醋酸乌利司他

醋酸乌利司他是用于紧急避孕子宫肌瘤的口服药物[1] [7] [8]。用于紧急避孕时,需在性交后 120 小时内使用[1]。用于子宫肌瘤时,可能需要服用至少 6 个月[9]

醋酸乌利司他
临床资料
商品名英语Drug nomenclatureElla, EllaOne, Esmya, others
其他名称CDB-2914; 11β-[4-(Dimethylamino)phenyl]-17α-acetoxy-19-norpregna-4,9-diene-3,20-dione
AHFS/Drugs.comMonograph
核准状况
给药途径口服给药
药物类别英语Drug class选择性孕酮受体调节剂英语Selective progesterone receptor modulator[1]
ATC码
法律规范状态
法律规范
药物动力学数据
生物利用度几乎100%
血浆蛋白结合率96.7–99.5%
药物代谢可能是CYP3A4
生物半衰期32小时[1]
排泄途径约90%由粪便
识别信息
  • [(8S,11R,13S,14S,17R)-17-acetyl-11-[4-(dimethylamino)phenyl]-13-methyl-3-oxo-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-17-yl] acetate
CAS号126784-99-4  checkY
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.207.349 编辑维基数据链接
化学信息
化学式C30H37NO4
摩尔质量475.63 g·mol−1
3D模型(JSmol英语JSmol
  • CC(=O)OC4(C(C)=O)CCC3C1CCC2=CC(=O)CCC2=C1C(CC34C)c5ccc(N(C)C)cc5
  • InChI=1S/C30H37NO4/c1-18(32)30(35-19(2)33)15-14-27-25-12-8-21-16-23(34)11-13-24(21)28(25)26(17-29(27,30)3)20-6-9-22(10-7-20)31(4)5/h6-7,9-10,16,25-27H,8,11-15,17H2,1-5H3/t25-,26+,27-,29-,30-/m0/s1 ☒N
  • Key:OOLLAFOLCSJHRE-ZHAKMVSLSA-N ☒N

常见副作用包括头痛、恶心、疲倦和腹痛[1]。已怀孕者不宜使用此药[1]。它属于选择性孕酮受体调节剂英语Selective progesterone receptor modulator(Selective progesterone receptor modulator,SPRM)[1]。作用机转是阻止孕酮作用,而停止排卵[10]

醋酸乌利司他于 2010 年在美国取得医疗使用许可[1]。名列世界卫生组织基本药物标准清单[11]。为提高药物可及性,有人建议为所有有怀孕风险的女性提供处方,以便于必要时使用[10]

参考文献

编辑
  1. ^ 1.0 1.1 1.2 1.3 1.4 1.5 1.6 1.7 Ulipristal Acetate. The American Society of Health-System Pharmacists. [8 December 2017]. (原始内容存档于10 December 2017). "Ulipristal Acetate". The American Society of Health-System Pharmacists. Archived from the original on 10 December 2017. Retrieved 8 December 2017.
  2. ^ Prescription medicines: registration of new chemical entities in Australia, 2015. Therapeutic Goods Administration (TGA). 21 June 2022 [10 April 2023]. 
  3. ^ ellaOne 30 mg - Summary of Product Characteristics (SmPC). (emc). 1 July 2021 [28 February 2022]. 
  4. ^ Esmya 5 mg Tablets (ulipristal acetate) - Summary of Product Characteristics (SmPC). (emc). 17 February 2021 [28 February 2022]. 
  5. ^ Ella- ulipristal acetate tablet. DailyMed. 1 November 2023 [26 September 2024]. 
  6. ^ ellaOne EPAR. European Medicines Agency (EMA). 3 June 2009 [8 July 2020]. 
  7. ^ Garnock-Jones, KP; Duggan, ST. Ulipristal Acetate: A Review in Symptomatic Uterine Fibroids.. Drugs. October 2017, 77 (15): 1665–1675. PMID 28900897. S2CID 207489367. doi:10.1007/s40265-017-0812-3. 
  8. ^ Ulipristal - Drugs.com. Drugs.com. [14 December 2017]. (原始内容存档于14 December 2017). 
  9. ^ British national formulary : BNF 69 69. British Medical Association. 2015: 510, 560. ISBN 9780857111562. 
  10. ^ 10.0 10.1 Likis, Frances E. Women's Gynecologic Health. Jones & Bartlett Publishers. 2016: 243. ISBN 9781284076028. (原始内容存档于10 December 2017) (英语). 
  11. ^ World Health Organization. World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. 2019. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.