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Spironolactone is also used to treat Bartter's syndrome due to its ability to raise potassium levels. [38] Spironolactone has antiandrogenic activity. For this reason, it is used to treat a variety of dermatological conditions in which androgens play a role. Some of these uses include acne, seborrhea, hirsutism, and pattern hair loss in women. [39]
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]
However, spironolactone is metabolized to three active metabolites, which give it prolonged activity (13.8 – 16. 5 hours). Spironolactone has a long half-life and is excreted 47-51% through kidneys. Patients with chronic kidney disease therefore require close monitoring when taking the drug. Spironolactone is also eliminated through feces (35-41%
Spironolactone interacts with the following medications: [17] - ACE inhibitors/ARBs: increases hyperkalemia risk - Alcohol: risk of orthostatic hypotension - Barbiturates: risk of orthostatic hypotension - Narcotics: risk of orthostatic hypotension - NSAIDs: increases hyperkalemia risk and decreases diuretic effect of potassium-sparing diuretics
1962: Spironolactone is first reported to produce gynecomastia in men [219] [221] 1966: Benorterone is the first known antiandrogen to be studied clinically, to treat acne and hirsutism in women [ 222 ] [ 223 ]
Canrenone is an active metabolite of spironolactone, canrenoic acid, and potassium canrenoate, and is considered to be partially responsible for their effects. [9] It has been found to have approximately 10 to 25% of the potassium-sparing diuretic effect of spironolactone, [ 16 ] whereas another metabolite, 7α-thiomethylspironolactone (7α-TMS ...
[10] [96] It is an analogue of other spirolactones like spironolactone, canrenone, and spirorenone. [10] [96] Drospirenone differs structurally from spironolactone only in that the C7α acetyl thio substitution of spironolactone has been removed and two methylene groups have been substituted in at the C6β–7β and C15β–16β positions. [97]
The trial was stopped early because the beneficial effect of spironolactone on all-cause death exceeded the prespecified discontinuation requirements. Spironolactone reduced the risk of death by 30% compared to placebo. Additionally, there was a 35% reduction in the risk of hospitalization for worsening heart failure in the spironolactone group.
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