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When weight loss, diet and exercise do not adequately improve the symptoms of polycystic ovary syndrome (PCOS), drug therapy is usually initiated. There are several types of medications for the treatment of PCOS. Drugs may be given alone or in combination, may require readjustment of dosages, or may require adjustments of the particular combinations over time or with varying circumstance, (e.g., when trying to conceive).

Drugs used for the treatment of symptoms of PCOS include:

• Antiandrogens
• Oral contraceptives
• Insulin sensitizing drugs
• Glucocorticoids
• Gonadotropin releasing hormone (GnRH) agonists
• Ovulation-inducing drugs

Antiandrogens

Antiandrogens are a class of drugs that block the actions of androgens (male sex hormones such as testosterone) by preventing androgens from binding to androgen receptors on cells or by inhibiting the enzyme that converts testosterone to androgen.

Antiandrogens may be prescribed with oral contraceptives. Some of the reasons for combining them include:

• Antiandrogens may be teratogenic (may cause deformities to the fetus) and so they must be given in conjunction with birth control pills in women who are at risk of becoming pregnant.

• Each drug works differently and their combined effect is greater than either alone.

• Oral contraceptives can prevent irregular bleeding which is often a side effect of antiandrogens.

There are several antiandrogen drugs that may be used for symptoms of PCOS:

• Spironolactone (Aldactone, Spitonol)
• Flutamide (Eulexin)
• Finasteride (Proscar)
• Cyproterone acetate (Cyprostat)
• Ketoconazole

Spironolactone

Spironolactone (Aldactone, Spitonol) is a diuretic and is used to treat hypertension. Spironolactone is also active at the level of the hair follicle where it blocks the effect of androgen, thereby reducing excessive hair growth. It is usually stopped approximately 3 months before a woman plans to conceive. Spironolactone is one of the most widely used antiandrogens in the U.S.

Side effects include:

• Menstrual irregularity
• Hypotension
• Lethargy
• Increased urinary frequency
• Headache
• Mood swings
• Gastrointestinal disturbances
• Dry skin

Flutamide

Flutamide (Eulexin) is a non-steroidal antiandrogen and is used to treat prostate cancer. However, it is also very effective for hirsutism and acne. The effects of flutamide include:

• Reducing circulating androgens
• Reducing overall ovarian size
• Restoring ovulatory cycles

The efficacy of flutamide is considered to be comparable to that of spironolactone and, in addition, may have the advantage of not affecting kidney function. It is a highly effective antiandrogen, however, patients must be monitored carefully for signs of hepatotoxicity (liver toxicity) since it is metabolized by the liver.

Side effects of flutamine include:

• Dry skin
• Decreased libido
• Increased appetite
• Amenorrhea

Finasteride

Finasteride (Proscar) is used to treat benign prostatic hyperplasia (enlarged prostate) in men. Finasteride inhibits the activity of 5-alpha reductase, an enzyme that binds androgens at the level of the hair follicle.

Side effects of finasteride are rare but may include decreased libido. Since it may be teratogenic, caution must be exercised when the patient may be trying to conceive.

Cyproterone Acetate

Cyproterone acetate (Cyprostat) is a strong progestin that is very effective as an antiandrogen since it increases the metabolic clearance of androgens from the body. It is usually given with estrogen in order to prevent uterine bleeding. Liver function should be monitored for hepatotoxicity. This drug is currently not available in the United States.