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Mefenamic acid

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
Yaa-Hui Dong, Chia-Hsuin Chang, Li-Chiu Wu, Jing-Shiang Hwang, Sengwee Toh
AIMS: Prior studies have suggested that non-steroidal anti-inflammatory drugs (NSAIDs) may be associated with higher cardiovascular risks. Few were active-comparison studies that directly assessed potential differential cardiovascular risk between NSAID classes or across individual NSAIDs. We compared the risk of major cardiovascular events between cyclooxygenase-2 enzyme (COX-2) selective NSAIDs and nonselective NSAIDs in patients with hypertension. METHODS: We conducted a cohort study of patients with hypertension who initiated COX-2 selective NSAIDs or nonselective NSAIDs in a population-based Taiwanese database...
February 22, 2018: British Journal of Clinical Pharmacology
Fatemeh Jahandar, Jinous Asgarpanah, Parvaneh Najafizadeh, Zahra Mousavi
Objectives: Pycnocycla bashagardiana is an endemic species found only in Iran. Due to the presence of myristicin as the major component of the fruit's oil we were prompted to assess the antinociceptive and anti-inflammatory properties of P. bashagardiana fruit's essential oil (PBFEO). Materials and Methods: The analgesic activities of PBFEO (100, 200, and 400 mg/kg, IP) were studied by hot-plate and formalin tests in mice. Control and standard groups received vehicle and morphine (5 mg/kg, IP), respectively...
February 2018: Iranian Journal of Basic Medical Sciences
Junwon Park, Naoyuki Yamashita, Hiroaki Tanaka
We investigated the effects of the addition of two coagulants-polyaluminium chloride (PACl) and chitosan-into the membrane bioreactor (MBR) process on membrane fouling and the removal of pharmaceuticals and personal care products (PPCPs). Their addition at optimized dosages improved the permeability of the membrane by reducing the concentration of soluble microbial products in mixed liquor, the content of inorganic elements, and irreversible fouling of the membrane surface. During long-term operation, the addition of PACl increased removal efficiencies of tetracycline, mefenamic acid, atenolol, furosemide, ketoprofen, and diclofenac by 17-23%...
January 17, 2018: Chemosphere
Shalenie P den Braver-Sewradj, Michiel W den Braver, Robin M Toorneman, Stephanie van Leeuwen, Yongjie Zhang, Stefan J Dekker, Nico P E Vermeulen, Jan N M Commandeur, J Chris Vos
Detoxicating enzymes NAD(P)H:quinone oxidoreductase 1 (NQO1) and NRH:quinone oxidoreductase 2 (NQO2) catalyze the two-electron reduction of quinone-like compounds. The protective role of the polymorphic NQO1 and NQO2 enzymes is especially of interest in the liver as the major site of drug bioactivation to chemically reactive drug metabolites. In the current study, we quantified the concentrations of NQO1 and NQO2 in 20 human liver donors and NQO1 and NQO2 activities with quinone-like drug metabolites. Hepatic NQO1 concentrations ranged from 8 to 213 nM...
December 27, 2017: Chemical Research in Toxicology
Jirapornchai Suksaeree, Patsakorn Siripornpinyo, Somruethai Chaiprasit
The crystallization of mefenamic acid in transdermal patch is a major problem that makes the patch unstable and decreases the drug release. The additive was used to inhibit crystallization of a mefenamic acid. Among the different types of additives, polyvinylpyrrolidone (PVP) K30 and PVP K90 were studied and found to be highly effective in inhibiting the crystallization of the drug. The PVP presented as a solubilizer agent for mefenamic acid in matrix patches at the different ratio between drug : PVP, 1 : 2 and 1 : 2...
2017: Journal of Drug Delivery
Siti Munirah Abd Wahib, Wan Aini Wan Ibrahim, Mohd Marsin Sanagi, Muhammad Afzal Kamboh, Aemi S Abdul Keyon
A facile dispersive-micro-solid phase extraction (D-μ-SPE) method coupled with HPLC for the analysis of selected non-steroidal anti-inflammatory drugs (NSAIDs) in water samples was developed using a newly prepared magnetic sporopollenin-cyanopropyltriethoxysilane (MS-CNPrTEOS) sorbent. Sporopollenin homogenous microparticles of Lycopodium clavatum spores possessed accessible functional groups that facilitated surface modification. Simple modification was performed by functionalization with 3-cyanopropyltriethoxysilane (CNPrTEOS) and magnetite was introduced onto the biopolymer to simplify the extraction process...
January 12, 2018: Journal of Chromatography. A
Marina Antonio, Rubén M Maggio
Mefenamic Acid (MFA) is a widely-used non-steroidal anti-inflammatory drug. MFA presents four possible crystal forms; Form I and Form II being the only two pure crystals that have been isolated and fully characterized. Both Form I and Form II were prepared following the literature and completely characterized by middle (MIR) and near (NIR) infrared spectroscopy, digital optical microscopy, differential scanning calorimetry, melting point and dissolution properties. In order to develop quantitative models to assess Form I in formulated products, two sets of samples, training (n=10) and validation (n=8) sets, were prepared by mixing both polymorphs and the matrix of excipient (simulating commercial tablets)...
February 5, 2018: Journal of Pharmaceutical and Biomedical Analysis
Kentaro Konishi, Daisuke Tenmizu, Shin Takusagawa
BACKGROUND AND OBJECTIVES: Mirabegron is cleared by multiple mechanisms, including drug-metabolizing enzymes. One of the most important clearance pathways is direct glucuronidation. In humans, M11 (O-glucuronide), M13 (carbamoyl-glucuronide), and M14 (N-glucuronide) have been identified, of which M11 is one of the major metabolites in human plasma. The objective of this study was to identify the uridine 5'-diphosphate (UDP)-glucuronosyltransferase (UGT) isoform responsible for the direct glucuronidation of mirabegron using human liver microsomes (HLMs) and recombinant human UGTs (rhUGTs)...
November 21, 2017: European Journal of Drug Metabolism and Pharmacokinetics
Lara F Stadlmair, Thomas Letzel, Johanna Graßmann
Up to now, knowledge of enzymes capable of degrading various contaminants of emerging concern (CEC) is limited, which is especially due to the lack of rapid screening methods. Thus, a miniaturized high-throughput setup using a chip-based robotic nanoelectrospray ionization system coupled to mass spectrometry has been developed to rapidly screen enzymatic reactions with environmentally relevant CECs. Three laccases, two tyrosinases, and two peroxidases were studied for their ability to transform ten pharmaceuticals and benzotriazole...
November 17, 2017: Analytical and Bioanalytical Chemistry
Somayeh Arghavani-Beydokhti, Maryam Rajabi, Alireza Asghari
In this work, a new, simple, rapid, and environmentally friendly method with a high sample clean-up capability termed as centrifugeless ultrasound-assisted dispersive micro solid-phase extraction coupled with salting-out ultrasound-assisted liquid-liquid microextraction based on solidification of a floating organic droplet followed by high performance liquid chromatography is introduced for the first time. In this method, the three non-steroidal anti-inflammatory drugs diclofenac, ibuprofen, and mefenamic acid are first extracted based on an effective nanoadsorbent named as the layered double hydroxide-carbon nanotube nanohybrid...
January 2, 2018: Analytica Chimica Acta
Helina Kahma, Anne M Filppula, Mikko Neuvonen, E Katriina Tarkiainen, Aleksi Tornio, Mikko T Holmberg, Matti K Itkonen, Moshe Finel, Pertti J Neuvonen, Mikko Niemi, Janne T Backman
The antiplatelet drug clopidogrel is metabolized to an acyl-β-D-glucuronide, which causes time-dependent inactivation of CYP2C8. Our aim was to characterize the UDP-glucuronosyltransferase (UGT) enzymes that are responsible for the formation of clopidogrel acyl-β-D-glucuronide. Kinetic analyses and targeted inhibition experiments were performed using pooled human liver and intestine microsomes (HLM and HIM, respectively) and selected human recombinant UGTs based on preliminary screening. The effects of relevant UGT polymorphisms on the pharmacokinetics of clopidogrel were evaluated in 106 healthy volunteers...
November 14, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
Andrea Palyzová, Jiří Zahradník, Helena Marešová, Lucie Sokolová, Eva Kyslíková, Michal Grulich, Václav Štěpánek, Tomáš Řezanka, Pavel Kyslík
The bacterial strain KDF8 capable of growth in the presence of diclofenac and codeine analgesics was obtained after chemical mutagenesis of nature isolates from polluted soils. The strain KDF8 was identified as Raoultella sp. based on its morphology, biochemical properties, and 16S rRNA gene sequence. It was deposited in the Czech Collection of Microorganisms under the number CCM 8678. A growing culture efficiently removed diclofenac (92% removal) and partially also codeine (about 30% degradation) from culture supernatants within 72 h at 28 °C...
November 11, 2017: Folia Microbiologica
Katarzyna Gniado, Pól MacFhionnghaile, Patrick McArdle, Andrea Erxleben
The amorphization of 18 different drugs on milling with one mole equivalent sodium taurocholate (NaTC) was investigated. In all cases the X-ray powder pattern showed an amorphous halo after milling at room temperature or after cryomilling and 14 of the 18 coamorphous drug-NaTC systems were physically stable for between one to eleven months under ambient storage conditions. In three cases, namely carbamazepine-NaTC, indomethacin-NaTC and mefenamic acid-NaTC, significant dissolution advantages over the crystalline drugs were observed, both for the freshly prepared samples and after storage for seven months...
January 15, 2018: International Journal of Pharmaceutics
Uayporn Kaosombatwattana, Julajak Limsrivilai, Ananya Pongpaibul, Monthira Maneerattanaporn, Phunchai Charatcharoenwitthaya
RATIONALE: Mefenamic acid-induced enteropathy may be an under-recognized condition because few reported cases and no review of literature to comprehensively describe all reported cases exist. From inception until February 2017, a systematic literature search identified twenty original reports of cases of mefenamic acid-induced enteropathy. Additional five cases were identified at our hospital. All cases were included in the analyses. PATIENT CONCERNS: Most patients had been regularly taking therapeutic dosages of mefenamic acid for at least three months before symptoms developed...
November 2017: Medicine (Baltimore)
Ying Tang, Lu-Lu Guo, Cheng-Yang Hong, Yong-Xin Bing, Zhen-Cheng Xu
A long term investigation, which covered 10 sampling campaigns over three years, was performed to evaluate the occurrence, removal and risk of ten pharmaceuticals in two full-scale sewage treatment plants (STPs) in Guangdong, South China. Target pharmaceuticals except for clofibrate and ibuprofen were detected in every sample, with mean concentrations of 12.5-685.6 ng/L and 7.9-130.3 ng/L in the influent and effluent, respectively. Salicylic acid was the most abundant compound in both the influents and effluents in the two STPs...
October 25, 2017: Environmental Technology
Humera Jahan, Muhammad Iqbal Choudhary, Amber Atta, Khalid Mohammad Khan, Atta-Ur- Rahman
BACKGROUND: Anthranilic acid derivatives are important pharmacophores in drug discovery. Several of them are currently used drugs, such as mefenamic acid and meclofenamates, possess analgesic, anti-inflammatory, and antipyretic activities. Some anthranilic acid-based scaffolds have also been reported for the management of metabolic disorders. OBJECTIVES: The aim of the current study was to investigate the antiglycation potential of anilino benzoic acid derivatives against fructose- human serum albumin (HSA) glycation...
October 20, 2017: Medicinal Chemistry
Ting Wang, Ian Cook, Thomas S Leyh
Non-steroidal anti-inflammatory drugs (NSAIDs) are among the most commonly prescribed drugs worldwide-more than 111 million prescriptions were written in the United States in 2014. NSAIDs allosterically inhibit cytosolic sulfotransferases (SULTs) with high specificity and therapeutically relevant affinities. This study focuses on the interactions of SULT1A1 and mefenamic acid (MEF)-a potent, highly specific NSAID inhibitor of 1A1. Here, the first structure of an NSAID allosteric site-the MEF-binding site of SULT1A1-is determined using spin-label triangulation NMR...
December 8, 2017: Journal of Biological Chemistry
Wail M Elzaki, Hassan M Ziada, Neamat H Abubakr, Yahia E Ibrahim
This study aimed to evaluate the secondary outcomes of gender and arch and their impact on pain reduction following initial endodontic therapy. 185 medications, including placebo were prepared, and 170 participants completed the trial. Group 1, received a single dose of Paracetamol alone (G-1), Group 2 received combined Ibuprofen/Paracetamol (G-2). Group 3 received combined Mefenamic acid/Paracetamol (G-3), group 4 received combined Diclofenac K/Paracetamol (G-4) and Group 5 received a placebo (G-5). There were no statistically significant differences in pain reduction between males and females whilst there were statistically significant differences between them and the placebo group...
October 16, 2017: Australian Endodontic Journal: the Journal of the Australian Society of Endodontology Inc
Mohammad Halayqa, Aneta Pobudkowska, Urszula Domańska, Maciej Zawadzki
Synthesis of three mefenamic acid (MEF) derivatives - ionic liquid compounds composed of MEF in an anionic form and ammonium cation (choline, MEF1), or {di(2-hydroxyethyl)dimethyl ammonium (MEF2)}, or {tri(2-hydroxyethyl)methyl ammonium compound (MEF3)} is presented. The basic thermal properties of pure compounds i.e. fusion temperatures, and the enthalpy of fusion of these compounds have been measured with differential scanning microcalorimetry technique (DSC). Molar volumes have been calculated with the Barton group contribution method...
October 3, 2017: European Journal of Pharmaceutical Sciences
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