庚酸雌二醇

庚酸雌二醇
臨床資料
商品名（英语：Drug nomenclature）	Perlutal, Topasel, Unalmes, Yectames, others
其他名稱	EEn; E2-EN; EE; E2E; Estradiol enanthate; Estradiol heptanoate; SQ-16150
给药途径	肌肉注射
藥物類別	雌激素、雌激素酯
ATC碼	G03CA03 (WHO) ;
法律規範狀態
法律規範	处方药（℞-only）;
藥物動力學數據
生物利用度	IM: High
血漿蛋白結合率	Estradiol: ~98% (to albumin and SHBG)
药物代谢	Cleavage via esterases in the liver, blood, and tissues
代謝產物	Estradiol, heptanoic acid, and metabolites of estradiol
生物半衰期	IM: 5.6–7.5 days
作用時間	IM (10 mg): ~20–30 days
排泄途徑	尿
识别信息
	IUPAC命名法 [(8R,9S,13S,14S,17S)-3-hydroxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-17-yl] heptanoate; ;
CAS号	4956-37-0
PubChem CID	21070;
ChemSpider	19815;
UNII	PAP315WZIA;
KEGG	D04064;
ChEMBL	ChEMBL1697792;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID3023001 ;
ECHA InfoCard	100.023.272
化学信息
化学式	C25H36O3
摩尔质量	384.56 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES CCCCCCC(=O)O[C@H]1CC[C@@H]2[C@@]1(CC[C@H]3[C@H]2CCC4=C3C=CC(=C4)O)C;
	InChI InChI=1S/C25H36O3/c1-3-4-5-6-7-24(27)28-23-13-12-22-21-10-8-17-16-18(26)9-11-19(17)20(21)14-15-25(22,23)2/h9,11,16,20-23,26H,3-8,10,12-15H2,1-2H3/t20-,21-,22+,23+,25+/m1/s1; Key:RFWTZQAOOLFXAY-BZDYCCQFSA-N;

庚酸雌二醇（英語：Estradiol enantate或estradiol enanthate，缩写EEn或E2-EN，商品名有：Perlutal、Topasel等）是一种有机化合物，分子式C₂₅H₃₆O₃，可看作雌二醇17β位置的正庚酸酯，用于女性的激素避孕^[1]^[2]。

参考文献

^ ^1.0 ^1.1 ^1.2 ^1.3 Jarquín González JD, Elda de Aguirre L, Rodríguez C, Abrego de Aguilar M, Carrillo F, León DA, et al. Dihydroxyprogesterone acetophenide 150 mg + estradiol enantate 10 mg as monthly injectable contraceptives. Advances in Contraception. September 1996, 12 (3): 213–225. PMID 8910663. S2CID 2522426. doi:10.1007/BF01849664.
^ ^2.0 ^2.1 Newton JR, D'arcangues C, Hall PE. A review of "once-a-month" combined injectable contraceptives. Journal of Obstetrics and Gynaecology. 1994, 4 (Suppl 1): S1–34. PMID 12290848. doi:10.3109/01443619409027641.
^ Stanczyk FZ, Archer DF, Bhavnani BR. Ethinyl estradiol and 17β-estradiol in combined oral contraceptives: pharmacokinetics, pharmacodynamics and risk assessment. Contraception. June 2013, 87 (6): 706–727. PMID 23375353. doi:10.1016/j.contraception.2012.12.011.
^ Falcone T, Hurd WW. Clinical Reproductive Medicine and Surgery. Elsevier Health Sciences. 2007: 22,362,388. ISBN 978-0-323-03309-1.
^ ^5.0 ^5.1 ^5.2 Oettel M, Schillinger E. Estrogens and Antiestrogens II: Pharmacology and Clinical Application of Estrogens and Antiestrogen. Springer Science & Business Media. 6 December 2012: 261, 271. 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. [...] Wiemeyer et al. (1986) measured elevated estradiol levels up to 31 days after an intramuscular dose of 10mg estradiol enanthate.
^ ^6.0 ^6.1 Kuhl H. Pharmacology of estrogens and progestogens: influence of different routes of administration. Climacteric. August 2005, 8 (Suppl 1): 3–63. PMID 16112947. S2CID 24616324. doi:10.1080/13697130500148875.
^ Bula do Algestona Acetofenida + Enantato de Estradiol. Consulta Remédios. [18 September 2018]. （原始内容存档于18 September 2018）.

外部链接

[pmid8910663-1] 1.0 ^1.1 ^1.2 ^1.3 Jarquín González JD, Elda de Aguirre L, Rodríguez C, Abrego de Aguilar M, Carrillo F, León DA, et al. Dihydroxyprogesterone acetophenide 150 mg + estradiol enantate 10 mg as monthly injectable contraceptives. Advances in Contraception. September 1996, 12 (3): 213–225. PMID 8910663. S2CID 2522426. doi:10.1007/BF01849664.

[pmid12290848-2] 2.0 ^2.1 Newton JR, D'arcangues C, Hall PE. A review of "once-a-month" combined injectable contraceptives. Journal of Obstetrics and Gynaecology. 1994, 4 (Suppl 1): S1–34. PMID 12290848. doi:10.3109/01443619409027641.

[pmid23375353-3] Stanczyk FZ, Archer DF, Bhavnani BR. Ethinyl estradiol and 17β-estradiol in combined oral contraceptives: pharmacokinetics, pharmacodynamics and risk assessment. Contraception. June 2013, 87 (6): 706–727. PMID 23375353. doi:10.1016/j.contraception.2012.12.011.

[FalconeHurd2007-4] Falcone T, Hurd WW. Clinical Reproductive Medicine and Surgery. Elsevier Health Sciences. 2007: 22,362,388. ISBN 978-0-323-03309-1.

[OettelSchillinger2012-5] 5.0 ^5.1 ^5.2 Oettel M, Schillinger E. Estrogens and Antiestrogens II: Pharmacology and Clinical Application of Estrogens and Antiestrogen. Springer Science & Business Media. 6 December 2012: 261, 271. 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. [...] Wiemeyer et al. (1986) measured elevated estradiol levels up to 31 days after an intramuscular dose of 10mg estradiol enanthate.

[pmid16112947-6] 6.0 ^6.1 Kuhl H. Pharmacology of estrogens and progestogens: influence of different routes of administration. Climacteric. August 2005, 8 (Suppl 1): 3–63. PMID 16112947. S2CID 24616324. doi:10.1080/13697130500148875.

[ConsultaRemédios-7] Bula do Algestona Acetofenida + Enantato de Estradiol. Consulta Remédios. [18 September 2018]. （原始内容存档于18 September 2018）.

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庚酸雌二醇

参考文献

外部链接

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