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Low-dose spironolactone is generally very well tolerated. [63] Even higher doses of spironolactone, such as 100 mg/day, are well tolerated in most individuals. [ 63 ] Dose-dependent side effects of spironolactone include menstrual irregularities, breast tenderness, and enlargement, orthostatic hypotension , and hyperkalemia. [ 63 ]
The price of a new drug (in most cases) is limited so that the cost of therapy with the new drug is in the range of the costs of therapy with existing drugs in the same therapeutic class. The price of a breakthrough drug is limited to the median of its prices in France, Germany, Italy, Sweden, Switzerland, Britain, and the United States.
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Spironolactone has been found to be effective in the treatment of hirsutism in women at a dosage of as low as 50 mg/day. [60] At dosages of 100 mg/day and 200 mg/day, observed reductions in hair shaft diameter were 19% ± 8% and 30% ± 3%, respectively ( p = 0.07).
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.
The following is a timeline of events in the history of antiandrogens: [218] 1941: Hudgins and Hodges show that androgen deprivation via high-dose estrogen therapy or surgical castration treats prostate cancer; 1957: The steroidal antiandrogen spironolactone is first synthesized [219]
[12] [13] Due to its activity as an androgen receptor antagonist and progesterone receptor agonist, spironolactone causes adverse effects, including gynecomastia or decreased libido in males and menstrual abnormalities in females. [14] Spironolactone also causes hyperkalemia [15] and renal insufficiency. [16]
Spironolactone is a prodrug with a short terminal half-life of 1.4 hours. [5] [6] [7] The active metabolites of spironolactone have extended terminal half-lives of 13.8 hours for 7α-TMS, 15.0 hours for 6β-OH-7α-TMS, and 16.5 hours for canrenone, and accordingly, these metabolites are responsible for the therapeutic effects of the drug. [5] [6