How anti androgens are used to treat acne

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Anti-androgens in Acne Treatment

Acne results from blockage of hair follicles with excessive sebum production. Androgens are sex hormones that stimulate the production of sebum and in effect are the main cause of acne formation. Therefore, for effective acne treatment, the influence of androgens must be reduced. Anti-androgens are drugs that block the effect of androgens on sebaceous glands. Common types of anti-androgens in use currently are inocoterone acetate, spironolactone, cyproterone acetate, flutamide and the newer 5 alpha reductase inhibitors.

1) Topical inocoterone acetate: Inocoterone is a non-steroidal antiandrogen. It has been shown to produced a small but significant reduction of inflamed acne. It however does not reduce the number of comedonal acne lesions and the rate of sebum secretion.

2) Spironolactone: This is a synthetic steroid that blocks the androgen receptor and inhibits the enzyme 5 alpha reductase in the skin. It decreases sebum secretion by 30 to 50%. Recommended doses are 50-100mg daily; however women with inflammatory acne lesions have been know to respond to a 25mg. dose. Common side effects include inducement of high potassium levels, breast tenderness, menstrual irregularities, testicular atrophy and erectile dysfunction. Pregnancy during spironolactone therapy should be avoided.

3) Cyproterone acetate: This synthetic steroidal antiandrogen acts by inhibiting ovulation and topically by blocking the androgen receptors on cells in sebaceous gland. Thus it serves both as an oral contraceptive and as anti-acne therapy. Given in doses of 2mg. to 100mg per day it has shown improvement in 75 – 90% women with acne. It has a comparable effects topically as compared to oral dosing after three months of therapy. However the levels achieve by topical application are naturally lower than oral medication. The most serious potential side effect is liver toxicity. Patients should be regularly monitored for changes in liver functions, especially if they are taking high doses.

4) Flutamide: It is the oldest antiandrogen with potent non-steroidal antiandrogenic actions. However it also has the most adverse side effects. It is administered orally in doses of 250mg daily in combination with an oral contraceptive. Liver function tests should be monitored during treatment since it can cause hepatitis. Being an antiandrogen it can be teratogenic, i.e. cause birth defect in children conceived by women on this drug during pregnancy. Hence the risk – benefit ratio should be well assessed prior to use of this drug in women. Flutamide has therefore been largely replaced by bicalutamide, a newer drug in this class with less serious side effccts.

5) 5-alpha reductase inhibitors: Finasteride is a 5-alpha reductase inhibitor, which leads to reduction in androgens in skin. Some small studies in Europe suggest finasteride can be quite effective for acne. Some doctors use finasteride alone in men and combine it with oral contraceptives in women treat acne. Such an approach is not approved for use in North America though.

Disadvantages of anti-androgens

The main disadvantage of antiandrogens is that they cannot be used in male patients orally, since they cause reversal of secondary male sex characteristics, reduced activity of the male organs and reduced sexual desire. For men the only practical option is finasteride. While officially used to treat pattern-baldness, some dermatologists use it to treat acne as well.

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