Ethinylestradiol/cyproterone acetate

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Ethinylestradiol/cyproterone acetate
Ethinylestradiol (top) and
cyproterone acetate (bottom)
Combination of
EthinylestradiolEstrogen
Cyproterone acetateProgestogen; Antiandrogen
Clinical data
Trade namesDiane, Diane-35, others
Other namesEE/CPA; Co-cyprindiol; SHB 209 AB; SHB 209 AE; SH-81041
Routes of
administration		By mouth
Drug classEstrogen; Progestogen; Antiandrogen
ATC code
Legal status
Legal status
Identifiers
CAS Number
PubChem CID

Ethinylestradiol/cyproterone acetate (EE/CPA), also known as co-cyprindiol and sold under the brand names Diane and Diane-35 among others, is a

scalp hair loss, and high androgen levels associated with ovaries with cysts.[3][4][5][6][7][8] The medication is taken by mouth once daily for 21 days, followed by a 7-day free interval.[2]

Medical uses

EE/CPA is used as a

female pattern hair loss, and hyperandrogenism due to polycystic ovary syndrome.[2][3][4][5][6][7][8]

Available forms

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

Side effects

decreased libido (3.1%), varicosities (2.9%), nausea (1.9%), edema (1.7%), and dizziness (1.1%).[2] The incidence of depression with EE/CPA is the same as that with other birth control pills.[9][10]

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.[11][12][13][14][15] 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.[16]

Risk of venous thromboembolism (VTE) with hormone therapy and birth control (QResearch/CPRD)
Type Route Medications Odds ratio (95% CITooltip confidence interval)
Menopausal hormone therapy
 Oral Estradiol alone
    ≤1 mg/day
    >1 mg/day		 1.27 (1.16–1.39)*
1.22 (1.09–1.37)*
1.35 (1.18–1.55)*
Conjugated estrogens alone
    ≤0.625 mg/day
    >0.625 mg/day		 1.49 (1.39–1.60)*
1.40 (1.28–1.53)*
1.71 (1.51–1.93)*
Estradiol/medroxyprogesterone acetate 1.44 (1.09–1.89)*
Estradiol/dydrogesterone
    ≤1 mg/day E2
    >1 mg/day E2		 1.18 (0.98–1.42)
1.12 (0.90–1.40)
1.34 (0.94–1.90)
Estradiol/norethisterone
    ≤1 mg/day E2
    >1 mg/day E2		 1.68 (1.57–1.80)*
1.38 (1.23–1.56)*
1.84 (1.69–2.00)*
Estradiol/norgestrel or estradiol/drospirenone
 1.42 (1.00–2.03)
Conjugated estrogens/medroxyprogesterone acetate 2.10 (1.92–2.31)*
Conjugated estrogens/norgestrel
    ≤0.625 mg/day CEEs
    >0.625 mg/day CEEs		 1.73 (1.57–1.91)*
1.53 (1.36–1.72)*
2.38 (1.99–2.85)*
Tibolone alone 1.02 (0.90–1.15)
Raloxifene alone 1.49 (1.24–1.79)*
Transdermal
 Estradiol alone
   ≤50 μg/day
   >50 μg/day		 0.96 (0.88–1.04)
0.94 (0.85–1.03)
1.05 (0.88–1.24)
Estradiol/progestogen 0.88 (0.73–1.01)
Vaginal
 Estradiol alone 0.84 (0.73–0.97)
Conjugated estrogens alone 1.04 (0.76–1.43)
Combined birth control
 Oral Ethinylestradiol/norethisterone 2.56 (2.15–3.06)*
Ethinylestradiol/levonorgestrel 2.38 (2.18–2.59)*
Ethinylestradiol/norgestimate
 2.53 (2.17–2.96)*
Ethinylestradiol/desogestrel 4.28 (3.66–5.01)*
Ethinylestradiol/gestodene 3.64 (3.00–4.43)*
Ethinylestradiol/drospirenone 4.12 (3.43–4.96)*
Ethinylestradiol/cyproterone acetate 4.27 (3.57–5.11)*
Notes: (1)
Bioidentical progesterone was not included, but is known to be associated with no additional risk relative to estrogen alone. Footnotes: * = Statistically significant
(p < 0.01). Sources: See template.

Pharmacology

Main article: Ethinylestradiol § Pharmacology of cyproterone acetate

EE is a

antigonadotropic effects and act as contraceptives in women by suppressing ovulation.[17] The antigonadotropic effects of EE and CPA also contribute to the antiandrogenic efficacy of the medication by suppressing androgen production by the ovaries.[18]

History

CPA/EE-containing birth control pills were developed by 1975[20][21] and were first introduced for medical use in 1978.[22] 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).[4][23][24]

Society and culture

Generic names

Co-cyprindiol, a shortened form of combination of cyproterone acetate and ethinylestradiol, is a

generic name of EE/CPA.[25][26][27] It is also known by its former developmental code names SHB 209 AB (Diane)[28][21][29] 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.[28][20][21]

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.[25]

Availability

Availability of CPA in countries throughout the world (as of March 2018). Turquoise is combined with an estrogen at a low dose, dark blue is alone at a high dose, and light blue is both available.

EE/CPA is available widely throughout the world, including in Europe, North America, South America, East Asia, South Asia, Southeast Asia, and Oceania.[25] It is notably not available in the United States or Japan.[25]

See also

References

  1. ^ "List of nationally authorised medicinal products" (PDF). European Medicines Agency.
  2. ^ a b c d e f g "Diane 35 Label" (PDF). Bayer. Archived from the original (PDF) on 2020-11-12.
  3. ^
    PMID 2941191
    .
  4. ^
    ISBN 978-3-642-74614-7
    .
  5. ^
    PMID 14583927
    .
  6. ^
    S2CID 38997400
    .
  7. ^
    PMID 28447864
    .
  8. ^
    PMID 28463030
    .
  9. S2CID 28436828
    .
  10. S2CID 3586619
    .
  11. S2CID 20299968
    .
  12. PMID 23384743
    .
  13. PMID 24030561
    .
  14. PMID 24590565
    .
  15. PMID 29388678
    .
  16. PMID 14663535
    .
  17. ^
    S2CID 24616324
    .
  18. ^
    ISSN 2380-548X
    .
  19. PMID 9476091
    .
  20. ^
    PMID 128684
    .
  21. ^
    PMID 126335
    .
  22. ISBN 978-3-642-59715-2
    .
  23. ^
    PMID 3727896
    .
  24. ^
    PMID 3621944
    .
  25. ^ a b c d "Cyproterone". Drugs.com.
  26. ISBN 978-0-387-09718-3
    .
  27. ISBN 978-1-906985-41-7
    .
  28. ^
    ISBN 978-3-642-81652-9
    .
  29. ^ Lachnitt-Fixson U, Kaufmann J (1977). "Zur bein flussung von androgenisierungsercheinungen-doppelblind. Studium eines cyproteronacetat-haltiges praparats (SHB 209 AB) gegen neogynon". Med. Klin. 72: 1922–1926.

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