에스트라디올 에난테이트
에스트라디올 에난테이트(Estradiol enantate, E2-En 또는 EEn)는 여성의 호르몬적 산아 제한에 사용되는 에스트로겐 약물이다.[6][9][10] DHPA와 함께 복합해서 사용하는 경우 한 달에 한 차례씩 근육 주사를 통해 투여되게 된다.[6][9]
체계적 명칭 (IUPAC 명명법) | |
---|---|
[(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 | |
식별 정보 | |
CAS 등록번호 | 4956-37-0 |
ATC 코드 | G03CA03 |
PubChem | 21070 |
ChemSpider | 19815 |
화학적 성질 | |
화학식 | C25H36O3 |
분자량 | ? |
유의어 | EE; E2E; E2-EN; EEn; Estradiol enanthate; Estradiol heptanoate; SQ-16150 |
약동학 정보 | |
생체적합성 | IM: High |
단백질 결합 | Estradiol: ~98% (to albumin and SHBG)[1][2] |
동등생물의약품 | ? |
약물 대사 | Cleavage via esterases in the liver, blood, and tissues[3][4] |
생물학적 반감기 | IM: 5.6–7.5 days[5][6][7][8] |
배출 | Urine[6] |
처방 주의사항 | |
임부투여안전성 | ? |
법적 상태 |
|
투여 방법 | Intramuscular injection[6][9] |
각주
편집- ↑ Stanczyk, Frank Z.; Archer, David F.; Bhavnani, Bhagu R. (2013). “Ethinyl estradiol and 17β-estradiol in combined oral contraceptives: pharmacokinetics, pharmacodynamics and risk assessment”. 《Contraception》 87 (6): 706–727. doi:10.1016/j.contraception.2012.12.011. ISSN 0010-7824. PMID 23375353.
- ↑ Tommaso Falcone; William W. Hurd (2007). 《Clinical Reproductive Medicine and Surgery》. Elsevier Health Sciences. 22,362,388쪽. ISBN 978-0-323-03309-1.
- ↑ Michael Oettel; Ekkehard Schillinger (2012년 12월 6일). 《Estrogens and Antiestrogens II: Pharmacology and Clinical Application of Estrogens and Antiestrogen》. Springer Science & Business Media. 261, 271쪽. 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.
- ↑ Kuhl H (2005). “Pharmacology of estrogens and progestogens: influence of different routes of administration” (PDF). 《Climacteric》. 8 Suppl 1: 3–63. doi:10.1080/13697130500148875. PMID 16112947. S2CID 24616324.
- ↑ Wiemeyer JC, Fernandez M, Moguilevsky JA, Sagasta CL (1986). “Pharmacokinetic studies of estradiol enanthate in menopausic women”. 《Arzneimittelforschung》 36 (11): 1674–7. PMID 3814225.
- ↑ 가 나 다 라 마 Jarquín González JD, Elda de Aguirre L, Rodríguez C, Abrego de Aguilar M, Carrillo F, León DA, Lima M, Trigueros S, Acosta R (September 1996). “Dihydroxyprogesterone acetophenide 150 mg + estradiol enantate 10 mg as monthly injectable contraceptives”. 《Adv Contracept》 12 (3): 213–25. doi:10.1007/BF01849664 . PMID 8910663. S2CID 2522426.
- ↑ Sang GW (April 1994). “Pharmacodynamic effects of once-a-month combined injectable contraceptives”. 《Contraception》 49 (4): 361–85. doi:10.1016/0010-7824(94)90033-7. PMID 8013220.
- ↑ “Bula do Algestona Acetofenida + Enantato de Estradiol”. 《Consulta Remédios》. 2018년 9월 18일에 원본 문서에서 보존된 문서. 2018년 9월 18일에 확인함.
- ↑ 가 나 다 Newton JR, D'arcangues C, Hall PE (1994). “A review of "once-a-month" combined injectable contraceptives”. 《J Obstet Gynaecol (Lahore)》. 4 Suppl 1: S1–34. doi:10.3109/01443619409027641. PMID 12290848.
- ↑ Bagade O, Pawar V, Patel R, Patel B, Awasarkar V, Diwate S (2014). “Increasing use of long-acting reversible contraception: safe, reliable, and cost-effective birth control” (PDF). 《World J Pharm Pharm Sci》 3 (10): 364–392. ISSN 2278-4357.