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醋酸乌利司他这种孕激素受体调节剂用于子宫肌瘤所致月经过多的历史及应用情况。

The history and use of the progesterone receptor modulator ulipristal acetate for heavy menstrual bleeding with uterine fibroids.

作者信息

Bouchard Philippe, Chabbert-Buffet Nathalie

机构信息

University Pierre et Marie Curie, Hospital saint Antoine, 75012, Paris, France; Department of Ob Gyn, Hospital Foch, 92150, Suresnes, France.

University Pierre et Marie Curie, Hospital saint Antoine, 75012, Paris, France; Department of Ob Gyn, Hospital Tenon, 75020, Paris, France.

出版信息

Best Pract Res Clin Obstet Gynaecol. 2017 Apr;40:105-110. doi: 10.1016/j.bpobgyn.2016.12.002. Epub 2016 Dec 18.

DOI:10.1016/j.bpobgyn.2016.12.002
PMID:28169130
Abstract

Progesterone receptor modulators (PRM) or selective progesterone receptor modulators have two remarkable effects in treated women. They considerably suppress endometrial bleeding by incompletely understood mechanisms, and when administered in women with symptomatic fibroids, they produce a significant and potentially long-term decrease in fibroid volume. The crucial advantage of this therapy lies with the absence of suppression of ovarian oestrogen secretion, which is in contrast to GnRH agonists. Long-term treatments have proven to be useful, especially in women approaching the menopausal transition. However, their use is associated with endometrial modifications called PRM-associated endometrial changes (PAECs). Although these abnormalities are now described as benign, the treatment is best administered in an intermittent manner where the PAECs rapidly disappear, while the beneficial effects on fibroid size and uterine bleeding are maintained or even improved in the long term.

摘要

孕激素受体调节剂(PRM)或选择性孕激素受体调节剂对接受治疗的女性有两个显著作用。它们通过尚不完全清楚的机制显著抑制子宫内膜出血,并且在有症状的子宫肌瘤女性中使用时,会使肌瘤体积显著且可能长期减小。这种疗法的关键优势在于不会抑制卵巢雌激素分泌,这与促性腺激素释放激素激动剂形成对比。长期治疗已被证明是有效的,尤其是对于接近绝经过渡期的女性。然而,它们的使用与称为PRM相关子宫内膜变化(PAECs)的子宫内膜改变有关。尽管现在将这些异常描述为良性,但最好以间歇方式给药,这样PAECs会迅速消失,而对肌瘤大小和子宫出血的有益作用在长期内得以维持甚至改善。

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引用本文的文献

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The effect of ulipristal acetate on tumor necrosis factor α, insulin-like growth factor 1, and plasminogen activator inhibitor-1 serum levels in patients with symptomatic uterine fibroids.醋酸乌利司他对有症状子宫肌瘤患者血清肿瘤坏死因子α、胰岛素样生长因子1和纤溶酶原激活物抑制剂-1水平的影响。
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Ulipristal Acetate Mediates Decreased Proteoglycan Expression Through Regulation of Nuclear Factor of Activated T-Cells (NFAT5).
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Reprod Sci. 2019 Feb;26(2):184-197. doi: 10.1177/1933719118816836. Epub 2018 Dec 19.
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Ulipristal Acetate Interferes With Actin Remodeling Induced by 17β-Estradiol and Progesterone in Human Endometrial Stromal Cells.醋酸乌利司他干扰17β-雌二醇和孕酮诱导的人子宫内膜基质细胞中的肌动蛋白重塑。
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Drug delivery for the treatment of endometriosis and uterine fibroids.用于治疗子宫内膜异位症和子宫肌瘤的药物输送。
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