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Cyproterone acetate

Cyproterone acetate (CPA), also Cyproterone acetate ( English Cyproterone acetate ), sold separately under the Androcur trademark or together with ethinyl estradiol under the Diane or Diane-35 trademark, is an antiandrogen and progestogen . Used in the treatment of androgen-dependent diseases, such as acne , excessive hair growth , early puberty; with prostate cancer ; as a component of feminizing hormone therapy in transgender women; and for [1] [2] [3] [4] [5] . It is used both separately and in combination with estrogen and is available both for oral use and for intramuscular injection . CPA is taken either orally one to three times a day, or by intramuscular injection once or twice a week.

Cyproterone acetate
Chemical compound
Gross formulaC 24 H 29 ClO 4
Cas
PubChem
Drugbank
Other names
Androcur, Cyproterone Acetate, Cyprostat, SH-714

Common side effects of high doses of CPA in men include gynecomastia (breast development) and feminization . In both men and women, side effects of CPA include decreased sex hormones, reversible infertility , sexual dysfunction, mental symptoms such as depression, fatigue and irritability, vitamin B12 deficiency, and . At very high doses, cardiovascular complications may occur. Rare but serious adverse reactions to CPA include blood clots , liver damage, and certain types of benign brain tumors . CPA can also cause adrenal insufficiency in the form of withdrawal symptoms with a sharp cessation of taking large doses of the drug. CPA blocks the action of androgens in the body, such as testosterone , preventing their interaction with their biological target, androgen receptor (AR), and reduces their production by gonads and, therefore, their concentration in the body [1] [3] [6] . In addition, it exerts a progesterone-like effect by activating (PR) [1] [3] . The drug also has weak cortisol-like effects at high doses [1] .

CPA was opened in 1961 [7] . Initially, it was developed as a progestin [7] . In 1965, its antiandrogenic effect was discovered [8] . CPA was first introduced on the market as an antiandrogen in 1973 and was the first antiandrogen to be introduced into medical practice [9] . A few years later, in 1978, CPA was introduced as a progestin in birth control pills [10] . It is considered a “first generation” progestin [11] .

Content

  • 1 Application
    • 1.1 Contraception
    • 1.2 Skin and hair
    • 1.3 High levels of androgens
    • 1.4 Hormone therapy
    • 1.5 Prostate Cancer
    • 1.6 Sexual Deviations
    • 1.7 Early puberty
    • 1.8 Other applications
  • 2 notes

Application

Contraception

CPA is used together with ethinyl estradiol as a combined birth control pill to prevent pregnancy in women. This combination of contraceptives has existed since 1978 [10] . The drug is taken once every day for 21 days, followed by a break of 7 days [12] . CPA has also been available in Finland since 1993 in combination with estradiol valerate (Femilar trademark) as a combined birth control pill [13] [14] .

Skin and Hair

High Androgen

Hormone Therapy

CPA is widely used as an antiandrogen and progestogen in feminizing hormone therapy for transgender women [15] [16] [17] [18] [19] [20] [21] . It is used either orally at a dose of 10 to 100 mg / day or intramuscularly at a dose of 300 mg once every 4 weeks [22] [23] . A study conducted in 2017 showed that in transgender women, a dose of 25 mg / day gave a similar dose of 50 mg / day inhibition of testosterone, combined with a moderate dosage of estradiol [24] . In light of the possible adverse side effects of CPA, such as depression, fatigue, blood clots, and liver damage, using lower doses of the drug can help minimize these risks [24] . CPA has also been used as a puberty blocker and, therefore, as an antiandrogen and anti-estrogen to suppress puberty in transgender youth, but now GnRH modulators are used for this [25] [26] [17] [27] [28] .

Prostate Cancer

CPA is used as anti-androgenic monotherapy and in the palliative treatment of prostate cancer in men [2] [29] [30] [31] [32] [33] . It is used in very high doses by mouth or intramuscularly to treat this disease. Antiandrogens do not treat prostate cancer, but can significantly extend the life of men with this disease [34] [35] [29] .

Sexual Deviation

CPA is used as an antiandrogen and a form of chemical castration in the treatment of such forms of sexual abnormalities as paraphilia and hypersexuality in men [36] [37] [38] [39] [40] [41] . Used to treat . For this, the drug is approved in more than 20 countries and is mainly used in Canada, Europe and the Middle East [42] . CPA reduces sexual drive and sexual arousal and causes sexual dysfunctions. CPA can also be used to reduce the sexual activity of people with inappropriate sexual behavior, such as people with intellectual disabilities and dementia [43] [44] . The medicine is also useful for treating self-harming sexual behavior, such as masochism [45] . CPA has efficacy comparable to in suppressing sexual desires and functions, but is less effective than type GnRH modulators and has more side effects [37] .

A high dose of CPA significantly reduces sexual fantasies and sexual activity in 80-90% of men with sexual disabilities [42] . In addition, it was found that the rate of relapse of sexual offenses decreased from 85% to 6%, with the majority of relapses committed by individuals who did not follow the course of treatment prescribed by them [42] . It was reported that in 80% of cases, 100 mg / day CPA is enough to achieve the desired reduction in sexuality, while in the remaining 20% ​​of cases, 200 mg / day is enough [46] . When only a partial reduction in sexuality is desired, a dosage of 50 mg / day may be effective [46] . Decrease in sexual desire and erectile function occurs by the end of the first week of treatment and becomes maximum within three to four weeks [46] [47] .

Early Puberty

Other Applications

Notes

  1. ↑ 1 2 3 4 Kuhl H. Pharmacology of estrogens and progestogens: influence of different routes of administration (English) // Climacteric. - 2005. - Vol. 8 Suppl 1 . - P. 3–63 . - DOI : 10.1080 / 13697130500148875 . - PMID 16112947 .
  2. ↑ 1 2 Barradell LB, Faulds D. Cyproterone. A review of its pharmacology and therapeutic efficacy in prostate cancer (English) // Drugs Aging. - 1994 .-- July ( vol. 5 , no. 1 ). - P. 59–80 . - DOI : 10.2165 / 00002512-199405010-00006 . - PMID 7919640 .
  3. ↑ 1 2 3 Neumann F. The antiandrogen cyproterone acetate: discovery, chemistry, basic pharmacology, clinical use and tool in basic research (Eng.) // Exp. Clin. Endocrinol .. - 1994. - Vol. 102 , no. 1 . - P. 1–32 . - DOI : 10.1055 / s-0029-1211261 . - PMID 8005205 .
  4. ↑ Neumann F. Pharmacology and potential use of cyproterone acetate (English) // Horm. Metab. Res .. - 1977. - January ( vol. 9 , no. 1 ). - P. 1–13 . - DOI : 10.1055 / s-0028-1093574 . - PMID 66176 .
  5. ↑ Neumann F, Töpert M. Pharmacology of antiandrogens (Eng.) // Journal of Steroid Biochemistry. - 1986. - November ( vol. 25 , no. 5B ). - P. 885–95 . - DOI : 10.1016 / 0022-4731 (86) 90320-1 . - PMID 2949114 .
  6. ↑ Jonathan S. Berek. Berek & Novak's Gynecology . - Lippincott Williams & Wilkins, 2007 .-- S. 1085. - ISBN 978-0-7817-6805-4 .
  7. ↑ 1 2 Pucci E, Petraglia F. Treatment of androgen excess in females: yesterday, today and tomorrow (English) // Gynecol. Endocrinol .. - 1997 .-- December ( vol. 11 , no. 6 ). - P. 411–33 . - DOI : 10.3109 / 09513599709152569 . - PMID 9476091 .
  8. ↑ Neumann F, Elger W. Permanent changes in gonadal function and sexual behavior as a result of early feminization of male rats by treatment with an antiandrogenic steroid (Eng.) // Endokrinologie. - 1966. - Vol. 50 . - P. 209–225 .
  9. ↑ Sarah H. Wakelin. Systemic Drug Treatment in Dermatology: A Handbook . - CRC Press, 2002. - S. 32. - ISBN 978-1-84076-013-2 .
  10. ↑ 1 2 G. Plewig; AM Kligman. ACNE and ROSACEA . - Springer Science & Business Media, 2012 .-- S. 662, 685. - ISBN 978-3-642-59715-2 .
  11. ↑ Louw-du Toit R, Storbeck KH, Cartwright M, Cabral A, Africander D. Progestins used in endocrine therapy and the implications for the biosynthesis and metabolism of endogenous steroid hormones (Eng.) // Mol. Cell. Endocrinol .. - 2017 .-- February ( vol. 441 ). - P. 31–45 . - DOI : 10.1016 / j.mce.2016.09.09.004 . - PMID 27616670 .
  12. ↑ Mercilon - Summary of Product Characteristics (SmPC) - (eMC) (neopr.) . www.medicines.org.uk. Date of treatment December 19, 2018.
  13. ↑ Fruzzetti F, Trémollieres F, Bitzer J. An overview of the development of combined oral contraceptives containing estradiol: focus on estradiol valerate / dienogest (English) // Gynecol. Endocrinol .. - 2012 .-- May ( vol. 28 , no. 5 ). - P. 400–8 . - DOI : 10.3109 / 09513590.2012.662547 . - PMID 22468839 .
  14. ↑ Fruzzetti F, Bitzer J. Review of clinical experience with estradiol in combined oral contraceptives (Eng.) // Contraception. - 2010 .-- Vol. 81 , no. 1 . - P. 8–15 . - DOI : 10.1016 / j.contraception.2009.08.08.010 . - PMID 20004267 .
  15. ↑ Gooren LJ, Giltay EJ, Bunck MC. Long-term treatment of transsexuals with cross-sex hormones: extensive personal experience (English) // J. Clin. Endocrinol. Metab .. - 2008 .-- January ( vol. 93 , no. 1 ). - P. 19–25 . - DOI : 10.1210 / jc.2007-1809 . - PMID 17986639 .
  16. ↑ Hembree WC, Cohen-Kettenis PT, Gooren L, Hannema SE, Meyer WJ, Murad MH, Rosenthal SM, Safer JD, Tangpricha V, T'Sjoen GG. Endocrine Treatment of Gender-Dysphoric / Gender-Incongruent Persons: An Endocrine Society Clinical Practice Guideline (English) // J. Clin. Endocrinol. Metab .. - 2017 .-- November ( vol. 102 , no. 11 ). - P. 3869-3903 . - DOI : 10.1210 / jc.2017-01658 . - PMID 28945902 .
  17. ↑ 1 2 Chew D, Anderson J, Williams K, May T, Pang K. Hormonal Treatment in Young People With Gender Dysphoria: A Systematic Review (Eng.) // Pediatrics. - 2018 .-- April ( vol. 141 , no. 4 ). - DOI : 10.1542 / peds . 2017-3742 . - PMID 29514975 .
  18. ↑ Deutsch, Madeline. Guidelines for the Primary and Gender-Affirming Care of Transgender and Gender Nonbinary People . - Center of Excellence for Transgender Health, 2016 .-- June 17. - P. 28 .
  19. ↑ James Barrett. Transsexual and Other Disorders of Gender Identity: A Practical Guide to Management . - CRC Press, 2017 .-- pp. 216–217,221. - ISBN 978-1-315-34513-0 .
  20. ↑ Randi Ettner; Stan Monstrey; Eli Coleman. Principles of Transgender Medicine and Surgery . - Routledge, 2016 .-- S. 169,171,216. - ISBN 978-1-317-51460-2 .
  21. ↑ Gianna E. Israel. Transgender Care: Recommended Guidelines, Practical Information, and Personal Accounts . - Temple University Press, 2001. - S. 66–. - ISBN 978-1-56639-852-7 .
  22. ↑ Winkler-Crepaz, K .; Müller, A .; Böttcher, B .; Wildt, L. Hormonbehandlung bei Transgenderpatienten (English) // Gynäkologische Endokrinologie. - 2017 .-- Vol. 15 , no. 1 . - P. 39–42 . - ISSN 1610-2894 . - DOI : 10.1007 / s10304-016-0116-9 .
  23. ↑ Urdl, W. Behandlungsgrundsätze bei Transsexualität (English) // Gynäkologische Endokrinologie. - 2009. - Vol. 7 , no. 3 . - P. 153-160 . - ISSN 1610-2894 . - DOI : 10.1007 / s10304-009-0314-9 .
  24. ↑ 1 2 Fung, Raymond; Hellstern-Layefsky, Miriam; Lega, Iliana. Is a lower dose of cyproterone acetate as effective at testosterone suppression in transgender women as higher doses? (English) // International Journal of Transgenderism. - 2017 .-- Vol. 18 , no. 2 . - P. 123–128 . - ISSN 1553-2739 . - DOI : 10.1080 / 15532739.2017.1290566 .
  25. ↑ Panagiotakopoulos, Leonidas. Transgender medicine - puberty suppression (Eng.) // Reviews in Endocrine and Metabolic Disorders. - 2018 .-- ISSN 1389-9155 . - DOI : 10.1007 / s11154-018-9457-0 .
  26. ↑ Rosenthal SM. Approach to the patient: transgender youth: endocrine considerations (English) // J. Clin. Endocrinol. Metab .. - 2014 .-- December ( vol. 99 , no. 12 ). - P. 4379–89 . - DOI : 10.1210 / jc.2014-1919 . - PMID 25140398 .
  27. ↑ Mahfouda S, Moore JK, Siafarikas A, Zepf FD, Lin A. Puberty suppression in transgender children and adolescents (English) // Lancet Diabetes Endocrinol. - 2017 .-- October ( vol. 5 , no. 10 ). - P. 816–826 . - DOI : 10.1016 / S2213-8587 (17) 30099-2 . - PMID 28546095 .
  28. ↑ Tack LJ, Heyse R, Craen M, Dhondt K, Bossche H, Laridaen J, Cools M. Consecutive Cyproterone Acetate and Estradiol Treatment in Late-Pubertal Transgender Female Adolescents (Eng.) // J Sex Med. - 2017 .-- May ( vol. 14 , no. 5 ). - P. 747–757 . - DOI : 10.1016 / j.jsxm.2017.03.03.251 . - PMID 28499525 .
  29. ↑ 1 2 Torri V, Floriani I. Cyproterone acetate in the therapy of prostate carcinoma (Eng.) // Arch Ital Urol Androl. - 2005 .-- June ( vol. 77 , no. 3 ). - P. 157–63 . - PMID 16372511 .
  30. ↑ Schröder, Fritz H. Cyproterone Acetate - Results of Clinical Trials and Indications for Use in Human Prostate Cancer. - 1996. - P. 45-51 . - DOI : 10.1007 / 978-3-642-45745-6_4 .
  31. ↑ Schröder FH. Cyproterone acetate - mechanism of action and clinical effectiveness in prostate cancer treatment (English) // Cancer. - 1993 .-- December ( vol. 72 , no. 12 Suppl ). - P. 3810–5 . - DOI : 10.1002 / 1097-0142 (19931215) 72: 12+ <3810 :: AID-CNCR2820721710> 3.0.CO; 2-O . - PMID 8252496 .
  32. ↑ de Voogt HJ. The position of cyproterone acetate (CPA), a steroidal anti-androgen, in the treatment of prostate cancer (English) // Prostate Suppl. - 1992. - Vol. 4 . - P. 91–5 . - DOI : 10.1002 / pros . 2990210514 . - PMID 1533452 .
  33. ↑ Goldenberg SL, Bruchovsky N. Use of cyproterone acetate in prostate cancer (English) // Urol. Clin. North Am .. - 1991 .-- February ( vol. 18 , no. 1 ). - P. 111–22 . - PMID 1825143 .
  34. ↑ Thomas L. Lemke; David A. Williams. Foye's Principles of Medicinal Chemistry . - Lippincott Williams & Wilkins, 2008. - S. 1288–. - ISBN 978-0-7817-6879-5 .
  35. ↑ Seidenfeld J, Samson DJ, Hasselblad V, Aronson N, Albertsen PC, Bennett CL, Wilt TJ. Single-therapy androgen suppression in men with advanced prostate cancer: a systematic review and meta-analysis (Eng.) // Ann. Intern. Med .. - 2000. - April ( vol. 132 , no. 7 ). - P. 566–77 . - DOI : 10.7326 / 0003-4819-132-7-200004040-00009 . - PMID 10744594 .
  36. ↑ Khan O, Ferriter M, Huband N, Powney MJ, Dennis JA, Duggan C. Pharmacological interventions for those who have sexually offended or are at risk of offending (Eng.) // Cochrane Database Syst Rev. - 2015 .-- February ( no. 2 ). - P. CD007989 . - DOI : 10.1002 / 14651858.CD007989.pub2 . - PMID 25692326 .
  37. ↑ 1 2 Silvani M, Mondaini N, Zucchi A. Androgen deprivation therapy (castration therapy) and pedophilia: What's new (Eng.) // Arch Ital Urol Androl. - 2015 .-- September ( vol. 87 , no. 3 ). - P. 222–6 . - DOI : 10.4081 / aiua.2015.3.222 . - PMID 26428645 .
  38. ↑ Reilly DR, Delva NJ, Hudson RW. Protocols for the use of cyproterone, medroxyprogesterone, and leuprolide in the treatment of paraphilia (English) // Can J Psychiatry. - 2000 .-- August ( vol. 45 , no. 6 ). - P. 559–63 . - DOI : 10.1177 / 070674370004500608 . - PMID 10986575 .
  39. ↑ Neumann F, Kalmus J. Cyproterone acetate in the treatment of sexual disorders: pharmacological base and clinical experience (Eng.) // Exp. Clin. Endocrinol .. - 1991. - Vol. 98 , no. 2 . - P. 71–80 . - DOI : 10.1055 / s-0029-1211103 . - PMID 1838080 .
  40. ↑ Freund K. Therapeutic sex drive reduction (Eng.) // Acta Psychiatr Scand Suppl . - 1980. - Vol. 287 . - P. 5–38 . - DOI : 10.1111 / j.1600-0447.1980.tb10433.x . - PMID 7006321 .
  41. ↑ Codispoti VL. Pharmacology of sexually compulsive behavior (Eng.) // Psychiatr. Clin. North Am .. - 2008 .-- December ( vol. 31 , no. 4 ). - P. 671–9 . - DOI : 10.1016 / j.psc.2008.06.002 . - PMID 18996306 .
  42. ↑ 1 2 3 Assumpção AA, Garcia FD, Garcia HD, Bradford JM, Thibaut F. Pharmacologic treatment of paraphilias (Eng.) // Psychiatr. Clin. North Am .. - 2014 .-- June ( vol. 37 , no. 2 ). - P. 173–81 . - DOI : 10.1016 / j.psc.2014.03.03.002 . - PMID 24877704 .
  43. ↑ Guay DR. Inappropriate sexual behaviors in cognitively impaired older individuals ( Am ) // Am J Geriatr Pharmacother. - 2008 .-- December ( vol. 6 , no. 5 ). - P. 269–88 . - DOI : 10.1016 / j.amjopharm.2008.12.004 . - PMID 19161930 .
  44. ↑ Clarke DJ. Antilibidinal drugs and mental retardation: a review (Eng.) // Med Sci Law. - 1989 .-- April ( vol. 29 , no. 2 ). - P. 136–46 . - DOI : 10.1177 / 002580248902900209 . - PMID 2526280 .
  45. ↑ Hucker SJ. Self-harmful sexual behavior (Eng.) // Psychiatr. Clin. North Am .. - 1985. - June ( vol. 8 , no. 2 ). - P. 323–37 . - PMID 3895195 .
  46. ↑ 1 2 3 Laschet U, Laschet L. Antiandrogens in the treatment of sexual deviations of men (Eng.) // J. Steroid Biochem .. - 1975. - June ( vol. 6 , no. 6 ). - P. 821–6 . - DOI : 10.1016 / 0022-4731 (75) 90310-6 . - PMID 1177426 .
  47. ↑ Neumann, Friedmund. Pharmacology of Cyproterone Acetate - A Short Review. - 1996. - P. 31–44 . - DOI : 10.1007 / 978-3-642-45745-6_3 .


Source - https://ru.wikipedia.org/w/index.php?title=Ciproterone_acetate&oldid=96953169


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