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Etodolac

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https://www.readbyqxmd.com/read/29327523/association-of-physicians-of-india-position-statement-on-role-of-chirally-pure-molecules-in-clinical-practice
#1
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
#2
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...
December 5, 2017: 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
#3
Zhihua Yue, Jinhai Shi, Haona Li, Huiyi Li
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. The frequency of AKI events in patients while simultaneously taking either acyclovir or valacyclovir and an NSAID was compared using the Chi-square test...
November 28, 2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28917009/preparation-characterization-and-in-vitro%C3%A2-%C3%A2-in-vivo-evaluation-of-oral-time-controlled-release-etodolac-pellets
#4
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...
September 15, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28875479/development-of-an-enantioselective-and-biomarker-informed-translational-population-pharmacokinetic-pharmacodynamic-model-for-etodolac
#5
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
#6
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
#7
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
#8
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
#9
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...
June 13, 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
#10
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
#11
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
#12
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
https://www.readbyqxmd.com/read/28474580/etodolac-and-the-risk-of-acute-pancreatitis
#13
Kuan-Fu Liao, Kao-Chi Cheng, Cheng-Li Lin, Shih-Wei Lai
OBJECTIVE: The aim of this study was to explore the association between etodolac use and acute in Taiwan. DESIGN: We designed a case-control study using the database of Taiwan's National Health Insurance. SUBJECTS: In all, 7577 subjects aged 20 years or older with newly diagnosed acute pancreatitis were defined as cases, and 27032 sex-matched and age-matched subjects without acute pancreatitis were defined as controls. The period considered for this study was from 1998 to 2011...
March 2017: BioMedicine
https://www.readbyqxmd.com/read/28388726/the-role-of-epithelial-to-mesenchymal-transition-in-human-amniotic-membrane-rupture
#14
Carla Janzen, Suvajit Sen, Margarida Y Y Lei, Marina Gagliardi de Assumpcao, John Challis, Gautam Chaudhuri
Context: Biochemical weakening of the amnion is a major factor preceding preterm premature rupture of membranes (PPROMs), leading to preterm birth. Activation of matrix metalloproteinases (MMPs) is known to play a key role in collagen degradation of the amnion; however, epithelial to mesenchymal transition (EMT) that is also induced by MMP activation has not been investigated as a mechanism for amnion weakening. Objective: To measure amniotic EMT associated with vaginal delivery (VD) compared with unlabored cesarean sections (CSs), and to assess changes in amniotic mechanical strength with pharmacologic inhibitors and inducers of EMT, thus testing the hypothesis that EMT is a key biochemical event that promotes amniotic rupture...
April 1, 2017: Journal of Clinical Endocrinology and Metabolism
https://www.readbyqxmd.com/read/28366649/fast-dissolving-drug-drug-eutectics-with-improved-compressibility-and-synergistic-effects
#15
Rajesh Thipparaboina, Dinesh Thumuri, Rahul Chavan, V G M Naidu, Nalini R Shastri
Combinational therapy has become increasingly popular in recent times due to various advantages like greater therapeutic effect, reduced number of prescriptions, lower administrative costs, and an increase in patient compliance. Drug-drug multicomponent adducts could help in combination of drugs at supramolecular level. Two drug-drug eutectics of etodolac with paracetamol (EP) and etodolac with propranolol hydrochloride (EPHC) were successfully designed and synthesized for the first time. These eutectics significantly improved dissolution and material properties...
June 15, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28353025/coxibs-refocus-attention-on-the-cardiovascular-risks-of-non-aspirin-nsaids
#16
Dixon Thomas, Zoya Ali, Seeba Zachariah, Kishore Gnana Sam Sundararaj, Matthew Van Cuyk, Jason C Cooper
Non-steroidal anti-inflammatory drugs (NSAIDs) were differentiated from steroidal anti-inflammatory medicines to help clinicians who needed to use anti-inflammatory agents that were safer than steroids. With market entry of rofecoxib in 1999, NSAIDs were then further classified into traditional NSAIDs and cyclooxygenase (COX)-2 inhibitors (coxibs), the latter posing potentially fewer gastrointestinal risks. In 2005, rofecoxib was withdrawn from the market because of concerns about the risk of heart attack and stroke with long-term use, and clinical practice began focusing more on the cardiovascular versus gastrointestinal safety of coxibs...
October 2017: American Journal of Cardiovascular Drugs: Drugs, Devices, and Other Interventions
https://www.readbyqxmd.com/read/28248111/inclusion-complexation-of-etodolac-with-hydroxypropyl-beta-cyclodextrin-and-auxiliary-agents-formulation-characterization-and-molecular-modeling-studies
#17
Atul P Sherje, Vaidehi Kulkarni, Manikanta Murahari, Usha Y Nayak, Pritesh Bhat, Vasanti Suvarna, Bhushan Dravyakar
The present investigation was aimed to prepare inclusion complexes of a therapeutically important nonsteroidal anti-inflammatory drug, etodolac (ETD) with hydroxypropyl-beta-cyclodextrin (HP-β-CD) and to study the effect of l-arginine (l-Arg) as an auxiliary agent on the complexation efficiency of HP-β-CD to improve aqueous solubility and the dissolution property of ETD. The binary and ternary complexes were prepared by physical mixing, coevaporation, and spray drying methods. The complexes were characterized using differential scanning colorimetry (DSC), Fourier transform-infrared spectroscopy (FT-IR), and powder X-ray diffraction (PXRD) studies...
April 3, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28154306/taste-masking-effect-of-chlorogenic-acid-cga-on-bitter-drugs-evaluated-by-taste-sensor-and-surface-plasmon-resonance-on-the-basis-of-cga-drug-interactions
#18
Sayuko Shiraishi, Tamami Haraguchi, Saki Nakamura, Dahong Li, Honami Kojima, Miyako Yoshida, Takahiro Uchida
The purpose of this study was to evaluate the taste-masking effects of chlorogenic acid (CGA) on bitter drugs using taste sensor measurements and surface plasmon resonance (SPR) analysis of CGA-drug interactions. Six different bitter drugs were used: amlodipine besylate (AMD), diphenhydramine hydrochloride (DPH), donepezil hydrochloride (DNP), rebamipide (RBM), diclofenac sodium (DCF) and etodolac (ETD). Taste sensor outputs were significantly inhibited by the addition of CGA to all drugs. The inhibition ratio of the taste sensor output decreased in the following order DPH>DNP>AMD≈DCF≈RBM≈ETD...
2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28093968/quantification-of-etodolac-in-human-plasma-for-pharmacokinetics-and-bioequivalence-studies-in-27-korean-subjects
#19
Il-Dong Song, Je-Seop Kang, Hyun-Jin Kim, Se-Mi Kim, Dong-Xu Zhao, Shin-Hee Kim, Min-Young Chun, Kyuhyun Lee
We developed a simple and validated liquid chromatography tandem mass spectrometry(LC-MS/MS) for quantification of etodolac using pioglitazone as an internal standard (IS) to assess pharmacokinetics and to appraise bioequivalence of two formulations of etodolac (reference and tested) in 27 healthy Korean subjects. Isocratic mobile phase consisted of 10 mM ammonium formate and acetonitrile were used to separate the analytes on a Gemini C18 column. Also, analytes were analyzed by MS/MS in multiple reaction monitoring (MRM) mode using the transitions of (M+H)+ ions, m/z 288...
January 16, 2017: Drug Metabolism Letters
https://www.readbyqxmd.com/read/27992249/the-role-of-epithelial-to-mesenchymal-transition-in-human-amniotic-membrane-rupture
#20
Carla Janzen, Suvajit Sen, Margarida Y Y Lei, Marina Gagliardi de Assumpcao, John Challis, Gautam Chaudhuri
CONTEXT: Biochemical weakening of the amnion is a major factor preceding preterm premature rupture of membranes (PPROM), leading to preterm birth. Activation of matrix metalloproteinases (MMPs) is known to play a key role in collagen degradation of the amnion, yet epithelial to mesenchymal transition (EMT) that is also induced by MMP activation, has not been investigated as a mechanism for amnion weakening. OBJECTIVE: To measure amniotic EMT associated with vaginal delivery (VD) as compared to non-labored cesarean sections (CS), and assess changes in amniotic mechanical strength with pharmacologic inhibitors and inducers of EMT, thus testing the hypothesis that EMT is a key biochemical event that promotes amniotic rupture...
December 19, 2016: Journal of Clinical Endocrinology and Metabolism
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