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  • ||||||||||  Review, Journal:  Safer anti-inflammatory therapy through dual COX-2/5-LOX inhibitors: A structure-based approach. (Pubmed Central) -  Aug 30, 2019   
    Here, this integrative review attempts to identify the promising pharmacophore that serves as dual inhibitors of COX-2/5-LOX enzymes with improved safety profile. A better acquaintance of structural features that balance safety and efficacy of dual inhibitors would be a different approach to the process of understanding and interpreting the designing of novel anti-inflammatory agents.
  • ||||||||||  setanaxib (GKT831) / Genkyotex
    Food Restriction Augmented Alpha1-Adrenergic Mediated Contraction in Rats Mesenteric Arteries (Zone 1, Science and Technology Hall) -  Aug 21, 2019 - Abstract #AHA2019AHA_6896;    
    Augmented of α1-adrenergic mediated contraction via inhibition of eNOS-NO pathway by increased activation of ROS through NOX2/4 in response to FR. Reduced eNOS-NO signaling might be a pathophysiological counterbalance to prevent hypovolemic shock in response to FR.
  • ||||||||||  celecoxib oral / Generic Mfg.
    Differences in Pharmacological Potency Influence Blood Pressure Response to Celecoxib and Naproxen (Zone 2, Science and Technology Hall) -  Aug 21, 2019 - Abstract #AHA2019AHA_2592;    
    Naproxen 500 mg inhibited COX-2 activity to a greater degree than celecoxib 200 mg, which resulted in a more pronounced blood pressure response. While PRECISION concluded non-inferiority of celecoxib with regard to cardiovascular risk, this is based on a comparison of doses that are not equipotent.
  • ||||||||||  Bronica (seratrodast) / Takeda
    Preclinical, Journal:  Neryl butyrate induces contractile effects on isolated preparations of rat aorta. (Pubmed Central) -  Aug 20, 2019   
    Antagonists of α-adrenergic receptors (prazosin and yohimbine), but not the thromboxane-prostanoid receptor seratrodast, reversed the contraction induced by neryl butyrate...In conclusion, the contractile effects of neryl butyrate were inhibited by α-adrenergic antagonists, indicating the involvement of α-adrenoceptors in the mechanism of action. In vivo, neryl butyrate caused hypotension, suggesting that other systemic influence than vasoconstriction may occur.
  • ||||||||||  ibuprofen / generics
    Review, Journal:  Joint pain and consumption of analgesics among young elite athletes : Nationwide data from youth basketball (Pubmed Central) -  Aug 15, 2019   
    Additionally, 1 and 2 displayed insignificant antioxidant activities compared to the positive control L-ascorbic acid. From the point of view of pain medicine, it is not only the high prevalence of pain that is remarkable but also the widespread use of analgesics without a prescription and the misguided conception of adolescent competitive athletes that such medications have preventive effects.
  • ||||||||||  ibuprofen / generics
    Clinical, Journal, Head-to-Head:  Early treatment versus expectative management of patent ductus arteriosus in preterm infants: a multicentre, randomised, non-inferiority trial in Europe (BeNeDuctus trial). (Pubmed Central) -  Aug 15, 2019   
    P=N/A, P4
    From the point of view of pain medicine, it is not only the high prevalence of pain that is remarkable but also the widespread use of analgesics without a prescription and the misguided conception of adolescent competitive athletes that such medications have preventive effects. As a conservative approach is gaining interest, we investigate whether in preterm infants, born at a GA less than 28 weeks, with a PDA an expectative management is non-inferior to early treatment with IBU regarding to the composite outcome of mortality and/or NEC and/or BPD at a PMA of 36 weeks.
  • ||||||||||  Analgin (metamizole) / Sedico, Prialt (ziconotide) / Jazz
    Journal:  Pharmacology of non-opioid analgesics (Pubmed Central) -  Aug 15, 2019   
    Acetaminophen and metamizole (dipyrone) are analgesics and antipyretic agents, while metamizole exhibits also spasmolytic effects. Capsaicin and intrathecal ziconotide are pure analgesics.
  • ||||||||||  aspirin / generics
    Clinical, Journal:  Clinical updates in aspirin-exacerbated respiratory disease. (Pubmed Central) -  Aug 3, 2019   
    Dietary modifications toward a diet that is high in omega-3 fatty acids and low in omega-6 fatty acids can reduce the production of the inflammatory leukotriene and prostaglandin D₂ lipids and help improve symptoms for patients with AERD. A lack of definitive understanding of the causative mechanisms of AERD and the absence of an AERD-specific patient-reported outcome measure are obstacles that remain in this field, but much progress has been made over the past decade.
  • ||||||||||  Preclinical, Journal:  The effects of prostaglandins and endocannabinoids on iris arterial vascularization in Wistar rats - Experimental analysis. (Pubmed Central) -  Aug 2, 2019   
    The nonselective NSAIDs induced vascular dilation in the iris vessels, while the selective COX2 inhibitors determined a variable degree of vasoconstriction. In view of the results of this experiment and the added evidence found in literature, we consider that further research will show the potential benefits for the additional use of NSAIDs in ocular pathology, otherwise unaffected by this medication until the present time (for example, glaucoma treatment).
  • ||||||||||  Journal:  New insights on a NGF-mediated pathway to induce ovulation in rabbits (Oryctolagus cuniculus). (Pubmed Central) -  Jul 28, 2019   
    The ovulatory responses were 0%, 83.3%, 66.7%, 16.7%, and 0% in PBS, NM, RS, ARS, and CIRS groups, respectively. Present data confirm that, although raw semen may induce ovulation via endocrine mechanisms through binding to NGF receptors in the ovary, a novel OIFs-mediated neural mechanism facilitates ovulation in rabbits.
  • ||||||||||  Clinical, Journal:  Pharmacoepidemiology of non-steroidal anti-inflammatory drugs. (Pubmed Central) -  Jul 19, 2019   
    Event rates in patients with no overt coronary heart disease are vanishingly low, and the real magnitude of the issue in the treatment of common pain is still unknown. Considering their purely symptomatic effects, they should be used at the lowest possible dose for the shortest possible time, based on the symptomatic relief of pain or fever.
  • ||||||||||  Review, Journal:  Epoxy-Oxylipins and Soluble Epoxide Hydrolase Metabolic Pathway as Targets for NSAID-Induced Gastroenteropathy and Inflammation-Associated Carcinogenesis. (Pubmed Central) -  Jul 12, 2019   
    In this review, we hope to bridge the gap between NSAID toxicity and sEH-mediated metabolic pathways to focus on the role of epoxy fatty acid metabolic pathway of PUFAs in NSAIDS-ulcer formation and healing as well as inflammation-related carcinogenesis. Specifically we address the potential application of sEH inhibition to enhance ulcer healing at the site of inflammation via their activity on altered lipid signaling, mitochondrial function, and diminished reactive oxygen species, and further discuss the significance of dual COX and sEH inhibitor in anti-inflammation and carcinogenesis.
  • ||||||||||  Preclinical, Journal:  The contribution of synovial macrophages to rat advanced osteoarthritis pain resistant to cyclooxygenase inhibitors. (Pubmed Central) -  Jun 28, 2019   
    ...Cyclooxygenase inhibitors, such as celecoxib and naproxen, and a steroid were ineffective, but an opioid and anti-nerve growth factor (NGF) antibody was effective for pain management in the advanced OA model...Intravenous injection of clodronate liposomes depleted synovial macrophages, which decreased the level of not only proinflammatory mediator IL-1β but also NGF in the knee joint, leading to pain suppression in the advanced OA model. These data suggest the involvement of synovial macrophages in advanced knee OA pain resistant to COX inhibitors by increasing proinflammatory mediators, and that drugs targeting synovial macrophages might have potent analgesic effects.
  • ||||||||||  ibuprofen / generics
    Journal:  A seven-step plan for becoming a moderately rich and famous biochemist. (Pubmed Central) -  Jun 28, 2019   
    ...Nonsteroidal anti-inflammatory drugs (e.g. aspirin, ibuprofen, and naproxen) block PG synthesis by inhibiting COX-1 and COX-2...I attribute my successes to the great good fortune of having been surrounded by people who helped me make the most of my talents. I have written this reflection in a light-hearted fashion as a self-help essay, while highlighting the people and factors that most impacted me during my upbringing and then during my maturation and evolution as a biochemist.
  • ||||||||||  dexamethasone / generics
    Preclinical, Journal:  Synthesis, in vitro and in vivo biological evaluation, COX-1/2 inhibition and molecular docking study of indole-N-acylhydrazone derivatives. (Pubmed Central) -  Jun 26, 2019   
    ...In the lymphoproliferation assay, using mice splenocytes, 3a and 3b showed inhibition of lymphocyte proliferation of 62.7% (±3.5) and 50.7% (±2), respectively, while dexamethasone presented an inhibition of 74.6% (±2.4)...The results for COX inhibition assays showed that compound 3b is a selective COX-2 inhibitor, but with less potency when compared to celecoxib, and compound 3a not presented selectivity towards COX-2...I addition to our experimental results, in silico analysis suggest that compounds 3a and 3b present a well-balanced profile between pharmacodynamics and pharmacokinetics. Thus, our preliminary results revealed the potentiality of a new COX-2 selective derivative in the modulation of the inflammatory process.
  • ||||||||||  Journal:  Celastrol ameliorates inflammatory pain and modulates HMGB1/NF-κB signaling pathway in dorsal root ganglion. (Pubmed Central) -  Jun 23, 2019   
    Furthermore, celastrol obviously inhibited COX-2 protein expression and down-regulated IL-6, IL-17, TNF-α, MCP-1, GFAP and CD11b mRNA levels in DRG of CFA rats. Collectively, the present study firstly provide evidences of the anti-inflammatory effect of celastrol via suppressing CFA-induced the activation of HMGB1/NF-κB signaling pathway in DRG, which maybe a potential therapeutic target for celastrol alleviating inflammatory pain.
  • ||||||||||  aspirin / generics
    Journal:  Aspirin as a COX Inhibitor and Anti-inflammatory Drug in Human Skeletal Muscle. (Pubmed Central) -  Jun 22, 2019   
    These results provide evidence that orally consumed aspirin can inhibit the COX pathway and reduce the inflammatory mediator PGE2 in human skeletal muscle. Findings from this study highlight the need to expand our knowledge regarding the potential role for aspirin regulation of the deleterious influence of inflammation on skeletal muscle health in aging and exercising individuals.
  • ||||||||||  aspirin / generics
    Review, Journal:  COX-2 Inhibitors, Aspirin, and Other Potential Anti-Inflammatory Treatments for Psychiatric Disorders. (Pubmed Central) -  Jun 21, 2019   
    Celecoxib has also been studied in schizophrenia and has shown efficacy, in particular, in early disease stages. The mixed COX inhibitor aspirin (acetylsalicylic acid) seems to have both protective and therapeutic effects on schizophrenia.This paper discusses the hypothesized role of inflammation in major depression and schizophrenia, including markers of inflammation; pertinent studies on celecoxib and aspirin; and additional immunomodulatory therapeutic strategies.
  • ||||||||||  Journal:  Resveratrol as an active ingredient for cosmetic and dermatological applications: a review. (Pubmed Central) -  Jun 15, 2019   
    Moreover, resveratrol also has the antioxidant properties, thus can protect cells against oxidative damage associated with the effects of free radicals and UV radiation on the skin by reducing the expression of AP-1 and NF-kB factors and it slows down the process of photoaging of the skin. This study reviews literature on the skin care properties of resveratrol and its dermal bioavailability, metabolism, and dermal safety of application.
  • ||||||||||  Review, Journal:  Evidence-based use of acetaminophen for hemodynamically significant ductus arteriosus in preterm infants. (Pubmed Central) -  Jun 15, 2019   
    Acetaminophen may therefore be an ideal first-line agent among moderately and extremely preterm infants, though there is a paucity of data from controlled trials regarding its use in infants at the border of viability (gestation age ≤25 weeks). Evidence from clinical studies of limited quality supports acetaminophen treatment as rescue therapy for infants with persistent PDA after unsuccessful cyclooxygenase inhibitor treatment, including those being considered for surgical ligation.
  • ||||||||||  glibenclamide / generics, clotrimazole / generics
    Preclinical, Journal:  Vasorelaxant and antihypertensive effects of Tianshu Capsule on rats: An in vitro and in vivo approach. (Pubmed Central) -  Jun 15, 2019   
    The NO/sGC/cGMP pathway, ATP-sensitive K channels, Ca-activated K channels, inhibition of extracellular Ca influx and intracellular Ca2 release were probably involved in this relaxation. The vasorelaxant effects of TSC may make the greatest contribution to the reduction in high blood pressure.
  • ||||||||||  Journal:  Cyclooxygenase Inhibitors in Epithelial Ovarian Cancer Treatment. (Pubmed Central) -  Jun 9, 2019   
    Several reports have shown that treatment of EOC cells with COX-1- and COX-2-specific inhibitors exhibits a therapeutic effect on EOC both in vitro and in vivo. However, more clinical investigations are needed to develop therapeutic COX inhibitors for the prevention and treatment of EOC without adverse effects.
  • ||||||||||  Journal:  Cyclo-oxygenase inhibitors for treating preterm labour: what is the molecular evidence? (Pubmed Central) -  Jun 9, 2019   
    The current study systematically searched existing scientific evidence to address the hypothesis that COX expression/activity is increased with the onset of human labour, in an effort to determine whether there is a rationale for the use of COX inhibitors as tocolytics. Our review identified 40 studies, but determined that there is insufficient evidence to support or refute a role of COX-1/-2 in the onset of preterm labour that supports COX-targetted tocolysis.