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Contraindications of spironolactone include hyperkalemia (high potassium levels), severe and end-stage kidney disease (due to high hyperkalemia risk, except possibly in those on dialysis), Addison's disease (adrenal insufficiency and low aldosterone levels), and concomitant use of eplerenone.
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 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
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%
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 ]
spironolactone 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 ...
Also, there are two case reports of spironolactone actually accelerating progression of metastatic prostate cancer in castrated men treated with it for heart failure, and for this reason, spironolactone has been regarded as contraindicated in patients with prostate cancer.
[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]