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Eplerenone lowers blood pressure in patients with primary hypertension. [9] Eplerenone also reduces arterial stiffness and vascular endothelial dysfunction. [10] For persons with resistant hypertension, eplerenone is safe and effective for reducing blood pressure, [11] particularly in persons with resistant hypertension due to ...
eplerenone; spironolactone; Aldosterone receptor antagonists are not recommended as first-line agents for blood pressure, [47] but spironolactone and eplerenone are both used in the treatment of heart failure and resistant hypertension.
Spironolactone has been identified as an inhibitor of NRG1‐ERBB4 signaling. [142] Spironolactone has been found to act as a potent inhibitor of the pannexin 1 channel, and this action appears to be involved in its antihypertensive effects independently of MR antagonism. [143] Spironolactone has been found to block hERG channels. [144]
Spironolactone is used in the treatment of hyperaldosteronism (high aldosterone levels or mineralocorticoid excess), for instance primary aldosteronism (Conn's syndrome). [47] Antimineralocorticoids like spironolactone and eplerenone are first-line treatments for hyperaldosteronism. [47]
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 ] )
They are typically used as an adjunct in management of hypertension, cirrhosis, and congestive heart failure. [3] The steroidal aldosterone antagonists can also be used for treatment of primary hyperaldosteronism. Spironolactone, a steroidal aldosterone antagonist, is also used in management of female hirsutism and acne from PCOS or other ...
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]
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]