Before we can identify which is more prone to gynecomastia between Eplerenone and Spironolactone as its adverse effect, let us first define both drugs:
Eplerenone is a steroidal antimineralocorticoid with the chemical formula of C24H30O6. It is manufactured and marketed by Pfizer under the trade name Inspra.
Meanwhile, Spironolactone is an antiandrogen receptor with the chemical formula C24H32O4S. It is also manufactured and marketed by Pfizer under the trade name Aldactone.
Both are antagonist of the aldosterone receptor (AR) and mineralocorticoid receptor (MR). They are also diuretic that spares potassium (water pill). They prevent your body from acquiring too much salt. They help your body get rid of water but still maintain your levels of potassium from getting excessively low.
However, spironolactone is generically available, is less susceptible to interactions among drugs. Yet, it is known as a source of gynecomastia and/or breast pain among male patients than eplerenone. There is also a trial which discovered that spironolactone resulted to breast enlargement and pain among 10% of patients with heart failure while only 0.5% of patients with heart failure on eplerenone. This low prevalence with eplerenone is constant also in patients with hypertension.
The reason why eplerenone causes fewer case of this disorder than spironolactone is due to the inhibition of aldestorone from the binding of the mineralocorticoid receptor (MR) and testosterone to receptors of androgen (AR). Meanwhile, the existence of a group in eplerenone which causes reduction in the development of testosterone and complexes on androgen receptor resulting to loss of inhibiting gene transcription required for the proliferation of breast tissues.
Therefore, due to the undesirable effect of taking spironolactone which is more prone to gynecomastia, reluctance to this drug is imminent. But a patient must take into consideration that eplerenone will add up more to your expenses and obliges guidance for considerations of current treatments to avoid interaction with other drugs wherein this is not so when taking spironolactone.
There were several mechanisms which have been proposed for the side effects of taking these drugs especially with spironolactone, such as a dose-dependent reduction of microsomal cytochrome P-450, alterations of ratio between the testosterone and estrogen, a fall of testosterone in the plasma, a significant increase in its metabolic clearance, and the peripheral conversion of testosterone to estradiol otherwise increased levels of serum among estrone and estradiol.
Nevertheless, the diuretic effects of eplerenone and spironolactone are marginal. Combination of these aldosterone antagonists with thiazide or loop diuretics will be highly more potent with the effect of thiazide or loop diuretics. In comparison to potassium supplement alone, this is more effective alternative.
Aside from taking these oral medications, nutritional guides are encouraged. Limiting salt and sodium 1,500 to 2,000 mg per day is essential so replacing your usual salt and seasonings to low sodium or none at all would be of help. Avoid processed foods and settle to fresh fruits and vegetables. It is also advised to read on food labels to determine the amount of sodium. It is also important to avoid drinking alcohol or alcoholic beverages. You must also maintain a diet low in saturated fat and cholesterol.
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