螺内酯 (Aldactazide, Aldactone, Carospir +1)

概览

Spironolactone is an aldosterone receptor antagonist used to treat edema, hypertension, heart failure, and aldosteronism.

作用机制

Aldosterone is a key hormone in the renin-angiotensin-aldosterone system. By binding to the mineralocorticoid receptor at the distal tubules and collecting duct, it causes sodium reabsorption and potassium secretion, increases vascular stiffness and remodelling, and activates pro-inflammatory pathways. Spironolactone and its active metabolites are aldosterone antagonists that produce a potassium-sparing diuretic effect. They competitively bind to receptors at the aldosterone-dependent sodium-potassium exchange site in the distal convoluted renal tubule. Spironolactone causes increased amounts of sodium and water to be excreted while potassium is retained. Spironolactone acts both as a diuretic and as an antihypertensive drug by this mechanism. It may be given alone or with other diuretic agents that act more proximally in the renal tubule.

适应症

Spironolactone is indicated for the treatment of the following conditions: As spironolactone has antiandrogenic activity, its off-label uses include the treatment of hirsutism, female pattern hair loss, and adult acne vulgaris.

• Edema
• Hypertension
• Primary Aldosteronism
• Primary Hyperaldosteronism
• Secondary hyperaldosteronism
• Chronic heart failure with reduced ejection fraction (NYHA Class III)
• Chronic heart failure with reduced ejection fraction (NYHA Class IV)
• Idiopathic hyperaldosteronism
• Refractory Edema