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https://www.readbyqxmd.com/read/30295105/proton-pump-inhibitors-use-and-misuse-in-the-clinical-setting
#1
Vincenzo Savarino, Elisa Marabotto, Patrizia Zentilin, Manuele Furnari, Giorgia Bodini, Costanza De Maria, Gaia Pellegatta, Claudia Coppo, Edoardo Savarino
The introduction of proton pump inhibitors (PPIs) into clinical practice has greatly improved our therapeutic approach to acid-related diseases for their efficacy and safety. Areas Covered: The following evidence-based indications for PPI use are acknowledged by many scientific societies: treatment of the various forms and complications of gastroesophageal reflux disease, eradication of H. pylori infection in combination with two or more antibiotics, short- and long-term therapy of H. pylori-negative peptic ulcers, healing, and prevention of NSAID/COXIB-associated gastric ulcers, co-therapy with endoscopic procedures to control upper digestive bleeding and medical treatment of Zollinger Ellison syndrome...
October 8, 2018: Expert Review of Clinical Pharmacology
https://www.readbyqxmd.com/read/30285927/-cardiovascular-risk-of-non-steroidal-anti-inflammatory-drugs
#2
Guillermo R Prozzi, Martín Cañás, Martín A Urtasun, Héctor O Buschiazzo, Cristian M Dorati, Perla Mordujovich-Buschiazzo
Non-steroidal anti-inflammatories (NSAIDs) are among the most commonly used drugs in clinical practice. They block cyclooxygenases (COX) enzymes, but the degree of inhibition of COX-1 and COX-2 varies between them. In general, NSAIDs are classified in selective COX-2 or coxibs and non-selective or traditional NSAIDs. Both the analgesic and antiinflammatory effects, as well as the cardiovascular adverse effects, depend on the COX-2 inhibition. This paper reviews the available evidence of the increased risk of thrombotic events for both coxibs and traditional NSAID...
2018: Medicina
https://www.readbyqxmd.com/read/30245627/raging-the-war-against-inflammation-with-natural-products
#3
REVIEW
Ali Attiq, Juriyati Jalil, Khairana Husain, Waqas Ahmad
Over the last few decade Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) are the drugs of choice for treating numerous inflammatory diseases including rheumatoid arthritis. The NSAIDs produces anti-inflammatory activity via inhibiting cyclooxygenase enzyme, responsible for the conversation of arachidonic acid to prostaglandins. Likewise, cyclooxegenase-2 inhibitors (COX-2) selectively inhibit the COX-2 enzyme and produces significant anti-inflammatory, analgesic, and anti-pyretic activity without producing COX-1 associated gastrointestinal and renal side effects...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/30231067/risk-of-ischemic-stroke-and-the-use-of-individual-non-steroidal-anti-inflammatory-drugs-a-multi-country-european-database-study-within-the-sos-project
#4
Tania Schink, Bianca Kollhorst, Cristina Varas Lorenzo, Andrea Arfè, Ron Herings, Silvia Lucchi, Silvana Romio, René Schade, Martijn J Schuemie, Huub Straatman, Vera Valkhoff, Marco Villa, Miriam Sturkenboom, Edeltraut Garbe
BACKGROUND AND PURPOSE: A multi-country European study using data from six healthcare databases from four countries was performed to evaluate in a large study population (>32 million) the risk of ischemic stroke (IS) associated with individual NSAIDs and to assess the impact of risk factors of IS and co-medication. METHODS: Case-control study nested in a cohort of new NSAID users. For each case, up to 100 sex- and age-matched controls were selected and confounder-adjusted odds ratios for current use of individual NSAIDs compared to past use calculated...
2018: PloS One
https://www.readbyqxmd.com/read/30176739/benefits-and-risks-of-nonsteroidal-anti-inflammatory-drugs-methodologic-limitations-lead-to-clinical-uncertainties
#5
Manas A Rane, Jennifer G Foster, Sarah K Wood, Patricia R Hebert, Charles H Hennekens
Nonsteroidal anti-inflammatory drugs (NSAIDs) include traditional (tNSAIDs), such as ibuprofen, naproxen, and diclofenac, as well as selective cyclooxygenase-2 inhibitors (COXIBs), principally celecoxib. COXIBs were developed to decrease gastrointestinal side effects. Recently, the US Food and Drug Administration strengthened its warning about the risks of non-aspirin NSAIDs on myocardial infarction and stroke. The Cyclooxygenase 2 and Non-Steroidal Anti-Inflammatory Drug Trialist collaboration conducted a comprehensive worldwide meta-analysis using individual patient data exploring the risks of various COXIBs and NSAIDs on cardiovascular disease (CVD)...
September 3, 2018: Therapeutic Innovation & Regulatory Science
https://www.readbyqxmd.com/read/30153531/in-vitro-comprehensive-analysis-of-va692-a-new-chemical-entity-for-the-treatment-of-osteoarthritis
#6
Sara Cheleschi, Valentina Calamia, Mercedes Fernandez-Moreno, Mariangela Biava, Antonio Giordani, Antonella Fioravanti, Maurizio Anzini, Francisco Blanco
Selective cyclooxigenase (COX)-2 inhibitors were developed to prevent traditional non-steroidal anti-inflammatory drugs (tNSAIDs) gastro-intestinal adverse effects. VA692, a recently disclosed selective COX-2 inhibitor, structurally related to well-known marketed coxibs, showed anti-inflammatory, and anti-nociceptive properties. The aim of this study was to analyze the anti-inflammatory effect of VA692, in comparison with celecoxib. At this purpose we evaluated the pro-inflammatory cytokines and anti-oxidant enzymes gene expression, apoptosis and ROS production, and PGE2 release in chondrocytes (both primary cultures and immortalized T/C-28a2 cell line) treated with the two drugs...
August 25, 2018: International Immunopharmacology
https://www.readbyqxmd.com/read/30149590/use-of-non-steroidal-anti-inflammatory-drugs-and-associated-gastroprotection-in-a-cohort-of-workers
#7
María Jesús Lallana, Cristina Feja, Isabel Aguilar-Palacio, Sara Malo, María José Rabanaque
BACKGROUND: This study describes the prevalence of non-steroidal anti-inflammatory drug (NSAID) use, and analyses prescribing patterns of NSAIDs and associated gastroprotection. METHODS: The study population consisted of 5650 workers at the General Motors automobile assembly plant in Zaragoza, Spain. NSAID prescription data for 2014 were obtained from the prescription database of Aragon (Spain). NSAID consumption was determined based on the number of defined daily doses purchased per year...
August 24, 2018: International Journal of Environmental Research and Public Health
https://www.readbyqxmd.com/read/30148083/robenacoxib-in-the-treatment-of-pain-in-cats-and-dogs-safety-efficacy-and-place-in-therapy
#8
REVIEW
Kavitha Kongara, John Paul Chambers
Robenacoxib is a novel nonsteroidal anti-inflammatory drug (NSAID) of coxib class developed for the control of inflammation and pain in dogs and cats. It shows high selectivity for the cyclooxygenase-2 (COX-2) enzyme in rats, cats, and dogs. Robenacoxib is available in both injectable and tablet formulations. This review initially focuses on the preclinical pharmacology of robenacoxib in rats that includes its high affinity for COX-2 enzyme and weaker and rapidly reversible binding for COX-1 enzyme in in vitro and ex vivo models of inflammation and its pharmacokinetics in the blood and inflammatory exudate, selective tissue distribution, and safety...
2018: Veterinary medicine
https://www.readbyqxmd.com/read/30139288/nsaid-induced-gastrointestinal-damage-and-designing-gi-sparing-nsaids
#9
Guillermo García-Rayado, Mercedes Navarro, Angel Lanas
NSAIDs are widely used to treat pain and rheumatic conditions, but they induce adverse events in different body systems, although the major, most frequent events occur in the upper and lower gastrointestinal (GI) tracts. Areas covered: This review is focused on damage caused by NSAIDs in the upper and lower GI tracts, the different mechanisms of damage and the GI-sparing NSAIDs designed to minimize adverse events based on understanding of these mechanisms. Expert commentary: Among the new NSAIDs, COX-2 selective inhibitors have been extensively investigated, and some were approved for human use...
October 2018: Expert Review of Clinical Pharmacology
https://www.readbyqxmd.com/read/30072617/in-vivo-brain-imaging-biodistribution-and-radiation-dosimetry-estimation-of-11-c-celecoxib-a-cox-2-pet-ligand-in-nonhuman-primates
#10
J S Dileep Kumar, Bing Bai, Francesca Zanderigo, Christine DeLorenzo, Jaya Prabhakaran, Ramin V Parsey, J John Mann
COX-2 selective inhibitors (COXIBs) are non-steroidal anti-inflammatory drugs (NSAIDs), with fewer side effects compared with non-selective NSAIDs, and are used for the treatment of arthritis, headaches, and other inflammatory diseases of the brain and peripheral tissues. Radiolabeled COXIBs may permit positron emission tomography (PET) imaging of COX-2 localization and activity in diseases, enable monitoring of inflammatory processes, and determine target occupancy of COX-2 activity by NSAIDs, thus, accelerating the development of novel CIXIBs...
August 2, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/30066292/cardiovascular-and-gastrointestinal-safety-of-selective-cyclooxygenase-2-inhibitors-a-case-non-case-study
#11
Luis Hermenegildo Martin Arias, Antonio Martin Gonzalez, Rosario Sanz Fadrique, Esther Salgueiro, Maria Sainz
Background Coxibs cardiovascular (CV) safety continues being a current issue after rofecoxib worldwide withdrawal in 2004. Objective To evaluate the cardiovascular and gastrointestinal (GI) risk of coxibs through case/non-case study. Setting The Spanish Pharmacovigilance System for Human Use Drugs (FEDRA) and the Uppsala Monitoring Centre (VigiBase) databases. Method We identified adverse drug reactions (ADRs) cases reported under the MedDRA system organ classes of "cardiac disorders", "vascular disorders", "nervous system disorder" and "gastrointestinal disorders"...
August 2018: International Journal of Clinical Pharmacy
https://www.readbyqxmd.com/read/29942156/comparison-of-nsaids-activity-in-cox-2-expressing-and-non-expressing-2d-and-3d-pancreatic-cancer-cell-cultures
#12
Ugnė Čeponytė, Miglė Paškevičiūtė, Vilma Petrikaitė
Purpose: In this study, we evaluated the anticancer activity of non-steroidal anti-inflammatory drugs (NSAIDs) in BxPC-3 and MIA PaCa-2 pancreatic cancer cell cultures. Methods: To test the effect of compounds on the viability of cells, the MTT assay was used. The activity of NSAIDs in 3D cell cultures was evaluated by measuring the size change of spheroids. The type of cell death was identified by cell staining with Hoechst 33342 and propidium iodide. To evaluate the effect on the colony-forming ability of cancer cells, the clonogenic assay was used...
2018: Cancer Management and Research
https://www.readbyqxmd.com/read/29913983/a-6-months-randomised-placebo-controlled-evaluation-of-efficacy-and-tolerability-of-a-low-dose-7-day-buprenorphine-transdermal-patch-in-osteoarthritis-patients-na%C3%A3-ve-to-potent-opioids
#13
Harald Breivik, Tone Marte Ljosaa, Kristian Stengaard-Pedersen, Jan Persson, Hannu Aro, John Villumsen, Dorthe Tvinnemose
Objective Patients with osteoarthritis (OA) pain often have insufficient pain relief from non-opioid analgesics. The aim of this trial was to study efficacy and tolerability of a low dose 7-day buprenorphine transdermal delivery system, added to a NSAID or coxib regimen, in opioid-naïve patients with moderate to severe OA pain. Methods A 6 months randomised, double-blind, parallel-group study at 19 centres in Denmark, Finland, Norway, and Sweden, in which OA patients (>40 years) with at least moderate radiographic OA changes and at least moderate pain in a hip and/or knee while on a NSAID or a coxib were randomised to a 7-day buprenorphine patch (n = 100) or an identical placebo patch (n = 99)...
July 1, 2010: Scandinavian Journal of Pain
https://www.readbyqxmd.com/read/29883727/safer-anti-inflammatory-therapy-through-dual-cox-2-5-lox-inhibitors-a-structure-based-approach
#14
REVIEW
Jaismy Jacob P, S L Manju, K R Ethiraj, Geetha Elias
Inflammatory mediators of the arachidonic acid cascade from cyclooxygenase (COX) and lipoxygenase (LOX) pathways are primarily responsible for many diseases in human beings. Chronic inflammation is associated with the pathogenesis and progression of cancer, arthritis, autoimmune, cardiovascular and neurological diseases. Traditional non-steroidal anti-inflammatory agents (tNSAIDs) inhibit cyclooxygenase pathway non-selectively and produce gastric mucosal damage due to COX-1 inhibition and allergic reactions and bronchospasm resulting from increased leukotriene levels...
June 5, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29877658/nsaids-and-heart-failure-a-dangerous-relationship
#15
Raffaele Rotunno, Igino Oppo, Gabriele Saetta, Pietro Aveta, Sergio Bruno
One of the potential cardiotoxic action of anti-inflammatory drugs is the occurrence of heart failure (HF), due to their effects on fluid retention and blood pressure. The risk of hospitalization for HF is roughly doubled for both Coxibs, cyclooxygenase-1 (COX-1) and cyclooxygenase- 2 (COX-2) inhibitors, and all the conventional nonsteroidal anti-inflammatory drugs (NSAIDs). These drugs are also associated with a risk of vascular thrombosis, which for NSAIDs is different in relation to their different ability to inhibit COX-1 and COX-2...
June 7, 2018: Monaldi Archives for Chest Disease, Archivio Monaldi Per le Malattie del Torace
https://www.readbyqxmd.com/read/29766729/cardiovascular-risk-of-non-steroidal-anti-inflammatory-drugs
#16
Štefan Alušík, Zoltán Paluch
Non-steroidal anti-inflammatory drugs (NSAIDs) belong to the most widely used drugs. Results of recent large meta-analyses have shown that the cardiovascular risk of NSAIDs is more serious than originally believed and is not associated exclusively with coxibs; it is also increased when using so called traditional NSAIDs. Data obtained to date show the safest drugs of this class in terms of cardiovascular risk are naproxen and ibuprofen at low doses. The position of naproxen as the safest NSAID has been challenged by some more recent findings...
2018: Vnitr̆ní Lékar̆ství
https://www.readbyqxmd.com/read/29755544/physicochemical-stress-degradation-evaluation-and-pharmacokinetic-study-of-azgh101-a-new-synthesized-cox2-inhibitor-after-i-v-and-oral-administration-in-male-and-female-rats
#17
Hoda Bahmanof, Simin Dadashzadeh, Afshin Zarghi, Alireza Shafaati, Seyed Mohsen Foroutan
Nonsteroidal anti-inflammatory drugs (NSAIDs) act mainly via inhibition of prostaglandins synthesis by inhibition of cyclooxygenase (COX) isoenzymes (COX-1 and COX-2). Selective COX-2 inhibitors which are also known as coxibs provide the main therapeutic effects of NSAIDs. Zarghi et al . reported 6-benzoyl-2-(4-(methylsulfonyl) phenyl) quinoline-4-carboxylic acid (AZGH101) as a novel derivative of ketoprofen with improved selectivity index (COX-1/COX-2 inhibitory potency) in comparison with ketoprofen. In this study, the log P and stability of AZGH101 were evaluated and the pharmacokinetic characteristics of this compound were investigated following intravenous (10 mg/kg), and oral administration (20 mg/kg), to Wistar rats...
2018: Iranian Journal of Pharmaceutical Research: IJPR
https://www.readbyqxmd.com/read/29663741/interactive-involvement-of-hippocampal-camp-pka-and-cyclooxygenase-2-signaling-pathways-in-spatial-learning-in-the-morris-water-maze
#18
Kaveh Tabrizian, Mahmoud Hashemzaei, Ali Akbar Nasiri, Sheyda Najafi, Fatemeh Amelinia, Mehdi Sanati, Farzaneh Shamshirgaran, Sahar Fanoudi
INTRODUCTION: Accumulated evidence shows that the cAMP-PKA signaling pathway plays a key role in memory functions. Cyclooxygenase-2, a critical player in neuroinflammation, has been confirmed in the pathogenesis of neurodegenerative diseases. This study is aimed to assess the effect of the interaction of cAMP-PKA and cyclooxygenase pathways on spatial memory acquisition in animal models. MATERIAL AND METHODS: In the present study, the effects of the four-day bilateral intra-hippocampal infusions of H-89 as a protein kinase AII inhibitor (10 µM/side), celecoxib (0...
2018: Folia Neuropathologica
https://www.readbyqxmd.com/read/29480373/molecular-docking-molecular-modeling-and-molecular-dynamics-studies-of-azaisoflavone-as-dual-cox-2-inhibitors-and-tp-receptor-antagonists
#19
Murtuza Hadianawala, Amarjyoti Das Mahapatra, Jitender K Yadav, Bhaskar Datta
Designed multi-target ligand (DML) is an emerging strategy for the development of new drugs and involves the engagement of multiple targets with the same moiety. In the context of NSAIDs it has been suggested that targeting the thromboxane prostanoid (TP) receptor along with cyclooxygenase-2 (COX-2) may help to overcome cardiovascular (CVS) complications associated with COXIBs. In the present work, azaisoflavones were studied for their COX-2 and TP receptor binding activities using structure based drug design (SBDD) techniques...
February 26, 2018: Journal of Molecular Modeling
https://www.readbyqxmd.com/read/29456107/design-synthesis-and-discovery-of-5-1-3-diphenyl-1h-pyrazol-4-yl-methylene-pyrimidine-2-4-6-1h-3h-5h-triones-and-related-derivatives-as-novel-inhibitors-of-mpges-1
#20
Kai Ding, Ziyuan Zhou, Shuo Zhou, Yaxia Yuan, Kyungbo Kim, Ting Zhang, Xirong Zheng, Fang Zheng, Chang-Guo Zhan
Human mPGES-1 has emerged as a promising target in exploring a next generation of anti-inflammatory drugs, as selective mPGES-1 inhibitors are expected to discriminatively suppress the production of induced PGE2 without blocking the normal biosynthesis of other prostanoids including homeostatic PGE2 . Therefore, this therapeutic approach is believed to reduce the adverse effects associated with the application of traditional non-steroidal anti-inflammatory drugs (tNSAIDs) and selective COX-2 inhibitors (coxibs)...
March 1, 2018: Bioorganic & Medicinal Chemistry Letters
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