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Raloxifene

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https://www.readbyqxmd.com/read/28224392/investigation-of-need-of-natural-bioenhancer-for-a-metabolism-susceptible-drug-raloxifene-in-a-designed-self-emulsifying-drug-delivery-system
#1
Poonam Singh Thakur, Narinder Singh, Abhay T Sangamwar, Arvind Kumar Bansal
Bioenhancers can increase the bioavailability of metabolism susceptible drugs. The present study was designed to understand the impact of bioenhancer on permeability and bioavailability of a biopharmaceutical drug disposition classification system (BDDCS) class II drug raloxifene (RLX). RLX undergoes extensive first pass metabolism by UGT enzymes in gastrointestinal tract (GIT) and has an oral bioavailability of about 2%. Self-emulsifying drug delivery system (SEDDS) of RLX was developed using a designed approach and this formulation was loaded with reported bioenhancers: quercetin and piperine...
February 21, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28185712/the-effect-of-selective-estrogen-receptor-modulators-on-type-2-diabetes-onset-in-women-basic-and-clinical-insights
#2
REVIEW
Beibei Xu, Dragana Lovre, Franck Mauvais-Jarvis
Selective estrogen receptor modulators (SERMs) are a class of compounds that interact with estrogen receptors (ERs) and exert agonist or antagonist effects on ERs in a tissue-specific manner. Tamoxifen, a first generation SERM, is used for treatment of ER positive breast cancer. Raloxifene, a second generation SERM, was used to prevent postmenopausal osteoporosis. The third-generation SERM bazedoxifene (BZA) effectively prevents osteoporosis while preventing estrogenic stimulation of breast and uterus. Notably, BZA combined with conjugated estrogens (CE) is a new menopausal treatment...
January 20, 2017: Journal of Diabetes and its Complications
https://www.readbyqxmd.com/read/28183030/estradiol-and-raloxifene-modulate-hippocampal-gamma-oscillations-during-a-spatial-memory-task
#3
Anna Schroeder, Matthew Hudson, Xin Du, Yee Wen Candace Wu, Jay Nakamura, Maarten van den Buuse, Nigel C Jones, Rachel A Hill
Previous work suggests that estradiol regulates the expression of hippocampal parvalbumin as well as hippocampus-dependent spatial memory in mice. Parvalbumin interneurons generate neuronal oscillatory activity in the gamma frequency range (30-80Hz) and gamma oscillations are closely linked with higher cognitive functions. Raloxifene, a selective estrogen receptor modulator, shows beneficial effects on human cognitive performance, and has few peripheral side effects unlike estradiol, but the biological mechanisms which underpin these benefits are not clear...
January 23, 2017: Psychoneuroendocrinology
https://www.readbyqxmd.com/read/28158228/extracorporeal-shock-waves-alone-or-combined-with-raloxifene-promote-bone-formation-and-suppress-resorption-in-ovariectomized-rats
#4
Adriano Lama, Anna Santoro, Bruno Corrado, Claudio Pirozzi, Orlando Paciello, Teresa Bruna Pagano, Sergio Russo, Antonio Calignano, Giuseppina Mattace Raso, Rosaria Meli
Osteoporosis is a metabolic skeletal disease characterized by an imbalance between osteoclast-mediated bone resorption and osteoblast-mediated bone formation. We examined the beneficial effect of shock waves (SW) alone or in combination with raloxifene (RAL) on bone loss in ovariectomized rats (OVX). Sixteen weeks after surgery, OVX were treated for five weeks with SW at the antero-lateral side of the right hind leg, one session weekly, at 3 Hz (EFD of 0.33 mJ/mm2), or with RAL (5 mg/kg/die, per os) or with SW+RAL...
2017: PloS One
https://www.readbyqxmd.com/read/28153426/factors-affecting-gastrointestinal-absorption-of-levothyroxine-a-review
#5
REVIEW
Marko Skelin, Tomo Lucijanić, Daniela Amidžić Klarić, Arnes Rešić, Miro Bakula, Ana-Marija Liberati-Čizmek, Hossein Gharib, Dario Rahelić
PURPOSE: Levothyroxine (LT4) is a drug with a narrow therapeutic index, applied in small amounts (micrograms), which makes interactions in the absorption phase clinically significant. The main aim of this article was to review and present the latest information on factors that affect the gastrointestinal absorption of this drug. METHODS: Relevant data were collected by using the MEDLINE, PubMed, EMBASE, Web of Science, Science Direct, and Scopus databases with the key words levothyroxine and absorption...
January 30, 2017: Clinical Therapeutics
https://www.readbyqxmd.com/read/28145413/stearoyl-coa-desaturase-1-a-novel-target-of-omega-3-fatty-acids-for-reducing-breast-cancer-risk-in-obese-postmenopausal-women
#6
A Manni, J P Richie, S E Schetter, A Calcagnotto, N Trushin, C Aliaga, K El-Bayoumy
BACKGROUND/OBJECTIVES: Conversion of saturated fatty acids to monounsaturated fatty acids by the enzyme stearoyl-Co-A-desaturase (SCD-1) is emerging as a major factor in promoting carcinogenesis including breast cancer. The aim of our study was to explore the regulation of SCD-1 by Raloxifene and omega-3 fatty acids in women at increased risk of breast cancer based on high breast density. SUBJECTS/METHODS: As a reflection of SCD-1 activity, we measured the ratios of palmitoleic acid (C16:1n7) to palmitic acid (C16:0) (SCD-16) and oleic acid (C18:1n9) to steric acid (C18:0) (SCD-18) in plasma samples of postmenopausal women enrolled in our clinical trial (NCT00723398) designed to test the effects of the antiestrogen, Raloxifene and/or the omega-3 preparation Lovaza, on breast density, a validated biomarker of breast cancer risk...
February 1, 2017: European Journal of Clinical Nutrition
https://www.readbyqxmd.com/read/28138957/role-of-inducible-nitric-oxide-synthase-in-endothelium-independent-relaxation-to-raloxifene-in-rat-aortas
#7
Chi Ming Wong, Chak Leung Au, Suk Ying Tsang, Chi Wai Lau, Xiaoqiang Yao, Zongwei Cai, Arthur Chi-Kong Chung
BACKGROUND AND PURPOSE: Raloxifene can induce both endothelium-dependent and -independent relaxation in different arteries. However, the underlying mechanisms of raloxifene to trigger endothelium-independent relaxation are still incompletely understood. The purpose of present study was to examine the roles of nitric oxide synthases (NOS) and Ca(2+) channels in the relaxant response to raloxifene in the isolated endothelium-denuded rat aorta. EXPERIMENTAL APPROACH: Changes of isometric tension, cyclic GMP, nitrite, inducible NOS protein expression and distribution in response to raloxifene in endothelium-denuded aortic rings were studied by organ baths, radioimmunoassay, Griess reaction, Western blot and immunohistochemistry, respectively...
January 31, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28127623/regulation-of-cannabinoid-cb2-receptor-constitutive-activity-in-vivo-repeated-treatments-with-inverse-agonists-reverse-the-acute-activation-of-jnk-and-associated-apoptotic-signaling-in-mouse-brain
#8
Glòria Salort, María Álvaro-Bartolomé, Jesús A García-Sevilla
RATIONALE: CB2 receptors express constitutive activity and inverse agonists regulate receptor basal activity, which might be involved in death mechanisms. This study assessed the effects of a selective CB2 agonist (JWH133) and different CB2 inverse agonists (AM630, JTE907, raloxifene) on death pathways in brain. OBJECTIVES: The acute (JWH13) and the acute/chronic effects (AM630, JTE907, raloxifene) of CB2 ligands regulating pro-apoptotic c-Jun NH2-terminal kinase (p-JNK/JNK ratio) and associated signaling of extrinsic (Fas receptor, Fas-Associated death domain protein, FADD) and intrinsic (Bax, cytochrome c) death pathways (nuclear poly (ADP-ribose) polymerase PARP) were investigated in mouse brain...
January 26, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28119898/raloxifene-administration-in-women-treated-with-long-term-gonadotropin-releasing-hormone-agonist-for-severe-endometriosis-effects-on-bone-mineral-density
#9
Young Hwa Cho, Mi Jung Um, Suk Jin Kim, Soo Ah Kim, Hyuk Jung
OBJECTIVES: To evaluate the efficacy of raloxifene in preventing bone loss associated with long term gonadotropin-releasing hormone agonist (GnRH-a) administration. METHODS: Twenty-two premenopausal women with severe endometriosis were treated with leuprolide acetate depot at a dosage of 3.75 mg/4 weeks, for 48 weeks. Bone mineral density (BMD) was evaluated at admission, and after 12 treatment cycles. RESULTS: At cycle 12 of GnRH-a plus raloxifene treatment, lumbar spine, trochanter femoral neck, and Ward's BMD differed from before the treatment...
December 2016: Journal of Menopausal Medicine
https://www.readbyqxmd.com/read/28119100/antiosteoporotic-effect-of-hemidesmus-indicus-linn-on-ovariectomised-rats
#10
Sharad Desai, Parth Babaria, Madhavi Nakarani, Kunal Shah, Archana Paranjape
PHARMACOLOGICAL RELEVANCE: Root of Hemidesmus indicus (L). R. Br., an herbal drug of India is traditionally used to prevent or treat female hormonal disturbance related disorders and assuaging symptoms of menopausal conditions. AIM OF THE STUDY: Lack of scientific data for potential use in bone loss, the present study was undertaken to investigate the effects of ethanol extract of Hemidesmus indicus root for osteoporosis in ovariectomised rats. MATERIALS AND METHODS: Thirty wistar female rats were randomly divided into five groups...
January 21, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28117994/novel-selective-estrogen-receptor-downregulators-serds-developed-against-treatment-resistant-breast-cancer
#11
Rui Xiong, Jiong Zhao, Lauren M Gutgesell, Yueting Wang, Sue Lee, Bhargava Karumudi, Huiping Zhao, Yunlong Lu, Debra A Tonetti, Gregory R J Thatcher
Resistance to the selective estrogen receptor modulator tamoxifen and to aromatase inhibitors that lower circulating estradiol occurs in up to 50% of patients, generally leading to an endocrine-independent ER+ phenotype. Selective ER downregulators (SERDs) are able to ablate ER and thus, theoretically, to prevent survival of both endocrine-dependent and -independent ER+ tumors. The clinical SERD fulvestrant is hampered by intramuscular administration and undesirable pharmacokinetics. Novel SERDs were designed using the 6-OH-benzothiophene (BT) scaffold common to arzoxifene and raloxifene...
February 10, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28054005/data-of-aromatase-inhibitors-alone-and-in-combination-with-raloxifene-on-microarchitecture-of-lumbar-vertebrae-and-strength-test-in-femoral-diaphysis-of-vcd-treated-ovotoxic-mice
#12
Abul Kalam, Sushama Talegaonkar, Divya Vohora
Currently, the third generation aromatase inhibitors are the drugs of choice for treatment of early and advanced breast cancer in postmenopausal women. The negative impact of these drugs on bone health is the significant limiting factor during this therapy. Here we report the effect of two aromatase inhibitors viz. letrozole and exemestane alone and in combination with raloxifene on lumbar vertebrae and femoral diaphysis after one month of treatment but no discernible effects were observed on bone when tested by micro CT and strength test except in trabecular number which was reduced in lumbar vertebrae following letrozole and exemestane...
February 2017: Data in Brief
https://www.readbyqxmd.com/read/28029084/variability-of-zaleplon-5-oxidase-activity-in-mice-and-humans-and-inhibition-by-raloxifene
#13
Chiaki Tanoue, Kazumi Sugihara, Yoshitaka Tayama, Naoto Uramaru, Yoko Watanabe, Shigeru Ohta, Shigeyuki Kitamura
Zaleplon (ZAL) is a sedative-hypnotic agent, which is mainly metabolized to inactive 5-oxidized zaleplon (5-oxo-ZAL) and N-des-ethylated ZAL (des-ethyl-ZAL) in mice and humans. The former reaction is considered to be catalyzed by aldehyde oxidase present in liver cytosol. Here, we examined sex and strain differences of ZAL metabolism to 5-oxo-ZAL among four strains of mice, as well as the inter-individual variation in humans, in order to evaluate the variability of 5-oxo-ZAL-forming activity and its relationship with aldehyde oxidase activity...
December 27, 2016: Drug Metabolism Letters
https://www.readbyqxmd.com/read/28028633/real-world-evidence-of-raloxifene-versus-alendronate-in-preventing-non-vertebral-fractures-in-japanese-women-with-osteoporosis-retrospective-analysis-of-a-hospital-claims-database
#14
Sakae Tanaka, Takanori Yamamoto, Eisei Oda, Masaki Nakamura, Saeko Fujiwara
We conducted a retrospective cohort study using a de-identified hospital administrative claims database to assess the risk of non-vertebral fracture in Japanese women with osteoporosis treated with raloxifene compared with alendronate. The study included Japanese women ≥50 years of age with newly initiated alendronate or raloxifene treatment between July 2008 and March 2013 (index date was defined as the day of first prescription for alendronate or raloxifene), and had any claim with an osteoporosis definition during the study period...
December 27, 2016: Journal of Bone and Mineral Metabolism
https://www.readbyqxmd.com/read/28012326/a-case-report-of-desmoid-tumour-a-forgotten-aspect-of-fap
#15
Sarah Xuereb, Rachel Xuereb, Chiara Buhagiar, Jonathan Gauci, Claude Magri
INTRODUCTION: Desmoid tumours are locally aggressive tumours which are common in Familial Adenomatous Polyposis (FAP). PRESENTATION OF CASE: A 20-year old Familial Adenomatous Polyposis (FAP) patient presented with abdominal pain and distention. Abdominal imaging showed small bowel obstruction and hydronephrosis due to a pelvic mass. This mass showed significant enlargement on repeat imaging, and a diagnostic biopsy confirmed desmoid tumour. The mass was deemed unresectable and he was initially started on sulindac and raloxifene...
December 1, 2016: International Journal of Surgery Case Reports
https://www.readbyqxmd.com/read/28003814/the-selective-estrogen-receptor-modulator-raloxifene-inhibits-neutrophil-extracellular-trap-formation
#16
Roxana Flores, Simon Döhrmann, Christina Schaal, Abdul Hakkim, Victor Nizet, Ross Corriden
Raloxifene is a selective estrogen receptor modulator typically prescribed for the prevention/treatment of osteoporosis in postmenopausal women. Although raloxifene is known to have anti-inflammatory properties, its effects on human neutrophils, the primary phagocytic leukocytes of the immune system, remain poorly understood. Here, through a screen of pharmacologically active small molecules, we find that raloxifene prevents neutrophil cell death in response to the classical activator phorbol 12-myristate 13-acetate (PMA), a compound known to induce formation of DNA-based neutrophil extracellular traps (NETs)...
2016: Frontiers in Immunology
https://www.readbyqxmd.com/read/27999800/effects-of-raloxifene-on-the-proliferation-and-apoptosis-of-human-aortic-valve-interstitial-cells
#17
Zhimin Fu, Bin Luo, Mingpeng Li, Bin Peng, Zheng Wang
We aimed to explore the effects of raloxifene (RAL) on the proliferation and apoptosis of human aortic valve interstitial cells (AVICs). Different concentrations of RAL were used to act on AVICs. MTS kit is used to test the effects of different concentrations of RAL on the proliferation of AVICs. Cell cycle and apoptosis test used flow cytometry after seven-day treatment. The relative expression levels of caspase-3 and caspase-8 are tested with RT-qPCR and Western blot. The results of MTS testing revealed that the absorbance value (OD value) of the cells in the concentration groups of 10 and 100 nmol/L RAL at a wavelength of 490 nm at five, seven, and nine days significantly decreased compared with that in the control group...
2016: BioMed Research International
https://www.readbyqxmd.com/read/27988379/raloxifene-microsphere-embedded-collagen-chitosan-%C3%AE-tricalcium-phosphate-scaffold-for-effective-bone-tissue-engineering
#18
Ming-Lei Zhang, Ji Cheng, Ye-Chen Xiao, Ruo-Feng Yin, Xu Feng
Engineering novel scaffolds that can mimic the functional extracellular matrix (ECM) would be a great achievement in bone tissue engineering. This paper reports the fabrication of novel collagen/chitosan/β-tricalcium phosphate (CCTP) based tissue engineering scaffold. In order to improve the regeneration ability of scaffold, we have embedded raloxifene (RLX)-loaded PLGA microsphere in the CCTP scaffold. The average pore of scaffold was in the range of 150-200μm with ideal mechanical strength and swelling/degradation characteristics...
December 14, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27974229/selective-estrogen-receptor-modulators-and-the-vitamin-d-analogue-eldecalcitol-block-bone-loss-in-male-osteoporosis
#19
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/27973466/treatment-of-menopausal-symptoms-new-era-with-new-options-or-new-options-for-menopausal-symptoms-after-15-years-of-whi-study
#20
Santiago Palacios, Pluvio J Coronado
Menopausal symptoms include vasomotor symptoms (VMS), vulvar-vaginal atrophy, and loss of bone mass associated with an increased risk of fracture. Treatment of VMS consists of lifestyle changes, hormone treatment (estrogens with and without progestogens, tissue selective estrogens complex or conjugated estrogens and bazedoxifene [CE/BZA], progestogens, and tibolone), and nonhormonal treatments. Genitourinary symptoms due to vulvar-vaginal atrophy are treated with systemic and local hormones, moisturizer creams and gels, CE/BZA, and a selective estrogen receptor modulator (ospemifene)...
December 14, 2016: Minerva Ginecologica
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