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Isabel Aparici-Espert, Miguel A Miranda, Virginie Lhiaubet-Vallet
Photosensitization by drugs is a problem of increasing importance in modern life. This phenomenon occurs when a chemical substance in the skin is exposed to sunlight. Photosensitizing drugs are reported to cause severe skin dermatitis, and indeed, it is generally advised to avoid sunbathing and to apply sunscreen. In this context, the nonsteroidal anti-inflammatory drug (NSAID) diclofenac is a photosensitive drug, especially when administered in topical form. In this work, efforts have been made to design and study an innovative pro-drug/pro-filter system containing diclofenac and the UVA filter avobenzone in order to develop a safer use of this topical drug...
March 16, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Collin D Edington, Wen Li Kelly Chen, Emily Geishecker, Timothy Kassis, Luis R Soenksen, Brij M Bhushan, Duncan Freake, Jared Kirschner, Christian Maass, Nikolaos Tsamandouras, Jorge Valdez, Christi D Cook, Tom Parent, Stephen Snyder, Jiajie Yu, Emily Suter, Michael Shockley, Jason Velazquez, Jeremy J Velazquez, Linda Stockdale, Julia P Papps, Iris Lee, Nicholas Vann, Mario Gamboa, Matthew E LaBarge, Zhe Zhong, Xin Wang, Laurie A Boyer, Douglas A Lauffenburger, Rebecca L Carrier, Catherine Communal, Steven R Tannenbaum, Cynthia L Stokes, David J Hughes, Gaurav Rohatgi, David L Trumper, Murat Cirit, Linda G Griffith
Microphysiological systems (MPSs) are in vitro models that capture facets of in vivo organ function through use of specialized culture microenvironments, including 3D matrices and microperfusion. Here, we report an approach to co-culture multiple different MPSs linked together physiologically on re-useable, open-system microfluidic platforms that are compatible with the quantitative study of a range of compounds, including lipophilic drugs. We describe three different platform designs - "4-way", "7-way", and "10-way" - each accommodating a mixing chamber and up to 4, 7, or 10 MPSs...
March 14, 2018: Scientific Reports
Young Hee Nam, Colleen M Brensinger, Warren B Bilker, Charles E Leonard, Scott E Kasner, Tilo Grosser, Xuanwen Li, Sean Hennessy
OBJECTIVE: To examine the comparative safety of individual NSAIDs when given concomitantly with clopidogrel. METHODS: We conducted a retrospective cohort study using Medicaid claims from five US states during 1999-2010, supplemented with Medicare claims for dual-enrollees. The exposure of interest was the first concomitant use of clopidogrel and one of the 10 selected NSAIDs after a 1-year baseline period. The outcomes were: all-cause mortality; acute myocardial infarction (AMI)/ischemic stroke; and gastrointestinal bleeding (GIB)/intracranial hemorrhage (ICH)...
2018: PloS One
Mariana Kozlowska, Pawel Rodziewicz, Tillmann Utesch, Maria Andrea Mroginski, Anna Kaczmarek-Kedziera
The solubility-permeability relationship of active pharmaceutical ingredients determines the efficacy of their usage. Diclofenac (DCL), which is a widely used nonsteroidal anti-inflammatory drug, is characterized by extremely good membrane permeability, but low water solubility limiting drug effectiveness. The present research focuses on the fundamental explanation of this limitation using the combination of ab initio and classical molecular dynamics simulations of different ionic forms of DCL in water, namely, ionized, un-ionized and the mixture of them both...
March 14, 2018: Physical Chemistry Chemical Physics: PCCP
Thibaut Le Guet, Ilham Hsini, Jérôme Labanowski, Leslie Mondamert
Sorption of pharmaceuticals onto sediments is frequently related to organic matter content. Thus, the present work aimed to compare the effect of humic substances (HS) extracted from a river sediment versus Aldrich (HS) on the sorption of selected pharmaceuticals onto this river sediment. The results exhibited no "unique" effect of the presence of HS from the same origin. Thus, the sediment HS increased the sorption of sulfamethoxazole (SMX), diclofenac (DCF), and trimethoprim (TMP), but reduced the sorption of atenolol (ATN)...
March 11, 2018: Environmental Science and Pollution Research International
Monika Wieczerzak, Błażej Kudłak, Galina Yotova, Stefan Tsakovski, Vasil Simeonov, Jacek Namieśnik
Assessment of the impact of pharmaceutical residues on living organisms is a very complex subject. Apart from taking into account the toxicity of individual compounds, environmental factors should also be taken into account. In this paper, attempts were made to assess the impact of coexisting inorganic ions and changes in pH on the toxicity of ten selected pharmaceuticals. Two bioassays were used to measure the estrogenic and androgenic effects (XenoScreen YES/YAS - Saccharomyces cerevisiae) and acute toxicity (Microtox® - Vibrio fischeri)...
March 7, 2018: Environmental Pollution
Xianjing Zhou, Yanxin Qi, Zhijun Zhang, Jingjing Nie, Yubin Huang, Bin-Yang Du
A novel engineered microgels with amphipathic network structures were designed and synthesized by copolymerizing N-isopropylacrylamide (NIPAm), 1-vinylimidazole (VIM) and 2-(cinnamoyloxy) ethyl methacrylate (CEMA) in the presence of 1, 6-dibromohexane. The engineered microgels possess hydrophilic quaternization crosslinking structures and hydrophobic crosslinking inner nanodomains, which are suitable for loading and simultaneous release of hydrophilic non-steroidal anti-inflammatory drug (NSAID), diclofenac sodium (DS), and hydrophobic antic cancer drug, doxorubicin (DOX), respectively...
March 9, 2018: ACS Applied Materials & Interfaces
Igor V Ukrainets, Ganna M Hamza, Anna A Burian, Svitlana V Shishkina, Natali I Voloshchuk, Oxana V Malchenko
In order to determine the regularities of the structure-analgesic activity relationship, the peculiarities of obtaining, the spatial structure, and biological properties of 4-methyl-2,2-dioxo-1 H -2λ⁶,1-benzothiazine-3-carboxylic acid and some of its derivatives have been studied. Using nuclear magnetic resonance (NMR) spectroscopy and X-ray diffraction analysis, it has been proven that varying the reaction conditions using alkaline hydrolysis of methyl 4-methyl-2,2-dioxo-1 H -2λ⁶,1-benzothiazine-3-carboxylate makes it possible to successfully synthesize a monohydrate of the target acid, its sodium salt, or 4-methyl-2,2-dioxo-1 H -2λ⁶,1-benzothiazine...
March 8, 2018: Scientia Pharmaceutica
Yashika Garg, Jatinder Singh, H S Sohal, Rajeshwari Gore, Arun Kumar
OBJECTIVE: Osteoarthritis (OA) is a chronic progressive degenerative disease of weight-bearing joints and the leading cause of disability in elderly. Current medical management of OA is mostly palliative with nonsteroidal anti-inflammatory drugs (NSAIDs) being the mainstay of therapy. Reports of gastrointestinal adverse effects with traditional NSAIDs and cardiovascular adverse effects associated with selective cyclooxygenase-2 (COX-2) inhibitors have prompted the hunt for a better NSAID with no or minimal adverse effects...
September 2017: Indian Journal of Pharmacology
Tom Tg Nieskens, Janny Gp Peters, Dina Dabaghie, Daphne Korte, Katja Jansen, Alexander H Van Asbeck, Neslihan N Tavraz, Thomas Friedrich, Frans Russel, Rosalinde Masereeuw, Martijn J Wilmer
Cisplatin is a cytostatic drug used for treatment of solid organ tumors. The main adverse effect is organic cation transporter 2 (OCT2)-mediated nephrotoxicity, observed in 30% of patients. The contribution of other renal drug transporters is elusive. Here, cisplatin-induced toxicity was evaluated in human-derived proximal tubule epithelial cells (ciPTEC) expressing renal drug transporters, including OCT2 and organic anion transporter 1 (OAT1) or 3 (OAT3). Parent ciPTEC demonstrated OCT2-dependent cisplatin toxicity (TC50 34±1 μM after 24 h exposure), as determined by cell viability...
March 7, 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
Esra Dilek, Sema Caglar, Kübra Erdogan, Bülent Caglar, Onur Sahin
In this study, the effects of four novel mononuclear palladium(II) and platinum(II) complexes on the activity of human serum paraoxanase1 were examined. First, four novel mononuclear palladium(II) and platinum(II) complexes were synthesized with a nitrogen donor ligand 1-(2-aminoethyl)pyrrolidine and nonsteroidal anti-inflammatory drugs diclofenac, mefenamic acid. These complexes were characterized by spectroscopic, thermal, and elemental analyses. The crystal structures of complex [Pd(2-amepyr)2 ](dicl)2 1 and [Pd(2-amepyr)2 ](mef)2 3 were determined by X-ray crystallography...
March 7, 2018: Journal of Biochemical and Molecular Toxicology
Atsushi Hanzawa, Toshiyuki Handa, Yoshihiko Kohkita, Tatsuya Ichinohe, Ken-Ichi Fukuda
We compared the effects of preoperative administration of diclofenac sodium, celecoxib, and acetaminophen on postoperative pain in patients undergoing minor oral surgery under general anesthesia. One hundred twenty-eight patients were randomly divided into 4 groups preoperatively treated with diclofenac sodium 50 mg, celecoxib 400 mg, acetaminophen 1000 mg, or placebo. Postoperative pain was managed using intravenous patient-controlled infusion of fentanyl. Assessments included levels of postoperative pain by using visual analog scale (VAS) scores at 4, 5, and 6 hours after administration of the test drug; consumption of fentanyl up to each time point; and time to first requirement for fentanyl...
2018: Anesthesia Progress
Toshiyuki Sakaki, Kaori Yasuda, Miyu Nishikawa, Shinichi Ikushiro
 Sesamin, derived from sesame seeds, is known to have various biological effects. Since some of these effects appear to be derived from its metabolites, the elucidation of sesamin metabolism is essential to understanding the molecular mechanism of its effects. In addition, it is important to clarify drug-sesamin interactions in order to address safety concerns, as some food factors are known to affect drug metabolism. Our previous studies revealed that sesamin was sequentially metabolized by cytochrome P450 (CYP) and UDP-glucuronosyltransferase or sulfotransferase...
2018: Yakugaku Zasshi: Journal of the Pharmaceutical Society of Japan
David B Miklos, Rebecca Hartl, Philipp Michel, Karl G Linden, Jörg E Drewes, Uwe Hübner
This study investigated the removal of 15 trace organic chemicals (TOrCs) occurring at ambient concentrations from municipal wastewater treatment plant effluent by advanced oxidation using UV/H2 O2 at pilot-scale. Pseudo first-order rate constants (kobs ) for photolytic as well as combined oxidative and photolytic degradation observed at pilot-scale were validated with results from a bench-scale collimated beam device. No significant difference was determined between pilot- and lab-scale performance. During continuous pilot-scale operation at constant UV fluence of 800 mJ/cm2 and H2 O2 dosage of 10 mg/L, the removal of various TOrCs was investigated...
February 21, 2018: Water Research
Sieta T de Vries, Maartje J M van der Sar, Anna Marie Coleman, Yvette Escudero, Alfonso Rodríguez Pascual, Miguel-Ángel Maciá Martínez, Amelia Cupelli, Ilaria Baldelli, Ivana Šipić, Adriana Andrić, Line Michan, Petra Denig, Peter G M Mol
INTRODUCTION: National competent authorities (NCAs) use Direct Healthcare Professional Communications (DHPCs) to communicate new drug safety issues to healthcare professionals (HCPs). More knowledge is needed about the effectiveness of DHPCs and the extent to which they raise awareness of new safety issues among HCPs. OBJECTIVE: The objective was to assess and compare general practitioners' (GPs'), cardiologists', and pharmacists' familiarity with DHPCs as communication tools, their awareness of specific drug safety issues, and the sources through which they had become aware of the specific issues...
March 2, 2018: Drug Safety: An International Journal of Medical Toxicology and Drug Experience
Isabelle M Larsen, Asbjørn M Drewes, Anne E Olesen
Pain involves responses in which both peripheral and central mechanisms contribute to the generation of pain. Pre-clinical laboratory data have supported that a topical formulation of combined diclofenac and methadone (Diclometh) may alleviate local pain, and potentially the side effect profile should be low. We hypothesized that anti-allodynic and anti-hyperalgesic effects of Diclometh could be demonstrated in a human experimental pain model, and that Diclometh would be safe to administer. Thus, the aims were: 1) To compare two doses of Diclometh versus placebo; 2) To assess the safety profile of Diclometh...
March 2, 2018: Basic & Clinical Pharmacology & Toxicology
Tuan-Mao Guo, Yong Yan, Wei-Ning Cao, Qiang Liu, Hai-Yun Zhu, Lan Yang, Mai-Cang Gao, Yan-Li Xing
Ankylosing spondylitis (AS) is a common chronic rheumatic disorder, accompanied by the differential expression of various microRNAs (miRNAs) in patients suffering from the condition, some of which have the potential to serve as novel complementary AS biomarkers. During this study, AS patients were recruited in connection with our investigation into the correlation of microRNA-132 (miR-132) in peripheral blood and its target gene NAG-1 expressions in relation with the clinical efficacy of non-steroidal anti-inflammatory drugs (NSAIDs) treatment in patients with AS...
March 1, 2018: Clinical Rheumatology
Shujie Tang, Zhuomao Mo, Renwen Zhang
OBJECTIVE: To evaluate evidence for the effectiveness of acupuncture in the treatment of lumbar disc herniation (LDH). METHODS: Electronic databases were searched to identify randomised controlled trials (RCTs) of acupuncture for LDH. A meta-analysis was conducted using RevMan 5.3 and the evidence level was assessed using GRADE methodology. RESULTS: Thirty RCTs involving 3503 participants were included in the study. Meta-analysis showed that acupuncture had a higher total effective rate than lumbar traction (RR=1...
March 1, 2018: Acupuncture in Medicine: Journal of the British Medical Acupuncture Society
Chawki Jebali, Lotfi Boukadida, Wael Chabaane, Achref Haj Ali, Ali Ousgi, Riadh Boukef
INTRODUCTION: Adult renal colic is a frequent lombo-abdominal painful syndrome in emergencies. Treatment is based on nonsteroidal anti-inflammatory drug (NSAID) but the choice between different NSAIDs remains a subject of controversy. Our aim was to compare the efficacy and the safety of two intramuscularly NSAIDs in renal colic. METHODS: We conducted a 32-week, randomized, double-blind, single-center study . Patients who had renal colic with a visual analogue scale (VAS) ≥ 5 were randomly assigned to receive, by intramuscularly injection, 100 mg of Ketoprofen (GK) or 75 mg of diclofenac (GD)...
April 2017: La Tunisie Médicale
Jacques E Chelly, Peter G Lacouture, Christian Russel D Reyes
BACKGROUND: Hydroxypropyl-β-cyclodextrin-diclofenac (HPβCD-diclofenac) is an NSAID used to treat acute moderate-to-severe postoperative pain. This post hoc analysis investigated the safety of HPβCD-diclofenac in patients aged ≥ 65 years. METHODS: Data from three phase III trials of HPβCD-diclofenac in adult patients with acute moderate-to-severe postoperative pain were pooled (NCT00448110, NCT00507026, and NCT00726388). Patients who received one or more dose of HPβCD-diclofenac or placebo were included and stratified according to age: < 65, 65-74, or ≥ 75 years...
March 1, 2018: Drugs & Aging
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