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https://www.readbyqxmd.com/read/29665554/inhibition-by-non-steroidal-anti-inflammatory-drugs-of-compound-action-potentials-in-frog-sciatic-nerve-fibers
#1
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
https://www.readbyqxmd.com/read/29625213/mechanistic-insights-of-the-controlled-release-properties-of-amide-adhesive-and-hydroxyl-adhesive
#2
Zheng Luo, Xiaocao Wan, Chao Liu, Liang Fang
Although interactions between drugs and acrylate pressure sensitive adhesives (PSAs) containing amide groups were reported in the previous studies, detailed studies elucidating their mechanism of action are still lacking. In the present study, an amide PSA (AACONH2 ) and a hydroxyl PSA (AAOH, as the control) were synthesized, and their molecular mechanism of controlled drug release was described. Using zolmitriptan (ZOL) and etodolac (ETO) as model drugs, in vitro drug release and skin permeation experiments were performed...
April 3, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29575045/synthesis-anticancer-activity-and-molecular-modeling-of-etodolac-thioether-derivatives-as-potent-methionine-aminopeptidase-type-ii-inhibitors
#3
Işıl Çoruh, Özge Çevik, Kemal Yelekçi, Teodora Djikic, Ş Güniz Küçükgüzel
A series of (R,S)-1-{[5-(substituted)sulfanyl-4-substituted-4H-1,2,4-triazole-3-yl]methyl}-1,8-diethyl-1,3,4,9-tetrahydropyrano[3,4-b]indoles (5a-v) were designed and synthesized using a five-step synthetic protocol that involves substituted benzyl chlorides and (R,S)-5-[(1,8-diethyl-1,3,4,9-tetrahydropyrano[3,4-b]indole-1-yl)methyl]-4-substituted-2,4-dihydro-3H-1,2,4-triazole-3-thiones in the final step. The synthesized derivatives were evaluated for cytotoxicity and anticancer activity in vitro using the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) colorimetric method against VERO, HEPG2 (human hepatocellular liver carcinoma), SKOV3 (ovarian carcinoma), MCF7 (human breast adenocarcinoma), PC3 and DU145 (prostate carcinoma) cells at 10-5  M (10 μM) for 24 h...
March 25, 2018: Archiv der Pharmazie
https://www.readbyqxmd.com/read/29545755/exploration-of-the-anti-inflammatory-drug-space-through-network-pharmacology-applications-for-drug-repurposing
#4
Guillermo de Anda-Jáuregui, Kai Guo, Brett A McGregor, Junguk Hur
The quintessential biological response to disease is inflammation. It is a driver and an important element in a wide range of pathological states. Pharmacological management of inflammation is therefore central in the clinical setting. Anti-inflammatory drugs modulate specific molecules involved in the inflammatory response; these drugs are traditionally classified as steroidal and non-steroidal drugs. However, the effects of these drugs are rarely limited to their canonical targets, affecting other molecules and altering biological functions with system-wide effects that can lead to the emergence of secondary therapeutic applications or adverse drug reactions (ADRs)...
2018: Frontiers in Physiology
https://www.readbyqxmd.com/read/29521135/determination-of-low-intrinsic-clearance-in-vitro-the-benefit-of-a-novel-internal-standard-in-human-hepatocyte-incubations
#5
Ugo Zanelli, Thomas Michna, Carl Petersson
1. A novel method utilizing an internal standard in hepatocytes incubations has been developed and demonstrated to decrease the variability in the determination of intrinsic clearance (CLint ) in this system. The reduced variability was shown to allow differentiation of lower elimination rate constants from noise. 2. The suggested method was able to compensate for a small but systematic error (0.5 µL/min/106 cells) caused by an evaporation of approximately 15% of the volume during the incubation time. 3. The approach was validated using six commercial drugs (ketoprofen, tolbutamide, phenacetin, etodolac and quinidine) which were metabolized by different pathways...
March 26, 2018: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29515279/comparison-of-clinical-effectiveness-and-safety-of-newer-nonsteroidal-anti-inflammatory-drugs-in-patients-of-osteoarthritis-of-knee-joint-a-randomized-prospective-open-label-parallel-group-study
#6
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
https://www.readbyqxmd.com/read/29428653/performance-and-microbial-shift-during-acidification-of-a-real-pharmaceutical-wastewater-by-using-an-anaerobic-sequencing-batch-reactor-ansbr
#7
Ilda Vergili, Ugur Golebatmaz, Yasemin Kaya, Z Beril Gönder, Halil Hasar, Gulsum Yilmaz
In this study, a lab-scale anaerobic sequencing batch reactor (AnSBR) was used for the acidification of a pharmaceutical wastewater sourced from etodolac chemical synthesis tanks. The effects of the organic loading rate (OLR), and etodolac and sulfate concentrations on the acidification rate and microbial community in AnSBR were investigated at 35 °C with a hydraulic retention time (HRT) of 37 h, a pH of 5, and OLRs up to 5.2 kgCOD/m3 ·day. The AnSBR accomplished a 60% acidification ratio and 50-60% etodolac removal at OLRs up to 2...
April 15, 2018: Journal of Environmental Management
https://www.readbyqxmd.com/read/29412363/preemptive-use-of-etodolac-on-tooth-sensitivity-after-in-office-bleaching-a-randomized-clinical-trial
#8
RANDOMIZED CONTROLLED TRIAL
Savil Costa Vaez, André Luís Faria-E-Silva, Alessandro Dourado Loguércio, Micaelle Tenório Guedes Fernandes, Flávia Pardo Salata Nahsan
This study determined the effectiveness of the preemptive administration of etodolac on risk and intensity of tooth sensitivity and the bleaching effect caused by in-office bleaching using 35% hydrogen peroxide. Fifty patients were selected for this tripleblind, randomized, crossover, and placebo-controlled clinical trial. Etodolac (400 mg) or placebo was administrated in a single-dose 1 hour prior to the bleaching procedure. The whitening treatment with 35% hydrogen peroxide was carried out in two sessions with a 7-day interval...
February 1, 2018: Journal of Applied Oral Science: Revista FOB
https://www.readbyqxmd.com/read/29327523/association-of-physicians-of-india-position-statement-on-role-of-chirally-pure-molecules-in-clinical-practice
#9
Milind Y Nadkar, Mangesh Tiwaskar, Sanjay Kalra, Siddharth N Shah, B R Bansode, Anjanlal Dutta, Sarita Bajaj, Sameer Aggarwal, Yatan Pal Singh Balhara, A K Das, Puneet Dhamija, Y K Gupta, Jubbin Jacob, Sundeep Mishra, S N Narasingan, C K Ponde, Ram Prabhoo, Balakrishnan S, Manisha Sahay, R K Sahay, I Sathyamurthy, Shilpa Tiwaskar, Agam Vora
Chirally pure molecules or enantiomers are non-superimposable mirror images of each other with a chiral center (such as carbon, sulphur, nitrogen or phosphorous atom). An equimolar mixture of enantiomers forms a racemate. Chirally pure molecules (single enantiomers) are important in the field of drug discovery as the drug targets such as enzymes and receptors are enantioselective in nature. Clinical studies have demonstrated that chirally pure drugs exhibit different pharmacokinetic and metabolic profiles, reduced adverse events, improved safety profiles and similar therapeutic activity at lowered drug dosage as compared with the racemate in many therapeutic areas...
December 2017: Journal of the Association of Physicians of India
https://www.readbyqxmd.com/read/29215465/expression-of-tissue-inhibitor-of-metalloproteinases-and-matrix-metalloproteinases-in-the-ischemic-brain-of-photothrombosis-model-mice
#10
Junsuke Hirono, Haruka Sanaki, Kana Kitada, Haruka Sada, Atsushi Suzuki, Laurensius K Lie, Eri Segi-Nishida, Kimie Nakagawa, Hiroshi Hasegawa
Middle cerebral artery occlusion (MCAO) is the most widely used animal model of ischemic stroke. This model well recapitulates the pathological features of most human cases; however, MCAO is technically difficult to achieve in mice and has some disadvantages for investigating the molecular mechanisms of pathological progression in stroke. The recently developed photothrombosis model may be more suitable for research on the molecular mechanisms of ischemic stroke in mice. Yet, similarities and differences between the photothrombosis and MCAO models are not well characterized...
February 7, 2018: Neuroreport
https://www.readbyqxmd.com/read/29187701/association-between-concomitant-use-of-acyclovir-or-valacyclovir-with-nsaids-and-an-increased-risk-of-acute-kidney-injury-data-mining-of-fda-adverse-event-reporting-system
#11
Zhihua Yue, Jinhai Shi, Haona Li, Huiyi Li
Nonsteroidal anti-inflammatory drugs (NSAIDs) are likely to be used concomitantly with acyclovir or valacyclovir in clinical practice, but the study on the safety of such combinations was seldom reported. The objective of the study was to investigate reports of acute kidney injury (AKI) events associated with the concomitant use of oral acyclovir or valacyclovir with an NSAID by using the United States Food and Drug Administration (FDA) Adverse Event Reporting System (AERS) database between January 2004 and June 2012...
February 1, 2018: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28917009/preparation-characterization-and-in-vitro-in-vivo-evaluation-of-oral-time-controlled-release-etodolac-pellets
#12
Xiaoyu Zhang, Qi Li, Mingzhu Ye, Zhinan Zhao, Jiayi Sun, Xinggang Yang, Weisan Pan
The objective of this study was to prepare time-controlled release etodolac pellets to facilitate drug administration according to the body's biological rhythm, optimize the drug's desired effects, and minimize adverse effects. The preparation consisted of three laminal layers from center to outside: the core, the swelling layer, and the insoluble polymer membrane. Factors influenced the core and the coating films were investigated in this study. The core pellets formulated with etodolac, lactose, and sodium carboxymethyl starch (CMS-Na) were prepared by extrusion-spheronization and then coated by a fluidized bed coater...
February 2018: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28875479/development-of-an-enantioselective-and-biomarker-informed-translational-population-pharmacokinetic-pharmacodynamic-model-for-etodolac
#13
Carolina de Miranda Silva, Adriana Rocha, Eduardo Tozatto, Lucienir Maria da Silva, Eduardo Antônio Donadi, Teresa Dalla Costa, Vera Lucia Lanchote, Stephan Schmidt, Jürgen B Bulitta
Cyclooxygenase-2 (COX-2) isoform has a critical role in the development of pain. Inhibition of COX-2 in vitro serves as a biomarker for nonsteroidal anti-inflammatory drugs (NSAIDs). The NSAID concentrations yielding 80% COX-2 inhibition (IC80) correlate with therapeutic doses to achieve analgesia across multiple COX-2 inhibitors. However, there are no time-course models relating COX-2 inhibition with decreased pain. This study aimed to characterize the relationship between NSAID concentrations, in vitro COX-2 inhibition, and acute pain decrease in humans over time by a translational approach using clinical pharmacokinetic and literature reported in vitro and clinical pharmacodynamic data...
November 2017: AAPS Journal
https://www.readbyqxmd.com/read/28809737/acute-liver-failure-due-to-etodolac-a-selective-cycloxygenase-2-cox-2-inhibitor-non-steroidal-anti-inflammatory-drug-established-by-rucam-based-causality-assessment
#14
Sunil Taneja, Pramod Kumar, Sahaj Rathi, Ajay Duseja, Virendra Singh, Radha Krishan Dhiman, Yogesh Kumar Chawla
Drug induced liver injury is a common cause of acute liver failure (ALF). While most of these cases are due to dose dependent hepatotoxicity with acetaminophen, idiosyncratic drug-induced liver injury (DILI) is responsible for about 15% cases of ALF. Antibiotics are the most common cause of idiosyncratic DILI as well as DILI induced ALF. Etodolac is a selective cycloxygenase- 2 (COX -2) inhibitor non-steroidal anti-inflammatory drug used as an analgesic and anti-inflammatory in musculoskeletal diseases. Severe liver impairment is extremely rare...
September 2017: Annals of Hepatology
https://www.readbyqxmd.com/read/28641674/removal-of-organic-matter-and-etodolac-from-pharmaceutical-industry-wastewater-by-pac-adsorption
#15
Ilda Vergili, Sezin Gencdal
  The removal of organic matter and etodolac (an anti-inflammatory pharmaceutical) from a real process wastewater by using powdered activated carbon (PAC) adsorption before and after Fenton oxidation has been studied. The wastewater sample is collected from the final stage of chemical synthesis of a pharmaceutical (etodolac). Fenton oxidation resulted with decrease in chemical oxygen demand (84% removal) and etodolac concentration was reduced to 0.7 mg L-1. Optimum adsorption equilibrium conditions were found as t = 16 hours, and m = 10 g L-1...
July 1, 2017: Water Environment Research: a Research Publication of the Water Environment Federation
https://www.readbyqxmd.com/read/28630833/anti-inflammatory-prophylaxis-prevents-heterotopic-ossification-in-contralateral-side-hip-arthroscopy-a-case-report
#16
Yaniv Warschawski, Zachary T Sharfman, Eyal Amar, Ehud Rath
INTRODUCTION: Heterotopic ossification (HO) after hip surgery is the formation of bone in non-skeletal tissue, usually between the muscle and the joint capsule. HO after hip surgery may be associated with clinical sequelae such as pain, impingement and decreased range of motion, compromising surgical outcomes. CASE REPORT: A 20-year-old basketball player presented with a 2-year duration of the left groin pain after a basketball-related injury. Due to continued disability and failure of conservative management the patient underwent hip arthroscopy...
January 2017: Journal of Orthopaedic Case Reports
https://www.readbyqxmd.com/read/28622543/quantitative-analysis-of-anti-inflammatory-drugs-using-ftir-atr-spectrometry
#17
Sonia T Hassib, Ghaneya S Hassan, Asmaa A El-Zaher, Marwa A Fouad, Enas A Taha
Four simple, accurate, sensitive and economic Attenuated Total Reflectance-Fourier Transform Infrared Spectroscopic (ATR-FTIR) methods have been developed for the quantitative estimation of some non-steroidal anti-inflammatory drugs. The first method involves the determination of Etodolac by direct measurement of the absorbance at 1716cm-1 . In the second method, the second derivative of the IR spectra of Tolfenamic acid and its reported degradation product (2-chlorobenzoic acid) was used and the amplitudes were measured at 1084...
November 5, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/28608452/chiral-separation-and-modeling-of-baclofen-bupropion-and-etodolac-profens-on-amylose-reversed-phase-chiral-column
#18
Imran Ali, Mohd Suhail, Zeid A Alothman, Abdulrahman Alwarthan
Chiral resolution of baclofen, bupropion, and etodolac profens was obtained with amylose derivatized chiral reversed stationary phase (carbamate groups). The eluent used for bupropion and etodolac was MeOH-water (20:80, v/v) and for baclofen was water-methanol (95:5, v/v). The eluent run rates, finding wavelength and temperature, were 1.0 mL/min, 220 nm and 27 ± 1 °C for all the eluents. The magnitude of the retardation factors for S- and R-enantiomers of baclofen, bupropion, and etodolac were 1.37, 2...
July 2017: Chirality
https://www.readbyqxmd.com/read/28535740/etodolac-transdermal-cubosomes-for-the-treatment-of-rheumatoid-arthritis-ex-vivo-permeation-and-in-vivo-pharmacokinetic-studies
#19
Salwa Salah, Azza A Mahmoud, Amany O Kamel
In this study, transdermal etodolac-loaded cubosomes were developed in order to relieve patient pain and joints stiffness by providing stable etodolac concentration at the targeting sites through controlled drug delivery via the noninvasive skin route with more sustaining and less frequent dosing. Different ratios and percentages of poloxamer 407 and monoolein were used to formulate the cubosomes using emulsification and homogenization processes. The etodolac-loaded cubosomes showed particle size values ranging from 135...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28490464/perioperative-cox-2-and-%C3%AE-adrenergic-blockade-improves-metastatic-biomarkers-in-breast-cancer-patients-in-a-phase-ii-randomized-trial
#20
Lee Shaashua, Maytal Shabat-Simon, Rita Haldar, Pini Matzner, Oded Zmora, Moshe Shabtai, Eran Sharon, Tanir Allweis, Iris Barshack, Lucile Hayman, Jesusa Arevalo, Jeffrey Ma, Maya Horowitz, Steven Cole, Shamgar Ben-Eliyahu
Purpose: Translational studies suggest that excess perioperative release of catecholamines and prostaglandins may facilitate metastasis and reduce disease-free survival. This trial tested the combined perioperative blockade of these pathways in breast cancer patients.Experimental Design: In a randomized placebo-controlled biomarker trial, 38 early-stage breast cancer patients received 11 days of perioperative treatment with a β-adrenergic antagonist (propranolol) and a COX-2 inhibitor (etodolac), beginning 5 days before surgery...
August 15, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
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