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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
#1
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
#2
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"...
July 31, 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
#3
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
#4
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
#5
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
#6
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
#7
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
#8
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
#9
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
#10
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
#11
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
https://www.readbyqxmd.com/read/29383397/nsaids-utilization-for-musculoskeletal-indications-in-elderly-patients-with-cerebro-cardiovascular-disease
#12
Giuseppe Roberto, Claudia Bartolini, Federico Rea, Graziano Onder, Cristiana Vitale, Gianluca Trifirò, Ursula Kirchmayer, Alessandro Chinellato, Ersilia Lucenteforte, Giovanni Corrao, Alessandro Mugelli, Francesco Lapi, Rosa Gini
OBJECTIVES: To describe NSAID utilization for musculoskeletal conditions in a large cohort of Italian elderly with cerebro/cardiovascular disease, a population in which NSAIDs should be generally avoided due to the prothrombotic potential. METHODS: Administrative data from five Italian geographic areas were analyzed. Patients aged ≥ 65 with a cerebro/cardiovascular event recorded between 2008 and 2011 (cohort entry) were selected. Prescription NSAIDs reimbursed for musculoskeletal conditions and dispensed during 1 year follow-up were retrieved to describe (i) prevalence of use, (ii) average amount of defined daily doses of NSAIDs claimed by users per day of follow-up, and (iii) distribution of the received daily dose (RDD) among patients with ≥ 2 dispensings...
May 2018: European Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29376495/therapeutic-potential-of-n-heterocyclic-analogs-as-anti-inflammatory-agents
#13
Ashwani K Dhingra, Bhawna Chopra, Jagdeep S Dua, Deo N Prasad
BACKGROUND: Various mediators and anti-inflammatory drugs were used since from a long time but it is still a challenge for the medicinal chemists to treat or reduce the symptoms of inflammatory diseases. Most of the clinically used anti-inflammatory drugs such as NSAIDs, Coxibs and GCs are allied with considerable toxicity. OBJECTIVE: The search of novel anti-inflammatory agent is not an ending process. Although the drug treatment has been improved steadily but yet, it is still there is a need to develop more potent therapeutic agents...
2017: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29345921/molecular-mechanisms-in-the-selectivity-of-nonsteroidal-anti-inflammatory-drugs
#14
Yasmin Shamsudin Khan, Hugo Gutiérrez-de-Terán, Johan Åqvist
Nonsteroidal anti-inflammatory drugs (NSAIDs) inhibit cyclooxygenase (COX) 1 and 2 with varying degrees of selectivity. A group of COX-2 selective inhibitors-coxibs-binds in a time-dependent manner through a three-step mechanism, utilizing a side pocket in the binding site. Coxibs have been extensively probed to identify the structural features regulating the slow tight-binding mechanism responsible for COX-2 selectivity. In this study, we further probe a structurally and kinetically diverse data set of COX inhibitors in COX-2 by molecular dynamics and free energy simulations...
February 20, 2018: Biochemistry
https://www.readbyqxmd.com/read/29236213/structural-probing-screening-and-structure-based-drug-repositioning-insights-into-the-identification-of-potential-cox-2-inhibitors-from-selective-coxibs
#15
Uma Devi Bommu, Kranthi Kumar Konidala, Rishika Pamanji, Suneetha Yeguvapalli
The rate-limiting enzyme cyclooxygenase-2 (COX-2) is considered as an insightful prognostic target for non-small cell lung cancer (NSCLC) therapy. Now, administration and prolonged utilization of selective COX-2 inhibitors (COXIBs) towards moderating the NSCLC has been associated with different side effects. In the present study, we focused on the structure-based drug repositioning approaches for predicting therapeutic potential de novo candidates for human COX-2. Due to discrepancies in the eminence of x-ray diffraction structures, creates a big barrier in drug discovery approach...
December 13, 2017: Interdisciplinary Sciences, Computational Life Sciences
https://www.readbyqxmd.com/read/29214381/exposure-to-cox-2-inhibitors-coxibs-during-the-first-trimester-and-pregnancy-outcome-a-prospective-observational-cohort-study
#16
Katarina Dathe, Stephanie Padberg, Stefanie Hultzsch, Luisa-Maria Köhler, Katja Meixner, Anne-Katrin Fietz, Tatjana Tissen-Diabaté, Reinhard Meister, Christof Schaefer
PURPOSE: Cox-2-inhibitors (coxibs) are not recommended in pregnancy but early exposure may occur, for instance in unplanned pregnancies. Experience in pregnancy is limited leading to concerns in patients and their health care providers. Therefore, further data on coxibs and their effects on embryogenesis are needed. METHODS: This observational cohort study evaluates pregnancies ascertained in Germany during the study period from January 2000 to January 2016. A cohort of 174 women exposed to coxibs in the first trimester was compared to a randomly selected cohort of 521 women without exposure to coxibs, other nonsteroidal anti-inflammatory drugs or known teratogens...
April 2018: European Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28979299/physicochemical-stress-degradation-evaluation-and-pharmacokinetic-study-of-azgh102-a-new-synthesized-cox2-inhibitors-after-i-v-and-oral-administration-in-male-and-female-rats
#17
Hoda Bahmanof, Simin Dadashzadeh, Afshin Zarghi, Alireza Shafaati, Seyed Mohsen Foroutan
Coxibs such as celecoxib, rofecoxib, and valdecoxib are introduced as selective COX-2 inhibitors to the market. It has been reported that inhibition of COX-2 beside traditional effects of NSAIDs, reduces the risk of colorectal, breast and lung cancers and also slow the progress of Alzheimer's disease. Zarghi et al. reported 8-benzoyl-2-(4-(methylsulfonyl)phenyl)quinoline-4-carboxylic acid (AZGH 102) as a novel compound with similar IC50 to celecoxib besides improved selectivity index (COX-1/COX-2 inhibitory potency) in comparison with celecoxib...
2017: Iranian Journal of Pharmaceutical Research: IJPR
https://www.readbyqxmd.com/read/28939645/cyclooxygenase-2-protein-protein-interactions-and-posttranslational-modifications
#18
REVIEW
Anna Alexanian, Andrey Sorokin
Numerous studies implicate the cyclooxygenase 2 (COX2) enzyme and COX2-derived prostanoids in various human diseases, and thus, much effort has been made to uncover the regulatory mechanisms of this enzyme. COX2 has been shown to be regulated at both the transcriptional and posttranscriptional levels, leading to the development of nonsteroidal anti-inflammatory drugs (NSAIDs) and selective COX2 inhibitors (COXIBs), which inhibit the COX2 enzyme through direct targeting. Recently, evidence of posttranslational regulation of COX2 enzymatic activity by s-nitrosylation, glycosylation, and phosphorylation has also been presented...
November 1, 2017: Physiological Genomics
https://www.readbyqxmd.com/read/28860667/a-genomic-exploration-identifies-mechanisms-that-may-explain-adverse-cardiovascular-effects-of-cox-2-inhibitors
#19
Ingrid Brænne, Christina Willenborg, Vinicius Tragante, Thorsten Kessler, Lingyao Zeng, Benedikt Reiz, Mariana Kleinecke, Simon von Ameln, Cristen J Willer, Markku Laakso, Philipp S Wild, Tanja Zeller, Lars Wallentin, Paul W Franks, Veikko Salomaa, Abbas Dehghan, Thomas Meitinger, Nilesh J Samani, Folkert W Asselbergs, Jeanette Erdmann, Heribert Schunkert
Cyclooxygenase-2 inhibitors (coxibs) are characterized by multiple molecular off-target effects and increased coronary artery disease (CAD) risk. Here, we systematically explored common variants of genes representing molecular targets of coxibs for association with CAD. Given a broad spectrum of pleiotropic effects of coxibs, our intention was to narrow potential mechanisms affecting CAD risk as we hypothesized that the affected genes may also display genomic signals of coronary disease risk. A Drug Gene Interaction Database search identified 47 gene products to be affected by coxibs...
August 31, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28821939/analgesic-use-in-patients-with-knee-and-or-hip-osteoarthritis-referred-to-an-outpatient-center-a-cross-sectional-study-within-the-amsterdam-osteoarthritis-cohort
#20
Jesper Knoop, Joyce van Tunen, Martin van der Esch, Leo D Roorda, Joost Dekker, Marike van der Leeden, Willem F Lems
Although analgesics are widely recommended in current guidelines, underuse and inadequate prescription of analgesics seem to result in suboptimal treatment effects in patients with knee and/or hip osteoarthritis (OA). This study aimed (i) to describe the use of analgesics; and (ii) to determine factors that are related to analgesic use in patients with knee and/or hip OA referred to an outpatient center. A cross-sectional study with data from 656 patients with knee and/or hip OA referred to an outpatient center (Amsterdam Osteoarthritis (AMS-OA) cohort) was conducted...
October 2017: Rheumatology International
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