Effects of eplerenone, a selective mineralocorticoid receptor antagonist, on clinical and experimental salt-sensitive hypertension.
Mineralocorticoid receptors (MRs) are expressed in non-epithelial tissues, such as blood vessels, the heart and adipose tissue. The combined effects of aldosterone and insulin link the metabolic syndrome with hypertension and salt sensitivity. Eplerenone is the newly developed inhibitor of MRs that has significantly fewer adverse effects than similar doses of spironolactone. Eplerenone has been reported to have anti-hypertensive and protective effects on cardiovascular and renal injury in salt-sensitive hypertensive animal models, such as the Dahl salt-sensitive (DS) hypertensive rat and leptin receptor-deficient spontaneously hypertensive rat (SHR/cp). Eplerenone also increases nitric oxide bioavailability and improves impaired endothelial function by decreasing oxidative stress. Clinical studies support the concept that eplerenone is effective for the treatment of salt-sensitive hypertension as well as idiopathic hyperaldosteronism and does not have adverse anti-androgenic adverse effects. In Japan, eplerenone has been used clinically since 2007 for the treatment of hypertension, with its price being marginally lower than all types of angiotensin II receptor antagonists. This will inevitably result in an increasing number of hypertensive patients and those with primary aldosteronism being treated with this agent in the near future.
Takeda
Yoshiyu
Y
Department of Internal Medicine, Graduate School of Medical Science, Kanazawa University, Kanazawa, Japan. takeday@ med.kanazawa-u.ac.jp
D000450:Aldosterone / Q000378:metabolism; D000818:Animals; D004195:Disease Models, Animal; D000077545:Eplerenone; D006801:Humans; D006973:Hypertension / Q000139:chemically induced / Q000188:drug therapy* / Q000378:metabolism; D000451:Mineralocorticoid Receptor Antagonists / Q000627:therapeutic use*; D051381:Rats; D020303:Rats, Inbred Dahl; D012965:Sodium Chloride / Q000009:adverse effects*; D013148:Spironolactone / Q000031:analogs & derivatives* / Q000627:therapeutic use
D000451:Mineralocorticoid Receptor Antagonists; D013148:Spironolactone; D012965:Sodium Chloride; D000450:Aldosterone; D000077545:Eplerenone