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https://www.readbyqxmd.com/read/28074640/evaluation-of-pharmacokinetic-interactions-between-lesinurad-a-new-selective-urate-reabsorption-inhibitor-and-commonly-used-drugs-for-gout-treatment
#1
Zancong Shen, Kathy Tieu, David Wilson, Gail Bucci, Michael Gillen, Caroline Lee, Bradley Kerr
Lesinurad is a novel selective uric acid reabsorption inhibitor approved for treatment of hyperuricemia associated with gout in combination with xanthine oxidase inhibitors (XOIs). Open-label pharmacokinetic studies were performed in volunteers or subjects with hyperuricemia (serum uric acid ≥ 8 mg/dL) to investigate interactions of lesinurad (with and without concurrent XOIs) with colchicine and 2 nonsteroidal anti-inflammatory drugs: naproxen and indomethacin. Colchicine studies included consecutive 7-day treatment periods of (1) allopurinol 300 mg, allopurinol 300 mg plus lesinurad 400 or 600 mg, and continued lesinurad 400 or 600 mg; or (2) febuxostat 40 or 80 mg, febuxostat 40 or 80 mg plus lesinurad 400 mg, and continued febuxostat 40 or 80 mg plus lesinurad 600 mg...
January 11, 2017: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/28063293/adsorption-of-non-steroidal-anti-inflammatory-drugs-from-aqueous-solution-using-activated-carbons-review
#2
REVIEW
Muthanna J Ahmed
Pharmaceutical pollutants are of significant effect on the environment, so that their treatments have been addressed in many studies. Activated carbon (AC) adsorbent shows best attraction for these compounds due to its unique characteristics represented by high capacity and porosity. In this article, the adsorption performance of AC towards non-steroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen, ketoprofen, naproxen, and diclofenac were reviewed. According to collected data, maximum adsorption capacities of 417, 25, 290, and 372 mg/g were obtained from Langmuir isotherm for these drugs, respectively...
January 4, 2017: Journal of Environmental Management
https://www.readbyqxmd.com/read/28063129/rates-of-nonsteroidal-anti-inflammatory-drug-use-in-patients-with-established-cardiovascular-disease-a-retrospective-cross-sectional-study-from-nhanes-2009-2010
#3
Gregory Castelli, Ashley Petrone, Jun Xiang, Carl Shrader, Dana King
PURPOSE: Nonsteroidal anti-inflammatory drugs (NSAIDs) are commonly used to treat pain, inflammation, and fever in the USA. Unfortunately, NSAIDs have been associated with an increased risk of adverse cardiovascular events, especially among NSAID users with established cardiovascular disease (CVD). In 2005, the Food and Drug Administration (FDA) released an initial warning regarding NSAID use and CVD risk, and recently, in July 2015, released an updated statement strengthening this initial warning...
January 6, 2017: American Journal of Cardiovascular Drugs: Drugs, Devices, and Other Interventions
https://www.readbyqxmd.com/read/28061011/simultaneous-enantiomeric-analysis-of-pharmacologically-active-compounds-in-environmental-samples-by-chiral-lc-ms-ms-with-a-macrocyclic-antibiotic-stationary-phase
#4
D Camacho-Muñoz, B Kasprzyk-Hordern
This paper presents a multi-residue method for direct enantioselective separation of chiral pharmacologically active compounds in environmental matrices. The method is based on chiral liquid chromatography and tandem mass spectrometry detection. Simultaneous chiral discrimination was achieved with a macrocyclic glycopeptide-based column with antibiotic teicoplanin as a chiral selector working under reverse phase mode. For the first time, enantioresolution was reported for metabolites of ibuprofen: carboxyibuprofen and 2-hydroxyibuprofen with this chiral stationary phase...
January 6, 2017: Journal of Mass Spectrometry: JMS
https://www.readbyqxmd.com/read/28056749/development-and-evaluation-of-naproxen-sodium-gel-using-piper-cubeba-for-enhanced-transdermal-drug-delivery-and-therapeutic-facilitation
#5
Sunetra Kaustubh Patwardhan, Manohar J Patil, Anbazhagan Sockalingam
BACKGROUND: The absorption of drug through skin avoids many side effects of oral route like gastric irritation, nausea, systemic toxicity etc and thus improves patient compliance. Naproxen sodium (NPRS) is one of the potent NSAID agents. OBJECTIVE: The present study was aimed to develop and evaluate the gel formulation containing NPRS for transdermal drug delivery reducing the side effects and improving patient compliance. The patents on topical delivery of NSAIDS (US 9012402 B1, US 9072659 B2, US 20150258196 A1) and patents indicating use of herbal penetration enhancers (US 20100273746A1, WO 2005009510 A2, US 6004969 A) helped in selecting the drug, excipients...
January 5, 2017: Recent Patents on Drug Delivery & Formulation
https://www.readbyqxmd.com/read/28056423/epiisopiloturine-hydrochloride-an-imidazole-alkaloid-isolated-from-pilocarpus-microphyllus-leaves-protects-against-naproxen-induced-gastrointestinal-damage-in-rats
#6
Lucas A D Nicolau, Nathalia S Carvalho, Dvison M Pacífico, Larisse T Lucetti, Karoline S Aragão, Leiz M C Véras, Marcellus H L P Souza, José R S A Leite, Jand Venes R Medeiros
OBJECTIVE: This study aimed to investigate the protective effect of epiisopiloturine hydrochloride (EPI), an imidazole alkaloid, on NAP-induced gastrointestinal damage in rats. METHODS: Initially, rats were pretreated with 0.5% carboxymethylcellulose (vehicle) or EPI (3, 10 and 30mg/kg, p.o. or i.p., groups 3-5, respectively) twice daily, for 2days. After 1h, NAP (80mg/kg, p.o.) was given. The control group received only vehicle (group 1) or vehicle+naproxen (group 2)...
January 2, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28043133/long-term-physical-stability-of-pvp-and-pvpva-amorphous-solid-dispersions
#7
Kristin Lehmkemper, Samuel O Kyeremateng, Oliver Heinzerling, Matthias Degenhardt, Gabriele Sadowski
The preparation of amorphous solid dispersion (ASD) formulations is a promising strategy to improve the bioavailability of an active pharmaceutical ingredient (API). By dissolving the API in a polymer it is stabilized in its amorphous form, which usually shows higher water solubility than its crystalline counterpart. To prevent recrystallization, the long-term physical stability of ASD formulations is of big interest. In this work, the solubility of the APIs acetaminophen and naproxen in the excipient polymers poly(vinylpyrrolidone) (PVP K25) and poly(vinylpyrrolidone-co-vinyl acetate) (PVPVA64) was calculated with three models: the Perturbed-Chain Statistical Associating Fluid Theory (PC-SAFT), the Flory-Huggins model (FH), and an empirical model (Kyeremateng et al...
January 3, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28043130/effect-of-extent-of-supersaturation-on-the-evolution-of-kinetic-solubility-profiles
#8
Yi Rang Han, Ping I Lee
Solubility limited compounds require enabling formulations such as amorphous solid dispersions (ASDs) to increase the apparent solubility by dissolving to a concentration higher than the equilibrium solubility of the drug. This may lead to subsequent precipitation and thus the loss of the solubility advantage. Although higher supersaturation is known to result in faster precipitation, the overall effect of this faster precipitation on the bioavailability is not well understood. The objective of this study is to gain a better understanding of the impact of extent of supersaturation (i...
January 3, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28041539/-pseudoporfyri-udl%C3%A3-st-af-naproxen
#9
Jon Erik Fraes Diernaes, Rewend Bustan, Daanyaal Wasim
No abstract text is available yet for this article.
December 19, 2016: Ugeskrift for Laeger
https://www.readbyqxmd.com/read/28040207/synthesis-characterization-and-pharmacological-evaluation-of-certain-enzymatically-cleavable-nsaids-amide-prodrugs
#10
Tilal Elsaman, Omar A A Aldeeb, Tarek Aboul-Fadl, Elnazeer I Hamedelneil
The presence of free carboxylic acid group in majority of non-steroidal anti-inflammatory drug (NSAIDs) is responsible from GI irritation. Coupling of the appropriate NSAIDs (diclofenac, naproxen, dexibuprofen and meclofenamic acid) 1-4, respectively with the appropriate amino acid ester 5 using dicyclohexylcarbodiimide afforded prodrugs 6-13. The structures of the prodrugs were verified based on spectral data. Chemical hydrolysis studies performed in three different non enzymatic buffer solutions at pH 1.2, 5...
December 23, 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28039572/formulation-and-optimization-of-multiparticulate-drug-delivery-system-approach-for-high-drug-loading
#11
Neha Shah, Tejal Mehta, Mukesh Gohel
The aim of the present work was to develop and optimize multiparticulate formulation viz. pellets of naproxen by employing QbD and risk assessment approach. Mixture design with extreme vertices was applied to the formulation with high loading of drug (about 90%) and extrusion-spheronization as a process for manufacturing pellets. Independent variables chosen were level of microcrystalline cellulose (MCC)-X 1, polyvinylpyrrolidone K-90 (PVP K-90)-X 2, croscarmellose sodium (CCS)-X 3, and polacrilin potassium (PP)-X 4...
December 30, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28034808/studying-of-crystal-growth-and-overall-crystallization-of-naproxen-from-binary-mixtures
#12
E Kaminska, O Madejczyk, M Tarnacka, K Jurkiewicz, K Kaminski, M Paluch
Broadband dielectric spectroscopy (BDS) and differential scanning calorimetry (DSC) were applied to investigate the molecular dynamics and phase transitions in binary mixtures composed of naproxen (NAP) and acetylated saccharides: maltose (acMAL) and sucrose (acSUC). Moreover, the application of BDS method and optical microscopy enabled us to study both crystallization kinetics and crystal growth of naproxen from the solid dispersions with the highest content of modified carbohydrates (1:5 weight ratio). It was found that the activation barriers of crystallization estimated from dielectric measurements are completely different for both studied herein mixtures...
December 26, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28025218/non-steroidal-anti-inflammatory-drug-use-is-associated-with-increased-risk-of-out-of-hospital-cardiac-arrest-a-nationwide-case-time-control-study
#13
Kathrine B Sondergaard, Peter Weeke, Mads Wissenberg, Anne-Marie Schjerning Olsen, Emil L Fosbol, Freddy K Lippert, Christian Torp-Pedersen, Gunnar H Gislason, Fredrik Folke
AIMS: Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used and have been associated with increased cardiovascular risk. Nonetheless, it remains unknown whether use of NSAIDs is associated with out-of-hospital cardiac arrest (OHCA). METHODS AND RESULTS: From the nationwide Danish Cardiac Arrest Registry, all persons with OHCA during 2001-2010 were identified. NSAID use 30 days before OHCA was categorized as follows: diclofenac, naproxen, ibuprofen, rofecoxib, celecoxib, and other...
December 26, 2016: European Heart Journal. Cardiovascular Pharmacotherapy
https://www.readbyqxmd.com/read/28019014/non-steroidal-anti-inflammatory-drug-induced-cardiovascular-adverse-events-a-meta-analysis
#14
REVIEW
B R Gunter, K A Butler, R L Wallace, S M Smith, S Harirforoosh
WHAT IS KNOWN AND OBJECTIVE: Although non-steroidal anti-inflammatory drugs (NSAIDs) have been studied in randomized, controlled trials and meta-analyses in an effort to determine their cardiovascular (CV) risks, no consensus has been reached. These studies continue to raise questions, including whether cyclooxygenase-2 (COX-2) selectivity plays a role in conferring CV risk. We performed a meta-analysis of current literature to determine whether COX-2 selectivity leads to an increased CV risk...
February 2017: Journal of Clinical Pharmacy and Therapeutics
https://www.readbyqxmd.com/read/28018307/variable-effects-of-non-steroidal-anti-inflammatory-drugs-nsaids-on-selected-biochemical-processes-mediated-by-soil-microorganisms
#15
Mariusz Cycoń, Sławomir Borymski, Bartłomiej Żołnierczyk, Zofia Piotrowska-Seget
Non-steroidal anti-inflammatory drugs (NSAIDs) are the most frequently used group of pharmaceuticals. The high consumption and the uncontrolled disposal of unused drugs into municipal waste or their deposit in landfills can result in an increased concentration of these compounds in soils. Moreover, these drugs can affect the microbial activity. However, there is a lack of knowledge about these effects or it is very limited. Therefore, the objective of this study was to compare the impact of selected commercially available NSAIDs, i...
2016: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28011407/non-steroidal-anti-inflammatory-drugs-in-the-watercourses-of-elbe-basin-in-czech-republic
#16
Petr Marsik, Jan Rezek, Monika Židková, Barbora Kramulová, Jan Tauchen, Tomáš Vaněk
Non-steroidal anti-inflammatory drugs (NSAIDs) belong to most used pharmaceuticals in the human and veterinary medicine. The widespread consumption of NSAIDs has led to their ubiquitous occurrence in water environment including large river systems. In the present study, concentrations of the five most frequently used NSAIDs (ibuprofen, diclofenac, naproxen, ketoprofen and indomethacin) were determined in the watercourses of the river Elbe basin in Czech Republic. The presence of the pharmaceuticals was measured at 29 sampling sites including urban and rural areas, small creeks and main tributaries of the Elbe monthly from April to December of 2011...
December 14, 2016: Chemosphere
https://www.readbyqxmd.com/read/28004343/naproxen-microparticulate-systems-prepared-using-in-situ-crystallisation-and-freeze-drying-techniques
#17
Amanda Solaiman, Adam Keenan Tatari, Amal Ali Elkordy
Poor drug solubility and dissolution rate remain to be one of the major problems facing pharmaceutical scientists, with approximately 40% of drugs in the industry categorised as practically insoluble or poorly water soluble. This in turn can lead to serious delivery challenges and poor bioavailability. The aim of this research was to investigate the effects of the surfactants, poloxamer 407 (P407) and caprol® PGE 860 (CAP), at various concentrations (0.1, 0.5, 1 and 3% w/v) on the enhancement of the dissolution properties of poorly water-soluble drug, naproxen, using in situ micronisation by solvent change method and freeze-drying...
December 21, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27998478/characterization-and-optimization-of-low-cost-microfluidic-thread-based-electroanalytical-device-for-micro-flow-injection-analysis
#18
Deonir Agustini, Márcio F Bergamini, Luiz Humberto Marcolino-Junior
The micro flow injection analysis (μFIA) is a powerful technique that uses the principles of traditional flow analysis in a microfluidic device and brings a number of improvements related to the consumption of reagents and samples, speed of analysis and portability. However, the complexity and cost of manufacturing processes, difficulty in integrating micropumps and the limited performance of systems employing passive pumps are challenges that must be overcome. Here, we present the characterization and optimization of a low cost device based on cotton threads as microfluidic channel to perform μFIA based on passive pumps with good analytical performance in a simple, easy and inexpensive way...
January 25, 2017: Analytica Chimica Acta
https://www.readbyqxmd.com/read/27989618/pharmacokinetic-interactions-between-pelubiprofen-and-eperisone-hydrochloride-a-randomized-open-label-crossover-study-of-healthy-korean-men
#19
Ju-Hee Ryu, Joo-Il Kim, Hyung Son Kim, Gyu-Jeong Noh, Kyung-Tae Lee, Eun Kyoung Chung
PURPOSE: Pelubiprofen is a novel nonsteroidal anti-inflammatory, analgesic, and antipyretic drug with at least similar efficacy and better tolerability compared with other nonsteroidal anti-inflammatory, analgesic, and antipyretic drugs such as naproxen and aceclofenac. Eperisone hydrochloride is a centrally acting muscle relaxant that performs by blocking calcium channels. The combined use of pelubiprofen and eperisone hydrochloride is increasingly anticipated to promote the clinical effectiveness of pelubiprofen in relieving musculoskeletal symptoms of osteoarthritis, rheumatoid arthritis, and low back pain...
December 15, 2016: Clinical Therapeutics
https://www.readbyqxmd.com/read/27988363/in-vitro-antiglioma-action-of-indomethacin-is-mediated-via-amp-activated-protein-kinase-mtor-complex-1-signalling-pathway
#20
Aleksandar Pantovic, Mihajlo Bosnjak, Katarina Arsikin, Milica Kosic, Milos Mandic, Biljana Ristic, Jelena Tosic, Danica Grujicic, Aleksandra Isakovic, Nikola Micic, Vladimir Trajkovic, Ljubica Harhaji-Trajkovic
We investigated the role of the intracellular energy-sensing AMP-activated protein kinase (AMPK)/mammalian target of rapamycin (mTOR) pathway in the in vitro antiglioma effect of the cyclooxygenase (COX) inhibitor indomethacin. Indomethacin was more potent than COX inhibitors diclofenac, naproxen, and ketoprofen in reducing the viability of U251 human glioma cells. Antiglioma effect of the drug was associated with p21 increase and G2M cell cycle arrest, as well as with oxidative stress, mitochondrial depolarization, caspase activation, and the induction of apoptosis...
December 14, 2016: International Journal of Biochemistry & Cell Biology
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