There are two main types of hormonal acne treatments prescribed today- oral contraceptives (birth control pills) and anti-androgens. Anti-androgens are a group of hormone receptor antagonist compounds that are capable of preventing or inhibiting the biologic effects of androgens, the male sex hormones on sebaceous glands, and are effective in acne treatment. Common anti-androgens in use for acne treatment are inocoterone acetate, spironolactone, cyproterone acetate, flutamide and the newer 5 alpha reductase inhibitors.
How do anti-androgens work?
Anti-androgens are a class of drugs that reduce androgen production in ovaries and adrenal glands, and block androgen reception by cells in sebaceous follicles. Reduction of excess androgen and reduction of androgen available in the sebaceous follicle are effects useful for acne treatment.
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Which are the common anti-androgens for acne treatment?
- Topical inocoterone acetate is a non-steroidal anti-androgen which is known to cause significant reduction of inflamed acne. It however does not decrease the number of comedonal acne lesions and the rate of sebum secretion.
- Spironolactone is a synthetic steroidal anti-androgen that decreases sebum secretion by 30 to 50%. The dose of spironolactone is usually slowly increased from 50 to 200 mg daily, taken at night. It may take six or more months to see improvement in acne. Common side effects include inducement of high potassium levels, breast tenderness, menstrual irregularities, testicular atrophy and erectile dysfunction.
- Cyproterone acetate is a synthetic steroidal anti-androgen that is effective in acne treatment. It has shown comparable efficacy in both oral and topical administration. Given in doses of 2-100mg daily, it has shown improvement in 75–90% women with acne. The most serious potential side effect is liver toxicity.
- Flutamide is a potent non-steroidal pure anti-androgen, orally taken, and has been shown to be effective in acne treatment. It is administered in doses of 250mg daily in combination with an oral contraceptive. Fatal hepatitis has rarely been reported with flutamide use. It can also cause birth defects in children conceived by women on this drug during pregnancy.
- Finasteride is a 5-alpha reductase inhibitor that can be quite effective in acne treatment. 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.
What are the side effects of anti-androgens?
Side effects of anti-androgen drugs may include irregular menstruation, tender breasts, headache, and fatigue.***Accompanying anti-androgens with oral contraceptives may ease these side effects.***
What is the drawback of using anti-androgens?
The main drawback of anti-androgens is that they cannot be used in male patients orally, since they cause turnaround of secondary male sex characteristics, minimize the 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 for acne treatment as well.
What are the contra-indications of anti-androgens?
You should not use anti-androgens if you are pregnant; have renal insufficiency or have abnormal menstrual bleeding.