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Mefenamic acid

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https://www.readbyqxmd.com/read/29281794/reduction-and-scavenging-of-chemically-reactive-drug-metabolites-by-nad-p-h-quinone-oxidoreductase-1-and-nrh-quinone-oxidoreductase-2-and-variability-in-hepatic-concentrations
#1
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
https://www.readbyqxmd.com/read/29259828/formulation-characterization-and-in-vitro-evaluation-of-transdermal-patches-for-inhibiting-crystallization-of-mefenamic-acid
#2
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
https://www.readbyqxmd.com/read/29241956/magnetic-sporopollenin-cyanopropyltriethoxysilane-dispersive-micro-solid-phase-extraction-coupled-with-high-performance-liquid-chromatography-for-the-determination-of-selected-non-steroidal-anti-inflammatory-drugs-in-water-samples
#3
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...
November 26, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/29202439/assessment-of-mefenamic-acid-polymorphs-in-commercial-tablets-using-chemometric-coupled-to-mir-and-nir-spectroscopies-prediction-of-dissolution-performance
#4
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)...
November 28, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29164523/identification-of-uridine-5-diphosphate-glucuronosyltransferases-responsible-for-the-glucuronidation-of-mirabegron-a-potent-and-selective-%C3%AE-3-adrenoceptor-agonist-in-human-liver-microsomes
#5
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
https://www.readbyqxmd.com/read/29150808/monitoring-enzymatic-degradation-of-emerging-contaminants-using-a-chip-based-robotic-nano-esi-ms-tool
#6
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
https://www.readbyqxmd.com/read/29149996/coupling-of-two-centrifugeless-ultrasound-assisted-dispersive-solid-liquid-phase-microextractions-as-a-highly-selective-clean-and-efficient-method-for-determination-of-ultra-trace-amounts-of-non-steroidal-anti-inflammatory-drugs-in-complicated-matrices
#7
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
https://www.readbyqxmd.com/read/29138287/clopidogrel-carboxylic-acid-glucuronidation-is-mediated-mainly-by-ugt2b7-ugt2b4-and-ugt2b17-implications-for-pharmacogenetics-and-drug-drug-interactions
#8
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
https://www.readbyqxmd.com/read/29127620/potential-of-the-strain-raoultella-sp-kdf8-for-removal-of-analgesics
#9
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
https://www.readbyqxmd.com/read/29107615/the-natural-bile-acid-surfactant-sodium-taurocholate-natc-as-a-coformer-in-coamorphous-systems-enhanced-physical-stability-and-dissolution-behavior-of-coamorphous-drug-natc-systems
#10
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...
October 28, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29095288/severe-enteropathy-with-villous-atrophy-in-prolonged-mefenamic-acid-users-a-currently-under-recognized-in-previously-well-recognized-complication-case-report-and-review-of-literature
#11
REVIEW
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)
https://www.readbyqxmd.com/read/29069966/seasonal-occurrence-removal-and-risk-assessment-of-10-pharmaceuticals-in-two-sewage-treatment-plants-of-guangdong-china
#12
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
https://www.readbyqxmd.com/read/29065839/anthranilic-acid-derivatives-novel-inhibitors-of-protein-glycation-and-the-associated-oxidative-stress-in-the-hepatocytes
#13
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
https://www.readbyqxmd.com/read/29038294/the-nsaid-allosteric-site-of-human-cytosolic-sulfotransferases
#14
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 Sates in 2014. NSAIDs allosterically inhibit cytosolic sulfotransferases (SULTs) with high specificity and therapeutically relevant affinities. The current 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...
October 16, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29034602/gender-and-arch-effects-on-the-use-of-non-opioid-analgesics-for-post-endodontic-pain-reduction
#15
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
https://www.readbyqxmd.com/read/28986197/studying-of-drug-solubility-in-water-and-alcohols-using-drug-ammonium-ionic-liquid-compounds
#16
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
https://www.readbyqxmd.com/read/28829237/comparative-ultrastructural-hepatic-alterations-induced-by-free-and-liposome-encapsulated-mefenamic-acid
#17
Qais Bashir Jarrar, Muhammad Nazrul Hakim, Manraj Singh Cheema, Zainul Amiruddin Zakaria
Mefenamic acid (MFA) is used as an anti-inflammatory, antinociceptive, and antipyretic agent for treatment of a wide range of pathological disorders. While the uncertainty of its safety and the poor oral bioavailability constitute the major limiting factors of its medical use, considerable efforts including liposomal encapsulation are needed to achieve maximum therapeutic advantages. The current work was conducted to investigate the ultrastructural alterations in the liver induced by free MFA and its liposomal preparation...
September 2017: Ultrastructural Pathology
https://www.readbyqxmd.com/read/28808332/magnetic-microsphere-based-portable-solid-phase-extraction-device-for-on-site-pre-concentration-of-organics-from-large-volume-water-samples
#18
Zhijian Yao, Qingqing Zhao, Yan Ma, Wei Wang, Qing Zhou, Aimin Li
In this research a new magnetic material called M88 was fully synthetized and characterized for the extraction of pharmaceutical and personal care products in water samples. In addition, a portable prototype of magnetic solidphase extraction (MSPE) device was developed for the onsite preconcentration. The MSPE coupling with high performance liquid chromatography-Diode array detector (HPLC-DAD) method was developed and validated for simultaneous analysis of 11 PPCPs (mefenamic acid, chloroamphenicol, ketoprofen, clofibric acid, indometacin, acetylsalicylic acid, bisphenol A, phenylphenol, gemfibrozil, triclosan, and ibuprofen) in environmental water samples...
August 14, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28759638/influence-of-the-microwave-technology-on-solid-dispersions-of-mefenamic-acid-and-flufenamic-acid
#19
Sultan Alshehri, Faiyaz Shakeel, Mohamed Ibrahim, Ehab Elzayat, Mohammad Altamimi, Gamal Shazly, Kazi Mohsin, Musaed Alkholief, Bader Alsulays, Abdullah Alshetaili, Abdulaziz Alshahrani, Bander Almalki, Fars Alanazi
The present studies were undertaken to develop solvent-free solid dispersions (SDs) for poorly soluble anti-inflammatory drugs mefenamic acid (MA) and flufenamic acid (FFA) in order to enhance their in vitro dissolution rate and in vivo anti-inflammatory effects. The SDs of MA and FFA were prepared using microwaves irradiation (MW) technique. Different carriers such as Pluronic F127® (PL), Eudragit EPO® (EPO), polyethylene glycol 4000 (PEG 4000) and Gelucire 50/13 (GLU) were used for the preparation of SDs...
2017: PloS One
https://www.readbyqxmd.com/read/28743296/case-report-of-hypnic-headache-a-rare-headache-disorder-with-nocturnal-symptoms
#20
Kanishka P Dissanayake, Damindi P Wanniarachchi, Udaya K Ranawaka
BACKGROUND: Headache is one of the commonest complaints reported to physicians worldwide. Yet, arriving at the proper diagnosis can be a challenge in many patients. Although most headaches belong to common categories of migraine and tension-type headache, which are diagnosed and managed relatively easily, several uncommon headache disorders can lead to delays in diagnosis. Certain medications are more efficacious than others in managing these headache disorders, hence establishing the correct diagnosis is of paramount importance...
July 25, 2017: BMC Research Notes
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