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https://www.readbyqxmd.com/read/28550603/development-of-novel-high-density-gastroretentive-multiparticulate-pulsatile-tablet-of-clopidogrel-bisulfate-using-quality-by-design-approach
#1
Nilesh Desai, Ravindra Purohit
Myocardial infarction, i.e., heart attack, is a fatal condition which is on the increase all over the world. It is reported that a large number of heart attack occur in morning hours which are attributable to platelet aggregation. Chronotherapy at this stage can be crucial. Clopidogrel bisulfate (CLB) is an antiplatelet agent and has become a drug of choice for prevention of heart attack. It is soluble in acidic pH and has a narrow absorption window. So, its long residence time in stomach is desirable. Therefore, a novel high density tablet was developed comprising multiparticulate pellets with pulsatile release necessary to maintain chronotherapy of heart attack...
May 26, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28549888/synthesis-of-n%C3%AE-vel-artemisinin-dimers-with-polyamine-linkers-and-evaluation-of-their-potential-as-anticancer-agents
#2
George E Magoulas, Tzoanna Tsigkou, Lina Skondra, Margarita Lamprou, Panagiota Tsoukala, Vassiliki Kokkinogouli, Evangelia Pantazaka, Dionissios Papaioannou, Constantinos M Athanassopoulos, Evangelia Papadimitriou
The natural product artemisinin and derivatives thereof are currently considered as the drugs of choice for the treatment of malaria. At the same time, a significant number of such drugs have also shown interesting anticancer activity. In the context of the present research work, artemisinin was structurally modified and anchored to naturally occurring polyamines to afford new artemisinin dimeric conjugates whose potential anticancer activity was evaluated. All artemisinin conjugates tested were more effective than artemisinin itself in decreasing the number of MCF7 breast cancer cells...
May 10, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28549568/using-visual-analytics-for-presenting-comparative-information-on-new-drugs
#3
Jean-Baptiste Lamy, Hélène Berthelot, Madeleine Favre, Adrien Ugon, Catherine Duclos, Alain Venot
OBJECTIVE: When a new drug is marketed, physicians must decide whether they will consider it for their future practice. However, information about new drugs can be biased or hard to find. In this work, our objective was to study whether visual analytics could be used for comparing drug properties such as contraindications and adverse effects, and whether this visual comparison can help physicians to forge their own well-founded opinions about a new drug. MATERIALS AND METHODS: First, an ontology for comparative drug information was designed, based on the expectations expressed during focus groups comprised of physicians...
May 23, 2017: Journal of Biomedical Informatics
https://www.readbyqxmd.com/read/28548950/enolase-1-stimulates-glycolysis-to-promote-chemoresistance-in-gastric-cancer
#4
Xiaoling Qian, Wenxia Xu, Jinye Xu, Qiqi Shi, Jiaqiu Li, Yu Weng, Zhinong Jiang, Lifeng Feng, Xian Wang, Jianwei Zhou, Hongchuan Jin
Chemotherapy is the major choice for the cancer treatment of early and advanced stages. However, intrinsic or acquired drug resistance significantly restricts the clinical efficacy of chemotherapy. It is critical to develop novel approaches to detect and overcome drug resistance. In this study, we demonstrated that accelerated glycolysis played a pivotal role in both intrinsic and acquired cisplatin-resistance of gastric cancer cells. The metabolic reprogramming of cisplatin-resistant cells was characterized by increased glycolysis dependence...
May 15, 2017: Oncotarget
https://www.readbyqxmd.com/read/28545825/the-effect-of-anesthetic-drug-choice-on-accuracy-of-high-definition-oscillometry-in-laterally-recumbent-horses
#5
Tanya Duke-Novakovski, Barbara Ambros, Cindy Feng, Anthony P Carr
OBJECTIVE: To determine the accuracy of high-definition oscillometry (HDO) for arterial pressure measurement during injectable or inhalation anesthesia in horses. STUDY DESIGN: Prospective, clinical study. ANIMALS: Twenty-four horses anesthetized for procedures requiring lateral recumbency. METHODS: Horses were premedicated with xylazine, and anesthesia induced with diazepam-ketamine. Anesthesia was maintained with xylazine-ketamine-guaifenesin combination [TripleDrip (TD; n = 12) or isoflurane (ISO; n = 12)]...
January 11, 2017: Veterinary Anaesthesia and Analgesia
https://www.readbyqxmd.com/read/28545189/outcomes-of-a-randomized-controlled-trial-comparing-modified-high-dose-omeprazole-and-amoxicillin-triple-therapy-with-standard-triple-therapy-for-helicobacter-pylori-eradication
#6
Kitti Chunlertlith, Uaepong Limpapanasit, Pisaln Mairiang, Suda Vannaprasaht, Wichittra Tassaneeyakul, Apichat Sangchan, Kookwan Sawadpanich, Tanita Suttichaimongkol, Jamrus Pongpit, Moragot Pattarapongsin
Background: Helicobacter pylori (H. pylori) infection is related to peptic ulcer diseases and gastric cancer and eradication of H. pylori should be expected to decrease the risk of their development. Factors affecting H. pylori eradication are antibiotic resistance, CYP2C19 genotypes, drug regimen and patient compliance. Increment of omeprazole and amoxicillin dosage in clarithromycin-containing triple therapy regimen may overcome these problems and may be a better choice than the conventional clarithromycin-containing triple therapy regimen...
April 1, 2017: Asian Pacific Journal of Cancer Prevention: APJCP
https://www.readbyqxmd.com/read/28544603/metabolic-reprogramming-of-macrophages-exposed-to-silk-poly-lactic-co-glycolic-acid-and-silica-nanoparticles
#7
Raquel Saborano, Thidarat Wongpinyochit, John D Totten, Blair F Johnston, F Philipp Seib, Iola F Duarte
Monitoring macrophage metabolism in response to nanoparticle exposure provides new insights into biological outcomes, such as inflammation or toxicity, and supports the design of tailored nanomedicines. This paper describes the metabolic signature of macrophages exposed to nanoparticles ranging in diameter from 100 to 125 nm and made from silk, poly(lactic-co-glycolic acid) or silica. Nanoparticles of this size and type are currently at various stages of preclinical and clinical development for drug delivery applications...
May 8, 2017: Advanced Healthcare Materials
https://www.readbyqxmd.com/read/28541755/epinephrine-but-not-vasopressin-attenuates-the-airway-response-to-anaphylactic-shock-in-rats
#8
Feng Zheng, Ruxandra Copotoiu, Charles Tacquard, Bruno Demoulin, Jean Marc Malinovsky, Bruno Levy, Dan Longrois, Grégoire Barthel, Paul Michel Mertes, François Marchal, Silvia Demoulin-Alexikova, Olivier Collange
PURPOSE: The two life-threatening signs of anaphylactic shock (AS) are severe arterial hypotension and bronchospasm. Guidelines recommend epinephrine as first-line treatment. Arginine vasopressin (AVP) has been proposed as an alternative if epinephrine does not correct arterial hypotension. These two drugs may have beneficial, neutral or deleterious effects on airflow either directly or by modifying factors that regulate vasodilatation and/or edema in the bronchial wall. AIM OF THE STUDY: To compare the effects of epinephrine and AVP on airflow and airway leakage in a rat model of AS...
May 25, 2017: Experimental Lung Research
https://www.readbyqxmd.com/read/28540072/standard-imaging-techniques-in-transcatheter-aortic-valve-replacement
#9
REVIEW
Arash Salemi, Berhane M Worku
Transcatheter aortic valve replacement (TAVR) has become a widely accepted therapeutic option for patients with severe, symptomatic aortic stenosis at intermediate, high, or extreme risk for conventional surgery as determined through a heart team approach. Two valve prostheses are currently available and the Food and Drug Administration (FDA) approved in the United States for TAVR: the self-expandable Medtronic CoreValve (Medtronic, Inc., Minneapolis, MN, USA) and the balloon-expandable Edwards Sapien Valve (Edwards Lifesciences, Irvine CA, USA)...
April 2017: Journal of Thoracic Disease
https://www.readbyqxmd.com/read/28539303/pharma-websites-and-professionals-only-information-the-implications-for-patient-trust-and-autonomy
#10
Mark Alan Graber, Eliyakim Hershkop, Rachel Ilana Graber
BACKGROUND: Access to information is critical to a patient's valid exercise of autonomy. One increasingly important source of medical information is the Internet. Individuals often turn to drug company ("pharma") websites to look for drug information. OBJECTIVE: The objective of this study was to determine whether there is information on pharma websites that is embargoed: Is there information that is hidden from the patient unless she attests to being a health care provider? We discuss the implications of our findings for health care ethics...
May 24, 2017: Journal of Medical Internet Research
https://www.readbyqxmd.com/read/28537745/deciphering-cryptic-binding-sites-on-proteins-by-mixed-solvent-molecular-dynamics
#11
S Roy Kimura, Haipeng Hu, Anatoly M Ruvinsky, Woody B Sherman, Angelo D Favia
In recent years, molecular dynamics simulations of proteins in explicit mixed-solvents have been applied to various problems in protein biophysics and drug discovery, including protein folding, protein surface characterization, fragment screening, allostery, and druggability assessment. In this study, we perform a systematic study on how mixtures of organic solvent probes in water can reveal cryptic ligand binding pockets that are not evident in crystal structures of apo proteins. We examine a diverse set of eight PDB proteins that show pocket opening induced by ligand binding and investigate whether solvent MD simulations on the apo structures can induce the binding site observed in the holo structures...
May 24, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/28536674/anti-idiotypic-antibodies-specific-to-prm-monoantibody-prevent-antibody-dependent-enhancement-of-dengue-virus-infection
#12
Miao Wang, Fan Yang, Dana Huang, Yalan Huang, Xiaomin Zhang, Chao Wang, Shaohua Zhang, Renli Zhang
Dengue virus (DENV) co-circulates as four serotypes (DENV1-4). Primary infection only leads to self-limited dengue fever. But secondary infection with another serotype carries a higher risk of increased disease severity, causing life-threatening dengue hemorrhagic fever/dengue shock syndrome (DHF/DSS). Serotype cross-reactive antibodies facilitate DENV infection in Fc-receptor-bearing cells by promoting virus entry via Fcγ receptors (FcγR), a process known as antibody dependent enhancement (ADE). Most studies suggested that enhancing antibodies were mainly specific to the structural premembrane protein (prM) of DENV...
2017: Frontiers in Cellular and Infection Microbiology
https://www.readbyqxmd.com/read/28535898/treatment-of-postmenopausal-osteoporosis-a-literature-based-algorithm-for-use-in-the-public-health-care-system
#13
Ellen Luz Pereira Caires, Mailze Campos Bezerra, Ana Flávia Torquato de Araújo Junqueira, Sheila Márcia de Araújo Fontenele, Silvana Cristina de Albuquerque Andrade, Catarina Brasil d'Alva
Bisphosphonates are considered first-line agents in the treatment of postmenopausal osteoporosis based on extensive experience of use, safety, and proven efficacy in reducing vertebral, non-vertebral and femur fractures. However, post-marketing reports based on the treatment of millions of patients/year over lengthy periods of time have revealed the occurrence of initially unexpected adverse effects, such as osteonecrosis of the jaw and atypical femoral fracture, leading to the restriction of treatment duration with bisphosphonates by global regulatory agencies...
May 2017: Revista Brasileira de Reumatologia
https://www.readbyqxmd.com/read/28535116/is-mannitol-the-treatment-of-choice-for-patients-with-ciguatera-fish-poisoning
#14
Michael E Mullins, Robert S Hoffman
CONTEXT: Ciguatera fish poisoning arises primarily from consumption of carnivorous reef fish caught in tropical and sub-tropical waters. Ciguatoxins, a class of tasteless, heat-stable, polycyclic toxins produced by dinoflagellates, accumulate through the food chain and concentrate in various carnivorous fish, such as groupers, barracudas, wrasses, amberjack, kingfishes, and eels. Characteristics of ciguatera fish poisoning include early nausea, vomiting, and diarrhea in the first one to two days post ingestion, followed by the appearance of sensory disturbances...
May 23, 2017: Clinical Toxicology
https://www.readbyqxmd.com/read/28535105/the-importance-of-economic-perspective-and-quantitative-approaches-in-oncology-value-frameworks-of-drug-selection-and-shared-decision-making
#15
A Reginald Waldeck, Marc F Botteman, Richard E White, Ben A van Hout
The debate around value in oncology drug selection has been prominent in recent years, and several professional bodies have furthered this debate by advocating for so-called value frameworks. Herein, we provide a viewpoint on these value frameworks, emphasizing the need to consider 4 key aspects: (1) the economic underpinnings of value; (2) the importance of the perspective adopted in the valuation; (3) the importance of the difference between absolute and relative measures of risk and measuring patient preferences; and (4) the recognition of multiple quality-of-life (QoL) domains, and the aggregation and valuation of those domains, through utilities within a multicriteria decision analysis, may allow prioritization of QoL above the tallying of safety events, particularly in a value framework focusing on the individual patient...
June 2017: Journal of Managed Care & Specialty Pharmacy
https://www.readbyqxmd.com/read/28533769/celecoxib-enhances-the-efficacy-of-low-dose-antibiotic-treatment-against-polymicrobial-sepsis-in-mice-and-clinical-isolates-of-eskape-pathogens
#16
Madhavi Annamanedi, Gajapati Y N Varma, K Anuradha, Arunasree M Kalle
Treatment of multidrug resistant bacterial infections has been a great challenge globally. Previous studies including our study have highlighted the use of celecoxib, a non-steroidal anti-inflammatory drug in combination with antibiotic has decreased the minimal inhibitory concentration to limit Staphylococcus aureus infection. However, the efficacy of this combinatorial treatment against various pathogenic bacteria is not determined. Therefore, we have evaluated the potential use of celecoxib in combination with low doses of antibiotic in limiting Gram-positive and Gram-negative bacteria in vivo in murine polymicrobial sepsis developed by cecum ligation and puncture (CLP) method and against clinically isolated human ESKAPE pathogens (Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacter species)...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28533319/evaluating-the-cardiovascular-safety-of-nonsteroidal-anti-inflammatory-drugs
#17
REVIEW
Elliott M Antman
Some drugs used to treat noncardiovascular conditions may adversely impact the cardiovascular status of individuals both with and without known cardiovascular disease. When the US Food and Drug Administration judges the potential cardiovascular safety signal to be of sufficient concern, it may require the pharmaceutical manufacturer of the drug in question to conduct a postmarketing (phase 4) randomized controlled trial (RCT). Although historically many phase 4 RCTs focused on efficacy (using a superiority design), contemporary phase 4 RCTs often are focused on safety and use a noninferiority design...
May 23, 2017: Circulation
https://www.readbyqxmd.com/read/28532144/physically-targeted-intravenous-polyurethane-nanoparticles-for-controlled-release-of-atorvastatin-calcium
#18
Behnaz Sadat Eftekhari, Akbar Karkhaneh, Ali Alizadeh
Background: Intravenous drug delivery is an advantageous choice for rapid administration, immediate drug effect, and avoidance of first-pass metabolism in oral drug delivery. In this study, the synthesis, formulation, and characterization of atorvastatin-loaded polyurethane (PU) nanoparticles were investigated for intravenous route of administration. Methods: First, PU was synthesized and characterized. Second, nanoparticles were prepared in four different ratios of drug to polymer through two different techniques including emulsion-diffusion and single-emulsion...
May 23, 2017: Iranian Biomedical Journal
https://www.readbyqxmd.com/read/28531203/potential-health-gains-for-patients-with-metastatic-renal-cell-carcinoma-in-daily-clinical-practice-a-real-world-cost-effectiveness-analysis-of-sequential-first-and-second-line-treatments
#19
S De Groot, H M Blommestein, W K Redekop, S Sleijfer, L A L M Kiemeney, E Oosterwijk, C A Uyl-de Groot
INTRODUCTION: Randomised controlled trials have shown that targeted therapies like sunitinib are effective in metastatic renal cell carcinoma (mRCC). Little is known about the current use of these therapies, and their associated costs and effects in daily clinical practice. We estimated the real-world cost-effectiveness of different treatment strategies comprising one or more sequentially administered drugs. METHODS: Analyses were performed using patient-level data from a Dutch population-based registry including patients diagnosed with primary mRCC from January 2008 to December 2010 (i...
2017: PloS One
https://www.readbyqxmd.com/read/28530627/-laparoscopic-treatment-of-retroperitoneal-fibrosis
#20
Carlos Hernández Fernández, David Subirá Rios, Mercedes Moralejo Gárate, Elena Rodríguez Fernández, Jorge Caño Velasco, Felipe Herranz Amo
Retroperitoneal fibrosis is a disease that may condition a severe involvement of various organs, mainly upper urinary tract, even causing renal insufficiency. It was first described by Albarran in 1905 and it is also known as Ormonds disease. The correct diagnosis includes, in many cases, the performance of one or more tests: CT scan, MRI, renal scan, etc. It is often necessary the insertion of double J catheters on percutaneous nephrostomy tubes with the aim to preserve renal function. Initial treatment is medical, based on corticoids, and , less frequent, immunosuppressive or chemotherapy drugs...
May 2017: Archivos Españoles de Urología
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