Cyproterone chemical structure
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Cyproterone

Cyproterone acetate (Androcur®, Cyprostat®, Cyproteron®, Procur®, Cyprone®, Cyprohexal®, Ciproterona®, Cyproteronum®, Neoproxil®) is an antiandrogen, i.e., it suppresses the actions of testosterone (and its metabolite dihydrotestosterone) on tissues. It acts by blocking androgen receptors which prevents dihydrotestosterone from binding to them and suppresses luteinizing hormone (which in turn reduces testosterone levels). more...

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Its main indications are prostate cancer, benign prostatic hyperplasia, priapism, hypersexuality and other conditions in which androgen action maintains the disease process. Due to its anti-androgen effect, it can also be used to treat hirsutism, and is a common component in hormone therapy for male-to-female transgendered people.

Until the development of leuprolide, cyproterone was one of the few drugs used to treat precocious puberty. It was also used in animal experimentation to investigate the actions of androgens in fetal sexual differentiation.

In addition, its acetate form (cyproterone acetate) has weak progestational activity (e.g., it acts like progesterone). As part of some contraceptive pills (Diane®) it decreases acne and hirsutism (male-pattern hair growth).

Side-effects in men include gynecomastia (breast growth) and galactorrhea (milk outflow). Erectile dysfunction is a direct result of its mode of action.

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Treatment of female pattern hair loss with oral antiandrogens
From Journal of Drugs in Dermatology, 7/1/05

Treatment of Female Pattern Hair Loss with Oral Antiandrogens

Sinclair R, MD, et al. British Journal of Dermatology. 2005;152:466-473.

Summary

The authors present an open intervention study to assess if antiandrogen therapy is effective in the treatment of female pattern hair loss. Eighty women were entered into the study, all of whom underwent clinical evaluation and biopsy of the central mid scalp to provide both clinical and histologic evidence of female pattern hair loss. Patients also had hematologic screening to exclude systemic lupus erythematosus, thyroid disease, zinc and iron deficiency, and hormone dysregulation. Patients were then divided into 2 treatment arms. Forty women received spironolactone 200 mg daily. The other 40 women received cyproterone acetate, the dose of which was determined by the presence or absence of menopause. Twenty-two post-menopausal women received 50 mg daily, while 18 pre-menopausal women received 100 mg daily for 10 days of every month in combination with oral contraceptive pills. Sixteen months was the average treatment duration. Patients were not allowed to use topical minoxidil. At baseline and then every 6 months, photography of the frontal and vertex scalp was performed on each patient. Assessment of these photographs was completed by 3 clinicians, blinded as to patient information and to treatment regimen, using a rating scale of increased hair density, decreased hair density, or no change. The frontal and vertex areas of the scalp were given independent ratings. Photographic assessment served as the primary outcome for efficacy. Clinical grading of the mid scalp using a standard scale was also done. Analysis of the data showed no difference between the 2 treatment arms so the authors combined the results of both arms. Forty-four percent of women had increased hair density in either the frontal or vertex areas, or both. Another 44% showed no increase or decrease in hair density. Twelve percent showed decreased hair density in one or both areas. Variables such as menopausal status, family history of hair loss, thyroid function, duration of hair loss, and patient age showed no statistically significant difference regarding treatment response. However, women with advanced hair loss of the mid scalp and hence a mid scalp clinical grade of 3 or 4 did show a statistically significant difference in regards to response compared with those of lesser grades. Adverse effects of the 2 treatments were not discussed in the article.

Comment

Despite no control arm, this was a well-designed study to assess the efficacy of oral antiandrogens in the treatment of women with female pattern hair loss. Patients were carefully selected after both clinical and histologic evaluation so as to include only those with true female pattern hair loss. Also, photography was standardized using a stereotactic device to allow for consistent imaging of the scalp. The results were encouraging. Regardless of hair regrowth, continued loss of hair can be very frustrating and upsetting for patients. While 44% of patients had regrowth of hair, another 44% had no continued loss and this may be seen as success in some patients' eyes. This study merits a place-bo-controlled trial to better evaluate the efficacy of these antiandrogens. Long-term follow-up after treatment is discontinued is needed to evaluate duration of treatment success.

COPYRIGHT 2005 Journal of Drugs in Dermatology, Inc.
COPYRIGHT 2005 Gale Group

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