醋酸乌利司他
醋酸乌利司他是用于紧急避孕和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]。
临床资料 | |
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商品名 | Ella, 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.com | Monograph |
核准状况 | |
给药途径 | 口服给药 |
药物类别 | 选择性孕酮受体调节剂[1] |
ATC码 | |
法律规范状态 | |
法律规范 |
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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 | |
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CAS号 | 126784-99-4 |
PubChem CID | |
IUPHAR/BPS | |
DrugBank | |
ChemSpider | |
UNII | |
KEGG | |
ChEBI | |
ChEMBL | |
CompTox Dashboard (EPA) | |
ECHA InfoCard | 100.207.349 |
化学信息 | |
化学式 | C30H37NO4 |
摩尔质量 | 475.63 g·mol−1 |
3D模型(JSmol) | |
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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(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
- ^ 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.
- ^ Prescription medicines: registration of new chemical entities in Australia, 2015. Therapeutic Goods Administration (TGA). 21 June 2022 [10 April 2023].
- ^ ellaOne 30 mg - Summary of Product Characteristics (SmPC). (emc). 1 July 2021 [28 February 2022].
- ^ Esmya 5 mg Tablets (ulipristal acetate) - Summary of Product Characteristics (SmPC). (emc). 17 February 2021 [28 February 2022].
- ^ Ella- ulipristal acetate tablet. DailyMed. 1 November 2023 [26 September 2024].
- ^ ellaOne EPAR. European Medicines Agency (EMA). 3 June 2009 [8 July 2020].
- ^ 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.
- ^ Ulipristal - Drugs.com. Drugs.com. [14 December 2017]. (原始内容存档于14 December 2017).
- ^ British national formulary : BNF 69 69. British Medical Association. 2015: 510, 560. ISBN 9780857111562.
- ^ 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).
- ^ 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.