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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 ]
[28] [16] In addition, the AR antagonism of spironolactone is involved in its feminizing side effects, such as gynecomastia in men. [28] Spironolactone has been found to produce gynecomastia without changes in testosterone or estradiol levels, implicating AR antagonism in this side effect. [30] Gynecomastia is a major known side effect of AR ...
Conversely, in studies of healthy men given high-dose spironolactone, gynecomastia occurred in 3 of 10 (30%) at 100 mg/day, in 5 of 8 (62.5%) at 200 mg/day, and in 6 of 9 (66.7%) at 400 mg/day, relative to none of 12 controls. [134] [135] The severity of gynecomastia with spironolactone varies considerably, but is usually mild. [110]
Potassium-sparing diuretics act to prevent sodium reabsorption in the collecting tubule by either binding ENaCs (amiloride, triamterene) or by inhibiting aldosterone receptors (spironolactone, eplerenone). This prevents excessive excretion of K + in urine and decreased retention of water, preventing hypokalemia. [10]
Hyperkalemia was more common in the spironolactone group, but the incidence of severe hyperkalemia was relatively low. Gynecomastia or breast pain occurred in 10% of men treated with spironolactone vs 1% of men in the placebo group, otherwise there were no other differences in safety or adverse events. [1] [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]
Mammoplasia can be an effect or side effect of various drugs, including estrogens, [2] [13] antiandrogens such as spironolactone, [14] cyproterone acetate, [15] bicalutamide, [16] [17] and finasteride, [18] [19] growth hormone, [20] [21] and drugs that elevate prolactin levels such as D 2 receptor antagonists like antipsychotics (e.g ...
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 ...