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Emergency contraception
Published in Suzanne Everett, Handbook of Contraception and Sexual Health, 2020
Ulipristal acetate is a synthetic progesterone which binds to human progesterone receptor; as a result it blocks the action of progestogen and may reduce the efficacy of contraceptives containing progestogen. Ulipristal acetate has a high affinity for glucocorticoid receptor, and anti-glucocorticoid effects have been observed in animals. It is therefore not recommended for use with women suffering from severe asthma insufficiently controlled by oral glucocorticoids (FSRH, 2017b).
Novel treatment modalities
Published in Seema Chopra, Endometriosis, 2020
In experimental studies, ulipristal acetate exhibited proapoptotic effects, thereby causing regression and atrophy of endometriotic lesions in rats. It helps in limiting the cell proliferation, as shown by a decrease in Ki-67 expression. Its anti-inflammatory effect was indicated by a decrease in cyclooxygenase-2 expression [42]. The clinical use of ulipristal acetate as a therapeutic agent for endometriosis is still under evaluation. It is approved as an emergency contraceptive in the United States. Europe and Canada allow ulipristal for the treatment of fibroids [43].
Iatrogenic disease
Published in T. Yee Khong, Annie N. Y. Cheung, Wenxin Zheng, Richard Wing-Cheuk Wong, Hao Chen, Diagnostic Endometrial Pathology, 2019
T. Yee Khong, Annie N. Y. Cheung, Wenxin Zheng
A selective progesterone receptor modulator (SPRM) is an agent that exerts agonist and antagonist activity at the progesterone receptor, depending on the target tissue. Two SPRMs, mifespristone and ulipristal acetate, are used as emergency contraception following unprotected intercourse, working by delaying or preventing ovulation depending on the time of the menstrual cycle. They are also used for treatment of uterine leiomyoma. At the time of writing, the European Medicines Agency was reviewing the benefits and risks with ulipristal acetate, following reports of serious liver injury. Reversible effects on the endometrium that might differ by agent and dose over time, labeled as progesterone receptor modulator-associated endometrial changes (PAEC), have been described.7 The changes consisted of irregular, cystic glands showing a flattened secretory-like epithelium with vacuolation, coexisting mitoses and apoptosis, dyssynchrony between the secretory glands and stroma absent of pre-decidualization, and clusters of thick-walled vessels, prominent anastomosing capillary networks or vascular ectasia (Figures 6.24 and 6.25).8–10
The pharmacotherapeutic management of premenstrual dysphoric disorder
Published in Expert Opinion on Pharmacotherapy, 2023
Nancy Ciccone, Maya B. Kovacheff, Benicio N. Frey
Ulipristal acetate is a selective progesterone receptor modulator that acts as a progesterone antagonist in the progesterone-responsive receptors in the brain, binding to progesterone receptors A and B with high affinity [64]. This medication induces ovulation suppression in approximately 80% of cases and is used for treatment of uterine fibroids. While the precise mechanisms of action in PMDD symptoms remain to be confirmed, both its effects on progesterone receptors and ovulation suppression are thought to be involved [65]. A recent proof-of-concept RCT found preliminary positive evidence especially for psychological symptoms, with a 41% mean decrease in DRSP scores in the ulipristal acetate group compared with 22% in those in the placebo group [65]. Of note, ulipristal acetate has been associated with liver failure, with a reported incidence rate of five acute liver failures among 765,000 patients, and no reports of liver failure in short-term clinical trials [66]
Novel pharmacological therapies for the treatment of endometriosis
Published in Expert Review of Clinical Pharmacology, 2022
Laura Buggio, Dhouha Dridi, Giussy Barbara, Camilla E.M. Merli, Giulia Emily Cetera, Paolo Vercellini
SPRMs are compounds that bind the progesterone receptor (PR) and have a mixed agonist-antagonist activity. PRs are expressed through two main isoforms: isoform A (PR-A) and isoform B (PR-B), which entail distinct functions depending on the type of cell expressing them [37]. In particular, mifepristone has a higher binding affinity (100%) for the human PR than progesterone (43%) and its metabolites in endometrial and myometrial samples [38,39]. Mifepristone is able to stimulate PR by inducing dimerization (as A:A, B:B, or A:B); these dimers possess different effects: A:A are functionally silent, A:B can activate transcription, and A:B markedly inhibit transcriptional activation in progesterone responsive cells [39]. Asoprisnil shows a 3-fold higher binding activity to PR than progesterone in the rabbit uterus [39,40]. In an animal model, large doses of asoprisnil have demonstrated a mixed agonist and antagonist effects [39]. Ulipristal acetate (UPA) shows a significant antagonistic and a partial agonistic effect on PR in humans; when UPA binds to PR, it decreases the binding capacity of endogenous progesterone to its receptor and blocks PR-mediated DNA transcription [39,41]. In addition, UPA is aslo able to increase the PR isoform ratio of PR-A to PR-B by reducing the level of PR-B receptor and augmenting PR-A expression [39].
Healthcare resource utilization and costs among women diagnosed with uterine fibroids compared to women without uterine fibroids
Published in Current Medical Research and Opinion, 2019
Vanessa Shih, Erika Banks, Nicole G. Bonine, Amanda Harrington, Dana Stafkey-Mailey, Binglin Yue, Jiatao Michael Ye, Rupali M. Fuldeore, Patrick Gillard
Treatment options for women with UF include pharmacologic therapy, minimally invasive procedures and major surgery. Currently available pharmacologic therapies used in the management of UF include: short-acting reversible contraceptive steroids (including oral, transdermal and vaginal ring contraceptives); long-acting reversible contraceptive steroids (including steroidal implants, depot medroxyprogesterone acetate and levonorgestrel-releasing intrauterine system); leuprolide acetate, a long-acting gonadotropin-releasing hormone (GnRH) agonist; and tranexamic acid, an oral antifibrinolytic agent. Most of these medications are not currently approved for the treatment of symptomatic UF, although the utility of low-dose combined oral contraceptives or tranexamic acid are acknowledged for the management of abnormal uterine bleeding4. Leuprolide acetate is approved for pre-operative use in this setting5. Ulipristal acetate is an orally administered selective progesterone receptor modulator that is approved in Europe (2012) and Canada (2013) for the treatment of abnormal uterine bleeding in women with UF6,7.