard to their intended uses.
在盐存在的情况下,醛固酮通过多种机制通过盐皮质激素受体(MR)导致高血压和器官损伤。MR 拮抗剂被认为是保钾利尿剂,通过在肾脏中阻断 MR 发挥作用,它们不是治疗高血压的首选药物。然而,最近在基础和临床领域都揭示了抑制醛固酮在高血压管理中的重要性和有用性。在日本,选择性 MR 拮抗剂依普利酮和非选择性 MR 拮抗剂螺内酯都被批准用于治疗高血压。尽管这些药物通常以相同的方式使用,但在某些情况下需要进行区分。这种区分由于它们的特征差异以及在日本的禁忌症差异而分为两种类型。基于最近发表的多项关于 MR 拮抗剂的研究,MR 拮抗剂的目标疾病和临床情况似乎在未来可能会增加。在日本,我们认为有必要仔细区分螺内酯和依普利酮在用途方面的差异。