Estradiol valerate/cyproterone acetate explained

Estradiol valerate/cyproterone acetate (EV/CPA), sold under the brand names Climen and Femilar among others, is a combination product of estradiol valerate (EV), an estrogen, and cyproterone acetate (CPA), a progestogen, which is used in menopausal hormone therapy and as a birth control pill to prevent pregnancy. It is taken by mouth. Climen, which is used in menopausal hormone therapy, is a sequential preparation that contains 2 mg estradiol valerate and 1 mg CPA.[1] [2] [3] It was the first product for use in menopausal hormone therapy containing CPA to be marketed and is available in more than 40 countries. Femilar, which is an estradiol-containing birth control pill, contains 1 to 2 mg estradiol valerate and 1 to 2 mg CPA, and has been approved for use in Finland since 1993.[4]

CPA alone has been found to suppress ovulation in 3 of 5 women at a dose of 0.5 mg/day and in 5 of 5 women at a dose of 1 mg/day.[5] [6] [7] [8] [9] [10] Ovulation inhibition with Femilar occurred in 94.4% of 108 women during the third treatment cycle in one study and in almost 100% of 26 women over 12 treatment cycles in another study (except for one woman who ovulated during her first treatment cycle).[11] [12]

See also

Notes and References

  1. Book: Husmann F . Clinical Experiences with a Combination of Estradiol Valerate and Cyproterone Acetate for Hormone Replacement . Women's Health and Menopause. 11. 1997. 257–261. 0928-9550. 10.1007/978-94-011-5560-1_38. Medical Science Symposia Series. Springer . 978-94-010-6343-2.
  2. Schneider HP . Androgens and antiandrogens . Annals of the New York Academy of Sciences . 997 . 1 . 292–306 . November 2003 . 14644837 . 10.1196/annals.1290.033 . 8400556 . 2003NYASA.997..292S .
  3. Schneider HP . The role of antiandrogens in hormone replacement therapy . Climacteric . 3 . Suppl 2 . 21–27 . December 2000 . 11379383 .
  4. Fruzzetti F, Trémollieres F, Bitzer J . An overview of the development of combined oral contraceptives containing estradiol: focus on estradiol valerate/dienogest . Gynecological Endocrinology . 28 . 5 . 400–408 . May 2012 . 22468839 . 3399636 . 10.3109/09513590.2012.662547 .
  5. Endrikat J, Gerlinger C, Richard S, Rosenbaum P, Düsterberg B . Ovulation inhibition doses of progestins: a systematic review of the available literature and of marketed preparations worldwide . Contraception . 84 . 6 . 549–557 . December 2011 . 22078182 . 10.1016/j.contraception.2011.04.009 .
  6. Spona J, Schneider WH, Bieglmayer C, Schroeder R, Pirker R . Ovulation inhibition with different doses of levonorgestrel and other progestogens: clinical and experimental investigations . Acta Obstetricia et Gynecologica Scandinavica. Supplement . 88 . 7–15 . 1979 . 393050 . 10.3109/00016347909157223 . 30486799 .
  7. Spona J, Huber J, Schmidt JB . [Inhibition of ovulation with 35 micrograms of ethinyl estradiol and 2 mg of cyproterone acetate (Diane 35)] . German . Geburtshilfe und Frauenheilkunde . 46 . 7 . 435–438 . July 1986 . 3093307 . 10.1055/s-2008-1026659 . 260156932 . Inhibition of ovulation with 35 micrograms of ethinyl estradiol and 2 mg of cyproterone acetate (Diane 35) .
  8. Spona J, Huber J . Efficacy of low-dose oral contraceptives containing levonorgestrel, gestoden and cyproterone acetate . Gynecologic and Obstetric Investigation . 23 . 3 . 184–193 . 1987 . 2954886 . 10.1159/000298860 .
  9. Book: Spona J, Huber J, Schmidt JB . Schindler AE . Antiandrogen-Estrogen Therapy for Signs of Androgenization . Ovulation inhibitory effect of SH B 209 AE (Diane-35)—a new antiandrogen-estrogen combination . De Gruyter . Berlin, Boston . 1987-12-31 . 10.1515/9783110866902-006 . 51–58. 9783110866902 .
  10. Book: Hammerstein J . Hair and Hair Diseases . Antiandrogens: Clinical Aspects . Springer Berlin Heidelberg . Berlin, Heidelberg . 1990 . 10.1007/978-3-642-74612-3_35 . 827–886. 978-3-642-74614-7 .
  11. Hirvonen E, Allonen H, Anttila M, Kulmala Y, Ranta T, Rautiainen H, Sipilä P, Ylöstalo P . 6 . Oral contraceptive containing natural estradiol for premenopausal women . Maturitas . 21 . 1 . 27–32 . January 1995 . 7731379 . 10.1016/0378-5122(94)00856-3 .
  12. Hirvonen E, Stenman UH, Mälkönen M, Rasi V, Vartiainen E, Ylöstalo P . New natural oestradiol/cyproterone acetate oral contraceptive for pre-menopausal women . Maturitas . 10 . 3 . 201–213 . October 1988 . 2972897 . 10.1016/0378-5122(88)90023-0 .

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