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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, a steroidal antimineralocorticoid of the spirolactone group; Estriol triacetate, an estrogen medication and an estrogen ester
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 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]
Unlike the related medication eplerenone, spironolactone is said to not be metabolized by CYP3A4. [245] However, hepatic CYP3A4 is likely responsible for the 6β-hydroxylation of 7α-TMS into 6β-OH-7α-TMS. [18] [246] 7α-TMS may also be hydroxylated at the C3α and C3β positions. [19] Spironolactone is dethioacetylated into canrenone. [20]
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]
The pharmacodynamics of spironolactone, an antimineralocorticoid and antiandrogen medication, concern its mechanisms of action, including its biological targets and activities, as well as its physiological effects.
Canrenone, sold under the brand names Contaren, Luvion, Phanurane, and Spiroletan, is a steroidal antimineralocorticoid [3] [4] of the spirolactone group related to spironolactone which is used as a diuretic in Europe, including in Italy and Belgium.