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N D Yeomans, D Y Graham, M E Husni, D H Solomon, T Stevens, J Vargo, Q Wang, L M Wisniewski, K E Wolski, J S Borer, P Libby, A M Lincoff, T F Lüscher, W Bao, C Walker, S E Nissen
BACKGROUND: We evaluated GI safety of celecoxib compared with 2 nonselective (ns) NSAIDs, as a secondary objective of a large trial examining multiorgan safety. METHODS: This randomised, double-blind controlled trial analysed 24 081 patients. Osteoarthritis or rheumatoid arthritis patients, needing ongoing NSAID treatment, were randomised to receive celecoxib 100-200 mg b.d., ibuprofen 600-800 mg t.d.s. or naproxen 375-500 mg b.d. plus esomeprazole, and low-dose aspirin or corticosteroids if already prescribed...
April 17, 2018: Alimentary Pharmacology & Therapeutics
Rika Suzuki, Tsugumi Fujita, Kotaro Mizuta, Eiichi Kumamoto
AIMS: Although antinociception produced by non-steroidal anti-inflammatory drugs (NSAIDs) is partly attributed to nerve conduction inhibition, this has not been thoroughly examined yet. The aim of the present study was to reveal quantitatively how various types of NSAIDs affect compound action potentials (CAPs), a measure of nerve conduction. MAIN METHODS: CAPs were recorded from the frog sciatic nerve by using the air-gap method. KEY FINDINGS: Soaking the sciatic nerve with acetic acid-based NSAIDs (diclofenac and aceclofenac) reduced the peak amplitude of CAP in a concentration-dependent manner; their IC50 values were 0...
April 14, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Chang Shu, Tengfei Li, Wen Yang, Duo Li, Shunli Ji, Li Ding
The present work is focused on the design and development of novel amphotericin B (AmB)-conjugated biocompatible and biodegradable polypeptide hydrogels to improve the antifungal activity. Using three kinds of promoting self-assembly groups (2-naphthalene acetic acid (Nap), naproxen (Npx) and dexamethasone (Dex)) and polypeptide sequence (Phe-Phe-Asp-Lys-Tyr, FFDKY), we successfully synthesized the Nap-FFDK(AmB)Y gels, Npx-FFDK(AmB)Y gels and Dex-FFDK(AmB)Y gels. The AmB-conjugated hydrogelators are highly soluble in different aqueous solutions...
March 2018: Royal Society Open Science
I S Filimonov, A P Berzova, V I Barkhatov, A V Krivoshey, N A Trushkin, P V Vrzheshch
The kinetic mechanism of the interaction of nonsteroidal anti-inflammatory drugs (NSAIDs) with their main pharmacological target, prostaglandin H synthase (PGHS), has not yet been established. We showed that inhibition of PGHS-1 from sheep vesicular glands by naproxen (a representative of NSAIDs) demonstrates a non-competitive character with respect to arachidonic acid and cannot be described within a framework of the commonly used kinetic schemes. However, it can be described by taking into account the negative cooperativity of naproxen binding to the cyclooxygenase active sites of the PGHS-1 homodimer (the first naproxen molecule forms a more stable complex (K1 = 0...
February 2018: Biochemistry. Biokhimii︠a︡
Manvi Sharma, Aisha Vadhariya, Michael L Johnson, Zachary A Marcum, Holly M Holmes
BACKGROUND: While many new medications may offer advantages over existing drugs, some newer drugs are reformulations of existing products that provide little innovation or incremental benefit while driving up drug costs. Despite the lack of benefit of these medications, prescribers may be motivated by payments made by the pharmaceutical industry. The objective of the study was to determine the association between payments made to physicians by the pharmaceutical industry and prescriptions for certain selected costly brand name drugs...
April 2, 2018: BMC Health Services Research
C H Tai, H B Oh, J E Seet, K Y Ngiam
Pseudogout, also known as calcium pyrophosphate deposition disease, is a rheumatological condition arising from accumulation of calcium pyrophosphate dihydrate crystals in connective tissues. We present a case of a 56-year-old Bangladeshi woman who underwent focused right inferior parathyroidectomy for primary hyperparathyroidism from a right inferior parathyroid adenoma. On the first post-operative day, she complained of left elbow painful swelling with redness and warmth. Arthrocentesis of left elbow was done due to suspicion of septic arthritis...
April 1, 2018: Annals of the Royal College of Surgeons of England
Poonam Malik, Ravi Bhushan
Enantioselective analysis of (RS)-fexofenadine has been carried out by achiral HPLC via derivatization approach using N-hydroxy-benzotriazolyl-(S)-naproxen ester (synthesised for this purpose) and three chirally pure amines as chiral derivatizing reagents (CDRs). There occurred formation of amide and anhydride types of diastereomeric derivatives. These were separated and isolated by HPLC (analytical and preparative). The structures and configurations were verified via recording full scan product ion mass spectra using LC-MS,1 HNMR spectra, Chem3D Pro 12...
March 30, 2018: Biomedical Chromatography: BMC
Maryam Shamsayei, Yadollah Yamini, Hamid Asiabi, Meysam Safari
The authors describe a 3-component nanoparticle system composed of a silica-coated magnetite (Fe3 O4 ) core and a layered double (Cu-Cr) hydroxide nanoplatelet shell. The sorbent has a high anion exchange capacity for extraction anionic species. A simple online system, referred to as "on-line packed magnetic-in-tube solid phase microextraction" was designed. The nanoparticles were placed in a stainless steel cartridge via dry packing. The cartridge was then applied to the preconcentration acidic drugs including naproxen and indomethacin from urine and plasma...
February 22, 2018: Mikrochimica Acta
Francielle Topolski, Alexandre Moro, Gisele Maria Correr, Sasha Cristina Schimim
Pain is an undesirable side effect of orthodontic tooth movement, which causes many patients to give up orthodontic treatment or avoid it altogether. The aim of this study was to investigate, through an analysis of the scientific literature, the best method for managing orthodontic pain. The methodological aspects involved careful definition of keywords and diligent search in databases of scientific articles published in the English language, without any restriction of publication date. We recovered 1281 articles...
2018: Journal of Pain Research
Xuan Feng, Xiaoyun Wang
OBJECTIVE: Non-steroidal anti-inflammatory drugs (NSAIDs) are used as first-line treatment of primary dysmenorrhea (PD) but there has been no optimal clinical choice among NSAIDs yet. The present study was to assess the relative benefits of different common NSAIDs for PD patients with a network meta-analysis. METHODS: Randomized controlled trials (RCTs) were screened by our criteria and included in the network meta-analysis. Pain relief was considered as primary outcomes and adverse effect was supplied as a safety outcome, while additional rescue, assessment score and pain intensity difference were secondary outcomes...
January 1, 2018: Molecular Pain
Anji Chen, Ifeanyi S Okafor, Consuelo Garcia, Guijun Wang
Sugar based low molecular weight gelators (LMWGs) are useful small molecules that can form reversible supramolecular gels with many applications. Selective functionalization of common monosaccharides has resulted in several classes of effective LMWGs. Recently we found that certain peracetylated sugars containing anomeric triazole functional groups were effective gelators. In this study we synthesized two series of 4,6-O-benzylidene acetal protected β-1,2,3-triazolyl glycoside of D-glucose and N-acetyl D-glucosamine derivatives and evaluated their self-assembling properties in a few solvents...
February 23, 2018: Carbohydrate Research
Neil D Danielson, Fotouh R Mansour, Ling Zhou, Casey V Connell, Erin M Dotlich, Justin N Gibler, Blake E Norman, Shau Grossman, Wenjun Wei, Ying Zhang
Fluorescence detection of various pharmaceuticals and the amino acid tryptophan (low molecular weight organic compounds) as well as the enzyme lactate dehydrogenase LDH (high molar mass compound) has been studied in aqueous solutions using alkyl ammonium formate ionic liquids as the primary solvent component. It was expected that the high viscosity of such ionic liquid-water mixtures would enhance fluorescence. Pharmaceuticals such as riboflavin and naproxen showed no such enhancement in the presence of ethylammonium formate (EAF) or isopropylammonium formate (IPAF) but the fluorescence of warfarin was substantially enhanced by a factor of 4 with 80% EAF and a factor of 7 with 70% IPAF...
March 14, 2018: Journal of Chromatography. A
Shao-Chi Wang, Yun Yang, Jing Liu, Ai-Dou Jiang, Zhao-Xing Chu, Si-Ying Chen, Guo-Qing Gong, Guang-Wei He, Yun-Gen Xu, Qi-Hua Zhu
Novel series of limonin derivatives (V-A-1-V-A-8, V-B-1-V-B-8) were synthesized by adding various tertiary amines onto the C (7)-position of limonin. The synthesized compounds possessed favorable physicochemical property, and the intrinsic solubility of the novel compounds were significantly improved, compared with limonin. Different pharmacological models were used to evaluate the analgesic and anti-inflammatory activities of the target compounds. Compound V-A-8 exhibited the strongest in vivo activity among the novel limonin analogs; its analgesic activity was more potent than aspirin and its anti-inflammatory activity was stronger than naproxen under our testing conditions...
March 2018: Chinese Journal of Natural Medicines
Arnoud de Wilt, Koen van Gijn, Tom Verhoek, Amber Vergnes, Mirit Hoek, Huub Rijnaarts, Alette Langenhoff
Individual treatment processes like biological treatment or ozonation have their limitations for the removal of pharmaceuticals from secondary clarified effluents with high organic matter concentrations (i.e. 17 mg TOC/L). These limitations can be overcome by combining these two processes for a cost-effective pharmaceutical removal. A three-step biological-ozone-biological (BO3 B) treatment process was therefore designed for the enhanced pharmaceutical removal from wastewater effluent. The first biological step removed 38% of ozone scavenging TOC, thus proportionally reducing the absolute ozone input for the subsequent ozonation...
March 12, 2018: Water Research
Weikun Yao, Syed Waqi Ur Rehman, Huijiao Wang, Hongwei Yang, Gang Yu, Yujue Wang
The electro-peroxone (E-peroxone) process is an emerging ozone-based advanced oxidation process (AOP) that has shown large potential for micropollutant abatement in water treatment. To evaluate its performance under more realistic conditions of water treatment, a continuous-flow pilot E-peroxone system was developed and compared with conventional ozonation and a UV/O3 process for micropollutant abatements in various water matrices (groundwater, surface water, and secondary wastewater effluent) in this study...
March 16, 2018: Water Research
Pajaree Sriuttha, Buntitabhon Sirichanchuen, Unchalee Permsuwan
Background: Nonsteroidal anti-inflammatory drugs (NSAIDs) are the most widely used medication in several countries, including Thailand. NSAIDs have been associated with hepatic side effects; however, the frequency of these side effects is uncertain. Aim of the Review: To systematically review published literature on randomized, controlled trials that assessed the risk of clinically significant hepatotoxicity associated with NSAIDs. Methods: Searches of bibliographic databases EMBASE, PubMed, and the Cochrane Library were conducted up to July 30, 2016, to identify randomized controlled trials of ibuprofen, naproxen, diclofenac, piroxicam, meloxicam, mefenamic acid, indomethacin, celecoxib, and etoricoxib in adults with any disease that provide information on hepatotoxicity outcomes...
2018: International Journal of Hepatology
Linhui Wang, Li Zhang, Yi Zhao, Qiuyi Fu, Wenjiao Xiao, Runxin Lu, Li Hai, Li Guo, Yong Wu
A new dual-targeting naproxen prodrug conjugated with glucose and ascorbic acid for central nervous system (CNS) drug delivery was designed and synthesized in order to effectively deliver naproxen to the brain. Naproxen could be released from the prepared prodrugs when incubated with various buffers, mouse plasma, and brain homogenate. Also, the prodrug showed superior neuroprotective effect in vivo over naproxen. Our results suggest that chemical modification of therapeutics with warheads of glucose and ascorbic acid represents a promising and efficient strategy for the development of brain targeting prodrugs by utilizing the endogenous transportation mechanism of the warheads...
March 22, 2018: Archiv der Pharmazie
Z Chen, L Cheng, G Feng
Chronic recurrent multifocal osteomyelitis (CRMO) is a sporadic condition of inflammatory bone pain that occurs as recurrent flares because of osteomyelitis, which presents in the form of multiple aseptic foci. The estimated prevalence of CRMO is 1-2 per million, affecting mostly children, in the age group of 2 to 17. Main symptoms of CRMO are bone inflammation and pain, which are generally worse at night. Other symptoms seen on radiographs indicate osteolytic lesions surrounded by sclerosis, at later stages of the disease...
March 2018: European Review for Medical and Pharmacological Sciences
Yujie He, Alette A M Langenhoff, Rob N J Comans, Nora B Sutton, Huub H M Rijnaarts
Natural dissolved organic matter (DOM) and nitrification can play an important role in biodegradation of pharmaceutically active compounds (PhACs) in aerobic zones of constructed wetlands (CWs). This study used an enrichment culture originating from CW sediment to study the effect of DOM and nitrification on aerobic biodegradation of seven PhACs. The enriched culture degraded caffeine (CAF), metoprolol (MET), naproxen (NAP), and ibuprofen (IBP) with a consistent biodegradability order of CAF>MET>NAP>IBP...
March 2, 2018: Science of the Total Environment
Shuang Luo, Lingwei Gao, Zongsu Wei, Richard Spinney, Dionysios D Dionysiou, Wei-Ping Hu, Liyuan Chai, Ruiyang Xiao
Hydroxyl radical (• OH) based advanced oxidation technologies (AOTs) are effective for removing non‒steroidal anti-inflammatory drugs (NSAIDs) during water treatment. In this study, we systematically investigated the degradation kinetics of naproxen (NAP), a representative NSAID, with a combination of experimental and theoretical approaches. The second-order rate constant (k) of• OH oxidation of NAP was measured to be (4.32 ± 0.04) × 109  M-1  s-1 , which was in a reasonable agreement with transition state theory calculated k value (1...
March 5, 2018: Water Research
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