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If levels of mineralocorticoids are decreased, then there are lower circulating levels to compete with spironolactone to influence gene expression as mentioned above. [23] The onset of action of the antimineralocorticoid effects of spironolactone is relatively slow, with the peak effect sometimes occurring 48 hours or more after the first dose ...
A potential side effect of spironolactone is hyperkalemia (high potassium levels), which, in severe cases, can be life-threatening. [8] Hyperkalemia can present as a normal anion-gap metabolic acidosis. [ 8 ]
Patients were randomized to receive either spironolactone (25 to 50 mg) daily or placebo. Both groups were continued on standard therapy. The primary endpoint was all-cause mortality. Secondary endpoints included hospitalization for heart failure, changes in symptoms of heart failure, and serum potassium levels. [1] [2]
Potassium-sparing diuretics or antikaliuretics [1] refer to drugs that cause diuresis without causing potassium loss in the urine. [2] They are typically used as an adjunct in management of hypertension , cirrhosis , and congestive heart failure . [ 3 ]
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 ...
Emergency lowering of potassium levels is needed when new arrhythmias occur at any level of potassium in the blood, or when potassium levels exceed 6.5 mmol/L. Several agents are used to temporarily lower K + levels. The choice depends on the degree and cause of the hyperkalemia, and other aspects of the person's condition.
Hans Selye, a Hungarian-Canadian endocrinologist, studied the effects of aldosterone antagonists on rats and found that the use of one of the first aldosterone antagonists, spironolactone, protected them from aldosterone-induced cardiac necrosis. The same year, 1959, spironolactone was launched as a potassium-sparing diuretic.
Spirolactones are a class of functional group in organic chemistry featuring a cyclic ester attached spiro to another ring system. The name is also used to refer to a class of synthetic steroids, called steroid-17α-spirolactones, 17α-spirolactosteroids, or simply 17α-spirolactones, which feature their spirolactone group at the C17α position.