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[43] [44] [45] However, in another case report, spironolactone was effective in normalizing prostate-specific antigen in a man with prostate cancer. [46] In addition, spironolactone has been studied in the treatment of prostate cancer. [47] [48] Canrenone binds to and blocks the AR in vitro. [29]
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]
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]
Eplerenone may have a lower incidence than spironolactone of sexual side effects such as feminization, gynecomastia, impotence, low sex drive and reduction of size of male genitalia. [18] This is because other antimineralocorticoids have structural elements of the progesterone molecule, causing progestogenic and antiandrogenic outcomes. [ 4 ]
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.
For people with hyperplasia of both glands, successful treatment is often achieved with spironolactone or eplerenone, drugs that block the aldosterone receptor. With its antiandrogen effect, spironolactone drug therapy may have a range of side effects in males and females, including gynecomastia and irregular menses. These symptoms occur less ...
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 ...