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用户:神乐坂秀吉/草稿/戊酸雌二醇

< User:神樂坂秀吉
戊酸雌二醇
临床资料
读音/ˌɛstrəˈdaɪoʊl ˈvæləreɪt/
ES-trə-DY-ohl VAL-ə-rayt[1]
商品名（英语：Drug nomenclature）Delestrogen、Progynon Depot、补佳乐（Progynova）等
其他名称EV; E2V; Oestradiol valerate; Estradiol pentanoate; Estradiol valerianate
给药途径口服给药、肌肉注射[2] 或皮下注射
药物类别（英语：Drug class）Estrogen; Estrogen ester
ATC码
法律规范状态
法律规范
  • 处方药（℞-only）
药物动力学数据
生物利用度Oral: 3–5%[3][4]
IM: 100%[3]
血浆蛋白结合率雌二醇：~98% （人血清白蛋白和性激素结合球蛋白）[5][6]
药物代谢在肝脏、血液和组织中通过酯酶以键结断裂[3]
代谢产物雌二醇及其代谢产物、戊酸[3]
生物半衰期Oral: 12–20 hours (as E2)[3][7]
IM: 4–5 days[3]
作用时间IM (5 mg): 7–8 days[8]
IM (10–30 mg): 1–4 weeks[9]
排泄途径尿液 (80%)[3]
识别信息
  • [(8R,9S,13S,14S,17S)-3-hydroxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-17-yl] pentanoate
CAS号979-32-8
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
化学信息
化学式C23H32O3
摩尔质量356.498 g/mol
3D模型（JSmol（英语：JSmol））
  • CCCCC(=O)O[C@H]1CC[C@@H]2[C@@]1(CC[C@H]3[C@H]2CCC4=C3C=CC(=C4)O)C
  • InChI=1S/C23H32O3/c1-3-4-5-22(25)26-21-11-10-20-19-8-6-15-14-16(24)7-9-17(15)18(19)12-13-23(20,21)2/h7,9,14,18-21,24H,3-6,8,10-13H2,1-2H3/t18-,19-,20+,21+,23+/m1/s1
  • Key:RSEPBGGWRJCQGY-RBRWEJTLSA-N

Estradiol valerate, sold under the brand names Delestrogen, Progynon Depot, and Progynova among others, is an estrogen medication which is used in hormone therapy for menopausal symptoms and low estrogen levels in women, in hormone therapy for transgender women, and in hormonal birth control for women.[4][3][9][10] It is also used in the treatment of prostate cancer in men.[9] The medication is taken by mouth or by injection into muscle once every 1 to 4 weeks.[9][10] Side effects of estradiol valerate include breast tenderness, breast enlargement, nausea, headache, and fluid retention.[11][9][10] Estradiol valerate is a synthetic estrogen and hence is an agonist of the estrogen receptor (ER), the biological target of estrogens like estradiol.[4][3][12] It is an estrogen ester and a prodrug of estradiol in the body.[12][4][3] Because of this, it is considered to be a natural and bioidentical form of estrogen.[12][3][13]

Estradiol valerate was first described in 1940 and was introduced for medical use in 1954.[14][15][16] Along with estradiol cypionate, it is one of the most widely used esters of estradiol.[17] Estradiol valerate is used in the United States, Canada, Europe, and throughout much of the rest of the world.[18][19] It is available as a generic medication.[20]

参考文献

  1. ^ https://www.drugs.com/cons/estradiol-and-dienogest.html
  2. ^ Christoph Zink. Dictionary of Obstetrics and Gynecology. Walter de Gruyter. 1 January 1988: 86 [20 May 2012]. ISBN 978-3-11-085727-6. 
  3. ^ 3.00 3.01 3.02 3.03 3.04 3.05 3.06 3.07 3.08 3.09 3.10 引用错误：没有为名为pmid7169965的参考文献提供内容
  4. ^ 4.0 4.1 4.2 4.3 Kuhl H. Pharmacology of estrogens and progestogens: influence of different routes of administration (PDF). Climacteric. 2005,. 8 Suppl 1: 3–63. PMID 16112947. doi:10.1080/13697130500148875. 
  5. ^ Stanczyk, Frank Z.; Archer, David F.; Bhavnani, Bhagu R. Ethinyl estradiol and 17β-estradiol in combined oral contraceptives: pharmacokinetics, pharmacodynamics and risk assessment. Contraception. 2013, 87 (6): 706–727. ISSN 0010-7824. PMID 23375353. doi:10.1016/j.contraception.2012.12.011. 
  6. ^ Tommaso Falcone; William W. Hurd. Clinical Reproductive Medicine and Surgery. Elsevier Health Sciences. 2007: 22,362,388. ISBN 0-323-03309-1. 
  7. ^ Stanczyk, Frank Z.; Archer, David F.; Bhavnani, Bhagu R. Ethinyl estradiol and 17β-estradiol in combined oral contraceptives: pharmacokinetics, pharmacodynamics and risk assessment. Contraception. 2013, 87 (6): 706–727. ISSN 0010-7824. PMID 23375353. doi:10.1016/j.contraception.2012.12.011. 
  8. ^ 引用错误：没有为名为pmid7389356的参考文献提供内容
  9. ^ 9.0 9.1 9.2 9.3 9.4 引用错误：没有为名为Delestrogen-Label的参考文献提供内容
  10. ^ 10.0 10.1 10.2 引用错误：没有为名为Progynova-Label的参考文献提供内容
  11. ^ 引用错误：没有为名为Ghosh2010的参考文献提供内容
  12. ^ 12.0 12.1 12.2 Michael Oettel; Ekkehard Schillinger. Estrogens and Antiestrogens II: Pharmacology and Clinical Application of Estrogens and Antiestrogen. Springer Science & Business Media. 6 December 2012: 261. ISBN 978-3-642-60107-1. Natural estrogens considered here include: [...] Esters of 17β-estradiol, such as estradiol valerate, estradiol benzoate and estradiol cypionate. Esterification aims at either better absorption after oral administration or a sustained release from the depot after intramuscular administration. During absorption, the esters are cleaved by endogenous esterases and the pharmacologically active 17β-estradiol is released; therefore, the esters are considered as natural estrogens. 
  13. ^ Nagrath Arun; Malhotra Narendra; Seth Shikha. Progress in Obstetrics and Gynecology--3. Jaypee Brothers Medical Publishers Pvt. Ltd. 15 December 2012: 419–. ISBN 978-93-5090-575-3. 
  14. ^ 引用错误：没有为名为KleemannEngel2014的参考文献提供内容
  15. ^ 引用错误：没有为名为Publishing2013的参考文献提供内容
  16. ^ 引用错误：没有为名为Duetsch1969的参考文献提供内容
  17. ^ 引用错误：没有为名为Yen1991的参考文献提供内容
  18. ^ 引用错误：没有为名为Elks2014的参考文献提供内容
  19. ^ Index Nominum 2000: International Drug Directory. Taylor & Francis US. 2000: 405 [20 May 2012]. ISBN 978-3-88763-075-1. 
  20. ^ https://www.drugs.com/availability/generic-delestrogen.html
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