戊酸雌二醇/醋酸环丙孕酮

组合药剂

戊酸雌二醇/醋酸环丙孕酮(英語:Estradiol valerate/cyproterone acetate,简称:EV/CPA),以克龄蒙(英語:Climen)和Femilar等品牌销售,是戊酸雌二醇(EV,一种雌激素)和醋酸环丙孕酮(CPA,一种孕激素)的组合产品,用于绝经期激素治疗和作为妇女避孕药使用,[1]其为口服药。[1]克龄蒙用于绝经期激素治疗,是一种序贯制剂,含有2毫克EV和1毫克CPA。[2][3][4]它是第一个上市的用于绝经期激素治疗的含有CPA的产品[3],在40多个国家有售。[2]Femilar是一种含雌二醇的避孕药,含有1至2毫克EV和1至2毫克CPA,自1993年以来在芬兰被批准使用。[5]

戊酸雌二醇/醋酸环丙孕酮
戊酸雌二醇(顶部)和醋酸环丙孕酮(下)
组成
戊酸雌二醇雌激素
醋酸环丙孕酮孕激素
臨床資料
商品名英语Drug nomenclature克龄蒙(Climen),Femilar
其他名稱EV/CPA
给药途径口服
藥物類別英语Drug class雌激素孕激素
法律規範狀態
法律規範
识别信息
CAS号108116-22-9

一项研究发现,单用CPA在0.5毫克/天的剂量下,5名妇女中有3名抑制排卵,在1毫克/天的剂量下,5名妇女中有5名抑制排卵。[6][7][8][9][10][11]在一项研究中,108名妇女中有94.4%在第三个治疗周期内发生Femilar的排卵抑制,在另一项研究中,26名妇女在12个治疗周期内几乎100%发生排卵抑制(除了一名妇女在第一个治疗周期内排了卵)。[5][12][1]

外部連結

参考文献

  1. ^ 1.0 1.1 1.2 Hirvonen E, Stenman UH, Mälkönen M, Rasi V, Vartiainen E, Ylöstalo P. New natural oestradiol/cyproterone acetate oral contraceptive for pre-menopausal women. Maturitas. October 1988, 10 (3): 201–13. PMID 2972897. doi:10.1016/0378-5122(88)90023-0. 
  2. ^ 2.0 2.1 Husmann, Friedrich. Clinical Experiences with a Combination of Estradiol Valerate and Cyproterone Acetate for Hormone Replacement. Women's Health and Menopause. Medical Science Symposia Series 11. 1997: 257–261. ISBN 978-94-010-6343-2. ISSN 0928-9550. doi:10.1007/978-94-011-5560-1_38. 
  3. ^ 3.0 3.1 Schneider HP. Androgens and antiandrogens. Ann. N. Y. Acad. Sci. November 2003, 997 (1): 292–306. Bibcode:2003NYASA.997..292S. PMID 14644837. S2CID 8400556. doi:10.1196/annals.1290.033. 
  4. ^ Schneider HP. The role of antiandrogens in hormone replacement therapy. Climacteric. December 2000,. 3 Suppl 2: 21–7. PMID 11379383. 
  5. ^ 5.0 5.1 Fruzzetti F, Trémollieres F, Bitzer J. An overview of the development of combined oral contraceptives containing estradiol: focus on estradiol valerate/dienogest. Gynecol Endocrinol. May 2012, 28 (5): 400–8. PMC 3399636 . PMID 22468839. doi:10.3109/09513590.2012.662547. 
  6. ^ 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. December 2011, 84 (6): 549–57. PMID 22078182. doi:10.1016/j.contraception.2011.04.009. 
  7. ^ 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 Obstet Gynecol Scand Suppl. 1979, 88: 7–15. PMID 393050. S2CID 30486799. doi:10.3109/00016347909157223. 
  8. ^ Spona J, Huber J, Schmidt JB. 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. July 1986, 46 (7): 435–8. PMID 3093307. doi:10.1055/s-2008-1026659 (德语). 
  9. ^ Spona J, Huber J. Efficacy of low-dose oral contraceptives containing levonorgestrel, gestoden and cyproterone acetate. Gynecol Obstet Invest. 1987, 23 (3): 184–93. PMID 2954886. doi:10.1159/000298860. 
  10. ^ Spona, J.; Huber, J.; Schmidt, J. B. Ovulation inhibitory effect of SH B 209 AE (Diane-35)—a new antiandrogen-estrogen combination. Schindler, Adolf E. (编). Antiandrogen-Estrogen Therapy for Signs of Androgenization. Berlin, Boston: De Gruyter. 1987-12-31: 51–58. ISBN 9783110866902. doi:10.1515/9783110866902-006. 
  11. ^ Hammerstein, J. Antiandrogens: Clinical Aspects. Hair and Hair Diseases. Berlin, Heidelberg: Springer Berlin Heidelberg. 1990: 827–886. ISBN 978-3-642-74614-7. doi:10.1007/978-3-642-74612-3_35. 
  12. ^ Hirvonen E, Allonen H, Anttila M, Kulmala Y, Ranta T, Rautiainen H, Sipilä P, Ylöstalo P. Oral contraceptive containing natural estradiol for premenopausal women. Maturitas. January 1995, 21 (1): 27–32. PMID 7731379. doi:10.1016/0378-5122(94)00856-3.