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Eplerenone, sold under the brand name Inspra, is an aldosterone antagonist type of potassium-sparing diuretic that is used to treat chronic heart failure and high blood pressure, particularly for people with resistant hypertension due to elevated aldosterone.
Aldosterone receptor antagonists, also known as mineralocorticoid receptor antagonist (MRA) can lower blood pressure by blocking the binding of aldosterone to the mineralocorticoid receptor. Spironolactone and eplerenone are MRAs that causes a block in the reabsorption of sodium, resulting in a decrease in blood pressure. [45] [46] eplerenone
Antihypertensive agents comprise multiple classes of compounds that are intended to manage hypertension (high blood pressure). Antihypertensive therapy aims to maintain a blood pressure goal of <140/90 mmHg in all patients, as well as to prevent the progression or recurrence of cardiovascular diseases (CVD) in hypertensive patients with established CVD. [2]
Antimineralocorticoids like spironolactone and eplerenone are first-line treatments for hyperaldosteronism. [47] They improve blood pressure and potassium levels, as well as left ventricular hypertrophy, albuminuria, and carotid intima-media thickness, in people with primary aldosteronism. [47]
Aldosterone binds to aldosterone receptors (mineralocorticoid receptors) increasing sodium reabsorption in an effort to increase blood pressure and improve fluid status in the body. When excessive sodium reabsorption occurs, there is an increasing loss of K + in the urine and can lead to clinically significant decreases, termed hypokalemia .
Guidelines on the choice of agents and how best to step up treatment for various subgroups in hypertension (high blood pressure) have changed over time and differ between countries. A Comparison of International Guidelines on Goal Blood Pressure and Initial Therapy for Adults With Hypertension (adapted from JNC 8 guidelines [ 1 ] )
Eplerenone is a newer drug that was developed as a spironolactone analog with reduced adverse effects. In addition to the y-lactone ring and the substituent on C-7, eplerenone has a 9α,11α-epoxy group. This group is believed to be the reason why eplerenone has a 20-40-fold lower affinity for the mineralocorticoid receptor than spironolactone. [7]
For most people, recommendations are to reduce blood pressure to less than or equal to somewhere between 140/90 mmHg and 160/100 mmHg. [2] In general, for people with elevated blood pressure, attempting to achieve lower levels of blood pressure than the recommended 140/90 mmHg will create more harm than benefits, [3] in particular for older people. [4]