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Eplerenone

依普利酮

Mechanism of action:

Eplerenone 是一種選擇性鹽皮質激素受體拮抗劑（selective mineralocorticoid receptor antagonist）。Eplerenone 能競爭性拮抗醛固酮（aldosterone），作用位置主要在腎臟遠端腎元（尤其是集尿管主細胞）。當醛固酮與鹽皮質激素受體結合後，會促進上皮細胞鈉離子通道（ENaC）與鈉鉀幫浦（Na⁺/K⁺-ATPase）表達量增加，導致鈉與水再吸收、鉀排泄上升。Eplerenone 能競爭性阻斷鹽皮質激素受體，抑制鈉離子通道與鈉鉀幫浦的表達量與相關轉運活性。

​Reference(s):

1. Moore TD et al. (2003). Eplerenone: a selective aldosterone receptor antagonist for hypertension and heart failure. Heart Dis. 


2. Fraccarollo D et al. (2003). Additive improvement of left ventricular remodeling and neurohormonal activation by aldosterone receptor blockade with eplerenone and ACE inhibition in rats with myocardial infarction. J Am Coll Cardiol.

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