A Literature Review of the Pharmacokinetics, Pharmacodynamics, and Possible Uses of Spironolactone

Spironolactone (SL) is an antimineralocorticoid derived from progesterone, and was therefore developed as a diuretic for hypertension and edema treatment (Kolkhof & Barfacker, 2017). As a prodrug, its effects are largely mediated by its metabolites, 7α-thiomethylspironolactone and canrenone (Janowski et al., 1996), which are ultimately eliminated through the urine (Abshagen et al., 1977). Later on, it was discovered that SL also exhibits moderate antiandrogenic activity due to its structural similarity to progesterone (Menard, 2004), allowing it to be used as an off-label treatment for hyperandrogenism and its associated symptoms, such as hirsutism and acne (Voegli et al., 2009).  As researchers continue to elucidate the role of mineralocorticoid receptors in cognition and behaviour, new possibilities for SL as an anxiolytic may also emerge in the future (Otte et al., 2007). With all that being said, SL’s sexual side-effects, especially in males, continue to limit the various applications of this multi-use drug.