Aldosterone Antagonists

Question 1

aldosterone inhibitors overview

Answer 1

block receptors for aldosterone
-two drugs available: eplerenone and spironolactine
(spironolactone is less selective)

Question 2

Eplerenone

Answer 2

Selective aldosterone receptor blocker

Question 3

Eplerenone Mechanism of Action

Answer 3

-in the kidney, activation of aldosterone receptors promotes excretion of potassium and retention of sodium and water
-receptor blockade has the opposite effect: retention of K and increased excretion of Na and water
-loss of Na and water reduced blood volume, and hence BP,
-blockade of aldosterone receptors at nonrenal sites may prevent or reverse pathologic effects of aldosterone on cardiovascular structure and function

Question 4

Eplerenone Therapeutic Uses

Answer 4

-Hypertension (max effects in reductions of BP take about 4 weeks to develop)
-Heart failure

Question 5

Eplerenone adverse effects

Answer 5

-generally well tolerated
-few adverse effects: diarrhea, abdominal pain, cough, fatigue, gynecomastia
-hyperkalemia (can occur secondary to K retention)