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米非司酮的临床应用:审视不断拓展的领域

Clinical Utility of Mifepristone: Apprising the Expanding Horizons.

作者信息

Karena Zalak V, Shah Harsh, Vaghela Hetvee, Chauhan Kalp, Desai Pranav K, Chitalwala Asjad Raza

机构信息

Department of Obstetrics and Gynecology, Nootan Medical College and Research Centre, Visnagar, IND.

Department of Obstetrics and Gynecology, Pandit Deendayal Upadhyay Medical College, Rajkot, IND.

出版信息

Cureus. 2022 Aug 23;14(8):e28318. doi: 10.7759/cureus.28318. eCollection 2022 Aug.

DOI:10.7759/cureus.28318
PMID:36158399
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9499832/
Abstract

Mifepristone is a progesterone and glucocorticoid receptor antagonist. Medical abortion with mifepristone and prostaglandin has revolutionized the abortion process extending abortion care to the doors of females. From as low as 2 mg/day to doses extending to 600 mg, from daily dosing to single dosage treatment, mifepristone has a wide perspective in the treatment of various pathologies. Cervical dilatation and myometrial contractility have made the utility of mifepristone feasible for second-trimester termination of pregnancy and induction of labor awaiting Food and Drug Administration approvals. Its anti-progesterone action on the menstrual cycle has a new dimension of use as a contraceptive, as well as use as a menstruation inductive agent. Its role in endometriosis, ectopic pregnancy, and adenomyosis requires more intensive research. Apoptotic action of mifepristone, interference of heterotypic cell adhesion to the basement membrane, cell migration, growth inhibition of various cancer cell lines, decreased epidermal growth factor expression, suppression of invasive and metastatic cancer potential, increase in tumor necrosis factor, downregulation of cyclin-dependent kinase 2, B-cell lymphoma 2, and Nuclear factor kappa B have opened its potential to be explored as anti-cancer treatment and its effects on leiomyoma. The drug needs to be studied more for the prospectus of its anti-glucocorticoid actions in a wider dimension beyond its acquiescence for the treatment of Cushing syndrome.

摘要

米非司酮是一种孕激素和糖皮质激素受体拮抗剂。米非司酮与前列腺素联合用于药物流产,彻底改变了流产方式,将流产服务延伸到女性身边。米非司酮的剂量从低至每日2毫克到高达600毫克,给药方式从每日给药发展到单次给药,在治疗各种病症方面具有广阔前景。宫颈扩张和子宫肌层收缩使米非司酮在中期妊娠终止和引产中的应用成为可能,不过仍有待美国食品药品监督管理局批准。其对月经周期的抗孕激素作用为其作为避孕药以及月经诱导剂开辟了新的应用维度。其在子宫内膜异位症、异位妊娠和子宫腺肌病中的作用还需要更深入的研究。米非司酮的凋亡作用、对异型细胞黏附于基底膜的干扰、细胞迁移、对各种癌细胞系的生长抑制、表皮生长因子表达降低、侵袭性和转移性癌症潜能的抑制、肿瘤坏死因子增加、细胞周期蛋白依赖性激酶2、B细胞淋巴瘤2和核因子κB的下调,为其作为抗癌治疗药物以及对平滑肌瘤的影响开辟了探索潜力。除了目前仅用于治疗库欣综合征外,该药物在更广泛维度上的抗糖皮质激素作用还需要更多研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/470d/9499832/b08b6990b554/cureus-0014-00000028318-i01.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/470d/9499832/b08b6990b554/cureus-0014-00000028318-i01.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/470d/9499832/b08b6990b554/cureus-0014-00000028318-i01.jpg

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Clin Cancer Res. 2022 Apr 14;28(8):1549-1559. doi: 10.1158/1078-0432.CCR-21-4049.
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Alcohol dependence and withdrawal increase sensitivity of central amygdalar GABAergic synapses to the glucocorticoid receptor antagonist mifepristone in male rats.酒精依赖和戒断增加了雄性大鼠中枢杏仁核 GABA 能突触对糖皮质激素受体拮抗剂米非司酮的敏感性。
Neurobiol Dis. 2022 Mar;164:105610. doi: 10.1016/j.nbd.2022.105610. Epub 2022 Jan 4.
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Int J Reprod Biomed. 2024 Dec 2;22(10):811-820. doi: 10.18502/ijrm.v22i10.17669. eCollection 2024 Oct.
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Asoprisnil as a Novel Ligand Interacting with Stress-Associated Glucocorticoid Receptor.阿索普瑞尼,一种与应激相关糖皮质激素受体相互作用的新型配体。
Biomedicines. 2024 Nov 30;12(12):2745. doi: 10.3390/biomedicines12122745.
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