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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]
Class of medications that are competitive antagonists that block the receptor sites for the endogenous catecholamines epinephrine (adrenaline) and norepinephrine (noradrenaline) on adrenergic beta receptors, of the sympathetic nervous system.
amiloride, spironolactone, eplerenone, triamterene, potassium canrenoate. Inhibition of Na+/K+ exchanger: Spironolactone inhibits aldosterone action, Amiloride inhibits epithelial sodium channels [17] 5. cortical collecting ducts: Thiazides: bendroflumethiazide, hydrochlorothiazide: Inhibits reabsorption by Na + /Cl − symporter: 4. distal ...
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 ...
Eplerenone, a steroidal antimineralocorticoid of the spirolactone group; Estriol triacetate, an estrogen medication and an estrogen ester
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]