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Spironolactone

螺內酯

Mechanism of action:

Spironolactone 是一種醛固酮受體拮抗劑（aldosterone antagonist），亦屬於保鉀型利尿劑（potassium-sparing diuretic）。Spironolactone 能競爭性阻斷腎臟遠曲小管與集尿管主細胞的鹽皮質激素受體（mineralocorticoid receptor），阻止醛固酮提升上皮鈉通道（ENaC）與鈉鉀幫浦（Na⁺/K⁺-ATPase）的基因表達，導致鈉與水再吸收下降、鉀與氫離子排出減少。

​Reference(s):

1. Takamura N et al. (1997). Interactions of aldosterone antagonist diuretics with human serum proteins. Pharm Res. 


2. LaCagnin LB et al. (1987). Conversion of spironolactone to 7 alpha-thiomethylspironolactone by hepatic and renal microsomes. Biochem Pharmacol. 


3. Los LE et al. (1994). Hepatic metabolism of spironolactone. Production of 3-hydroxy-thiomethyl metabolites. Drug Metab Dispos.

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