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Spironolactone, sold under the brand name Aldactone among others, is a diuretic medication primarily used to treat fluid build-up due to heart failure, liver scarring, or kidney disease. [4] It is also used in the treatment of high blood pressure , and low blood potassium that does not improve with supplementation , early puberty in boys, acne ...
Spironolactone has been identified as an inhibitor of NRG1‐ERBB4 signaling. [142] Spironolactone has been found to act as a potent inhibitor of the pannexin 1 channel, and this action appears to be involved in its antihypertensive effects independently of MR antagonism. [143] Spironolactone has been found to block hERG channels. [144]
Spironolactone – most widespread use, inexpensive; Eplerenone – more selective so reduced side-effects but more expensive and less potent; Finerenone – non-steroidal, more selective and potent than spironolactone and eplerenone; Canrenone – very limited use
The Randomized Aldactone Evaluation Study (RALES) trial is a landmark clinical study that assessed the impact of spironolactone, an aldosterone antagonist, on morbidity and mortality in patients with severe heart failure due to systolic dysfunction. [1]
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]
Chemical/generic names are listed first, with developmental code names, synonyms, and brand names in parentheses. ... Spironolactone (Aldactone) – androgen receptor ...