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Naproxen

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https://www.readbyqxmd.com/read/28329421/naproxen-inhibits-uvb-induced-basal-cell-and-squamous-cell-carcinoma-development-in-ptch1-skh-1-hairless-mice
#1
Sandeep C Chaudhary, Mohammad Waseem, Mehtab Rana, Hui Xu, Levy Kopelovich, Craig A Elmets, Mohammad Athar
Naproxen possesses anti-proliferative and pro-apoptotic effects besides its known anti-inflammatory functions. Here, we demonstrate the anti-cancer effects of naproxen against UVB-induced BCCs and SCCs in a highly susceptible murine model of UVB carcinogenesis. Naproxen significantly inhibited UVB-induced BCCs and SCCs in this model. Tumor number and volume were significantly decreased (p<0.005 and p<0.05, respectively). Inhibition in UVB-induced SCCs and BCCs was 77% and 86%, respectively, which was associated with reduced PCNA and cyclin D1 and increased apoptosis...
March 22, 2017: Photochemistry and Photobiology
https://www.readbyqxmd.com/read/28322471/synthesis-of-naproxen-imprinted-polymer-using-pickering-emulsion-polymerization
#2
Małgorzata Kujawska, Tongchang Zhou, Andrzej W Trochimczuk, Lei Ye
For the last decades, molecular imprinting is developing intensively, especially in the case of the application of new imprinting techniques. In this work, for the first time, a Pickering emulsion polymerization was used to synthesize the S-naproxen-imprinted polymer spheres following a noncovalent protocol. To enhance the knowledge about imprinting process using mentioned technique, thorough analysis of the synthesis process was performed. Optimization of polymerization conditions included the selection of functional monomer, cross-linking agent, type of porogen, surfactant, and the choice of appropriate amount of the template and porogen...
March 21, 2017: Journal of Molecular Recognition: JMR
https://www.readbyqxmd.com/read/28315341/low-doses-of-tizanidine-synergize-the-anti-nociceptive-and-anti-inflammatory-effects-of-ketorolac-or-naproxen-while-reducing-of-side-effects
#3
Selene I Patiño-Camacho, Myrna Déciga-Campos, Karla Beltrán-Villalobos, Dalia A Castro-Vidal, Rosa M Montiel-Ruiz, Francisco J Flores-Murrieta
The aim of the present study was to determine whether tizanidine, an alpha2-adrenoceptor agonist, is able to increase the anti-inflammatory and anti-nociceptive effects of naproxen and ketorolac with a low incidence of gastric injury and spontaneous activity in rats. The anti-inflammatory effect was assayed in a carrageenan test, and oral administration of tizanidine (ED40 = 0.94 ± 0.2mg/kg), naproxen (ED40 = 3.18 ± 0.4mg/kg), and ketorolac (ED40 = 16.4 ± 1.9mg/kg) showed a dose-dependent effect on inflammation...
March 14, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28314234/investigating-natural-attenuation-of-pharmaceuticals-through-unsaturated-column-tests
#4
Virtudes Martínez-Hernández, Raffaella Meffe, Claus Kohfahl, Irene de Bustamante
The growing consumption of pharmaceuticals together with their incomplete removal in wastewater treatment plants (WWTPs) implies the occurrence of these compounds in natural water resources. To investigate the natural attenuation of selected pharmaceuticals (caffeine, acetaminophen, sulfamethoxazole, naproxen and carbamazepine) during vadose zone infiltration, unsaturated column (L 26.67 cm, Ø 7.62 cm) experiments, filled with a sandy-loamy soil, were performed using two input concentrations (100 and 1000 μg L(-1))...
March 7, 2017: Chemosphere
https://www.readbyqxmd.com/read/28284648/the-relative-risk-and-its-distribution-of-endocrine-disrupting-chemicals-pharmaceuticals-and-personal-care-products-to-freshwater-organisms-in-the-bohai-rim-china
#5
Meng Zhang, Yajuan Shi, Yonglong Lu, Andrew C Johnson, Suriyanarayanan Sarvajayakesavalu, Zhaoyang Liu, Chao Su, Yueqing Zhang, Monika D Juergens, Xiaowei Jin
In this study, the risks to aquatic organisms posed by 12 commonly detected pharmaceuticals and personal care products (PPCPs) and endocrine disrupting chemicals (EDCs) that are extensively used in Bohai coastal region of China were examined. These were linear alkylbenzene sulfonate (LAS), nonylphenol (NP), diethylhexyl phthalate (DEHP), norfloxacin (NOR), sulfamethoxazole (SMX), erythromycin (ERY), bisphenol A (BPA), ofloxacin (OFL), carbamazepine (CBZ), naproxen (NPX), atenolol (ATL) and metoprolol (MET)...
March 8, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28284639/transport-behavior-of-the-pharmaceutical-compounds-carbamazepine-sulfamethoxazole-gemfibrozil-ibuprofen-and-naproxen-and-the-lifestyle-drug-caffeine-in-saturated-laboratory-columns
#6
Klaus H Hebig, Laura G Groza, Michelle J Sabourin, Traugott J Scheytt, Carol J Ptacek
Despite the large number of pharmaceutically active compounds found in natural environments little is known about their transport behavior in groundwater, which is complicated by their wide range of physical and chemical properties. The transport behavior of five widely used and often detected pharmaceutical compounds and one lifestyle drug has therefore been investigated, using a set of three column experiments. The investigated compounds were the anticonvulsant carbamazepine, the lifestyle drug caffeine, the antibiotic sulfamethoxazole, the lipid regulator gemfibrozil, and the nonsteroidal anti-inflammatories ibuprofen and naproxen...
March 8, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28277163/predictions-of-bisphenol-a-hepatic-clearance-in-the-isolated-perfused-rat-liver-iprl-impact-of-albumin-binding-and-of-co-administration-with-naproxen
#7
Sara Bounakta, Michel Bteich, Marc Mantha, Patrick Poulin, Sami Haddad
1. This study aimed (i) to characterise hepatic clearance (CL) of bisphenol A (BPA) and naproxen (NAP) administered alone or in binary mixtures to highlight the influence of a binding to albumin (ALB) using an isolated perfused rat liver (IPRL) system; and (ii) to compare results of prediction algorithms with measured clearance rates. 2. The IPRL system and liver microsomes were used to determine the metabolic constants of BPA and NAP either in the presence or absence of ALB. In this study, the IPRL was used as proxy for the in vivo situation...
March 3, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28276722/non-steroidal-anti-inflammatory-drugs-and-blood-pressure-control-in-patients-treated-for-hypertension-results-from-the-swedish-primary-care-cardiovascular-database
#8
Charlotta Ljungman, Thomas Kahan, Linus Schiöler, Björn Wettermark, Kristina B Boström, Jan Hasselström, Per Hjerpe, Karin Manhem
PURPOSE: The aim of this observational cohort study was to investigate blood pressure level and the possibility to reach target blood pressure during concomitant use of NSAID in hypertensive patients. MATERIALS AND METHODS: From the Swedish primary care cardiovascular database (SPCCD) a cohort of 5463 patients (2007 to 2008) with at least one prescription of NSAID dispensed 6 months prior to the last blood pressure measurement were included. Clinical data were extracted from computerized medical records and linked to the Prescribed Drug Register...
February 13, 2017: Blood Pressure
https://www.readbyqxmd.com/read/28262316/an-imprinted-interpenetrating-polymer-network-for-microextraction-in-packed-syringe-of-carbamazepine
#9
Sara Asgari, Habib Bagheri, Ali Es-Haghi, Roya AminiTabrizi
An imprinted interpenetrating polymer network (IPN) was synthesized and used as a medium for isolation of carbamazepine from urine samples. The polymer network consisted of a homogeneous polystyrene-sol gel hybrid constructed by in-situ radical polymerization method. In this process, within the sol-gel reaction duration, styrene monomer could penetrate into the reaction mixture and after the polymerization initiation, a monolithic IPN structure was prepared. The scanning electron microscopy (SEM) image and energy dispersive spectroscopy (EDX) are indications of the polystyrene dispersion at nano- to micro-meter level in the sol gel matrix...
March 31, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28262313/high-performance-liquid-chromatography-mass-spectrometry-analysis-of-the-parent-drugs-and-their-metabolites-in-extracts-from-cress-lepidium-sativum-grown-hydroponically-in-water-containing-four-non-steroidal-anti-inflammatory-drugs
#10
Lisa Emhofer, Markus Himmelsbach, Wolfgang Buchberger, Christian W Klampfl
In this paper the metabolism of four non-steroidal anti-inflammatory drugs, (ketoprofen, mefenamic acid, naproxen, and diclofenac) by cress (Lepidium sativum) is described. Cress was cultivated hydroponically in water spiked with the parent drugs at levels ranging from 0.01mgL(-1) to 1mgL(-1). Employing an approach based on the analysis of the plant extracts by HPLC coupled either with quadrupole-time-of-flight mass spectrometry, or Orbitrap MS or triple quadrupole (QqQ) MS allowed the identification of twenty substances (sixteen metabolites and four parent drugs)...
March 31, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28262249/immunotoxic-effects-of-single-and-combined-pharmaceuticals-exposure-on-a-harbor-seal-phoca-vitulina-b-lymphoma-cell-line
#11
Christine Kleinert, Emilie Lacaze, Méryl Mounier, Sylvain De Guise, Michel Fournier
The potential risk of pharmaceuticals in the environment to top-predators is still largely unknown. In this study, we assessed the immunotoxic effects of ten pharmaceuticals individually and as mixtures on a harbor seal (Phoca vitulina) B lymphoma cell line. A significant reduction in lymphocyte transformation was observed following an exposure to 12,500μg/L 17α-ethinyl estradiol and 25,000μg/L naproxen. Exposure to 12,500μg/L 17α-ethinyl estradiol decreased the percentage of cell in the G0/G1 phase of the cell cycle while increasing the percentage of cells in the S phase...
March 2, 2017: Marine Pollution Bulletin
https://www.readbyqxmd.com/read/28260506/ph-dependent-behavior-of-novel-gellan-beads-loaded-with-naproxen
#12
Tomasz Osmałek, Anna Froelich, Bartłomiej Milanowski, Magdalena Białas, Kinga Hyla, Mirosław Szybowicz
We have designed, formulated and characterized low-acyl gellan gum (GG) macrobeads to be applied as potential carriers for the delivery of naproxen (NPX) to the distal parts of the gastrointestinal tract. The beads were obtained by ionotropic gelation technique. CaCl2 solution (1%, 9.0×10-2 M) was used as a cross-linking medium. Nine different polymer, drug and surfactant (Tween®80) mixtures were used for beads production. The surface and morphology of the dried beads were analyzed by SEM. Raman spectra of NPX powder and the beads confirmed that NPX did not undergo structural changes during production process...
March 3, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28259831/melt-extrusion-vs-spray-drying-the-effect-of-processing-methods-on-crystalline-content-of-naproxen-povidone-formulations
#13
Abbe Haser, Tu Cao, Joe Lubach, Tony Listro, Larry Acquarulo, Feng Zhang
Our hypothesis is that melt extrusion is a more suitable processing method than spray drying to prepare amorphous solid dispersions of drugs with a high crystallization tendency. Naproxen-povidone K25 was used as the model system in this study. Naproxen-povidone K25 solid dispersions at 30% and 60% drug loadings were characterized by modulated DSC, powder X-ray diffraction, FT-IR, and solid-state (13)C NMR to identify phase separation and drug recrystallization during processing and storage. At 30% drug loading, hydrogen bond (H-bond) sites of povidone K25 were not saturated and the glass transition (Tg) temperature of the formulation was higher...
March 1, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28257010/structure-and-physicochemical-characterization-of-a-naproxen-picolinamide-cocrystal
#14
Hannah E Kerr, Lorna K Softley, Kuthuru Suresh, Paul Hodgkinson, Ivana Radosavljevic Evans
Naproxen (NPX) is a nonsteroidal anti-inflammatory drug with pain- and fever-relieving properties, currently marketed in the sodium salt form to overcome solubility problems; however, alternative solutions for improving its solubility across all pH values are desirable. NPX is suitable for cocrystal formation, with hydrogen-bonding possibilities via the COOH group. The crystal structure is presented of a 1:1 cocrystal of NPX with picolinamide as a coformer [systematic name: (S)-2-(6-methoxynaphthalen-2-yl)propanoic acid-pyridine-2-carboxamide (1/1), C14H14O3·C6H6N2O]...
March 1, 2017: Acta Crystallographica. Section C, Structural Chemistry
https://www.readbyqxmd.com/read/28248487/practical-stereochemistry
#15
Richard M Kellogg
The relationship between fundamental and applied is often uneasy, particularly in modern political climates. A familiar political view, aimed negatively at the scientific community, is that the former is a waste of money whereas the latter gives value for investment. The answer that fundamental is required as the basis for practical suffers from the fact that the timelines between fundamental and practical are often long and the routes contorted and unexpected. This has been my experience. In this Account, examples are given from the research in which I have been involved wherein quite fundamental considerations have led to various applications...
March 1, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28246127/modeling-sex-differences-in-pharmacokinetics-pharmacodynamics-and-disease-progression-effects-of-naproxen-in-rats-with-collagen-induced-arthritis
#16
Xiaonan Li, Debra C DuBois, Richard R Almon, William J Jusko
Naproxen (NPX) is a frequently used nonsteroidal anti-inflammatory drug (NSAID) for rheumatoid arthritis (RA). Lack of quantitative information about the drug exposure-response relationship has resulted in empirical dosage regimens for use of NPX in RA. Few studies included sex as a factor, although RA predominates in women. A pharmacokinetic, pharmacodynamic, and disease progression (PK/PD/DIS) model described the anti-inflammatory effects of NPX in collagen-induced arthritic (CIA) male and female rats. Three groups of rats were included for each sex: healthy animals, CIA controls, and CIA rats given 50 mg/kg single dose NPX intraperitoneally (IP)...
February 28, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28246126/effect-of-disease-related-changes-in-plasma-albumin-on-the-pharmacokinetics-of-naproxen-in-male-and-female-arthritic-rats
#17
Xiaonan Li, Debra C DuBois, Richard R Almon, William J Jusko
Naproxen (NPX) is used in the treatment of rheumatoid arthritis (RA) for alleviation of pain and inflammation. In view of the extensive albumin binding of NPX, this study investigates whether chronic inflammation and sex will influence the physiological albumin concentrations, plasma protein binding, and pharmacokinetics (PK) of NPX. The PK of NPX was evaluated in a rat model of RA (collagen-induced arthritis (CIA) in Lewis rats) and in healthy controls. These PK studies included: 1) NPX in female and male CIA rats that received 10, 25 or 50 mg/kg NPX intraperitoneally (IP), and 2) NPX in healthy female and male rats after IP dosing of NPX at 50 mg/kg...
February 28, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28238723/non-steroidal-anti-inflammatory-drugs-are-caspase-inhibitors
#18
Christina E Smith, Subada Soti, Torey A Jones, Akihisa Nakagawa, Ding Xue, Hang Yin
Non-steroidal anti-inflammatory drugs (NSAIDs) are among the most commonly used drugs in the world. While the role of NSAIDs as cyclooxygenase (COX) inhibitors is well established, other targets may contribute to anti-inflammation. Here we report caspases as a new pharmacological target for NSAID family drugs such as ibuprofen, naproxen, and ketorolac at physiologic concentrations both in vitro and in vivo. We characterize caspase activity in both in vitro and in cell culture, and combine computational modeling and biophysical analysis to determine the mechanism of action...
March 16, 2017: Cell Chemical Biology
https://www.readbyqxmd.com/read/28236430/hand-ground-nanoscale-zn-ii-coordination-polymers-derived-from-nsaids-cell-migration-inhibition-of-human-breast-cancer-cells
#19
Parthasarathi Dastidar, Mithun Paul, Koushik Sarkar, Jolly Deb
Increased level of intracellular prostaglandin E2 (PGE2) has been linked with the unregulated cancer cell migration that often leads to metastasis. Non-steroidal-anti-inflammatory-drugs (NSAIDs) are known inhibitors of cyclooxygenase (COX) enzymes responsible for increased PGE2 concentration in inflammated as well as cancer cells. In this article, we demonstrated that NSAID derived Zn(II)-coordination polymers were able to inhibit cell migration of human breast cancer cells. Various NSAIDs were anchored to a series of 1D Zn(II)-coordination polymers via carboxylate-Zn coordination and fully characterized by single crystal X-ray diffraction...
February 25, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28223391/evaluation-of-para-aminosalicylic-acid-pas-as-a-substrate-of-multiple-solute-carrier-slc-uptake-transporters-and-possible-drug-interactions-with-nsaids-in-vitro
#20
Md Masud Parvez, Ho Jung Shin, Jin Ah Jung, Jae-Gook Shin
para-Aminosalicylic acid (PAS) is a second-line anti-tuberculosis drug used to treat multidrug-resistant and extensively drug-resistant tuberculosis for more than 60 years. Renal secretion and glomerular filtration are the major pathways for elimination of PAS. We comprehensively studied PAS transport by using cell lines that overexpressed various transporters, and found that PAS acts as a novel substrate of organic anionic polypeptide (OATP1B1), organic cationic transporters (OCT1 and OCT2), and organic anion transporters (OAT1 and OAT3) but not a substrate of any ATP-binding cassette (ABC) transporters...
February 21, 2017: Antimicrobial Agents and Chemotherapy
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