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https://www.readbyqxmd.com/read/28098599/is-there-a-serm-in-your-menopause-toolkit
#1
James H Liu
Over the past 3 decades, compounds called selective estrogen receptor modulators (SERMs) have been developed that block the estrogen receptor in some tissues (estrogen receptor antagonists) or stimulate the estrogen receptor in other tissues (estrogen receptor agonists). This Practice Pearl focuses on SERMs that clinicians can use for menopausal patients.
January 16, 2017: Menopause: the Journal of the North American Menopause Society
https://www.readbyqxmd.com/read/28060751/the-small-heat-shock-protein-b8-hspb8-modulates-proliferation-and-migration-of-breast-cancer-cells
#2
Margherita Piccolella, Valeria Crippa, Riccardo Cristofani, Paola Rusmini, Mariarita Galbiati, Maria Elena Cicardi, Marco Meroni, Nicola Ferri, Federica F Morelli, Serena Carra, Elio Messi, Angelo Poletti
Breast cancer (BC) is one of the major causes of cancer death in women and is closely related to hormonal dysregulation. Estrogen receptor (ER)-positive BCs are generally treated with anti hormone therapy using antiestrogens or aromatase inhibitors. However, BC cells may become resistant to endocrine therapy, a process facilitated by autophagy, which may either promote or suppress tumor expansion. The autophagy facilitator HSPB8 has been found overexpressed in some BC. Here we found that HSPB8 is highly expressed and differentially modulated by natural or synthetic selective ER modulators (SERMs), in the triple-positive hormone-sensitive BC (MCF-7) cells, but not in triple-negative MDA-MB-231 BC cells...
January 2, 2017: Oncotarget
https://www.readbyqxmd.com/read/28054434/in-vitro-phase-i-metabolism-of-selective-estrogen-receptor-modulators-in-horse-using-ultra-high-performance-liquid-chromatography-high-resolution-mass-spectrometry
#3
Karen Y Kwok, George H M Chan, Wai Him Kwok, Jenny K Y Wong, Terence S M Wan
Selective estrogen receptor modulators (SERMs) are chemicals that possess the anti-oestrogenic activities that are banned "in" and "out" of competition by the World Anti-Doping Agency (WADA) in human sports, and by the International Federation of Horseracing Authorities (IFHA) in horseracing. SERMs can be used as performance enhancing drugs to boost the level of androgens or to compensate for the adverse effects as a result of extensive use of androgenic anabolic steroids (AASs). SERMs have indeed been abused in human sports; hence, a similar threat can be envisaged in horseracing...
January 5, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/28032978/exploring-the-structural-compliancy-versus-specificity-of-the-estrogen-receptor-using-isomeric-three-dimensional-ligands
#4
Naina Sharma, Kathryn E Carlson, Jerome C Nwachukwu, Sathish Srinivasan, Abhishek Sharma, Kendall W Nettles, John A Katzenellenbogen
The estrogen receptors (ERs) bind with high affinity to many structurally diverse ligands by significantly distorting the contours of their ligand-binding pockets. This raises a question: To what degree is ER able to distinguish between structurally related regioisomers and enantiomers? We have explored the structural compliance and specificity of ERα with a set of ligands having a 7-oxa-bicyclo[2.2.1]hept-5-ene sulfonate core and basic side chains typical of selective ER modulators (SERMs). These ligands have two regioisomers, each of which is a racemate of enantiomers...
December 29, 2016: ACS Chemical Biology
https://www.readbyqxmd.com/read/28030966/systemic-drugs-that-influence-titanium-implant-osseointegration
#5
Dragos Apostu, Ondine Lucaciu, Gheorghe Dan Osvald Lucaciu, Bogdan Crisan, Liana Crisan, Mihaela Baciut, Florin Onisor, Grigore Baciut, Radu Septimiu Câmpian, Simion Bran
Titanium implants are widely used on an increasing number of patients in orthopedic and dental medicine. Despite the good survival rates of these implants, failures that lead to important socio-economic consequences still exist. Recently, research aimed at improving implant fixation, a process called osseointegration, has focused on a new, inovative field: systemic delivery of drugs. Following implant fixation, patients receive systemic drugs that could either impair or enhance osseointegration; these drugs include anabolic and anti-catabolic bone-acting agents in addition to new treatments...
December 28, 2016: Drug Metabolism Reviews
https://www.readbyqxmd.com/read/27974229/selective-estrogen-receptor-modulators-and-the-vitamin-d-analogue-eldecalcitol-block-bone-loss-in-male-osteoporosis
#6
Yuiko Sato, Toshimi Tando, Mayu Morita, Kana Miyamoto, Tami Kobayashi, Ryuichi Watanabe, Takatsugu Oike, Morio Matsumoto, Masaya Nakamura, Takeshi Miyamoto
Rapid increases in the number of elderly people have dramatically increased the number of female and male osteoporosis patients. Osteoporosis often causes bone fragility fractures, and males exhibit particularly poor prognosis after these fractures, indicating that control of osteoporosis is crucial to maintain quality of men's lives. However, osteoporosis therapies available for men have lagged behind advances available for women. Here, we show that three selective estrogen receptor modulators (SERMs), namely, raloxifene, bazedoxifene, and tamoxifen, plus the vitamin D analogue ED71, also called eldecalcitol, completely block orchiectomy-induced, testosterone-depleted bone loss in male mice in vivo...
January 22, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/27941208/-current-views-on-the-interaction-between-the-treatment-of-osteoporosis-and-cardiovascular-diseases
#7
Tomasz Zapolski, Andrzej Wysokiński
The most common medical conditions after menopause are osteoporosis and atherosclerotic disease. Traditionally these two conditions were considered unrelated and their coexistence has been attributed to independent processess exclusively reated to age. The possible link between cardiovascular disease and osteoporosis stimulates today to analyse not only the evidence of a possible association, but also to identify mutual beneficial and adverse effects of drugs used in these two diseases. That's why, the focus on the interference between osteoporosis treatment and drugs used for atherosclerosis is made...
2016: Wiadomości Lekarskie: Organ Polskiego Towarzystwa Lekarskiego
https://www.readbyqxmd.com/read/27941109/assessing-acceptability-of-a-diagnostic-and-malaria-treatment-package-delivered-by-community-health-workers-in-malaria-endemic-settings-of-burkina-faso-nigeria-and-uganda
#8
Ayodele S Jegede, Frederick O Oshiname, Armande K Sanou, Jesca Nsungwa-Sabiiti, IkeOluwapo O Ajayi, Mohamadou Siribié, Chinenye Afonne, Luc Sermé, Catherine O Falade
BACKGROUND:  The efficacy of artemisinin-based combination therapy (ACT) and rectal artesunate for severe malaria in children is proven. However, acceptability of a package of interventions that included use of malaria rapid diagnostic tests (RDTs), ACTs, and rectal artesunate when provided by community health workers (CHWs) is uncertain. This study assessed acceptability of use of CHWs for case management of malaria using RDTs, ACTs, and rectal artesunate. METHODS:  The study was carried out in Burkina Faso, Nigeria, and Uganda in 2015 toward the end of an intervention using CHWs to provide diagnosis and treatment...
December 15, 2016: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/27941108/quantifying-and-valuing-community-health-worker-time-in-improving-access-to-malaria-diagnosis-and-treatment
#9
Joëlle Castellani, Borislava Mihaylova, IkeOluwapo O Ajayi, Mohamadou Siribié, Jesca Nsungwa-Sabiiti, Chinenye Afonne, Luc Sermé, Andrew Balyeku, Vanessa Kabarungi, Josephine Kyaligonza, Silvia M A A Evers, Aggie T G Paulus, Max Petzold, Jan Singlovic, Melba Gomes
BACKGROUND:  Community health workers (CHWs) are members of a community who are chosen by their communities as first-line, volunteer health workers. The time they spend providing healthcare and the value of this time are often not evaluated. Our aim was to quantify the time CHWs spent on providing healthcare before and during the implementation of an integrated program of diagnosis and treatment of febrile illness in 3 African countries. METHODS:  In Burkina Faso, Nigeria, and Uganda, CHWs were trained to assess and manage febrile patients in keeping with Integrated Management of Childhood Illness recommendations to use rapid diagnostic tests, artemisinin-based combination therapy, and rectal artesunate for malaria treatment...
December 15, 2016: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/27941107/malaria-rapid-diagnostic-tests-and-malaria-microscopy-for-guiding-malaria-treatment-of-uncomplicated-fevers-in-nigeria-and-prereferral-cases-in-3-african-countries
#10
Catherine O Falade, IkeOluwapo O Ajayi, Jesca Nsungwa-Sabiiti, Mohamadou Siribié, Amidou Diarra, Luc Sermé, Chinenye Afonne, Oyindamola B Yusuf, Zakaria Gansane, Ayodele S Jegede, Jan Singlovic, Melba Gomes
BACKGROUND:  The World Health Organization recommends that malaria treatment be based on demonstration of the infecting Plasmodium parasite specie. Malaria rapid diagnostic tests (RDTs) are recommended at community points of care because they are accurate and rapid. We report on parasitological results in a malaria study in selected rural communities in 3 African countries. METHODS:  In Nigeria, community health workers (CHWs) performed RDTs (SD-Bioline) and thick blood smears on all children suspected to have malaria...
December 15, 2016: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/27941105/compliance-with-malaria-rapid-diagnostic-testing-by-community-health-workers-in-3-malaria-endemic-countries-of-sub-saharan-africa-an-observational-study
#11
Jan Singlovic, IkeOluwapo O Ajayi, Jesca Nsungwa-Sabiiti, Mohamadou Siribié, Armande K Sanou, Ayodele S Jegede, Catherine O Falade, Luc Sermé, Zakaria Gansane, Chinenye Afonne, Vanessa Kabarungi, Josephine Kyaligonza, Joëlle Castellani, Max Petzold, Melba Gomes
BACKGROUND:  The World Health Organization recommends that all malaria management be based on parasitological identification. We monitored performance of trained community health workers (CHWs) in adhering to this recommendation to restrict artemisinin-based combination therapies (ACTs) to positive rapid diagnostic test (RDT)-confirmed cases in children in 3 malaria-endemic sub-Saharan African countries. METHODS:  In 33 villages in Burkina Faso, 45 villages in Nigeria, and 84 villages in Uganda, 265 CHWs were trained over a minimum of 3 days to diagnose malaria using RDTs (prepare, read, record results, and inform the patient about results) and treat RDT-confirmed uncomplicated malaria cases with ACTs...
December 15, 2016: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/27941104/motivation-of-community-health-workers-in-diagnosing-treating-and-referring-sick-young-children-in-a-multicountry-study
#12
Armande K Sanou, Ayodele S Jegede, Jesca Nsungwa-Sabiiti, Mohamadou Siribié, IkeOluwapo O Ajayi, Asaf Turinde, Frederick O Oshiname, Luc Sermé, Vanessa Kabarungi, Catherine O Falade, Josephine Kyaligonza, Chinenye Afonne, Andrew Balyeku, Joëlle Castellani, Melba Gomes
BACKGROUND:  Community health workers (CHWs) are an important element of care provision for a wide range of conditions, but their turnover rate is high. Many studies have been conducted on health workers' motivation, focusing on formal sector staff but not CHWs. Although CHWs are easy to recruit, motivating and retaining them for service delivery is difficult. This article investigates factors influencing CHW motivation and retention in health service delivery. METHODS:  Quantitative and qualitative data were collected to identify the key factors favoring motivation and retention of CHWs as well as those deterring them...
December 15, 2016: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/27941103/training-community-health-workers-to-manage-uncomplicated-and-severe-malaria-experience-from-3-rural-malaria-endemic-areas-in-sub-saharan-africa
#13
Mohamadou Siribié, IkeOluwapo O Ajayi, Jesca Nsungwa-Sabiiti, Chinenye Afonne, Andrew Balyeku, Catherine O Falade, Zakaria Gansane, Ayodele S Jegede, Lillian Ojanduru, Frederick O Oshiname, Vanessa Kabarungi, Josephine Kyaligonza, Armande K Sanou, Luc Sermé, Joëlle Castellani, Jan Singlovic, Melba Gomes
BACKGROUND:  Use of community health workers (CHWs) to increase access to diagnosis and treatment of malaria is recommended by the World Health Organization. The present article reports on training and performance of CHWs in applying these recommendations. METHODS:  Two hundred seventy-nine CHWs were trained for 3-5 days in Burkina Faso, Nigeria, and Uganda, and 19 were certified to diagnose and treat only uncomplicated malaria and 235 to diagnose and treat both uncomplicated and severe malaria...
December 15, 2016: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/27941102/impact-of-improving-community-based-access-to-malaria-diagnosis-and-treatment-on-household-costs
#14
Joëlle Castellani, Jesca Nsungwa-Sabiiti, Borislava Mihaylova, IkeOluwapo O Ajayi, Mohamadou Siribié, Chinenye Afonne, Andrew Balyeku, Luc Sermé, Armande K Sanou, Benjamin S Sombié, Alfred B Tiono, Sodiomon B Sirima, Vanessa Kabarungi, Catherine O Falade, Josephine Kyaligonza, Silvia M A A Evers, Aggie T G Paulus, Max Petzold, Jan Singlovic, Melba Gomes
BACKGROUND:  Community health workers (CHWs) were trained in Burkina Faso, Nigeria, and Uganda to diagnose febrile children using malaria rapid diagnostic tests, and treat positive malaria cases with artemisinin-based combination therapy (ACT) and those who could not take oral medicines with rectal artesunate. We quantified the impact of this intervention on private household costs for childhood febrile illness. METHODS:  Households with recent febrile illness in a young child in previous 2 weeks were selected randomly before and during the intervention and data obtained on household costs for the illness episode...
December 15, 2016: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/27941101/feasibility-of-malaria-diagnosis-and-management-in-burkina-faso-nigeria-and-uganda-a-community-based-observational-study
#15
IkeOluwapo O Ajayi, Jesca Nsungwa-Sabiiti, Mohamadou Siribié, Catherine O Falade, Luc Sermé, Andrew Balyeku, Chinenye Afonne, Armande K Sanou, Vanessa Kabarungi, Frederick O Oshiname, Zakaria Gansane, Josephine Kyaligonza, Ayodele S Jegede, Alfred B Tiono, Sodiomon B Sirima, Amidou Diarra, Oyindamola B Yusuf, Florence Fouque, Joëlle Castellani, Max Petzold, Jan Singlovic, Melba Gomes
BACKGROUND:  Malaria-endemic countries are encouraged to increase, expedite, and standardize care based on parasite diagnosis and treat confirmed malaria using oral artemisinin-based combination therapy (ACT) or rectal artesunate plus referral when patients are unable to take oral medication. METHODS:  In 172 villages in 3 African countries, trained community health workers (CHWs) assessed and diagnosed children aged between 6 months and 6 years using rapid histidine-rich protein 2 (HRP2)-based diagnostic tests (RDTs)...
December 15, 2016: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/27936172/tamoxifen-isomers-and-metabolites-exhibit-distinct-affinity-and-activity-at-cannabinoid-receptors-potential-scaffold-for-drug-development
#16
Benjamin M Ford, Lirit N Franks, Anna Radominska-Pandya, Paul L Prather
Tamoxifen (Tam) is a selective estrogen receptor (ER) modulator (SERM) that is an essential drug to treat ER-positive breast cancer. Aside from known actions at ERs, recent studies have suggested that some SERMs like Tam also exhibit novel activity at cannabinoid subtype 1 and 2 receptors (CB1R and CB2Rs). Interestingly, cis- (E-Tam) and trans- (Z-Tam) isomers of Tam exhibit over a 100-fold difference in affinity for ERs. Therefore, the current study assessed individual isomers of Tam and subsequent cytochrome P450 metabolic products, 4-hydroxytamoxifen (4OHT) and 4-hydroxy-N-desmethyl tamoxifen (End) for affinity and activity at CBRs...
2016: PloS One
https://www.readbyqxmd.com/read/27935770/from-breast-cancer-to-antimicrobial-combating-extremely-resistant-gram-negative-superbugs-using-novel-combinations-of-polymyxin-b-with-selective-estrogen-receptor-modulators
#17
Maytham H Hussein, Elena K Schneider, Alysha G Elliott, Meiling Han, Felisa Reyes-Ortega, Faye Morris, Mark A T Blastovich, Raad Jasim, Bart Currie, Mark Mayo, Mark Baker, Matthew A Cooper, Jian Li, Tony Velkov
Novel therapeutic approaches are urgently needed to combat nosocomial infections caused by extremely drug-resistant (XDR) "superbugs." This study aimed to investigate the synergistic antibacterial activity of polymyxin B in combination with selective estrogen receptor modulators (SERMs) against problematic Gram-negative pathogens. In vitro synergistic antibacterial activity of polymyxin B and the SERMs tamoxifen, raloxifene, and toremifene was assessed using the microdilution checkerboard and static time-kill assays against a panel of Gram-negative isolates...
December 9, 2016: Microbial Drug Resistance: MDR: Mechanisms, Epidemiology, and Disease
https://www.readbyqxmd.com/read/27891390/effectiveness-of-centchroman-on-regression-of-fibroadenosis-and-mastalgia
#18
Udayakumar Rajswaroob, Rajendiran Kannan, Narayanasamy Subbaraju Kannan, T Tirouaroul
INTRODUCTION: Fibroadenosis and mastalgia are common among the women in reproductive age group. Treatment for these conditions is not yet standardised. Most of the drugs used for fibroadenosis and mastalgia are expensive and have side effects. AIM: To find out the efficacy of centchroman, a Selective Estrogens Receptor Modulator (SERM) on regression of fibroadenosis and mastalgia. MATERIALS AND METHODS: Fifty one patients with mastalgia/fibroadenosis were treated with centchroman 30mg once daily on alternate days for a period of 3 months and followed up weekly for six months with Mastalgia chart and Visual Analog Scale (VAS) pain score...
October 2016: Journal of Clinical and Diagnostic Research: JCDR
https://www.readbyqxmd.com/read/27857920/effectiveness-of-osteoporosis-drug-in-postmenopausal-women-with-spinal-compression-fracture-combined-consecutive-therapy-of-teriparatide-and-raloxifene-versus-bisphosphonate-single
#19
Chang Jin Shin, Sion Kim, Chun Sik Choi, Hyun Chul Shin, Young Joon Kwon
OBJECTIVE: Bisphosphonate, a typical bone resorption inhibitor, is an important first-line drug for treating osteoporosis. Recent studies show a novel paradigm in stimulating bone formation. Teriparatide, which is composed of recombinant human parathyroid hormone, stimulates osteoblasts and induces bone regeneration. Bone mineral density (BMD) that was used before and after the treatment with anti-osteoporosis drug was compared for the effectiveness in therapy between a combination of teriparatide and selective estrogen receptor modulator (SERM), and bisphosphonate...
October 2016: Korean Journal of Neurotrauma
https://www.readbyqxmd.com/read/27855957/age-and-duration-of-testosterone-therapy-predict-time-to-return-of-sperm-count-after-human-chorionic-gonadotropin-therapy
#20
Taylor P Kohn, Matthew R Louis, Stephen M Pickett, Mark C Lindgren, Jaden R Kohn, Alexander W Pastuszak, Larry I Lipshultz
OBJECTIVE: To determine factors that influence sperm recovery after T-associated infertility. DESIGN: Clinical retrospective study. SETTING: Academic male-infertility urology clinic. PATIENT(S): Sixty-six men who presented with infertility after T use. INTERVENTION(S): T cessation and combination high-dose hCG and selective estrogen modulator (SERM) therapy. MAIN OUTCOME MEASURE(S): Whether patients successfully achieved or failed to achieve a total motile count (TMC) of greater than 5 million sperm within 12 months of T cessation and initiation of therapy...
November 14, 2016: Fertility and Sterility
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