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Ulipristal acetate

Pavel Šauer, Alžběta Stará, Oksana Golovko, Olga Valentová, Adam Bořík, Roman Grabic, Hana Kocour Kroupová
Vast numbers of xenobiotics are known still to be present in treated municipal wastewater treatment plant (WWTP) effluents. Some of these possess endocrine-disrupting potency and pose risks for exposed aquatic animals. We searched for 17 potential environmental contaminants having affinity to the progesterone receptor. Relative potency values of these progesterone receptor-active chemicals were obtained. On the basis of relative potencies and measured environmental concentrations, the contribution of progestins to measured progestagenic activities was evaluated...
March 2, 2018: Water Research
Natalie Woodhead, Rachel Pounds, Shirin Irani, Poonam Pradhan
Ulipristal acetate (UPA), is a selective progesterone-receptor modulator, it decreases fibroid size and reduces menstrual bleeding. We reviewed its use at the Heart of England Foundation Trust (HEFT), one of the largest prescribing trusts in the UK. The electronic records of patients treated with UPA from January 2013 to August 2015 were reviewed. One hundred and thirty four patients received UPA, 20 women (15%) received a second course. Eighty percent reported subjective global improvements in symptoms after the first course; 45...
March 12, 2018: Journal of Obstetrics and Gynaecology: the Journal of the Institute of Obstetrics and Gynaecology
Michał Ciebiera, Marta Włodarczyk, Małgorzata Wrzosek, Aneta Słabuszewska-Jóźwiak, Grażyna Nowicka, Grzegorz Jakiel
OBJECTIVE: To evaluate and compare transforming growth factor β3 (TGF-β3) serum concentration in patients with uterine fibroids (UFs) without hormone treatment, treated with ulipristal acetate (UPA), and controls; to evaluate TGF-β3 concentrations in UF tissue in patients without hormone treatment and those treated with UPA; and to evaluate the correlations of age and body mass index (BMI) with TGF-β3 serum and UF tissue levels between the groups. DESIGN: Retrospective cohort study...
March 7, 2018: Fertility and Sterility
Silvia Baggio, Paola Pomini, Fabiana Galeone, Francesca Presti, Lorenza Santi, Ricciarda Raffaelli, Massimo Franchi
OBJECTIVES: To investigate the modifications of uterine and fibroid volume, to study Doppler changes in uterine arteries and fibroid-supplying vessels, and to assess possible symptomatic relief after 3 months of treatment with ulipristal acetate. METHODS: Forty-two premenopausal women with symptomatic fibroids were included in the study. They were evaluated clinically for the symptoms reported and underwent ultrasound examinations before starting treatment and after 3 months of therapy with ulipristal acetate...
March 2, 2018: Journal of Ultrasound in Medicine: Official Journal of the American Institute of Ultrasound in Medicine
Jacques Donnez, Pablo Arriagada, Olivier Donnez, Marie-Madeleine Dolmans
Uterine fibroids (also known as leiomyomas or myomas) are the most common form of benign uterine tumors. Current management strategies involve mainly surgical interventions, but the choice of treatment is guided by patient age and desire to preserve fertility or avoid 'radical' surgery such as hysterectomy. Areas covered: There is growing evidence of the crucial role of progesterone pathways in the pathophysiology of uterine fibroids, leading to increasing use of selective progesterone receptor modulators (SPRMs) such as ulipristal acetate...
February 28, 2018: Expert Opinion on Emerging Drugs
Karolina Piecak, Paweł Milart, Ewa Woźniakowska, Tomasz Paszkowski
Uterine fibroids are the most common benign uterine tumours. Clinical symptoms include abnormal bleeding, pelvic pressure, pelvic pain, infertility and obstetric complications. Approximately one third of women with fibroids will require treatment. The management also depends on the number, size, and location of the fibroids. There are surgical and non-surgical treatment options. The choice of therapy depends on different factors, such as the severity of symptoms, tumour characteristics, age, and wish to preserve the uterus and fertility...
December 2017: Przeglad Menopauzalny, Menopause Review
Meric A Altinoz, Aysel Ozpinar, Ilhan Elmaci
Female gender, contraceptives, and menopausal hormone replacement treatments containing progesterone analogues associate with higher risk of meningiomas yet with lower risk of gliomas. Progesterone receptor (PR) expression and mifepristone treatment was highly discussed for meningiomas. However, much less is known in regard to progesterone actions in gliomas despite PR expression strongly correlates with their grade. Meningiomas and gliomas may grow faster during gestation; but paradoxically, parousity reduces lifetime risk of gliomas which can be explained with dichotomous cell growth-stimulating and inhibitory actions of progesterone at low versus high levels...
February 17, 2018: Neurosurgical Review
James A Simon, William Catherino, James H Segars, Rick E Blakesley, Anna Chan, Vilma Sniukiene, Ayman Al-Hendy
OBJECTIVE: To assess efficacy and tolerability of ulipristal acetate, a selective progesterone receptor modulator, for treatment of symptomatic uterine leiomyomas. METHODS: This phase 3, double-blind, placebo-controlled study enrolled premenopausal women (aged 18-50 years) with abnormal uterine bleeding, one or more discrete leiomyomas, and uterine size 20 weeks of gestation or less. Patients were randomized 1:1:1 to 5 mg ulipristal, 10 mg ulipristal, or placebo once daily for 12 weeks followed by 12-week drug-free follow-up...
March 2018: Obstetrics and Gynecology
Brandon K Bellows, Casey R Tak, Jessica N Sanders, David K Turok, Eleanor B Schwarz
BACKGROUND: The copper intrauterine device is the most effective form of emergency contraception and can also provide long-term contraception. The levonorgestrel intrauterine device has also been studied in combination with oral levonorgestrel for women seeking emergency contraception. However, intrauterine devices have higher upfront costs than oral methods, such as ulipristal acetate and levonorgestrel. Healthcare payers and decision makers (e.g., healthcare insurers, government programs) with financial constraints must determine if the increased effectiveness of intrauterine device emergency contraception methods are worth the additional costs...
January 31, 2018: American Journal of Obstetrics and Gynecology
Guillaume E Courtoy, Patrick Henriet, Etienne Marbaix, Matthieu de Codt, Mathieu Luyckx, Jacques Donnez, Marie-Madeleine Dolmans
Context: Ulipristal acetate (UPA), a selective progesterone receptor modulator, clinically reduces uterine myoma size in 80% of cases. However, the molecular mechanism of action is still poorly understood, as is the reason why 20% of myomas do not respond to treatment. Objective: To elucidate whether matrix metalloproteinases (MMPs) and tissue inhibitors of MMPs (TIMPs) are associated with myoma volume shrinkage after UPA therapy. Design: Prospective study...
February 1, 2018: Journal of Clinical Endocrinology and Metabolism
Brigitta Badiani, Marco Chiumente, Andrea Messori
OBJECTIVES: The aim of this study was to evaluate the pharmacoeconomic profile in Italy of preoperative treatment with ulipristal acetate at the dose of 5 mg/day for 13 weeks in comparison with placebo prior to surgical management of symptomatic uterine fibroids. STUDY DESIGN: The pharmacoeconomic analysis was based on the calculation of incremental cost-effectiveness ratio (ICER). Effectiveness data were derived from the randomized-controlled trial PEARL-1, whilst costs data were retrieved from the published literature...
March 2018: European Journal of Obstetrics, Gynecology, and Reproductive Biology
J C Molina Martín, M Balboa Alonso, J García Sánchez, M González Herrera, J R Hueso Abancens, E Mengual Verdú
CASE REPORT: The case concerns a 31 year-old woman with no previous history who consulted due to decreased vision in both eyes. She mentioned taking 1 pill of ulipristal acetate (30mg) as an emergency contraceptive four days before the visual symptoms appeared. In the examination, a better corrected visual acuity of 0.6 was found in the right eye and 0.8 in left eye (by Snellen chart), and bilateral macular serous detachment. It was decided to observe, and 15 days later she showed a functional and anatomical improvement...
February 1, 2018: Archivos de la Sociedad Española de Oftalmología
N Chabbert-Buffet, K Kolanska, E Daraï, P Bouchard
Selective progesterone receptor modulators (SPRMs) are steroid progesterone receptor ligands able to induce agonistic or antagonistic activities. Mifepristone, the class leader, was primarily used for pregnancy termination from the 1980s. Emergency contraception with extended activity was the second major development 30 years later, with mifepristone in some countries and ulipristal acetate world-wide. More recently, ulipristal acetate was released for the treatment of myoma-related uterine bleeding. In addition to a very rapid cessation of bleeding, SPRMs allow a decrease in myoma volume, as do gonadotropin releasing hormone analogs...
January 17, 2018: Climacteric: the Journal of the International Menopause Society
Jean-Luc Brun, José Rajaonarison, Alizée Froeliger, Anne-Coline Monseau-Thiburce, Rado Randriamboavonjy, Andrej Vogler
OBJECTIVES: To determine the proportion and the characteristics of patients who did or did not respond after 3 months of ulipristal acetate (UPA) therapy. STUDY DESIGN: In this retrospective cohort study conducted in the University Hospital of Bordeaux (France) and University Medical Center Ljubljana (Slovenia), symptomatic non-menopausal patients with fibroids that qualified for surgery were pretreated by 3 months of oral UPA 5 mg/day. Clinical success was defined by normalization of the bleeding score, and/or regression of pelvic pain, and/or abdominal distension...
March 2018: European Journal of Obstetrics, Gynecology, and Reproductive Biology
Kim E Kortekaas, Harold M P Pelikan
This case report describes a very rare coexistence of retroperitoneal lymphogenic and pulmonary metastases of a benign leiomyoma: benign metastasising leiomyoma (BML). Despite surgical treatment growth of multiple nodules in the lungs, omentum, mesenterium and retroperitoneum was observed by CT scan. We started off-label ulipristal acetate treatment with impressive results. The lesions on the CT scan disappeared, and the patient was asymptomatic after treatment.
January 3, 2018: BMJ Case Reports
Josep Estadella, Pia Español, Fiorella Ascencio, Josep Perelló, Joaquim Calaf
Heavy menstrual bleeding is a common condition among women of childbearing age. Although hysterectomy was the usual approach in acute cases in the past, other minimally invasive therapies or pharmacological alternatives, such as the levonorgestrel intrauterine device have shown to be highly effective. This case report presents the case of a pluripathological patient with acute heavy menstrual bleeding and severe anemia, who was successfully managed with ulipristal acetate, a selective progesterone receptor modulator...
December 20, 2017: Gynecological Endocrinology
Simone Ferrero, Valerio Gaetano Vellone, Fabio Barra
Uterine fibroids are the most common form of benign gynecological tumors in women of reproductive ages. Although surgery is the main option to treat them, alternative pharmacological approaches are being investigated to control their symptoms. Among them, ulipristal acetate (UPA) has been the first selective progesterone-receptor modulator (SPRM) approved for the pre-operative and long-term treatment of uterine fibroids. Areas covered: The aim of this article is to review the literature on the pharmacodynamics, pharmacokinetics (PK), clinical efficacy and safety of UPA for the treatment of uterine fibroids...
January 2018: Expert Opinion on Drug Metabolism & Toxicology
Athilakshmi Kannan, Arpita Bhurke, Regine Sitruk-Ware, Parameswaran G Lalitkumar, Kristina Gemzell-Danielsson, Alistair R W Williams, Robert N Taylor, Milan K Bagchi, Indrani C Bagchi
Ulipristal acetate (UPA) is a selective progesterone receptor modulator (PRM), which is used as an emergency contraceptive in women. Recent studies demonstrated the efficacy of an UPA contraceptive vaginal ring (UPA-CVR) as a blocker of ovulation. However, the endometrium of women exposed to UPA over a 6-month period display glandular changes, termed PRM-associated endometrial changes (PAECs). We, therefore, investigated whether UPA-induced PAECs are associated with altered expression of the transcription factor heart- and neural crest derivatives-expressed protein 2 (HAND2) whose downregulation is observed in endometrial epithelial hyperplasia and cancer...
January 1, 2017: Reproductive Sciences
Guillaume E Courtoy, Jacques Donnez, Etienne Marbaix, Matilde Barreira, Mathieu Luyckx, Marie-Madeleine Dolmans
OBJECTIVE: To investigate whether ulipristal acetate (UPA) treatment modifies the expression of progesterone receptor (PR), its nuclear cofactors steroid receptor coactivator-1 (SRC1) and nuclear corepressor-1 (NCoR1), prosurvival factor B-cell lymphoma 2 (Bcl-2), and Akt in uterine myomas. PATIENTS: Prospective study of 59 women with symptomatic myomas undergoing myomectomy. Forty-two patients were treated preoperatively with UPA; the remaining 17 were not and they served as controls...
December 11, 2017: Gynecologic and Obstetric Investigation
Nanna Sarvilinna, Leila Unkila-Kallio, Päivi Härkki, Aila Tiitinen, Oskari Heikinheimo
Progesterone regulates several female reproductive functions. Progesterone and synthetic progestins derived from it have long been utilized in gynecology. The effects of these steroids in target cells are mediated via progesterone receptors, Progesterone receptors are also the target of action of selective progesterone receptor modulators. Of the molecules of this newer group of drugs, two are presently in clinical use. Mifepristone is used in nonsurgical abortion, in softening of the cervix before surgical abortion, and in the induction of labor in cases of intrauterine death...
2017: Duodecim; Lääketieteellinen Aikakauskirja
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