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[39] [64] [112] Aside from these adverse effects, the side effects of spironolactone in women taking high doses are minimal, and it is well tolerated. [ 64 ] [ 86 ] [ 113 ] A potential side effect of spironolactone is hyperkalemia (high potassium levels), which, in severe cases, can be life-threatening. [ 8 ]
[12] [13] Due to its activity as an androgen receptor antagonist and progesterone receptor agonist, spironolactone causes adverse effects, including gynecomastia or decreased libido in males and menstrual abnormalities in females. [14] Spironolactone also causes hyperkalemia [15] and renal insufficiency. [16]
[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 ...
Certain side effects, like breast enlargement, reduced premenstrual symptoms, and less oily skin/greasy hair, could be beneficial. Side effects often could not be unambiguously attributed to spironolactone due concomitant use of other medications, particularly birth control pills.
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]
The choice between the drugs is to a large degree determined by the characteristics of the patient being prescribed for, the drugs' side effects, and cost. Most drugs have other uses; sometimes the presence of other symptoms can warrant the use of one particular antihypertensive. Examples include: Age can affect the choice of medications.
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]
Aldosterone antagonists: spironolactone, which is a competitive antagonist of aldosterone. Aldosterone normally adds sodium channels in the principal cells of the collecting duct and late distal tubule of the nephron. Spironolactone prevents aldosterone from entering the principal cells, preventing sodium reabsorption.