Aldosterone Antagonists (Potassium-Sparing Diuretics)
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Overview
Aldosterone antagonists competitively block mineralocorticoid receptors in the distal nephron, promoting sodium and water excretion while retaining potassium. Spironolactone is the principal agent, used for heart failure, primary hyperaldosteronism, edema, hypertension, and hormonal therapy in transgender women.
How do aldosterone antagonists (potassium-sparing diuretics) work?
Spironolactone competitively antagonizes aldosterone at the mineralocorticoid receptor in the cortical collecting duct, preventing transcription of proteins that increase the number and activity of luminal sodium channels (ENaC) and basolateral Na/K-ATPase pumps. The result is reduced sodium reabsorption and potassium excretion. Spironolactone also has anti-androgenic activity through binding to androgen receptors, accounting for its use in hormonal therapy and conditions such as polycystic ovary syndrome.
Drugs in this class
- Spironolactone (Aldactone)