Friday, May 11, 2012
Classification And Structure
Spironolactone (marketed under the trade names Aldactone) is a synthetic steroid which is commonly used as a diuretic or as an antiandrogen. Pharmacologically spironolactone is a synthetic 17-lactone steroid which is a renal competitive aldosterone antagonist in a class of pharmaceuticals called potassium-sparing diuretics, used primarily to treat ascites in patients with liver disease, low-renin hypertension, hypokalemia, and Conn's syndrome. On its own, spironolactone is only a weak diuretic, but it can be combined with other diuretics to great effect. About one person in one hundred with hypertension has elevated levels of aldosterone; in these persons the antihypertensive effect of spironolactone may exceed that of complex combined regimens of other anti-hypertensives. Due to its anti-androgen effect, it can also be used to treat hirsutism, and is a common component in hormone therapy for male-to-female Transsexual and transgendered people. It is also used for treating hair loss and acne in women.
Spironolactone inhibits the effect of aldosterone by competing for intracellular aldosterone receptor in the distal tubule cells. This increases the secretion of water and sodium, while decreasing the excretion of potassium. Spironolactone has a fairly slow onset of action, taking several days to develop and similarly the effect diminishes slowly. Spironolactone has anti-androgen activity by binding to the androgen receptor and thus preventing it to interact with dihydrotestosterone
Spironolactone is fairly rapidly absorbed from the gastrointestinal tract. It is also rapidly metabolized and bound in plasma proteins (the reason it has such a slow onset of action). Spironolactone’s half-life is 85 minutes; with many of its metabolites being active for days after the parent compound has been eliminated. The main elimination route is in the urine and some also in the bile.Concluding Remarks
Safe predictable potassium sparing diuretics have become an integral part of modern bodybuilding preparation and presentation. Spironolactone is a mild, slow acting and very controllable drug, well suited to the task of manipulating an athlete’s hydration and water gradient without applying “radical” stresses to an already taxed physiology.
Spironolactone’s anti-androgen effects could make it applicable as an anti-masculinizing compound post androgen cycle for female athletes. The androgen/DHT blocking effects could help estrogen starved hair and skin regain some of the feminine qualities often lost with over use of AAS.
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