Spironolactone is a popular anti androgen treatment for hirsutism

Information on hirsutism and hair removal treatments
Cosmetic hair removal
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Finasteride
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Spironolactone
Flutamide
Cyproterone acetate
Eflornithine
Ketoconazole
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Spironolactone for Hirsutism

Spironolactone medication is an effective method of treating hyperandrogenism and its related disorders. Spironolactone acts as an antiandrogen, aldosterone antagonist and mild potassium-sparing diuretic. It was originally used in the treatment of hypertension and was first suggested as a therapy for hirsutism (excess hair growth in women) caused by hyperandrogenism in 1978.

The anti-androgenic activity of spironolactone

Spironolactone has various androgen suppressing activities. They are:

  • Inhibits various enzymes that regulate biosynthesis of androgens. Most importantly it inhibits cytochrome P4S0 enzymes that has a key role in ovarian and adrenal steroidogenesis
  • Blocks DHT binding to skin androgen receptors
  • Elevates sex hormone–binding globulin (SHBG) concentration
  • Boosts testosterone clearance from the body
  • Competes with and reduces 5 a-reductase activities

Effectiveness

Though spironolactone has shown considerable therapeutic results in reducing hirsutism, irrespective of the seriousness of the condition, it is the prescribed dose that determines its effectiveness.

Herein, the dosage is dependent on the weight of the patient. In case of lean women and mild cases, a starting dose of 100 mg per day is substantial. However, in case of severe hirsutism and obese patients, a higher daily dose of 200 or 300 mg may be required for effective results. Thereafter, the maintenance dose can be dropped to 25–100 mg daily.

The success rate of spironolactone in the treatment of hirsutism has been investigated and published in a study called the Cochrane Review in 2003. This statistical survey reported a noteworthy decrease in hirsutism (at the backdrop of the most popular Ferriman–Gallwey (F–G) evaluation method) in women administered both the 100 and 200 mg daily doses of the drug.

Comparisons with other anti-androgens treating hirsutism has reported mixed results:

  • Spironolactone (100 mg/day) more effective than finasteride (5 mg/day) and cyproterone acetate (12.5 mg/day)
  • Spironolactone at the same dose less effective than flutamide (500 mg/day) in reducing F–G scores. Herein, flutamide also acted faster causing a considerable reduction in hirsutism scores after only 3 months of usage. An additional 5 months of spironolactone was needed for better results.

Side-effects of spironolactone

The adverse effects of the usage of this drug include dyspepsia, polydypsia, polyuria, nausea, headaches, weakness, gastritis, breast tenderness, ovulatory disorders (causing polymenorrhea), reduced libido, sun hypersensitivity and atopic reactions.

As an aldosterone antagonistic agent, spironolactone also has a diuretic effect and can also cause hyperkalemia. However, hyperkalemia has till date been reported in older women, diabetic patients, those using drugs (potassium-saving diuretic) or have a diet that increase serum potassium levels or cases with renal disorders. It has still now spared fit, young PCOS women.

The best way to decrease side-effects is to use an initial daily dose of 25 mg, which should be gradually increased over a span of 3 weeks. Spironolactone should generally be given for a maximum of 6 months at a stretch to achieve the best therapeutic results for hirsutism.

Gradual re-growth of hair also occurs by the use of spironolactone. This maybe due to effects of long-term drug use or the restoration of the normal hair production process. This can be managed with a variation in the administered doses.

In reproductive women who are not using oral contraceptives while on spironolactone, an estimated one in five cases will have more frequent menses. This is possibly the result of the weak progestational potency of spironolactone.

Use of spironolactone on pregnant women is also not advisable, though the drug has not reported ambiguous genitalia in exposed fetuses. Since there is also a possibility of teratogenic effects (that result in the feminization of a male fetus) by using spironolactone, a combination of the drug and an oral contraceptive pill (OCP) is often prescribed. A combined treatment of androgen receptor blockers such as spironolactone, flutamide, and cyproterone acetate and oral contraceptives is also beneficial to check the teratogenic effects of the anti-androgens. Herein, oral contraceptives often help decrease menstrual irregularity, provide safe and adequate contraception and at the same time increase the effectiveness of the treatment by inhibiting serum androgen concentration.

A patient must undergo at least 2 years of this kind of combined therapy (with a gradual progressive decrease of the dose of the anti-androgen) for best results and minimum side effects.

Spironolactone and acne treatment

Spironolactone has also proved effective in reducing sebum production and acne treatment. The suggested clinical dose for acne cure is 50–100 mg/day. However, some patients show results with only a daily dose of 25 mg of the drug. Here to, dermatologists often use a combination of spironolactone and oral contraceptives for more resistant adult patients and better results.


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