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They are common during spironolactone therapy, with 10 to 50% of women experiencing them at moderate doses and almost all experiencing them at a high doses. [86] [111] For example, about 20% of women experienced menstrual irregularities with 50 to 100 mg/day spironolactone, whereas about 70% experienced menstrual irregularities at 200 mg/day. [63]
[61] [62] In addition, other studies have found that 100 mg/day spironolactone is significantly or near-significantly inferior to 500 mg/day flutamide in improving symptoms of acne and hirsutism. [ 63 ] [ 64 ] [ 65 ] One study compared placebo and dosages of spironolactone of 50, 100, 150, and 200 mg/day in the treatment of acne in women and ...
Eplerenone is a newer drug that was developed as a spironolactone analog with reduced adverse effects. In addition to the y-lactone ring and the substituent on C-7, eplerenone has a 9α,11α-epoxy group. This group is believed to be the reason why eplerenone has a 20-40-fold lower affinity for the mineralocorticoid receptor than spironolactone. [7]
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.
Potassium-sparing diuretics act to prevent sodium reabsorption in the collecting tubule by either binding ENaCs (amiloride, triamterene) or by inhibiting aldosterone receptors (spironolactone, eplerenone). This prevents excessive excretion of K + in urine and decreased retention of water, preventing hypokalemia. [10]
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.
Eplerenone differs from spironolactone in its extensive metabolism, with a short half-life and inactive metabolites. [4] Eplerenone seems to be about 50 to 75% as potent as spironolactone as an antimineralocorticoid. [24] Hence, 25 mg/day spironolactone may be equivalent to approximately 50 mg/day eplerenone. [25]
2–10 mg/wk or 5–20 mg every 2 wks Estradiol dipropionate: Agofollin: Estrogen: IM, SC: 2–10 mg/wk or 5–20 mg every 2 wks Estradiol benzoate: Progynon-B: Estrogen: IM, SC: 0.5–1.5 mg every 2–3 days Estriol: Ovestin [c] Estrogen: Oral: 4–6 mg/day Spironolactone: Aldactone: Antiandrogen: Oral: 100–400 mg/day Cyproterone acetate ...