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Eplerenone is an antimineralocorticoid, or an antagonist of the mineralocorticoid receptor (MR). [21] Eplerenone is also known chemically as 9,11α-epoxy-7α-methoxycarbonyl-3-oxo-17α-pregn-4-ene-21,17-carbolactone and "was derived from spironolactone by the introduction of a 9α,11α-epoxy bridge and by substitution of the 17α-thoacetyl ...
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]
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]
eplerenone In the United States, the JNC8 (Eighth Joint National Committee on the Prevention, Detection, Evaluation, and Treatment of High Blood Pressure) recommends thiazide-type diuretics to be one of the first-line drug treatments for hypertension, either as monotherapy or in combination with calcium channel blockers , ACEis, or ARBs. [ 7 ]
Eplerenone, a steroidal antimineralocorticoid of the spirolactone group; Estriol triacetate, an estrogen medication and an estrogen ester
For this reason, men are typically not prescribed spironolactone for any longer than a short period of time, e.g., for an acute exacerbation of heart failure. A newer medication, eplerenone, has been approved by the US Food and Drug Administration (FDA) for the treatment of heart failure, and lacks the antiandrogenic effects of spironolactone ...
These symptoms occur less frequently with eplerenone drug therapy. [30] In the absence of treatment, individuals with hyperaldosteronism often have poorly controlled high blood pressure, which may be associated with increased rates of stroke, heart disease, and kidney failure. With appropriate treatment, the prognosis is considered good. [31]
Aldosterone antagonists (such as spironolactone or eplerenone) or epithelial sodium channel blockers such as amiloride have also been suggested as possible treatments, because they decrease urinary wasting of potassium. However, a consensus expert statement from 2017 warns that such drugs should only be used with caution in Gitelman syndrome ...