What is the mechanism of action of spironolactone?
Mechanism of action: Aldactone (spironolactone) is a specific pharmacologic antagonist of aldosterone, acting primarily through competitive binding of receptors at the aldosterone-dependent sodium-potassium exchange site in the distal convoluted renal tubule.
How does spironolactone work as an anti-androgen?
The specific actions of spironolactone as an antiandrogen are not well understood. It appears to act at two sites: it blocks androgens at the hair follicle/sebaceous gland and it reduces the secretion of androgens from the adrenal gland.
What is spironolactone and how does it work?
Spironolactone is a potassium-sparing diuretic (water pill). It prevents your body from absorbing too much salt and keeps your potassium levels from getting too low. This medicine is also used to treat or prevent hypokalemia (low potassium levels in the blood).
How does spironolactone work for PCOS?
Spironolactone acts as an anti-androgen by blocking androgen receptors, including the receptors on hair follicles, which prevents testosterone from binding and exerting its hirsutism-causing effect. Spironolactone also decreases androgen production from the ovaries and adrenal glands (Sirmans, 2013).
Does spironolactone inhibit 5 alpha reductase?
Spironolactone inhibits 5-alpha reductase weakly. Unfortunately, finasteride does not reduce sebum production and is not effective in the treatment of acne.
How does spironolactone act as a diuretic?
Spironolactone competitively inhibits aldosterone dependant sodium potassium exchange channels in the distal convoluted tubule. This action leads to increased sodium and water excretion, but more potassium retention. The increased excretion of water leads to diuretic and also antihypertensive effects.
What are androgen blockers?
Antiandrogens, also known as androgen antagonists or testosterone blockers, are a class of drugs that prevent androgens like testosterone and dihydrotestosterone (DHT) from mediating their biological effects in the body.
Does spironolactone suppress testosterone?
Interestingly, administration of the main metabolite of spironolactone, canrenone, appears to decrease testosterone by 50–60% within hours in healthy men (13) and in conjunction with oestradiol, spironolactone decreases testosterone (14).
Is spironolactone a thiazide diuretic?
Hydrochlorothiazide is a thiazide diuretic (water pill). Spironolactone is a potassium-sparing diuretic. Hydrochlorothiazide and spironolactone is a combination medicine used to treat fluid retention (edema) in people with congestive heart failure, cirrhosis of the liver, or a kidney disorder called nephrotic syndrome.
How does spironolactone cause hyperkalemia?
The pump acts to re-absorb sodium and water in exchange for potassium, which is then eliminated in the urine. Consequently, aldosterone antagonism can cause hyperkalemia. Hyperkalemia is an established adverse effect of both spironolactone and eplerenone. The symptoms of hyperkalemia begin with muscle weakness.
Can spironolactone help with hormonal imbalance?
Anti-Androgen Drugs (such as Spironolactone) are another class of oral drugs that help treat hormonal imbalance acne in females. Like oral-contraceptives, Spironolactone treats acne by regulating the hormones that are behind the breakouts to begin with.
Does spironolactone increase estrogen?
Hormone levels A 2018 systematic review of 18 studies found that spironolactone showed no significant effects on levels of estrogen, estradiol, testosterone, androstenedione, dehydroepiandrosterone sulfate, luteinizing hormone, or follicle-stimulating hormone in women.
How is spironolactone used to treat hirsutism?
Use of spironolactone in treatment of hirsutism Spironolactone (Aldactone), 100 mg to 200 mg daily, has antiandrogenic effects that may enhance treatment of androgen-excess syndromes, particularly severe hirsutism. Combination therapy with an oral contraceptive or with dexamethasone appears to have a beneficial effect.
What is the role of spironolactone in androgen excess syndromes?
The role of spironolactone in androgen excess syndromes such as hirsutism is to reduce the rate of testosterone production and increase the metabolic clearance of testosterone, which supports its use in select patients adjunctively with dexamethasone and oral contraceptives. [14] Mechanism of Action
Spironolactone specifically works by competitively blocking aldosterone receptor-mediated action. The effect of the blockade is that sodium reabsorption with water retention does not occur, and there is increased potassium retention.
Is Aldactone effective for hirsutism?
Spironolactone (Aldactone), 100 mg to 200 mg daily, has antiandrogenic effects that may enhance treatment of androgen-excess syndromes, particularly severe hirsutism. Combination therapy with an oral contraceptive or with dexamethasone appears to have a beneficial effect. Side effects are transient.