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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
Vicente Ruiz-García, Eduardo López-Briz, Rafael Carbonell-Sanchis, Sylvia Bort-Martí, José Luis Gonzálvez-Perales
In 1993, megestrol acetate (MA) was approved by the US Food and Drug Administration for the treatment of anorexia, cachexia, or unexplained weight loss in patients with acquired immunodeficiency syndrome. The mechanism by which MA increases appetite is unknown, and its effectiveness for anorexia and cachexia in neoplastic, elderly, and acquired immunodeficiency syndrome patients is under investigation. This is an updated version of a Cochrane systematic review first published in 2005 and later updated in 2013 entitled 'Megestrol acetate for the treatment of anorexia-cachexia syndrome'...
March 14, 2018: Journal of Cachexia, Sarcopenia and Muscle
Ewa Zabrocka, Marek Z Wojtukiewicz, Ewa Sierko
Advanced cancer patients in hospice are at notably increased risk of venous thromboembolism (VTE) due to age, local and distal advancement of the malignancy and bed confinement, among other factors. Asymptomatic VTE prevalence among palliative care patients has been found to reach 50%, whereas the clinically overt form occurs in 10%. Hospice patients are frequently given medications increasing VTE risk, for instance megestrol which is a drug commonly used in cancer cachexia. Many of the available guidelines encourage the implementation of thromboprophylaxis (TPX) in cancer patients, e...
February 2018: Advances in Clinical and Experimental Medicine: Official Organ Wroclaw Medical University
Halis Kaan Akturk, Ana Maria Chindris, Jolaine M Hines, Ravinder J Singh, Victor J Bernet
OBJECTIVE: To assess whether dietary supplements that are herbal and/or animal-derived products, marketed for enhancing metabolism or promoting energy, "adrenal fatigue," or "adrenal support," contain thyroid or steroid hormones. METHODS: Twelve dietary adrenal support supplements were purchased. Pregnenolone, androstenedione, 17-hydroxyprogesterone, cortisol, cortisone, dehydroepiandrosterone sulfate, synthetic glucocorticoids (betamethasone, dexamethasone, fludrocortisone, megestrol acetate, methylprednisolone, prednisolone, prednisone, budesonide, and triamcinolone acetonide) levels were measured twice in samples in a blinded fashion...
March 2018: Mayo Clinic Proceedings
Bizhan Kouchaki, Ghasem Janbabai, Abbas Alipour, Shahram Ala, Samaneh Borhani, Ebrahim Salehifar
PURPOSE: Previous studies reported promising efficacy for celecoxib in the treatment of cancer cachexia. We designed this study to test the hypothesis that combination therapy with megestrol acetate (MA) plus celecoxib is superior to MA alone. METHODS: Ninety eligible gastrointestinal cancer patients randomly received either MA 320 mg/day plus placebo (arm1) or MA 320 mg/day plus celecoxib 200 mg/day (arm2). Patients were evaluated at baseline, then 1 and 2 months after starting interventions...
February 13, 2018: Supportive Care in Cancer: Official Journal of the Multinational Association of Supportive Care in Cancer
Frances K Wen, James Millar, Linda Oberst-Walsh, Joan Nashelsky
No. Megestrol acetate (MA) is neither safe nor effective for stimulating appetite in malnourished nursing home residents. It increases the risk of deep vein thrombosis (strength of recommendation [SOR]: C, 2 retrospective chart reviews), but isn't associated with other new or worsening events or disorders (SOR: B, single randomized controlled trial [RCT]). Over a 25-week period, MA wasn't associated with increased mortality (SOR: B, single RCT). After 44 months, however, MA-treated patients showed decreased median survival (SOR: B, single case-control study)...
February 2018: Journal of Family Practice
Martin Mücke, Megan Weier, Christopher Carter, Jan Copeland, Louisa Degenhardt, Henning Cuhls, Lukas Radbruch, Winfried Häuser, Rupert Conrad
We provide a systematic review and meta-analysis on the efficacy, tolerability, and safety of cannabinoids in palliative medicine. The Cochrane Central Register of Controlled Trials (CENTRAL), MEDLINE, PsycINFO, PubMed, Scopus, and, and a selection of cancer journals were searched up until 15th of March 2017. Of the 108 screened studies, nine studies with a total of 1561 participants were included. Overall, the nine studies were at moderate risk of bias. The quality of evidence comparing cannabinoids with placebo was rated according to Grading of Recommendations Assessment, Development, and Evaluation as low or very low because of indirectness, imprecision, and potential reporting bias...
February 5, 2018: Journal of Cachexia, Sarcopenia and Muscle
Huifang Zhao, Yushuang Yao, Hongjuan Yang, Dehua Ma, Aiping Chen
RATIONALE: Endometrial cancer patients with lung metastases are rare, and more rarely with long-term management of progesterone after recurrence. PATIENT CONCERNS: Informed consent of the patients and their families. DIAGNOSES: Endometrial cancer (IVB) (Refer to 2009 FIGO stag of endometrial cancer). INTERVENTIONS: the patient was treated with Megestrol Acetate Dispersible Tablets (trade name Yilizhi), 160 mg, orally, once daily, without interruption...
December 2017: Medicine (Baltimore)
Arie J Verschoor, Fabiënne A R M Warmerdam, Tjalling Bosse, Judith V M G Bovée, Hans Gelderblom
BACKGROUND: Pazopanib is an oral tyrosine kinase inhibitor registered for metastatic renal cell carcinoma and soft tissue sarcoma. Liver toxicity is a common side effect for this class of agents. The current opinion is that in case of severe liver toxicity pazopanib should be interrupted and restarted at a lower dose after returning to Common Terminology Criteria for Adverse Events (CTCAE) grade 1. After recurrence of liver toxicity at the lower dose it is advised to permanently stop pazopanib...
January 22, 2018: BMC Cancer
Tomás Reinert, Carlos H Barrios
We reviewed randomized phase II/III trials comparing first- or second-line endocrine therapy as monotherapy or in combination with targeted therapies for treatment of postmenopausal patients with hormone receptor-positive advanced breast cancer. First-line was defined as treatment for endocrine therapy-naïve advanced breast cancer or advanced disease treated with endocrine therapy in the adjuvant/neoadjuvant setting. Second-line was defined as endocrine therapy for advanced breast cancer following disease progression on endocrine therapy for advanced disease...
November 2017: Therapeutic Advances in Medical Oncology
Vicky Makker, Angela K Green, Robert M Wenham, David Mutch, Brittany Davidson, David Scott Miller
Endometrial cancer is the most common gynecologic malignancy in the United States, accounting for 6% of cancers in women. In 2017, an estimated 61,380 women were diagnosed with endometrial cancer, and approximately 11,000 died from this disease. From 1987 to 2008, there was a 50% increase in the incidence of endometrial cancer, with an approximate 300% increase in the number of associated deaths. Although there are many chemotherapeutic and targeted therapy agents approved for ovarian, fallopian tube and primary peritoneal cancers, since the 1971 approval of megestrol acetate for the palliative treatment of advanced endometrial cancer, only pembrolizumab has been Food and Drug Administration (FDA)-approved for high microsatellite instability (MSI-H) or mismatch repair deficient (dMMR) endometrial cancer; this highlights the need for new therapies to treat advanced, recurrent, metastatic endometrial cancer...
2017: Gynecologic Oncology Research and Practice
Zhi-Yuan Zhang, Xin Wang, Dan Liu, Hua Zhang, Qiang Zhang, Ying-Yuan Lu, Pu Li, Ya-Qing Lou, Bao-Xue Yang, Chuang Lu, Ya-Xin Lou, Guo-Liang Zhang
A specific, sensitive and stable high-performance liquid chromatographic-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the quantitative determination of methyl 3-amino-6-methoxythieno [2,3-b]quinoline-2-carboxylate (PU-48), a novel diuretic thienoquinolin urea transporter inhibitor in rat plasma. In this method, the chromatographic separation of PU-48 was achieved with a reversed-phase C18 column (100 × 2.1 mm, 3 μm) at 35°C. The mobile phase consisted of acetonitrile and water with 0...
November 28, 2017: Biomedical Chromatography: BMC
Oksana Golovko, Pavel Šauer, Ganna Fedorova, Hana Kocour Kroupová, Roman Grabic
The aim of this study was to develop a reliable analytical method for the measurement of 17 selected progestogens in waste water and surface water. Automated whole water solid phase extraction (SPE) was used for sample concentration. Liquid chromatography tandem atmospheric pressure chemical ionization/atmospheric pressure photoionization with hybrid quadrupole/orbital trap mass spectrometry operated in high resolution product scan mode (LC-APCI/APPI-HRPS) was applied for the analyses. The whole-method recoveries ranged from 60% to 140% for all analytes at two different spike levels (5 and 50ng/L) in the studied matrices...
October 25, 2017: Science of the Total Environment
Seo Young Dai, Su-Eon Jin, Daehyun Kim, Don Haeng Lee, Su-Geun Yang
Megestrol acetate (MGA) is used as a progestagen to treat advanced cancers in the breast or uterus and anorexia-cachexia syndrome in cancer patients. Due to its low solubility (BCS class II), MGA bioavailability needs to be enhanced for efficacy and safety. We developed MGA-encapsulated Eudragit(®) L100 (EUD) nanoparticles (MGA-EUD (1:1) and MGA-EUD (2:1)) using an ultrasonic nebulization method. MGA-EUD (1:1) and MGA-EUD (2:1) consisted of MGA and EUD at the mass ratios of 1:1 and 2:1. Their physicochemical properties, i...
November 2, 2017: Pharmaceutical Development and Technology
Naomi S Clement, Thomas Rw Oliver, Hunain Shiwani, Juliane Rf Sanner, Caroline A Mulvaney, William Atiomo
BACKGROUND: Endometrial cancer is one of the most common gynaecological cancers in the world. Rates of endometrial cancer are rising, in part because of rising obesity rates. Endometrial hyperplasia is a precancerous condition in women that can lead to endometrial cancer if left untreated. Endometrial hyperplasia occurs more commonly than endometrial cancer. Progesterone tablets currently used to treat women with endometrial hyperplasia are associated with adverse effects in up to 84% of women...
October 27, 2017: Cochrane Database of Systematic Reviews
William L Read, Sumita Trivedi, Felicia Williams
•Progestins can produce clinical benefit in a subset of women with metastatic endometrial cancer.•Corticosteroid-related effects of megestrol can cause morbidity over the long term.•Norethindrone is a progestin without corticosteroid side effects.•A switch from megestrol to norethindrone decreased toxicity with continued benefit.•A clinical trial of norethindrone for this population of patients would be welcome.
November 2017: Gynecologic Oncology Reports
Larry House, Michael Seminerio, Snezana Mirkov, Jacqueline Ramirez, Maxwell Skor, Joseph Sachleben, Masis Isikbay, Hari Singhal, Geoffrey Greene, Donald Vander Griend, Suzanne Conzen, Mark J Ratain
There is limited knowledge regarding the metabolism of megestrol acetate (MA), as it was approved by FDA in 1971, prior to the availability of modern tools for identifying specific drug-metabolizing enzymes. We determined the cytochrome P450s (P450s) and UDP-glucuronosyltransferases (UGTs) that metabolize MA, identified oxidative metabolites, and determined pharmacologic activity at the progesterone, androgen and glucocorticoid receptors (PR, AR, and GR, respectively). Oxidative metabolites were produced using human liver microsomes (HLMs), and isolated for mass spectral (MS) and nuclear magnetic resonance (NMR) analyses...
October 20, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
Chutima Leelalertlauw, Pat Mahachoklertwattana, Suradej Hongeng, Preamrudee Poomthavorn
No abstract text is available yet for this article.
October 12, 2017: Journal of Paediatrics and Child Health
Wei Wen, Gina Lowe, Cai M Roberts, James Finlay, Ernest S Han, Carlotta A Glackin, Thanh H Dellinger
Endometrial cancer is the most common gynecologic cancer in the United States and its incidence and mortality has been rising over the past decade. Few treatment options are available for patients with advanced and recurring endometrial cancers. Novel therapies, which are frequently toxic, are difficult to establish in this patient population which tends to be older and plagued by comorbidities such as diabetes mellitus and hypertension. Therefore, novel, non-toxic therapies are urgently needed. Megestrol acetate is a frequently used drug in endometrial cancer patients...
October 6, 2017: Scientific Reports
Ana Coelho Gomes, José Maria Aragüés, Sílvia Guerra, Joana Fernandes, Mário Rui Mascarenhas
Hypogonadotropic hypogonadism (HH) is common and occurs prematurely in HIV-infected men. However, HH with very low testosterone has not been described. Three men with normal pubertal development and HIV1 diagnosis at the ages of 22, 34 and 35 years. All complained of decreased libido, anejaculation and erectile dysfunction thirteen years, six months and one year after HIV diagnosis, respectively. Two had depressive syndrome and two were treated with antiretroviral therapy. Laboratory tests revealed isolated HH in all...
2017: Endocrinology, Diabetes & Metabolism Case Reports
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