Spironolactone is a synthetic steroid, an androgen and mineralocorticoid antagonist, a reversible competitive antagonist of aldosterone receptors (a steroid hormone that is produced by the adrenal glands and is a regulator of potassium and sodium in the human body). It has a structure that resembles the natural corticosurrenal hormone, aldosterone.

It is insoluble in water, soluble in alcohol, benzene and chloroform. 

What it is used for and where

Medical

Take only under medical supervision

Spironolactone is a diuretic drug (serves to produce more urine) and is used in heart failure, to reduce systolic blood pressure and brachial artery stiffness (1), in the treatment of female acne (2), to improve pulmonary fibrosis (3), effective and safe treatment for hyperandrogenic skin disorders (4), effective in lowering blood pressure in essential hypertension (5), primary medical treatment for hirsutism and female hair loss (6) and has the advantage of being rapidly absorbed and metabolised.

Safety

It is considered a safe drug in heart failure, hypertension and liver disease if properly monitored (7).

Like all drugs it can cause side effects. Always ask the physician.

• Molecular Formula   C₂₄H₃₂O₄S
• Molecular Weight   416,6 g/mol
• CAS  52-01-7
• UNII    27O7W4T232
• EC Number   200-133-6 

Synonyms:

• Aldactone
• Aldactone A
• Practon

References_____________________________________________________________________

(1) Davies, J., Gavin, A., Band, M., Morris, A. and Struthers, A., 2005. Spironolactone reduces brachial pulse wave velocity and PIIINP levels in hypertensive diabetic patients. British journal of clinical pharmacology, 59(5), pp.520-523.

Abstract.  Aims. To assess whether spironolactone has beneficial effects on blood pressure (BP), N-terminal propeptide of type III procollagen (PIIINP) and pulse wave velocity (PWV) in hypertensive, type II diabetics. Methods. Ten patients with type II diabetes and hypertension were enrolled in a randomized, double-blind crossover study comparing 4 months’ treatment with spironolactone and placebo with a 4-week washout phase. BP, PIIINP and carotid-radial PWV were measured at the end of each treatment phase.... Conclusions. Spironolactone is effective at reducing systolic BP and brachial artery stiffness as indicated by PWV. It also reduces PIIINP in type II diabetic patients with hypertension.

(2) Friedman, A.J., 2015. Spironolactone for adult female acne. Cutis, 96(4), pp.216-217.

Abstract. Many cases of acne are hormonal in nature, meaning that they occur in adolescent girls and women and are aggravated by hormonal fluctuations such as those that occur during the menstrual cycle or in the setting of underlying hormonal imbalances as seen in polycystic ovary syndrome. For these patients, antihormonal therapy such as spironolactone is a valid and efficacious option. Herein, initiation and utilization of this medication is reviewed.

(3) Atalay, C., Dogan, N., Aykan, S., Gundogdu, C. and Keles, M.S., 2010. The efficacy of spironolactone in the treatment of acute respiratory distress syndrome-induced rats. Singapore Med J, 51(6), pp.501-505.

Abstract. Introduction: This study aimed to test the feasibility of spironolactone treatment in comparison with a surfactant in the early stage of acute respiratory distress syndrome (ARDS) in rats, as assessed by the acute lung injury (ALI) score, blood gas, brain natriuretic peptide (BNP) and N-terminal pro-brain natriuretic peptide (NT-proBNP). ...Conclusion: Spironolactone is an effective form of treatment for ARDS at an early stage, as reflected by an increased blood O2 /FiO2 ratio, decreased BNP and NT-proBNP levels, and ALI score.

(4) Sabbadin, C., Beggiao, F., Vedolin, K., Orlando, G., Ragazzi, E., Ceccato, F., Barbot, M., Bordin, L., Donà, G., Andrisani, A. and Scaroni, C., 2022. Long-Lasting Effects of Spironolactone After its Withdrawal in Patients with Hyperandrogenic Skin Disorders. Endocrine, Metabolic & Immune Disorders Drug Targets.

Abstract. Objective. Hyperandrogenic skin disorders, such as hirsutism, acne and alopecia, affect approximately 10-20% of women of reproductive age, reducing quality of life and causing psychological impairment. Spironolactone is a commonly used antiandrogen, especially in women who are not sexually active or have contraindications to hormonal contraceptives. The aim of this study was to evaluate the effects of spironolactone, especially after its withdrawal, in patients with hyperandrogenic skin disorders. Methods. Retrospective analysis of 63 women with hyperandrogenic skin symptoms due to polycystic ovary syndrome (PCOS), treated with spironolactone for at least 6 months as first-line treatment. Results. After a mean time of treatment of 25.7 months, all patients reported a significant improvement in hyperandrogenic skin disorders; only 5 patients were dissatisfied and required the addition of an oral contraceptive. The therapy was well tolerated and the most frequent side-effect was intermestrual bleeding in 68.2% of cases, affecting mainly classic PCOS phenotype. Thirthyeight patients showed prolonged effects 33.7 months after spironolactone withdrawal, whereas 20 relapsed 17.5 months after discontinuation. No significant difference in clinical and biochemical parameters was observed between these two groups both at baseline and after spironolactone treatment. Ovulatory PCOS patients were treated for a shorter time and reported earlier relapse than classic PCOS patients. Conclusion. Spironolactone is an effective and safe treatment for hyperandrogenic skin disorders, showing long-lasting effects even several months after its discontinuation.

(5) Zannad, F., 1991. Vascular and cardiac actions of aldosterone and spironolactone. Zeitschrift fur Kardiologie, 80, pp.103-105.

Abstract. Classical pharmacology confines the mechanism of action of aldosterone and its antagonists to the modulation of ion transport in the distal tubule of the nephron. The purpose of this overview is to examine the evidence for the presence of extrarenal and, namely, vascular and cardiac sites of action for aldosterone and spironolactone. Beside its specific action in primary and secondary hyperaldosteronism, spironolactone is effective in lowering blood pressure in essential hypertension, despite normal levels of aldosterone production, and without necessarily producing significant changes in Na+ and K+ urinary excretion. This is particularly the case when therapy is applied chronically and at relatively low doses. This suggests that spironolactone may act by antagonizing the effects of aldosterone directly on the cardiovascular system. Electrophysiological studies have shown that spironolactone may reduce contractions of rat portal vein strips. This action was found to be mediated by the inhibition of the slow calcium channels. Spironolactone binds to the calcium channels, at sites different from those of dihydropyridines and phenylalkylamines. It interacts at these binding sites in vascular membranes by decreasing their density and accelerating the rate of dissociation of the ligand. In humans, spironolactone 50 mg and 75 mg o.d. produced a dose-dependent decrease of total vascular resistance and in vascular reactivity to vasopressor agents....

(6) Rathnayake, D. and Sinclair, R., 2010. Use of spironolactone in dermatology. Skinmed, 8(6), pp.328-32.

Abstract. Spironolactone has been used as a potassium-sparing diuretic for more than 30 years. It is a synthetic 17-lactone steroid and primarily acts as an aldosterone antagonist. Since the accidental discovery of its antiandrogenic effects, it has been used in the treatment of many dermatologic conditions in which androgen plays a role in the pathogenesis. Antiandrogenic effects of spironolactone are exerted by reducing testosterone production and inhibiting its action on the target tissues. Spironolactone is used as a primary medical treatment for hirsutism and female pattern hair loss. Continuous treatment is required to sustain the effect. It is an effective alternative treatment for acne in women. It has the benefit of a long-term safety profile. Spironolactone should not be used in pregnancy due to its teratogenic effects and is not used in men due to the risk of feminization.

(7) Wei, L., Struthers, A.D., Fahey, T., Watson, A.D. and MacDonald, T.M., 2010. Spironolactone use and renal toxicity: population based longitudinal analysis. Bmj, 340.

Abstract. ... Despite a marked increased in the use of spironolactone in patients with and without heart failure, no increase was seen in hospital admissions for hyperkalaemia and outpatient hyperkalaemia actually fell. Careful monitoring of patients prescribed spironolactone seems to have been associated with no increase in risk of hyperkalaemia.