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Raloxifene

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https://www.readbyqxmd.com/read/28334925/simultaneous-lc-ms-ms-determination-of-lopinavir-and-rifabutin-in-human-plasma
#1
Swati Jaiswal, Abhisheak Sharma, Mahendra Shukla, Jawahar Lal
Tuberculosis (TB) with human immunodeficiency virus (HIV)/acquired immunodeficiency syndrome represents the most common infectious diseases worldwide. Anti-TB drugs are used concurrently with antiretroviral drug for treatment of TB-HIV co-morbidities. Due to lower risk of interaction with protease inhibitors, rifabutin is preferred over rifampicin in treatment of HIV and TB co-morbidity. A simple and specific liquid chromatography tandem mass spectrometry method was developed for quantification of rifabutin (RBT) and lopinavir (LPV) simultaneously in human plasma...
March 3, 2017: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/28293779/effect-of-osteoporosis-medication-on-changes-in-bone-mineral-density-and-bone-turnover-markers-after-24-month-administration-of-daily-teriparatide-comparison-among-minodronate-raloxifene-and-eldecalcitol
#2
Shinichi Nakatoh
This study reveals the changes in bone mineral density (BMD), the turnover rate, and the balance [multiple of median formation/multiple of median resorption (MoMf/MoMr)] affected by the selection of different bone resorption inhibitors after 24-month daily teriparatide (20 µg/day) administration. The turnover rate was calculated as √(MoMf(2) + MoMr(2)), where MoMf = bone-specific alkaline phosphatase (BAP) value/18.6 and MoMr = tartrate-resistant acid phosphatase 5b (TRACP-5b) value/463. One hundred and twenty-one osteoporotic women (mean age 82...
March 14, 2017: Journal of Bone and Mineral Metabolism
https://www.readbyqxmd.com/read/28283467/responsiveness-of-brca1-and-trp53-deficiency-induced-mammary-preneoplasia-to-selective-estrogen-modulators-versus-an-aromatase-inhibitor-in-mus-musculus
#3
Sahar J Alothman, Weisheng Wang, David S Goerlitz, Md Islam, Xiaogang Zhong, Archana Kishore, Redha I Azhar, Bhaskar V Kallakury, Priscilla A Furth
An intervention study initiated at age 4 months compared the impact of tamoxifen (25 mg), raloxifene (22.5 mg), and letrozole (2.5 mg) administered by 60-day release subcutaneous pellet on mammary preneoplasia prevalence at age 6 months in conditional genetically engineered mouse models with different Breast cancer 1 (Brca1) gene dosages targeted to mammary epithelial cells and germline Tumor protein P53 (Trp53) haploinsufficiency (10-16/cohort). The proportion of unexposed control mice demonstrating mammary preneoplasia at age 6 months was highest in Brca1(fl11/fl11/Cre/p53-/+) (54%) mice followed by Brca1(WT/fl11/Cre/p53-/+) mice (30%)...
March 10, 2017: Cancer Prevention Research
https://www.readbyqxmd.com/read/28265881/raloxifene-lowers-plasma-lipoprotein-a-concentrations-a-systematic-review-and-meta-analysis-of-randomized-placebo-controlled-trials
#4
Gianna Ferretti, Tiziana Bacchetti, Luis E Simental-Mendía, Željko Reiner, Maciej Banach, Amirhossein Sahebkar
BACKGROUND AND AIMS: Lipoprotein(a) (Lp(a)) is a proatherogenic plasma lipoprotein and an independent risk factor for atherosclerotic cardiovascular disease. We investigated the effects of raloxifene, selective estrogen receptor modulator, on circulating Lp(a) levels in postmenopausal women using a systematic review and meta-analysis of randomized controlled trials (RCTs). METHODS: To identify relevant studies, electronic databases (PUBMED, Scopus, Web of Science, and Google Scholar) were searched by up to May 2015 to find controlled trials exploring the effects of oral raloxifene treatment on plasma Lp(a) levels in postmenopausal women...
March 7, 2017: Cardiovascular Drugs and Therapy
https://www.readbyqxmd.com/read/28261281/induction-of-mitochondrial-apoptotic-pathway-by-raloxifene-and-estrogen-in-human-endometrial-stromal-thesc-cell-line
#5
Ivana Nikolic, Marija Andjelkovic, Milan Zaric, Ivanka Zelen, Petar Canovic, Zoran Milosavljevic, Marina Mitrovic
INTRODUCTION: Endometrial hyperplasia is a condition that occurs as a result of hormonal imbalance between estrogen and progesterone. Morphological disturbance of endometrial cells occurs consequently leading towards endometrial cancer. In therapy of endometrial hyperplasia SERMs are used to supress effects of locally high estrogen level in uterus. There is strong evidence suggesting that estrogen could be involved in cell death - apoptosis. There are no experimental data demstrating the direct apoptotic effect of both raloxifene and estrogen on the ThESC cell line...
March 1, 2017: Archives of Medical Science: AMS
https://www.readbyqxmd.com/read/28246928/raloxifene-improves-bone-mechanical-properties-in-mice-previously-treated-with-zoledronate
#6
Cory N Meixner, Mohammad W Aref, Aryaman Gupta, Erin M B McNerny, Drew Brown, Joseph M Wallace, Matthew R Allen
Bisphosphonates represent the gold-standard pharmaceutical agent for reducing fracture risk. Long-term treatment with bisphosphonates can result in tissue brittleness which in rare clinical cases manifests as atypical femoral fracture. Although this has led to an increasing call for bisphosphonate cessation, few studies have investigated therapeutic options for follow-up treatment. The goal of this study was to test the hypothesis that treatment with raloxifene, a drug that has cell-independent effects on bone mechanical material properties, could reverse the compromised mechanical properties that occur following zoledronate treatment...
February 28, 2017: Calcified Tissue International
https://www.readbyqxmd.com/read/28246081/the-4ps-of-breast-cancer-chemoprevention-putting-proven-principles-into-practice
#7
EDITORIAL
V Craig Jordan
The pioneering Royal Marsden Tamoxifen Prevention Trial recruited 2,471 eligible high-risk women to be randomized to either placebo or tamoxifen (20 mg daily) for 8 years. Breast cancer incidence was evaluated at a median of 18.4 years from the start of the study. There was a 32% reduction in estrogen/progesterone receptor (ER/PR)-positive breast cancers after tamoxifen treatment finished. Translational research, to study "the good, the bad, and the ugly of tamoxifen" in the 1980s, subsequently ensured women's safety from possible increases in osteoperosis, coronary heart disease, and endometrial cancer...
February 28, 2017: Cancer Prevention Research
https://www.readbyqxmd.com/read/28243883/two-year-persistence-and-compliance-with-osteoporosis-therapies-among-postmenopausal-women-in-a-commercially-insured-population-in-the-united-states
#8
Emily Durden, Lionel Pinto, Lorena Lopez-Gonzalez, Paul Juneau, Richard Barron
This retrospective, observational study assessed 2-year persistence and compliance by treatment, route of administration, and dosing frequency in postmenopausal women initiating a new osteoporosis therapy. Two-year persistence and compliance rates were higher in women receiving injectables compared with oral agents. PURPOSE: This study extends previous studies limited to 1-year follow-up by examining persistence with osteoporosis therapies over a 2-year period and compares short- and long-term trends in persistence and compliance among postmenopausal women with commercial or Medicare supplemental insurance in the USA...
December 2017: Archives of Osteoporosis
https://www.readbyqxmd.com/read/28239652/estrogens-regulate-glycosylation-of-igg-in-women-and-men
#9
Altan Ercan, Wendy M Kohrt, Jing Cui, Kevin D Deane, Marija Pezer, Elaine W Yu, Jonathan S Hausmann, Harry Campbell, Ursula B Kaiser, Pauline M Rudd, Gordan Lauc, James F Wilson, Joel S Finkelstein, Peter A Nigrovic
The immunologic potency of IgG is modulated by glycosylation, but mechanisms regulating this process are undefined. A role for sex hormones is suggested by differences in IgG glycans between women and men, most prominently with respect to galactose. We therefore assessed IgG galactosylation in 713 healthy adults from 2 cohorts as well as in 159 subjects from 4 randomized controlled studies of endocrine manipulation: postmenopausal women receiving conjugated estrogens, raloxifene, or placebo; premenopausal women deprived of gonadal hormones with leuprolide and treated with estradiol or placebo; men deprived of gonadal hormones with goserelin and given testosterone or placebo; and men deprived of gonadal hormones with goserelin and given testosterone or placebo together with anastrozole to block conversion of testosterone to estradiol...
February 23, 2017: JCI Insight
https://www.readbyqxmd.com/read/28238769/effects-of-raloxifene-on-portal-hypertension-and-hepatic-encephalopathy-in-cirrhotic-rats
#10
Ching-Chih Chang, Wen-Shin Lee, Chiao-Lin Chuang, I-Fang Hsin, Shao-Jung Hsu, Ting Chang, Hui-Chun Huang, Fa-Yauh Lee, Shou-Dong Lee
Raloxifene, a selective estrogen receptor modulator, has been used extensively for osteoporosis. In addition to the effect of osteoporosis treatment, emerging evidences show that raloxifene affects the vascular function in different tissues. Cirrhosis is characterized with portal hypertension and complicated with hepatic encephalopathy. Portal hypertension affects portal-systemic shunt which leads to hepatic encephalopathy that the vascular modulation might influence severity of hepatic encephalopathy. Herein, we evaluated the impact of raloxifene on bile duct ligation (BDL)-induced cirrhotic rats...
February 24, 2017: European Journal of Pharmacology
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
#11
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
#12
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...
April 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
#13
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
#14
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
#15
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...
February 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
#16
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
#17
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
#18
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
#19
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
#20
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
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