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 Spironolactone for female baldness
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 Cyproterone acetate for baldness

Spironolactone is an aldosterone antagonist, potassium-sparing diuretic used to clinically treat high blood pressure. Potassium-sparing diuretic acts on the kidneys to increase the flow of urine, resulting therefore to decreased amount of water in the body. The reduction of water in the body in turn helps reduce the blood pressure. Unlike some other diuretics, however, potassium-sparing diuretic medicines do not cause the body to lose an important electrolyte required by the body—potassium.

To individuals with no hyperandrogenism (an excessive production of male hormones), spironolactone therapy may reduce hair loss and it may even promote some hair growth. Moreover, in women with hirsutism, the drug decreases the growth rate and mean diameter of facial hair.

Spironolactone is a steroid that has a basic four ring steroid nucleus and is 98 percent protein bound. Its primary metabolite canrenone is at least 90 percent protein bound. Canrenone is the primary metabolite contributing to the diuretic effect of spironolactone, and it is also the active antagonist of the hormone aldosterone.

Spironolactone Absorption and Metabolism in the Body

Spironolactone is rapidly absorbed and its absorption increases with food intake; maximum plasma levels being reached in 30 to 60 minutes after ingestion. Depending on the tablet manufacturer, the percentage of the drug that is detected in the systemic circulation after oral administration exceeds 90 percent.

The liver rapidly metabolizes spironolactone. The hydrolytic product of canrenone is coronate; canrenone is inter-converted into this product enzymatically. The major metabolites canrenone and potassium canrenoate are excreted through the urine and bile, and there is no un-metabolized drug that is passed out via the urine.

Spironolactone Mechanism of Treatment

As define by Dorfman, the term anti-androgen implies prevention of the action of androgen activity at target sites. It does not include other mechanisms of decreasing androgen action such as decreasing the production of androgens, interference with androgen metabolism, or change in androgen plasma protein binding. An example of potent anti-androgen is spironolactone.

The action of spironolactone, however, is directed at both decreasing production and blocking the effect of androgens at the cellular level. Spironolactone decreases the testosterone production in the adrenal gland by depleting the microsomal cytochrome P450-dependent enzymes 17a-hydroxylase and desmolase. However, the destruction of spironolactone to the microsomal cytocrome P450 may be limited to those tissues in which microsomal 17-hydroxylase activity is high. After spironolactone binds to the 17-hydroxylase-cytochrome P450, it may convert it to spironolactone metabolite that destroys the heme portion (molecule containing iron) of cytochrome P450 resulting to the decrease in steroid 17-hydroxylation.

Spironolactone is a competitive inhibitor of DHT-receptor binding and it also interferes with the translocation of this complex into the nucleus. A strong competitor for the androgen receptor, spironolactone is a potent agonist, while canrenone on the other hand is a weak competitor thus a potent antagonist. The weak agonists are the true antagonists of endogenous and exogenous androgens; weak antagonists rely mainly on a continuous supply of the compound to achieve full inhibition. The possible production of the parent compound in the adrenal gland and the metabolite on the receptor site produces the anti-androgen effect of spironolactone.

Although it varies, the protestation activity of spironolactone influences the ratio of luteinizing hormone (LH) to follicle-stimulating hormone (FSH) by decreasing the response of LH to gonadotropin-releasing hormone (GnRH), thereby decreasing also the androgen production.

Dosage in Treatment

Spironolactone preparation is available only in 25-mg and 50-mg table. In clinical practice, spironolactone is given in dosage that varies from 50 to 300 mg per day. It can be given as a single dose or in divided doses. Similar to that found in hirsutism, the minimum threshold for effective treatment of pattern hair loss has also been found to be 100 mg daily. Minimal changes in circulating androgens are observed at doses of 100 mg per day; however, higher doses of 300 mg or more per day decreases the plasma testosterone level significantly. Moreover, this increase dosage has almost no clinical advantage at all; it only serves to increase the side effects.

Studies on the Use of Spironolactone on Hair Loss Treament

Documented reports in the literature regarding the use of spironolactone in the treatment of pattern hair loss are rare. Some small clinical trials have shown clinical effect in pattern baldness, however, spironolactone rarely offers the benefit of hair re-growth.

Studies performed so far includes women only.

  • A 12 months study in 12 women with androgen-dependent alopecia was conducted; with 6 subjects on spironolactone therapy of 75 to 100 mg per day and with the other 6 on controls, resulted in both groups to decrease in target area non-vellus hairs. However, the decrease in the control group was statistically significant. Two subjects who had their spironolactone dose doubled after 12 months from the 75 to 100 mg per day used during the first year showed enhanced non-vellus growth.
  • Six out seven female with pattern baldness treated daily with 200 mg spironolactone showed an improvement in a second study.

Spironolactone Side Effects

Hyperkalemia, an acute intoxication from potassium, is one of the potential side effects of spironolactone on both men and women. Worse effect of spironolactone on men, however, is gynocomastia – excessive development of the male breast, thus confining the systemic use to women. Other side effects on men are decreased libido and impotence. In women, the common side effects are breast tenderness, irregular menses, and mood swings. The use of concomitant oral contraceptive pill in women of childbearing age is advised because feminization of male fetus is a possible risk if pregnancy occurs while they are on spironolactone.

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