User:神樂坂秀吉/草稿/戊酸雌二醇
![]() | |
![]() | |
臨床資料 | |
---|---|
读音 | /ˌɛstrəˈdaɪoʊl ˈvæləreɪt/ ES-trə-DY-ohl VAL-ə-rayt[1] |
商品名 | Delestrogen、Progynon Depot、补佳乐(Progynova)等 |
其他名稱 | 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 |
藥物類別 | Estrogen; Estrogen ester |
ATC碼 | |
法律規範狀態 | |
法律規範 |
|
藥物動力學數據 | |
生物利用度 | Oral: 3–5%[3][4] IM: 100%[3] |
血漿蛋白結合率 | 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] |
代謝產物 | 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] |
作用時間 | IM (5 mg): 7–8 days[8] IM (10–30 mg): 1–4 weeks[9] |
排泄途徑 | 尿液 (80%)[3] |
识别信息 | |
| |
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) | |
| |
|
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
- ^ https://www.drugs.com/cons/estradiol-and-dienogest.html
- ^ Christoph Zink. Dictionary of Obstetrics and Gynecology. Walter de Gruyter. 1 January 1988: 86 [20 May 2012]. ISBN 978-3-11-085727-6.
- ^ 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 - ^ 4.0 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.
- ^ 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.
- ^ Tommaso Falcone; William W. Hurd. Clinical Reproductive Medicine and Surgery. Elsevier Health Sciences. 2007: 22,362,388. ISBN 0-323-03309-1.
- ^ 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.
- ^ 引用错误:没有为名为
pmid7389356
的参考文献提供内容 - ^ 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 - ^ 10.0 10.1 10.2 引用错误:没有为名为
Progynova-Label
的参考文献提供内容 - ^ 引用错误:没有为名为
Ghosh2010
的参考文献提供内容 - ^ 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.
- ^ 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.
- ^ 引用错误:没有为名为
KleemannEngel2014
的参考文献提供内容 - ^ 引用错误:没有为名为
Publishing2013
的参考文献提供内容 - ^ 引用错误:没有为名为
Duetsch1969
的参考文献提供内容 - ^ 引用错误:没有为名为
Yen1991
的参考文献提供内容 - ^ 引用错误:没有为名为
Elks2014
的参考文献提供内容 - ^ Index Nominum 2000: International Drug Directory. Taylor & Francis US. 2000: 405 [20 May 2012]. ISBN 978-3-88763-075-1.
- ^ https://www.drugs.com/availability/generic-delestrogen.html