Ethinylestradiol/cyproterone acetate explained

Ethinylestradiol/cyproterone acetate (EE/CPA), also known as co-cyprindiol and sold under the brand names Diane and Diane-35 among others, is a combination of ethinylestradiol (EE), an estrogen, and cyproterone acetate (CPA), a progestin and antiandrogen, which is used as a birth control pill to prevent pregnancy in women.[1] It is also used to treat androgen-dependent conditions in women such as acne, seborrhea, excessive facial/body hair growth, scalp hair loss, and high androgen levels associated with ovaries with cysts.[2] [3] [4] [5] [6] [7] The medication is taken by mouth once daily for 21 days, followed by a 7-day free interval.

Medical uses

EE/CPA is used as a combined birth control pill to prevent ovulation and pregnancy in women. It is also approved and used to treat androgen-dependent conditions in women such as acne, seborrhea, hirsutism, female pattern hair loss, and hyperandrogenism due to polycystic ovary syndrome.

Available forms

EE/CPA comes in the form of oral tablets and contains 35 or 50 μg EE and 2 mg CPA per tablet. It is taken once daily for 21 days, followed by a 7-day free interval.

Side effects

Side effects of EE/CPA include dysmenorrhea (10.2%), breast tension or tenderness (6.5%), headache (5.2%), nervousness (4.4%), chloasma (4.2%), depressed mood (3.4%), decreased libido (3.1%), varicosities (2.9%), nausea (1.9%), edema (1.7%), and dizziness (1.1%). The incidence of depression with EE/CPA is the same as that with other birth control pills.[8] [9]

Blood clots

The risk of venous thromboembolism with EE/CPA-containing birth control pills is similar to that with EE and gestodene-, desogestrel-, and drospirenone-containing birth control pills and about 50 to 80% higher than with EE and levonorgestrel-containing birth control pills.[10] [11] [12] [13] [14] The absolute risk of venous thromboembolism with EE/CPA-containing birth control pills is about 1.2 to 9.9 per 10,000 women-years.[15]

Pharmacology

EE is a synthetic estrogen, or an agonist of the estrogen receptors, the biological target of estrogens like estradiol.[16] It also has functional antiandrogenic effects by decreasing the circulating free fractions of androgens.[17] CPA is a progestin (synthetic progestogen), or an agonist of the progesterone receptors, the biological target of progestogens like progesterone. It also acts as an antiandrogen, or as an antagonist of the androgen receptor, the biological target of androgens like testosterone and dihydrotestosterone. However, it is thought that the antiandrogenic activity of CPA may only be significant at higher doses than are present in birth control pills.[18] Both EE and CPA have antigonadotropic effects and act as contraceptives in women by suppressing ovulation. The antigonadotropic effects of EE and CPA also contribute to the antiandrogenic efficacy of the medication by suppressing androgen production by the ovaries.

History

CPA/EE-containing birth control pills were developed by 1975 and were first introduced for medical use in 1978.[19] They originally contained 50 μg EE (Diane); subsequently, the EE dosage was decreased to 35 μg in a new "low-dose" preparation in 1986 (Diane-35).

Society and culture

Generic names

Co-cyprindiol, a shortened form of combination of cyproterone acetate and ethinylestradiol, is a generic name of EE/CPA.[20] [21] It is also known by its former developmental code names SHB 209 AB (Diane)[22] and SHB 209 AE (Diane-35).[23] [24] The developmental code name SH-81041 referred to a combination of high-dose 100 mg CPA and 40–50 μg EE administered in a reverse sequential regimen.[25] [26] [27]

Brand names

Brand names of EE/CPA include Diane and Diane-35, as well as Adco-Fem, Alisma, Althea, Ancea, Anuar, Avancel, Axira, Bella HEXAL, Bellgyn, Bellune, Brenda-35 ED, Chloe, Clairette, Claudia, Co-Cyprindiol, Cybelle, CyEstra-35, Cypestra-35, Cyprelle, Cyprest, Cypretil, Cypretyl, Cyproderm, Cyprodiol, Cypromix, Dafne-35, Daphne, Dialider, Diane mite, Diane-35 ED, Dianette, Diclin, Dinac, Diva-35, Dixi, Dixi-35, Drina, Elestra, Elisamylan, Elleacnelle, Erika-35, Esdian, Estelle, Estelle-35, Evashine, Evépar, Evilin, Facetix, Femina, Feminac, Feminil mite, Frauline, Giane, Giane-35, Ginet, Ginette, Gynelle, Gyneplen, Gynofen, Holgyeme, Isbela, Jennifer-35, Juliet-35 ED, Juliette, Jene, Lady-Ten, Laila-35 ED, Linface, Lunar, Manoane, Midane, Mileva, Minerva, Morea sanol, Neynna, Nortin, OC-35, Selene, Sucee, Syndi, Tess, Visofid, Vreya, Xylia, Zinnia, and Zyrona.[28]

Availability

EE/CPA is available widely throughout the world, including in Europe, North America, South America, East Asia, South Asia, Southeast Asia, and Oceania. It is notably not available in the United States or Japan.

See also

External links

Notes and References

  1. Web site: Diane 35 Label . Bayer . https://web.archive.org/web/20201112012257/https://www.bayer.ca/omr/online/diane-35-pm-en.pdf . 2020-11-12 .
  2. Miller JA, Jacobs HS . Treatment of hirsutism and acne with cyproterone acetate . Clinics in Endocrinology and Metabolism . 15 . 2 . 373–389 . May 1986 . 2941191 . 10.1016/S0300-595X(86)80031-7 .
  3. Book: Hammerstein J . Antiandrogens: Clinical Aspects . Orfanos CE, Happle R . Hair and Hair Diseases. 1990. 827–886. 10.1007/978-3-642-74612-3_35. 978-3-642-74614-7.
  4. Van der Spuy ZM, le Roux PA . Cyproterone acetate for hirsutism . The Cochrane Database of Systematic Reviews . 2003 . 4 . CD001125 . 2003 . 14583927 . 8955083 . 10.1002/14651858.CD001125 .
  5. Jing Z, Liang-Zhi X, Tai-Xiang W, Ying T, Yu-Jian J . The effects of Diane-35 and metformin in treatment of polycystic ovary syndrome: an updated systematic review . Gynecological Endocrinology . 24 . 10 . 590–600 . October 2008 . 19012104 . 10.1080/09513590802288242 . 38997400 .
  6. Bitzer J, Römer T, Lopes da Silva Filho A . The use of cyproterone acetate/ethinyl estradiol in hyperandrogenic skin symptoms - a review . The European Journal of Contraception & Reproductive Health Care . 22 . 3 . 172–182 . June 2017 . 28447864 . 10.1080/13625187.2017.1317339 . free .
  7. Ruan X, Kubba A, Aguilar A, Mueck AO . Use of cyproterone acetate/ethinylestradiol in polycystic ovary syndrome: rationale and practical aspects . The European Journal of Contraception & Reproductive Health Care . 22 . 3 . 183–190 . June 2017 . 28463030 . 10.1080/13625187.2017.1317735 . free .
  8. Raudrant D, Rabe T . Progestogens with antiandrogenic properties . Drugs . 63 . 5 . 463–492 . 2003 . 12600226 . 10.2165/00003495-200363050-00003 . 28436828 .
  9. Abstracts of the 22nd International Conference on Pharmacoepidemiology and Therapeutic Risk Management, Lisbon, Portugal, 24-27 August 2006 . Pharmacoepidemiology and Drug Safety . 15 . S1 . S1-302 . August 2006 . 16986216 . 10.1002/pds.1295 . 3586619 .
  10. Martínez F, Ramírez I, Pérez-Campos E, Latorre K, Lete I . Venous and pulmonary thromboembolism and combined hormonal contraceptives. Systematic review and meta-analysis . The European Journal of Contraception & Reproductive Health Care . 17 . 1 . 7–29 . February 2012 . 22239262 . 10.3109/13625187.2011.643836 . 20299968 .
  11. Plu-Bureau G, Maitrot-Mantelet L, Hugon-Rodin J, Canonico M . Hormonal contraceptives and venous thromboembolism: an epidemiological update . Best Practice & Research. Clinical Endocrinology & Metabolism . 27 . 1 . 25–34 . February 2013 . 23384743 . 10.1016/j.beem.2012.11.002 .
  12. Stegeman BH, de Bastos M, Rosendaal FR, van Hylckama Vlieg A, Helmerhorst FM, Stijnen T, Dekkers OM . Different combined oral contraceptives and the risk of venous thrombosis: systematic review and network meta-analysis . BMJ . 347 . f5298 . September 2013 . 24030561 . 3771677 . 10.1136/bmj.f5298 .
  13. de Bastos M, Stegeman BH, Rosendaal FR, Van Hylckama Vlieg A, Helmerhorst FM, Stijnen T, Dekkers OM . Combined oral contraceptives: venous thrombosis . The Cochrane Database of Systematic Reviews . 2014 . 3 . CD010813 . March 2014 . 24590565 . 10637279 . 10.1002/14651858.CD010813.pub2 .
  14. Dragoman MV, Tepper NK, Fu R, Curtis KM, Chou R, Gaffield ME . A systematic review and meta-analysis of venous thrombosis risk among users of combined oral contraception . International Journal of Gynaecology and Obstetrics . 141 . 3 . 287–294 . June 2018 . 29388678 . 5969307 . 10.1002/ijgo.12455 .
  15. Spitzer WO . Cyproterone acetate with ethinylestradiol as a risk factor for venous thromboembolism: an epidemiological evaluation . Journal of Obstetrics and Gynaecology Canada . 25 . 12 . 1011–1018 . December 2003 . 14663535 . 10.1016/S1701-2163(16)30342-5 .
  16. Kuhl H . Pharmacology of estrogens and progestogens: influence of different routes of administration . Climacteric . 8 . Suppl 1 . 3–63 . August 2005 . 16112947 . 10.1080/13697130500148875 . 24616324 .
  17. Ekback MP . Hirsutism, What to do? . International Journal of Endocrinology and Metabolic Disorders . 3 . 3 . 2017 . 10.16966/2380-548X.140 . 2380-548X . PDF . free .
  18. Pucci E, Petraglia F . Treatment of androgen excess in females: yesterday, today and tomorrow . Gynecological Endocrinology . 11 . 6 . 411–433 . December 1997 . 9476091 . 10.3109/09513599709152569 .
  19. Book: Plewig G, Kligman AM . Antiandrogens and Aldosterone Antagonists . Acne and Rosacea . https://books.google.com/books?id=0cD-CAAAQBAJ&pg=PA685 . 6 December 2012. Springer Science & Business Media. 978-3-642-59715-2. 662, 685.
  20. Book: Benvenga S . Therapy of Hirsutism . Farid NR, Diamanti-Kandarakis E . Diagnosis and Management of Polycystic Ovary Syndrome. https://books.google.com/books?id=fgMYVxmPDnMC&pg=PA237. 27 February 2009. Springer Science & Business Media. 978-0-387-09718-3. 237–.
  21. Book: Layton M . Treatment of hyperandrogenism in polycystic ovary syndrome . Balen A, Franks S, Homburg R, Kehoe S . Current Management of Polycystic Ovary Syndrome. https://books.google.com/books?id=0rtUBAAAQBAJ&pg=PA131. October 2010. Cambridge University Press. 978-1-906985-41-7. 131–.
  22. Lachnitt-Fixson U, Kaufmann J . Zur bein flussung von androgenisierungsercheinungen-doppelblind. Studium eines cyproteronacetat-haltiges praparats (SHB 209 AB) gegen neogynon. . Med. Klin. . 72 . 1977 . 1922–1926 .
  23. Fedele L, Cavalli G, Marchini M, Carinelli S, Candiani GB . Effect of a new oral antiandrogen-estrogen combination on the endometrium: histological and ultrastructural scanning electron microscopy study . Acta Europaea Fertilitatis . 17 . 1 . 9–13 . 1986 . 3727896 .
  24. Fedele L, Marchini M, Cavalli G, Baglioni A, Taccagni GL . Marked deciliation and insufficient secretory modification of endometrial surface during treatment with a new progestogen-estrogen combination . Contraception . 35 . 5 . 497–505 . May 1987 . 3621944 . 10.1016/0010-7824(87)90086-2 .
  25. Book: Hammerstein J . Antiandrogens — Basic Concepts for Treatment . Orfanos CE, Montagna W, Stüttgen G. Hair Research. 1981. 330–335. 10.1007/978-3-642-81650-5_49. 978-3-642-81652-9.
  26. Grund E, Schmidt-Elmendorff H . Behandlung von Virilisierungs-Erscheinungen: vergleichende Klinische Untersuchung zweier antiandrogenwirksamer Gestagene--Cyproteronazetat, Megestrolazetat . The treatment of virilizing syndromes. Comparative clinical studies of 2 antiandrogen-active gestagens (cyproterone acetate, megestrol acetate . de . Die Medizinische Welt . 26 . 48 . 2180–2187 . November 1975 . 128684 .
  27. Hammerstein J, Meckies J, Leo-Rossberg I, Moltz L, Zielske F . Use of cyproterone acetate (CPA) in the treatment of acne, hirsutism and virilism . Journal of Steroid Biochemistry . 6 . 6 . 827–836 . June 1975 . 126335 . 10.1016/0022-4731(75)90311-8 .
  28. Web site: Cyproterone. Drugs.com.

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Ethinylestradiol/cyproterone acetate".

Except where otherwise indicated, Everything.Explained.Today is © Copyright 2009-2024, A B Cryer, All Rights Reserved. Cookie policy.