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https://www.readbyqxmd.com/read/28231454/zinc-complexes-of-diflunisal-synthesis-characterization-structure-antioxidant-activity-and-in-vitro-and-in-silico-study-of-the-interaction-with-dna-and-albumins
#1
Alketa Tarushi, Chrisoula Kakoulidou, Catherine P Raptopoulou, Vassilis Psycharis, Dimitris P Kessissoglou, Ioanna Zoi, Athanasios N Papadopoulos, George Psomas
From the reaction of ZnCl2 with the non-steroidal anti-inflammatory drug diflunisal (Hdifl), complex [Zn(difl-O)2(MeOH)4], 1 was formed, while in the presence of a N,N'-donor heterocyclic ligand 2,2'-bipyridylamine (bipyam), 2,2'-bipyridine (bipy), 1,10-phenanthroline (phen) and 2,2'-dipyridylketone oxime (Hpko), the complexes [Zn(difl-O,O')2(bipyam)], 2, [Zn(difl-O,O')2(bipy)], 3, [Zn(difl-O,O')2(phen)], 4 and [Zn(difl-O)2(Hpko)2], 5 were isolated, respectively. The complexes were characterized by physicochemical and spectroscopic techniques and the crystal structures of complexes 2, 3 and 5 were determined by X-ray crystallography...
February 12, 2017: Journal of Inorganic Biochemistry
https://www.readbyqxmd.com/read/28230613/osteoid-osteoma-of-the-acetabulum-diagnosis-and-medical-treatment
#2
Nikolaos A Laliotis, Antonia S Bindoudi, Ioannis A Tsitouridis, Iordanis G Petrakis, John M Kirkos
We describe the medical management of an acetabular osteoid osteoma in an 11-year-old girl. There was a 2-year delay until proper diagnosis of the patient's pathology was made. Accurate localization of the nidus in the subchondral bone, involving the cartilage, is difficult on the basis of plain radiographs. All imaging methods, including computed tomography, MRI, and bone scintigraphy, were used to confirm the diagnosis. We proposed medical treatment to avoid possible severe complications from surgical intervention...
February 22, 2017: Journal of Pediatric Orthopedics. Part B
https://www.readbyqxmd.com/read/28228088/aryl-heteroaryl-substituted-celecoxib-derivatives-as-cox-2-inhibitors-synthesis-anti-inflammatory-activity-and-molecular-docking-studies
#3
Golla Madhava, Katla Venkata Ramana, Saddala Madhu Sudhana, Devineni Subba Rao, Kuntrapakam Hema Kumar, Valluru Lokanatha, Asupatri Usha Rani, Chamarthi Naga Raju
BACKGROUND: Cyclooxygenase (COX-2) inhibitors have been developed to provide better anti-inflammatory and analgesic efficacy than those of traditional NSAIDs. Several compounds having selective COX-2 inhibitors such as SC-558, Celecoxib, Rofecoxib, Valdecoxib and Etoricoxib are marketed as new generation NSAIDs and block the production of prostaglandins (PGs) in inflammatory cells. New anti-inflammatory dynamic agents with improved potency and safety profile are still needed. OBJECTIVE: As a part of our continuation research work towards the synthesis of anti-inflammatory agents, the synthesis of N-substituted aryl/heteroaryl-pyrazole-1yl benzene sulfonamide (Celecoxib) derivatives, and evaluated their anti-inflammatory activity in both methods in vitro and in vivo, and molecular docking study on COX-2 enzyme will be discussed in this study...
February 20, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28228068/stress-in-gastrointestinal-tract-and-stable-gastric-pentadecapeptide-bpc-157-finally-do-we-have-a-solution
#4
Predrag Sikiric, Sven Seiwerth, Rudolf Rucman, Domagoj Drmic, Mirjana Stupnisek, Antonio Kokot, Marko Sever, Ivan Zoricic, Zoran Zoricic, Lovorka Batelja, Tihomil Ziger, Josipa Vlainic, Zarko Rasic, Martina Lovric Bencic
Selye's syndrome produced by diverse nocuous agents and "response to damage as such" means Selye's stress triad in stress coping response to reestablish homeostasis. Logically, from the gastrointestinal tract viewpoint, such organoprotective/healing response implies the angiogenic growth factors that commonly signify the healing. Thereby, the gastric pentadecapeptide BPC 157-organoprotection (huge range of beneficial effects) signifies the Selye's stress concept/stress coping response implemented in and from gastrointestinal tract, and BPC 157 as an integrative mediator that integrates the adaptive bodily response to stress...
February 20, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28228058/enteric-coated-extended-release-and-sustained-release-formulations-of-nsaids
#5
Lamia AlHajri
The scaffold of this commentary is oriented to gravitate toward shedding light on the misconception regarding the use of enteric-coated, extended-release or sustained-release forms of nonsteroidal anti-inflammatory drugs (NSAIDs) and the reduction in gastrointestinal (GI) risks. Although evidence is sufficiently available with regard to the inability of these forms to ameliorate GI risks, it has been widely neglected by health care professionals. This dilemma will be approached and elaborated by uncovering historical evidence about the topic of interest followed by theoretical pharmacological explanations...
April 2017: Annals of Pharmacotherapy
https://www.readbyqxmd.com/read/28226401/natural-evolution-in-patients-with-non-steroidal-anti-inflammatory-drugs-induced-urticaria-angioedema
#6
Inmaculada Doña, Esther Barrionuevo, María Salas, José Antonio Cornejo-García, James R Perkins, Gádor Bogas, Ana Prieto, María José Torres
BACKGROUND: Non-steroidal anti-inflammatory drugs (NSAIDs) are the most frequent triggers of drug hypersensitivity with NSAIDs-induced urticaria/angioedema (NIUA) the most common phenotype. Loss of hypersensitivity has been reported for IgE-mediated reactions; however it has not been assessed in non-immunological reactions such as NIUA. We evaluated NSAID-hypersensitivity over time in NIUA patients. METHODS: Patients confirmed as NIUA by positive drug provocation test (DPT) with acetylsalicylic acid (ASA) during 2005-2012 (V1) were included (n=38)...
February 22, 2017: Allergy
https://www.readbyqxmd.com/read/28223391/evaluation-of-para-aminosalicylic-acid-pas-as-a-substrate-of-multiple-solute-carrier-slc-uptake-transporters-and-possible-drug-interactions-with-nsaids-in-vitro
#7
Md Masud Parvez, Ho Jung Shin, Jin Ah Jung, Jae-Gook Shin
para-Aminosalicylic acid (PAS) is a second-line anti-tuberculosis drug used to treat multidrug-resistant and extensively drug-resistant tuberculosis for more than 60 years. Renal secretion and glomerular filtration are the major pathways for elimination of PAS. We comprehensively studied PAS transport by using cell lines that overexpressed various transporters, and found that PAS acts as a novel substrate of organic anionic polypeptide (OATP1B1), organic cationic transporters (OCT1 and OCT2), and organic anion transporters (OAT1 and OAT3) but not a substrate of any ATP-binding cassette (ABC) transporters...
February 21, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28222891/coumarins-scaffolds-as-cox-inhibitors
#8
REVIEW
Hrishikesh Mohan Revankar, Syed Nasir Abbas Bukhari, Gajjela Bharath Kumar, Hua-Li Qin
The discovery of COX enzymes has led to a better understanding of inflammation and its related biological pathways. Apart from being related to inflammation and pain, it has also been associated with cancer and neuropsychiatric diseases such as schizophrenia. Proverbially speaking, study of these enzymes has been crucial as they happen to "have fingers in many pies". Non-steroidal anti-inflammatory drugs (NSAID) that act specifically as COX-2 inhibitors have been known for a while; however these are also associated with severe side effects such as cardiac problems...
February 9, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28222837/use-of-the-rat-grimace-scale-to-evaluate-neuropathic-pain-in-a-model-of-cervical-radiculopathy
#9
Blythe H Philips, Christine L Weisshaar, Beth A Winkelstein
Although neck and low-back pain are common sources of neuropathic pain with high societal costs, the pathophysiology of neuropathic pain is not well-defined. Traditionally, most rodent pain studies rely on evoked reflex-based testing to measure pain. However, these testing methods do not reveal spontaneous pain, particularly early after injury. The rat grimace scale (RGS) for quantifying spontaneous pain has been validated after visceral, incisional, orthopedic, and inflammatory insults but not neuropathic pain...
February 1, 2017: Comparative Medicine
https://www.readbyqxmd.com/read/28222030/sub-chronic-indomethacin-treatment-and-its-effect-on-the-male-reproductive-system-of-albino-rats-possible-protective-role-of-black-tea-extract
#10
Ishwar B Bagoji, Gavishiddappa A Hadimani, Saeed M Yendigeri, Kusal K Das
BACKGROUND: Indomethacin is commonly used as a nonsteroidal anti-inflammatory drug (NSAID) to treat inflammation, arthritis and joint pains. Unfortunately, it has a wide range of adverse effects on the physiological system, including gonads. This study aimed to assess possible beneficial effects of black tea extract (BTE) against indomethacin-induced alteration of gonadal hormone levels in male rats. MATERIALS AND METHODS: Adult male rats were divided into Group I (control), Group II (indomethacin, 5 mg/kg body weight [bwt...
February 21, 2017: Journal of Basic and Clinical Physiology and Pharmacology
https://www.readbyqxmd.com/read/28220959/evaluating-clinical-dietary-and-psychological-risk-factors-for-relapse-of-ulcerative-colitis-in-clinical-endoscopic-and-histological-remission
#11
Rajan Dhingra, Saurabh Kedia, Pratap Mouli Venigalla, Sushil Kumar, Namrata Singh, Sawan Bopanna, Vikas Singla, Bikash Narayan Choudhury, Prashant Verma, Veena Tiwari, Siddhartha Datta Gupta, Govind Makharia, Vineet Ahuja
BACKGROUND: The literature on possible factors that could trigger a relapse in patients with ulcerative colitis (UC) in clinical, endoscopic and histological remission on long term follow up is scarce. AIM: To determine the relapse rate in patients with UC in clinical, endoscopic and histological remission and identify factors that may influence the risk of relapse. METHODS: Patients with UC in clinical, endoscopic and histological remission were enrolled between January-July 2010 and followed up for 1 year to determine the effect of clinical, dietary and psychological factors on relapse...
February 21, 2017: Journal of Gastroenterology and Hepatology
https://www.readbyqxmd.com/read/28220520/factors-associated-with-villus-atrophy-in-symptomatic-coeliac-disease-patients-on-a-gluten-free-diet
#12
S Mahadev, J A Murray, T-T Wu, V S Chandan, M S Torbenson, C P Kelly, M Maki, P H R Green, D Adelman, B Lebwohl
BACKGROUND: Duodenal injury persists in some coeliac disease patients despite gluten-free diet, and is associated with adverse outcomes. AIM: To determine the prevalence and clinical risk factors for persistent villus atrophy among symptomatic coeliac disease patients. METHODS: A nested cross-sectional analysis was performed on coeliac disease patients with self-reported moderate or severe symptoms while following a gluten-free diet, who underwent protocol-mandated duodenal biopsy upon enrolment in the CeliAction clinical trial...
February 20, 2017: Alimentary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28219426/pseudophakic-cystoid-macular-edema-prevention-and-risk-factors-prospective-study-with-adjunctive-once-daily-topical-nepafenac-0-3-versus-placebo
#13
Sean McCafferty, April Harris, Corin Kew, Tala Kassm, Lisa Lane, Jason Levine, Meisha Raven
BACKGROUND: Define the effectiveness of a topical non-steroidal anti-inflammatory drug (NSAID) added to topical steroid use after uncomplicated phacoemulsification for the prevention of pseudophakic cystoid macular edema (PCME) using a prospective, randomized, double-masked, placebo-controlled clinical study. METHODS: Eyes (1000) were randomized to placebo (497) or nepafenac 0.3% (503) used once daily, post-operatively for 5 weeks at two ophthalmology clinics. Diagnosis of PCME was made by clinical, ocular coherence tomography (OCT), and with fluorescein angiography confirmation...
February 20, 2017: BMC Ophthalmology
https://www.readbyqxmd.com/read/28218370/incidence-of-heterotopic-ossification-in-minimally-invasive-short-stem-tha-using-the-modified-anterolateral-approach
#14
Karl P Kutzner, Marlene Hechtner, Dominik Pfeil, Philipp Rehbein, Mark P Kovacevic, Michael Schneider, Werner Siebert, Joachim Pfeil
INTRODUCTION: Heterotopic ossification (HO) is known to be a common complication after total hip arthroplasty (THA). The minimal invasive (MIS) modified anterolateral approach has become popular in combination with a short stem. We analysed the incidence of HO following short-stem THA using this approach in combination with a postoperative administration of nonsteroidal anti-inflammatory drugs (NSAIDs). MATERIALS AND METHODS: 216 short stems were implanted in 162 patients...
February 8, 2017: Hip International: the Journal of Clinical and Experimental Research on Hip Pathology and Therapy
https://www.readbyqxmd.com/read/28216685/comparative-efficacy-of-oral-meloxicam-and-phenylbutazone-in-2-experimental-pain-models-in-the-horse
#15
Heidi Banse, Alastair E Cribb
The efficacy of oral phenylbutazone [PBZ; 4.4 mg/kg body weight (BW), q12h], a non-selective non-steroidal anti-inflammatory drug (NSAID), and oral meloxicam (MXM; 0.6 mg/kg BW, q24h), a COX-2 selective NSAID, were evaluated in 2 experimental pain models in horses: the adjustable heart bar shoe (HBS) model, primarily representative of mechanical pain, and the lipopolysaccharide-induced synovitis (SYN) model, primarily representative of inflammatory pain. In the HBS model, PBZ reduced multiple indicators of pain compared with the placebo and MXM...
February 2017: Canadian Veterinary Journal. la Revue Vétérinaire Canadienne
https://www.readbyqxmd.com/read/28215167/chemical-modifications-of-ketoprofen-nsaid-in-search-of-better-lead-compounds-a-review-of-literature-from-2004-2016
#16
Gita Chawla, Chanda Ranjan, Anees A Siddiqui, Jagdish Kumar, Ankita Pathak
BACKGROUND: Ketoprofen, a potent anti-inflammatory, analgesic and anti-pyretic drug belonging to the propionic acid class was synthesized in 1968. Rapid absorption, simple metabolism, faster blood brain barrier crossing and high antinociceptive activity are the features responsible for its high use. But, free acidic moiety present in its structure is the major factor that declines its popularity by causing various gastric side effects .Many researchers have chemically modified this drug with the aim to discover an improved and safe NSAID candidate or a new drug with altered activity...
February 16, 2017: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28215165/synthesis-characterization-and-comparison-of-local-analgesic-anti-inflammatory-ulcerogenic-activity-of-copper-and-zinc-complexes-of-indomethacin
#17
Abhijit Sukul, Saikat Kumar Poddar, Sanjana Haque, Sajal Kumar Saha, Sreedam Chandra Das, Zobaer Al Mahmud, S M AbdurRahman, Abhijit Sukul
BACKGROUND: Non-steroidal anti-inflammatory drugs (NSAID) exert gastrointestinal upset by inhibiting mucosal cyclooxygenase (COX) activity for which complexation technique with metals has been adopted to overcome this drawback. OBJECTIVE: The study aimed to overcome the gastrointestinal side effects associated with indomethacin treatment by synthesizing copper (Cu) and zinc (Zn) complexes of indomethacin along with assessing potential pharmacological effects of these complexes...
February 16, 2017: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28214737/identification-of-non-steroidal-anti-inflammatory-drug-use-disorder-a-case-report
#18
Margo E Godersky, Laura K Vercammen, Alicia S Ventura, Alexander Y Walley, Richard Saitz
Commonly used for analgesic and anti-inflammatory effects, non-steroidal anti-inflammatory drugs (NSAIDs) are among the most frequently used medications in the world. In spite of their prevalence, reports of NSAID misuse and NSAID use disorder are uncommon. This case report describes a research participant who met criteria for DSM-5 moderate substance use disorder based on her use of prescribed ibuprofen as assessed by the validated Mini International Neuropsychiatric Interview (MINI). This case demonstrates that the DSM-5 criteria within the MINI can be applied to diagnose an NSAID use disorder...
February 9, 2017: Addictive Behaviors
https://www.readbyqxmd.com/read/28212985/nonsteroidal-anti-inflammatory-drugs-in-clinical-and-experimental-epilepsy
#19
REVIEW
Beatrice Mihaela Radu, Florin Bogdan Epureanu, Mihai Radu, Paolo Francesco Fabene, Giuseppe Bertini
Current antiepileptic drugs have limited efficacy and provide little or no benefits in 30% of the patients. Given that a role for brain inflammation in epilepsy has been repeatedly reported in recent years, the potential of anti-inflammatory drugs should be explored in depth, as they may provide new therapeutical approaches in preventing or reducing epileptogenesis. Here, we review preclinical (both in vivo and in vitro) and clinical epilepsy studies in which nonsteroidal antiinflammatory drugs (NSAIDs), i...
February 9, 2017: Epilepsy Research
https://www.readbyqxmd.com/read/28211343/immediate-reactions-to-more-than-1-nsaid-must-not-be-considered-cross-hypersensitivity-unless-tolerance-to-asa-is-verified
#20
D Pérez-Alzate, J A Cornejo-García, N Pérez-Sánchez, I Andreu, A García-Moral, J A Agúndez, J Bartra, I Doña, M J Torres, M Blanca, N Blanca-López, G Canto
BACKGROUND AND OBJECTIVES: Individuals who develop drug hypersensitivity reactions (DHRs) to chemically unrelated nonsteroidal anti-inflammatory drugs (NSAIDs) are considered cross-hypersensitive. The hallmark for this classification is that the patient presents a reaction after intake of or challenge with acetylsalicylic acid (ASA). Whether patients react to 2 or more NSAIDs while tolerating ASA remains to be studied (selective reactions, SRs). Objective: To identify patients with SRs to 2 or more NSAIDs including strong COX-1 inhibitors...
2017: Journal of Investigational Allergology & Clinical Immunology
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