Estradiol valerate/cyproterone acetate

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 in women.[1] It is taken by mouth.[1] Climen, which is used in menopausal hormone therapy, is a sequential preparation that contains 2 mg estradiol valerate and 1 mg CPA.[2][3][4] It was the first product for use in menopausal hormone therapy containing CPA to be marketed[3] and is available in more than 40 countries.[2] 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.[5]

Estradiol valerate /
cyproterone acetate
Estradiol valerate (top) and
cyproterone acetate (bottom)
Combination of
Estradiol valerateEstrogen
Cyproterone acetateProgestogen
Clinical data
Trade namesClimen, Femilar
Other namesEV/CPA
Routes of
administration		By mouth
Drug classEstrogen; Progestogen
Legal status
Legal status
Identifiers
CAS Number

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.[6][7][8][9][10][11] 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).[5][12][1]

See also

References
  1. Hirvonen E, Stenman UH, Mälkönen M, Rasi V, Vartiainen E, Ylöstalo P (October 1988). "New natural oestradiol/cyproterone acetate oral contraceptive for pre-menopausal women". Maturitas. 10 (3): 201–13. doi:10.1016/0378-5122(88)90023-0. PMID 2972897.
  2. Husmann, Friedrich (1997). "Clinical Experiences with a Combination of Estradiol Valerate and Cyproterone Acetate for Hormone Replacement". Women's Health and Menopause. Medical Science Symposia Series. Vol. 11. pp. 257–261. doi:10.1007/978-94-011-5560-1_38. ISBN 978-94-010-6343-2. ISSN 0928-9550.
  3. Schneider HP (November 2003). "Androgens and antiandrogens". Ann. N. Y. Acad. Sci. 997 (1): 292–306. Bibcode:2003NYASA.997..292S. doi:10.1196/annals.1290.033. PMID 14644837. S2CID 8400556.
  4. Schneider HP (December 2000). "The role of antiandrogens in hormone replacement therapy". Climacteric. 3 Suppl 2: 21–7. PMID 11379383.
  5. Fruzzetti F, Trémollieres F, Bitzer J (May 2012). "An overview of the development of combined oral contraceptives containing estradiol: focus on estradiol valerate/dienogest". Gynecol Endocrinol. 28 (5): 400–8. doi:10.3109/09513590.2012.662547. PMC 3399636. PMID 22468839.
  6. Endrikat J, Gerlinger C, Richard S, Rosenbaum P, Düsterberg B (December 2011). "Ovulation inhibition doses of progestins: a systematic review of the available literature and of marketed preparations worldwide". Contraception. 84 (6): 549–57. doi:10.1016/j.contraception.2011.04.009. PMID 22078182.
  7. Spona J, Schneider WH, Bieglmayer C, Schroeder R, Pirker R (1979). "Ovulation inhibition with different doses of levonorgestrel and other progestogens: clinical and experimental investigations". Acta Obstet Gynecol Scand Suppl. 88: 7–15. doi:10.3109/00016347909157223. PMID 393050. S2CID 30486799.
  8. Spona J, Huber J, Schmidt JB (July 1986). "Inhibierung der Ovulation mit 35 μg Athinylöstradiol und 2 mg Cyproteronazetat (Diane®-35)" [Inhibition of ovulation with 35 micrograms of ethinyl estradiol and 2 mg of cyproterone acetate (Diane 35)]. Geburtshilfe Frauenheilkd (in German). 46 (7): 435–8. doi:10.1055/s-2008-1026659. PMID 3093307.
  9. Spona J, Huber J (1987). "Efficacy of low-dose oral contraceptives containing levonorgestrel, gestoden and cyproterone acetate". Gynecol Obstet Invest. 23 (3): 184–93. doi:10.1159/000298860. PMID 2954886.
  10. Spona, J.; Huber, J.; Schmidt, J. B. (1987-12-31). "Ovulation inhibitory effect of SH B 209 AE (Diane-35)—a new antiandrogen-estrogen combination". In Schindler, Adolf E. (ed.). Antiandrogen-Estrogen Therapy for Signs of Androgenization. Berlin, Boston: De Gruyter. pp. 51–58. doi:10.1515/9783110866902-006. ISBN 9783110866902.
  11. Hammerstein, J. (1990). "Antiandrogens: Clinical Aspects". Hair and Hair Diseases. Berlin, Heidelberg: Springer Berlin Heidelberg. pp. 827–886. doi:10.1007/978-3-642-74612-3_35. ISBN 978-3-642-74614-7.
  12. Hirvonen E, Allonen H, Anttila M, Kulmala Y, Ranta T, Rautiainen H, Sipilä P, Ylöstalo P (January 1995). "Oral contraceptive containing natural estradiol for premenopausal women". Maturitas. 21 (1): 27–32. doi:10.1016/0378-5122(94)00856-3. PMID 7731379.



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