Journal articles: 'Nonsteroidal anti-inflammatory agents Physiological effect'

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Mason, HH. "Morphine sulfate, transdermal fentanyl citrate and ketorolac tromethamine: effects on postoperative pulmonary function." American Journal of Critical Care 2, no. 1 (January 1, 1993): 61–64. http://dx.doi.org/10.4037/ajcc1993.2.1.61.

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The physiological effects of morphine sulfate and fentanyl citrate on postoperative pulmonary function demonstrate varying degrees of respiratory depression related to dose, route of administration and pre-existing pathologies. Current postoperative analgesic therapies that include concomitant use of narcotic agonists and nonsteroidal anti-inflammatory drugs require adjustment of drug dosages to provide adequate pain relief while avoiding drug-induced complications. Specific nursing considerations include understanding therapeutic and adverse effects of these agents on pain and ventilation, continuous pain assessment and early recognition and treatment of respiratory depression.

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Alem, Mohammed A. S., and L. Julia Douglas. "Effects of Aspirin and Other Nonsteroidal Anti-Inflammatory Drugs on Biofilms and Planktonic Cells of Candida albicans." Antimicrobial Agents and Chemotherapy 48, no. 1 (January 2004): 41–47. http://dx.doi.org/10.1128/aac.48.1.41-47.2004.

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ABSTRACT Prostaglandins are now known to be produced by Candida albicans and may play an important role in fungal colonization. Their synthesis in mammalian cells is decreased by inhibitors of the cyclooxygenase isoenzymes required for prostaglandin formation. In the present study, a catheter disk model system was used to investigate the effects of nonsteroidal anti-inflammatory drugs (all cyclooxygenase inhibitors) on biofilm formation by three strains of C. albicans. Seven of nine drugs tested at a concentration of 1 mM inhibited biofilm formation. Aspirin, etodolac, and diclofenac produced the greatest effects, with aspirin causing up to 95% inhibition. Celecoxib, nimesulide, ibuprofen, and meloxicam also inhibited biofilm formation, but to a lesser extent. Aspirin was active against growing and fully mature (48-h) biofilms; its effect was dose related, and it produced significant inhibition (20 to 80%) at pharmacological concentrations. Simultaneous addition of prostaglandin E2 abolished the inhibitory effect of 25 or 50 μM aspirin. At 1 mM, aspirin reduced the viability of biofilm organisms to 1.9% of that of controls. Surviving cells had a wrinkled appearance, as judged by scanning electron microscopy, and consisted of both yeasts and hyphae. Treatment with other cyclooxygenase inhibitors, such as etodolac, resulted in biofilms that consisted almost entirely of yeast cells. In conventional assays for germ tube formation, these drugs produced significant inhibition, whereas aspirin had little effect. Our findings suggest that cyclooxygenase-dependent synthesis of fungal prostaglandin(s) is important for both biofilm development and morphogenesis in C. albicans and may act as a regulator in these physiological processes. Our results also demonstrate that aspirin possesses potent antibiofilm activity in vitro and could be useful in combined therapy with conventional antifungal agents in the management of some biofilm-associated Candida infections.

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Rizaldy Pinzon. "Closing the Gap of Unmet Needs in Inflammatory Pain Management: Case Series of Predimenol for Pain." MEDICINUS 34, no. 2 (August 1, 2021): 29–33. http://dx.doi.org/10.56951/medicinus.v34i2.65.

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Chronic inflammatory pain is major medical problem worldwide. Nonsteroidal anti-inflammatory drugs (NSAIDs) and selective cyclooxygenase (COX)-2 inhibitors are commonly used medications to treat chronic pain. However, these agents have been associated with serious gastrointestinal, renal and cardiovascular adverse effects. This limitation indicates a clear unmet need in terms of safety of current treatment options for the management of chronic inflammatory pain. Those adverse effects may caused by overlapping roles of COX-1 and COX-2 in physiological and pathophysiological processes. Predimenol is a herbal medicine that can be used to treat pain. Recent findings showed that these phytochemicals may directly act upon several inflammatory processes and offer compelling evidence that predimenol could reduce pain and inflammation. We report two cases and short review of the use of predimenol for pain management. Our review showed that predimenol formulations could be a valuable alternative treatment to relieve symptoms of pain with good safety profile. Further researches through large, high quality RCTs to investigate the clinical benefit of predimenol for pain management are needed.

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Chan, Melissa V., and John L. Wallace. "Hydrogen sulfide-based therapeutics and gastrointestinal diseases: translating physiology to treatments." American Journal of Physiology-Gastrointestinal and Liver Physiology 305, no. 7 (October 1, 2013): G467—G473. http://dx.doi.org/10.1152/ajpgi.00169.2013.

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Hydrogen sulfide (H2S) is a gaseous meditator that has various physiological and pathophysiological roles in the body. It has been shown to be an important mediator of gastrointestinal (GI) mucosal defense and contributes significantly to repair of damage and resolution of inflammation. Synthesis of H2S increases markedly after mucosal injury, and inhibition of H2S in such circumstances leads to delayed healing and exacerbated inflammation. The beneficial effects of H2S may be attributable to its ability to elevate mucosal blood flow, prevent leukocyte-endothelial adhesion, reduce oxidative stress, and stimulate angiogenesis. The use of H2S-donating agents and inhibitors of the key enzymes contributing to H2S synthesis have provided strong evidence for the importance of H2S in enhancing mucosal resistance to damage, as well as modulating inflammation and repair. In recent years, significant evidence has been generated to support the notion that these positive aspects of H2S can be exploited in drug design, particularly for arthritis, inflammatory bowel disease, and colon cancer chemoprevention. Thus novel H2S-based therapies have been shown to be effective anti-inflammatories that can promote the resolution of inflammation and accelerate the healing of GI ulcers. Encouraging results have already been seen experimentally with a mesalamine derivative and with H2S-releasing derivatives of nonsteroidal anti-inflammatory drugs.

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Chan, A., and V. Ramachandra. "Comparing the analgesic effect of nonsteroidal anti-inflammatory agents." Anaesthesia 48, no. 12 (February 22, 2007): 1117. http://dx.doi.org/10.1111/j.1365-2044.1993.tb07569.x.

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Pegg, Anthony E. "Spermidine/spermine-N1-acetyltransferase: a key metabolic regulator." American Journal of Physiology-Endocrinology and Metabolism 294, no. 6 (June 2008): E995—E1010. http://dx.doi.org/10.1152/ajpendo.90217.2008.

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Spermidine/spermine- N1-acetyltransferase (SSAT) regulates cellular polyamine content. Its acetylated products are either excreted from the cell or oxidized by acetylpolyamine oxidase. Since polyamines play critical roles in normal and neoplastic growth and in ion channel regulation, SSAT is a key enzyme in these processes. SSAT is very highly regulated. Its content is adjusted in response to alterations in polyamine content to maintain polyamine homeostasis. Certain polyamine analogs can mimic the induction of SSAT and cause a loss of normal polyamines. This may have utility in cancer chemotherapy. SSAT activity is also induced via a variety of other stimuli, including toxins, hormones, cytokines, nonsteroidal anti-inflammatory agents, natural products, and stress pathways, and by ischemia-reperfusion injury. These increases are initiated by alterations in Sat1 gene transcription reinforced by alterations at the other regulatory steps, including protein turnover, mRNA processing, and translation. Transgenic manipulation of SSAT activity has revealed that SSAT activity links polyamine metabolism to lipid and carbohydrate metabolism by means of alterations in the content of acetyl-CoA and ATP. A high level of SSAT stimulates flux through the polyamine biosynthetic pathway, since biosynthetic enzymes are induced in response to the fall in polyamines. This sets up a futile cycle in which ATP is used to generate S-adenosylmethionine for polyamine biosynthesis and acetyl-CoA is consumed in the acetylation reaction. A variety of other effects of increased SSAT activity include death of pancreatic cells, blockage of regenerative tissue growth, behavioral changes, keratosis follicularis spinulosa decalvans, and hair loss. These are very likely due to changes in polyamine and putrescine levels, although increased oxidative stress via the oxidation of acetylated polyamines may also contribute. Recently, it was found that the SSAT protein and/or a related protein, thialysine acetyltransferase, interacts with a number of other important proteins, including the hypoxia-inducible factor-1 α-subunit, the p65 subunit of NF-κB, and α9β1-integrin, altering the function of these proteins. It is not yet clear whether this functional alteration involves protein acetylation, local polyamine concentration changes, or other effects. It has been suggested that SSAT may also be a useful target in diseases other than cancer, but the wide-ranging physiological and pathophysiological effects of altered SSAT expression will require very careful limitation of such strategies to the relevant cells to avoid toxic effects.

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Thaller, John, Matthew Walker, Alex J Kline, and D. Greg Anderson. "The Effect of Nonsteroidal Anti-Inflammatory Agents on Spinal Fusion." Orthopedics 28, no. 3 (March 1, 2005): 299–303. http://dx.doi.org/10.3928/0147-7447-20050301-15.

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Hanson, Curtis A., Paul S. Weinhold, Hessam M. Afshari, and Laurence E. Dahners. "The Effect of Analgesic Agents on the Healing Rat Medial Collateral Ligament." American Journal of Sports Medicine 33, no. 5 (May 2005): 674–79. http://dx.doi.org/10.1177/0363546504269722.

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Background Studies have suggested that some nonselective nonsteroidal anti-inflammatory drugs, including piroxicam, may improve ligament healing, whereas other nonsteroidal anti-inflammatory drugs, including ibuprofen and the cyclooxygenase-2 inhibitor celecoxib, may have no effect on the mechanical properties or may even deter the healing process. These results might reflect variations in cyclooxygenase enzyme selectivity by different drugs or, alternatively, may be related to their analgesic properties because it is generally accepted that early activity improves ligament healing. Hypothesis Nonselective nonsteroidal anti-inflammatory drugs improve ligament healing, whereas other analgesics provide lesser degrees of improvement, and cyclooxygenase-2 inhibitors are detrimental. Study Design Controlled laboratory study. Methods One hundred fifty-five Sprague-Dawley rats were divided into 7 treatment groups (piroxicam, naproxen, rofecoxib, butorphanol, 2 doses of acetaminophen, and control). The right medial collateral ligament of each rat was transected, and the drugs were administered postoperatively on days 1 to 6. On day 14, the rats were sacrificed, and mechanical testing was performed on the medial collateral ligament. Results The piroxicam group demonstrated significantly greater load to failure (27%) compared with the control. No significant differences were observed between other groups. Conclusions Piroxicam improves ligament healing, but this effect cannot be attributed to all nonselective nonsteroidal anti-inflammatory drugs. Opiate analgesics, acetaminophen, and cyclooxygenase-2 inhibitors do not appear to categorically affect ligament healing. Clinical Relevance In the treatment of ligament injury, piroxicam may be a drug of choice.

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Miranda, H. F., F. Sierralta, and G. Pinardi. "Carbachol interactions with nonsteroidal anti-inflammatory drugs." Canadian Journal of Physiology and Pharmacology 80, no. 12 (December 1, 2002): 1173–79. http://dx.doi.org/10.1139/y02-145.

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The inhibition of cyclooxygenase enzymes by nonsteroidal anti-inflammatory drugs (NSAIDs) does not completely explain the antinociceptive efficacy of these agents. It is known that cholinergic agonists are antinociceptive, and this study evaluates the interactions between carbachol and some NSAIDs. Antinociceptive activity was evaluated in mice by the acetic acid writhing test. Doseresponse curves were constructed for NSAIDs and carbachol, administered either intraperitoneally (i.p.) or intrathecally (i.t.). The interactions of carbachol with NSAIDs were evaluated by isobolographic analysis after the simultaneous administration of fixed proportions of carbachol with each NSAID. All of the drugs were more potent after spinal than after systemic administration. The combinations of NSAIDs and carbachol administered i.p. were supra-additive; however, the i.t. combinations were only additive. Isobolographic analysis of the coadministration of NSAIDs and carbachol and the fact that atropine antagonized the synergistic effect suggest that carbachol may strongly modulate the antinociceptive activity of NSAIDs; thus, central cholinergic modulation would be an additional mechanism for the antinociceptive action of NSAIDs, unrelated to prostaglandin biosynthesis inhibition.Key words: antinociception, nonsteroidal anti-inflammatory drugs, cholinergic, carbachol, writhing test.

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Yücesoy, M., I. M. A. Öktem, and Z. Gülay. "In-VitroSynergistic Effect of Fluconazole with Nonsteroidal Anti-Inflammatory Agents AgainstCandida albicansStrains." Journal of Chemotherapy 12, no. 5 (January 2000): 385–89. http://dx.doi.org/10.1179/joc.2000.12.5.385.

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IRANI, J., V. RAVERY, J. L. PARIENTE, E. CHARTIER-KASTLER, E. LECHEVALLIER, M. SOULIÉ, D. CHAUTARD, et al. "Effect of Nonsteroidal Anti-Inflammatory Agents and Finasteride on Prostate Cancer Risk." Journal of Urology 168, no. 5 (November 2002): 1985–88. http://dx.doi.org/10.1016/s0022-5347(05)64277-2.

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Gasco, Alberto, Donatella Boschi, Konstantin Chegaev, Clara Cena, Antonella Di Stilo, Roberta Fruttero, Loretta Lazzarato, Barbara Rolando, and Paolo Tosco. "Multitarget drugs: Focus on the NO-donor hybrid drugs." Pure and Applied Chemistry 80, no. 8 (January 1, 2008): 1693–701. http://dx.doi.org/10.1351/pac200880081693.

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The article addresses the design of multitarget drugs, namely, compounds capable of interacting with more than one target simultaneously. These agents could be useful tools in the therapy of complex diseases such as cardiovascular and inflammatory diseases. An interesting case of multitarget compounds are nitric oxide (NO)-donor hybrids, structures which combine the physiological properties of NO with those of a lead drug. In particular, the authors discuss the symbiotic approach used to design NO-donor nonsteroidal anti-inflammatory drugs (NO-NSAIDs) and NO-donor antioxidants. The former could be useful agents in the treatment of anti-inflammatory diseases being devoid of gastro- and cardiotoxicity, the latter could be a valid approach to the treatment of many cardiovascular diseases.

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Thoo, Sophie, Sudha Cugati, Andrew Lee, and Celia Chen. "Successful treatment of fingolimod-associated macular edema with intravitreal triamcinolone with continued fingolimod use." Multiple Sclerosis Journal 21, no. 2 (April 2, 2014): 249–51. http://dx.doi.org/10.1177/1352458514528759.

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The occurrence of macular edema as an adverse effect of fingolimod is well documented. Treatment modalities used to manage fingolimod-associated macular edema (FAME) have included nonsteroidal anti-inflammatory agents and sub-tenon injection. We describe two cases where intravitreal injection is used to successfully treat FAME in patients who were previously unsuccessfully treated with topical nonsteroidal anti-inflammatories.

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Jacobsen, Steven J., and Rosebud O. Roberts. "RE: EFFECT OF NONSTEROIDAL ANTI-INFLAMMATORY AGENTS AND FINASTERIDE ON PROSTATE CANCER RISK." Journal of Urology 169, no. 5 (May 2003): 1798–99. http://dx.doi.org/10.1097/01.ju.0000057804.01025.13.

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Pruthi, Raj S., J. Eric Derksen, and Kris Gaston. "RE: EFFECT OF NONSTEROIDAL ANTI-INFLAMMATORY AGENTS AND FINASTERIDE ON PROSTATE CANCER RISK." Journal of Urology 169, no. 6 (June 2003): 2304. http://dx.doi.org/10.1097/01.ju.0000065383.98815.8e.

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Negm, Maged M. "Effect of intracanal use of nonsteroidal anti-inflammatory agents on posttreatment endodontic pain." Oral Surgery, Oral Medicine, Oral Pathology 77, no. 5 (May 1994): 507–13. http://dx.doi.org/10.1016/0030-4220(94)90233-x.

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Serafini, Mauro, Ilaria Peluso, and Anna Raguzzini. "Flavonoids as anti-inflammatory agents." Proceedings of the Nutrition Society 69, no. 3 (June 23, 2010): 273–78. http://dx.doi.org/10.1017/s002966511000162x.

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Epidemiological evidence suggests that a high intake of plant foods is associated with lower risk of chronic diseases. However, the mechanism of action and the components involved in this effect have not been identified clearly. In recent years, the scientific community has agreed to focus its attention on a class of secondary metabolites extensively present in a wide range of plant foods: the flavonoids, suggested as having different biological roles. The anti-inflammatory actions of flavonoids in vitro or in cellular models involve the inhibition of the synthesis and activities of different pro-inflammatory mediators such as eicosanoids, cytokines, adhesion molecules and C-reactive protein. Molecular activities of flavonoids include inhibition of transcription factors such as NF-κB and activating protein-1 (AP-1), as well as activation of nuclear factor-erythroid 2-related factor 2 (Nrf2). However, the in vitro evidence might be somehow of limited impact due to the non-physiological concentrations utilized and to the fact that in vivo flavonoids are extensively metabolized to molecules with different chemical structures and activities compared with the ones originally present in the food. Human studies investigating the effect of flavonoids on markers of inflammation are insufficient, and are mainly focused on flavonoid-rich foods but not on pure molecules. Most of the studies lack assessment of flavonoid absorption or fail to associate an effect on inflammation with a change in circulating levels of flavonoids. Human trials with appropriate placebo and pure flavonoid molecules are needed to clarify if flavonoids represent ancillary ingredients or key molecules involved in the anti-inflammatory properties of plant foods.

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Schendrigin, I. N., and S. I. Piskov. "Anti-inflammatory effect of anakinra, an interleukin-1 receptor inhibitor, in patients with refractory tophaceous gout." Clinical pharmacology and therapy 35, no. 4 (November 3, 2022): 48–50. http://dx.doi.org/10.32756/0869-5490-2022-4-48-50.

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The first line treatments for acute gouty arthritis are nonsteroidal anti-inflammatory drugs (NSAID), corticosteroids, and colchicine. However, these agents are ineffective or contraindicated in a proportion of patients. Interleukin (IL)-1 is a key mediator in the pathogenesis of acute gouty arthritis. Recently, three IL-1-targeted agents have been developed, including anakinra, the IL-1 receptor antagonist. The authors present two patients with a flare of refractory tophaceous gout who were treated with anakinra.

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Михайловская, Н. А., and Т. Н. Слободин. "Nonsteroidal Anti-Inflammatory Drugs: Risks and Benefits." Неврология и нейрохирургия. Восточная Европа, no. 3 (November 17, 2020): 414–34. http://dx.doi.org/10.34883/pi.2020.10.3.037.

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До настоящего времени селективные и неселективные ингибиторы циклооксигеназы (ЦОГ) остаются наиболее эффективными лекарствами для лечения воспалительной боли. Однако их использование ассоциировано с нежелательными побочными эффектами со стороны желудочно-кишечного тракта, сердечно-сосудистой, мочевыделительной системы, печени, хрящевой ткани и т. д. В связи с этим огромное количество пациентов не получают адекватную противовоспалительную и обезболивающую терапию, что значительно снижает качество их жизни и наносит большой экономический ущерб. С повышением средней продолжительности жизни человека потребность в препаратах подобного действия неуклонно возрастает и проблема эффективной и безопасной терапии воспалительной боли становится все более актуальной и приобретает мировую значимость.В обзоре рассмотрены основные побочные явления, связанные с приемом нестероидных противовоспалительных средств (НПВС), механизмы их развития, пути предотвращения. Также рассмотрены факторы, влияющие на развитие того или иного физиологического ответа организма пациента на НПВС, – свойства самого лекарства, генетический полиморфизм, микробиота кишечника, характер питания, соматические заболевания, сопутствующий прием других лекарственных препаратов и т. д. В заключение рассмотрены основные перспективы и направления, в которых ведется поиск не менее эффективной и более безопасной альтернативы НПВС – двойные блокаторы циклооксигеназного и липоксигеназного путей метаболизма арахидоновой кислоты, NO- и H2S-высвобождающие препараты, ингибиторы микросомальной простагландин-Е-синтетазы (mPGES-1) и агонисты EP-рецепторов, влияющих на низшие, конечные звенья ЦОГ-пути, искусственные аналоги резолвинов, эндогенные регуляторы воспаления и т. д. И пока ни один из этих препаратов не был допущен в клиническую практику мы должны учиться рационально использовать уже имеющиеся в наличии НПВС, подбирая наиболее эффективную и безопасную тактику для каждого пациента. Until now, selective and non-selective inhibitors of cyclooxygenase (COX) remain the most effective medicines for the treatment of inflammatory pain. However, their use is associated with undesirable adverse effects – gastrointestinal, cardiovascular, urinary, hepatic, etc. In this regard, a huge number of patients do not receive adequate anti-inflammatory and analgesic therapy, which significantly worsens their quality of life and causes great economic losses. With the increase of the average human life expectancy, the need for drugs of this effect is steadily increasing, and the problem of effective and safe treatment of inflammatory pain is becoming more and more urgent and gaining global significance.In the review, there are considered the main side effects associated with the use of non-steroidal anti- inflammatory drugs (NSAIDs), the mechanisms of their development, and the ways of prevention. The factors that influence the development of one or another physiological response of the patient’s body to NSAIDs are also considered – the properties of the drug itself, genetic polymorphism, intestinal microbiota, diet, somatic diseases, concomitant intake of other drugs, etc. In conclusion, the main prospects and directions are considered, where the search for an alternative to NSAIDs is going, which is equally effective and more safe – double blockers of the cyclooxygenase and lipoxygenase pathways of arachidonic acid metabolism, NO- and H2S-releasing drugs, inhibitors of microsomal prostaglandin E-synthetase (mPGES-1) and EP-receptor agonists, affecting the final links of the COX pathway, artificial analogs of resolvins, endogenous regulators of inflammation, etc. And while none of these drugs has been allowed into clinical practice, we should learn to use the NSAIDs rationally, choosing the most effective and safe tactics for each patient.

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Hassan, Ghaneya S., Gehan H. Hegazy, Noha M. Ibrahim, and Samar H. Fahim. "New ibuprofen derivatives as H2S and NO donors as safer anti-inflammatory agents." Future Medicinal Chemistry 11, no. 23 (December 2019): 3029–45. http://dx.doi.org/10.4155/fmc-2018-0467.

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Aim: Nonsteroidal anti-inflammatory drugs are expansively used worldwide. However, their prolonged administration is associated with serious side effects, especially gastrointestinal ulceration. Materials & methods: New ibuprofen derivatives hybridized with H2S- or NO-donating moieties were synthesized and evaluated for their anti-inflammatory activity and ulcerogenic effect. COX-1/COX-2 isozymes selectivity test for the most promising derivatives was performed. Molecular docking studies were performed. Results: Most of the compounds showed promising anti-inflammatory activity comparable to that of ibuprofen (% edema inhibition = 76.6 and ulcer index = 21.26) with much better gastrointestinal tract tolerance (ulcer indices ranging from 0 to 14.67), especially compound 2 -H2S donor- (% edema inhibition = 75.5 and ulcer index = 11.75) and compound 16 -NO donor- (% edema inhibition = 65.4 and ulcer index = 8.66).

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Wawro, Marta Ewelina, Katarzyna Sobierajska, Wojciech Michał Ciszewski, and Jolanta Niewiarowska. "Nonsteroidal Anti-Inflammatory Drugs Prevent Vincristine-Dependent Cancer-Associated Fibroblasts Formation." International Journal of Molecular Sciences 20, no. 8 (April 20, 2019): 1941. http://dx.doi.org/10.3390/ijms20081941.

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Vincristine is used in the clinical treatment of colon cancer, especially in patients diagnosed in the advanced phase of cancer development. Unfortunately, similar to other agents used during antitumor therapy, vincristine might induce chemoresistance. Studies of this process focus mainly on the analysis of the molecular mechanisms within cancer, usually ignoring the role of stromal cells. Our present findings confirm that vincristine stimulates the secretion of tumor growth factors class beta and interleukin-6 from cancer-associated fibroblasts as a result of paracrine stimulation by cancer cells. Based on alterations in morphology, modulation of capillary formation, and changes in endothelial and mesenchymal marker profile, our findings demonstrate that higher levels of tumor growth factor-βs and interleukin-6 enhance cancer-associated fibroblast-like cell formation through endothelial–mesenchymal transition and that nonsteroidal anti-inflammatory drug treatment (aspirin and ibuprofen) is able to inhibit this phenomenon. The process appears to be regulated by the rate of microtubule polymerization, depending on β-tubulin composition. While higher levels of tubulin-β2 and tubulin-β4 caused slowed polymerization and reduced the level of factors secreted to the extracellular matrix, tubulin-β3 induced the opposite effect. We conclude that nonsteroidal anti-inflammatory drugs should be considered for use during vincristine monotherapy in the treatment of patients diagnosed with colorectal cancer.

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Inotai, András, and Ágnes Mészáros. "Economic evaluation of nonsteroidal anti-inflammatory drug strategies in rheumatoid arthritis." International Journal of Technology Assessment in Health Care 25, no. 02 (April 2009): 190–95. http://dx.doi.org/10.1017/s0266462309090242.

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Objectives:Although disease modifying antirheumatic drugs (DMARDs) are the first choice drugs in the treatment of rheumatoid arthritis, many patients still take nonsteroidal anti-inflammatory drugs (NSAIDs) as well. These drugs may cause serious gastric adverse events with continuous usage. Cyclooxygenase-2 (COX2) inhibitors were supposed to have a gastrointestinal (GI) friendly side effect profile. The aim of the study is to compare three therapeutic strategies: conventional NSAIDs, NSAID in combination with proton pump inhibitors (PPIs), and the selective COX2 inhibitor therapy (celecoxib).Methods:A decision tree model was developed, for 1 year, to simulate cohorts within the three arms (NSAIDs, NSAID + PPI, celecoxib). The efficacy of the different active agents of NSAIDs in therapeutically relevant doses was assumed to be the same, consequently differences can be seen in the side effect profile of the drugs. Medical costs, the costs of the side effects (GI, cardiovascular [CV] events), and quality-adjusted life-years (QALYs) were calculated to gain an incremental cost-effectiveness ratio (ICER). Evaluations were made from a third party payer's perspective. We performed one-way deterministic sensitivity analyses; the results were displayed in tornado diagrams.Results:Our model indicates that NSAID + PPI offers extra health gain for extra costs compared with conventional NSAIDs (ICER:14,287 euro/QALY), while it dominates celecoxib because of celecoxib's higher costs and lower effectiveness. According to the sensitivity analyses, QALYs had the highest influence on ICER.Conclusions:Although COX2 inhibitors have elevated GI efficacy compared with NSAIDs, celecoxib seems to be an adequate choice only for a limited group of patients with specific conditions because of the significantly higher price and CV risk profile.

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F. Mahdi, Monther. "Synthesis and Preliminary Pharmacological Evaluation of Aminobenzensulfonamides Derivatives of Mefenamic Acid as a Potential Anti-inflammatory Agents." Iraqi Journal of Pharmaceutical Sciences ( P-ISSN: 1683 - 3597 , E-ISSN : 2521 - 3512) 17, no. 1 (March 30, 2017): 7–15. http://dx.doi.org/10.31351/vol17iss1pp7-15.

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A group of amino derivatives [4-aminobenzenesulfonamide,4-amino-NÂ¹ methylbenzenesulfonamide, or NÂ¹-(4-aminophenylsulfonyl)acetamide] bound to carboxyl group of mefenamic acid a well known nonsteroidal anti-inflammatory drugs (NSAIDs) were designed and synthesized for evaluation as a potential anti-inflammatory agent. In vivo acute anti-inflammatory activity of the final compounds (9, 10 and 11) was evaluated in rat using egg-white induced edema model of inflammation in a dose equivalent to (7.5mg/Kg) of mefenamic acid. All tested compounds produced a significant reduction in paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, the 4-amino-N-methylbenzenesulfonamide derivative (compound 10) exhibited comparable anti-inflammatory activity to diclofenac (3mg/Kg) at times 180-300 minute with the same onset of action. The results of this study indicate that the incorporation of the 4-aminobenzenesulfonamide pharmacophore and its derivatives in to mefenamic acid maintain its anti-inflammatory activity. Key ward: benzenesulfonamide, anti-inflammatory, paw edema, NSAIDs, mefenamic acid

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Yimer, Ebrahim M., Ousman A. Mohammed, and Seid I. Mohammedseid. "Pharmacological Exploitation of Non-Steroidal Anti-inflammatory Drugs as Potential Sources of Novel Antibacterial Agents." Anti-Infective Agents 17, no. 2 (July 5, 2019): 81–92. http://dx.doi.org/10.2174/2211352516666181008114542.

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The ever-increasing threat of bacterial infections and antimicrobial resistance calls for a global effort to deal with this problem. This fast and universal dissemination of antimicrobialresistant bacterial strains resulted in the diminution of therapeutic alternatives for various infectious diseases. Besides, the unaffordability of efficacious antimicrobials coupled with the occurrence of unpleasant adverse effects calls for the exploration of alternative agents with possible antibacterial effect. All these challenges of microbes have posed new drives to the scientific communities. Researchers are now assessing the possible alternative antimicrobial agents for fighting bacterial infections and antimicrobial resistance. Therefore, this review emphasizes on the role of nonsteroidal anti-inflammatory agents as potential sources of novel antibacterial agents on which preliminary studies and randomized controlled trials had been performed. The review also deals with the possible antibacterial mechanism of actions and the likely effects of non-steroidal antiinflammatory drugs when combined along with conventional antibacterial agents.

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Fisher, Courtney L., and Stacie L. Demel. "Nonsteroidal Anti-Inflammatory Drugs: A Potential Pharmacological Treatment for Intracranial Aneurysm." Cerebrovascular Diseases Extra 9, no. 1 (April 30, 2019): 31–45. http://dx.doi.org/10.1159/000499077.

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Background: Saccular intracranial aneurysms (IAs) are outpouchings of the vessel wall of intracranial arteries. Rupture of IAs results in subarachnoid hemorrhage which is associated with high morbidity and mortality. Surgical interventions, such as clipping and coiling, have associated risks. Currently, there are no proven pharmacological treatments to prevent the growth or rupture of IAs. Infiltration of proinflammatory cytokines in response to increased wall sheer stress is a hallmark of IA. Nonsteroidal anti-inflammatory drugs (NSAIDs) are being investigated as potential therapeutic agents for reduction in growth and/or prevention of IA through inhibition of inflammatory pathways. Summary: This review will discuss the role of NSAIDs in attenuating the inflammation that drives IA progression and rupture. There are two main subtypes of NSAIDs, nonselective COX and selective COX-2 inhibitors, both of which have merit in treating IA. Evidence will be presented which shows that NSAIDs inhibit several key inflammatory mediators involved in IA progression including nuclear factor-κB, tumor necrosis factor-α, and matrix metalloproteinases. In addition, the role of NSAIDs in limiting inflammatory cell adhesion to endothelial cells and attenuating endothelial cell senescence will be discussed. Key Messages: There is an abundance of basic science and preclinical data that support NSAIDs as a promising treatment for IA. Additionally, a combination treatment strategy of low-dose aspirin given concomitantly with a selective COX-2 inhibitor may result in a reduced side effect profile compared to aspirin or selective COX-2 inhibitor use alone. Several large clinical trials are currently planned to further investigate the efficacy of NSAIDs as an effective nonsurgical treatment for IAs.

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Kuskov, Andrey, Dragana Nikitovic, Aikaterini Berdiaki, Mikhail Shtilman, and Aristidis Tsatsakis. "Amphiphilic Poly-N-vinylpyrrolidone Nanoparticles as Carriers for Nonsteroidal, Anti-Inflammatory Drugs: Pharmacokinetic, Anti-Inflammatory, and Ulcerogenic Activity Study." Pharmaceutics 14, no. 5 (April 24, 2022): 925. http://dx.doi.org/10.3390/pharmaceutics14050925.

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Nanoparticles are increasingly utilized as drug delivery agents. Previously, we have developed a drug delivery system based on amphiphilic derivatives of poly-N-vinylpyrrolidone (PVP-OD4000) with excellent biocompatibility. In the current study, we assessed the pharmacokinetics, anti-inflammatory profile, and ulcerogenic potential of indomethacin (IMC)-loaded PVP-OD4000 nanoparticles compared to the free drug. Wistar male rats were utilized for a pharmacokinetics study and an anti-inflammatory study. Loaded IMC exhibited a slower elimination rate (p < 0.05) and a higher blood plasma concentration at 8 and 24 h after intraperitoneal injection compared with free IMC. In addition, decreased uptake of loaded IMC in the liver and kidney compared to free IMC (p < 0.05) was detected. Furthermore, PVP-OD4000 nanoparticles loaded with IMC showed an enhanced anti-inflammatory effect compared to free IMC (p < 0.05) in carrageenan-induced and complete Freund’s adjuvant-induced–(CFA) sub-chronic and chronic paw edema treatment (p < 0.01; p < 0.01). Notably, upon oral administration of loaded IMC, animals had a significantly lower ulcer score and Paul’s Index (3.9) compared to the free drug (p < 0.05). The obtained results suggest that IMC loaded to PVP nanoparticles exhibit superior anti-inflammatory activity in vivo and a safe gastrointestinal profile and pose a therapeutic alternative for the currently available NSAIDs’ administration.

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Kuskov, Andrey, Dragana Nikitovic, Aikaterini Berdiaki, Mikhail Shtilman, and Aristidis Tsatsakis. "Amphiphilic Poly-N-vinylpyrrolidone Nanoparticles as Carriers for Nonsteroidal, Anti-Inflammatory Drugs: Pharmacokinetic, Anti-Inflammatory, and Ulcerogenic Activity Study." Pharmaceutics 14, no. 5 (April 24, 2022): 925. http://dx.doi.org/10.3390/pharmaceutics14050925.

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Nanoparticles are increasingly utilized as drug delivery agents. Previously, we have developed a drug delivery system based on amphiphilic derivatives of poly-N-vinylpyrrolidone (PVP-OD4000) with excellent biocompatibility. In the current study, we assessed the pharmacokinetics, anti-inflammatory profile, and ulcerogenic potential of indomethacin (IMC)-loaded PVP-OD4000 nanoparticles compared to the free drug. Wistar male rats were utilized for a pharmacokinetics study and an anti-inflammatory study. Loaded IMC exhibited a slower elimination rate (p < 0.05) and a higher blood plasma concentration at 8 and 24 h after intraperitoneal injection compared with free IMC. In addition, decreased uptake of loaded IMC in the liver and kidney compared to free IMC (p < 0.05) was detected. Furthermore, PVP-OD4000 nanoparticles loaded with IMC showed an enhanced anti-inflammatory effect compared to free IMC (p < 0.05) in carrageenan-induced and complete Freund’s adjuvant-induced–(CFA) sub-chronic and chronic paw edema treatment (p < 0.01; p < 0.01). Notably, upon oral administration of loaded IMC, animals had a significantly lower ulcer score and Paul’s Index (3.9) compared to the free drug (p < 0.05). The obtained results suggest that IMC loaded to PVP nanoparticles exhibit superior anti-inflammatory activity in vivo and a safe gastrointestinal profile and pose a therapeutic alternative for the currently available NSAIDs’ administration.

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Johnson, Deanna L., Tina M. Hisel, and Beth Bryles Phillips. "Effect of Cyclooxygenase-2 Inhibitors on Blood Pressure." Annals of Pharmacotherapy 37, no. 3 (March 2003): 442–46. http://dx.doi.org/10.1345/aph.1c277.

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OBJECTIVE: To evaluate the effect of cyclooxygenase-2 selective inhibitors (CSIs) on blood pressure. DATA SOURCES: Clinical literature accessed through MEDLINE (1966–May 2002). Key search terms included COX-2 selective inhibitors; anti-inflammatory agents, nonsteroidal; celecoxib; rofecoxib; and hypertension. DATA SYNTHESIS: Data from prospective studies on the effects of CSIs on blood pressure are conflicting. Several studies have reported increased blood pressure as an adverse effect of CSIs. CONCLUSIONS: Additional studies are needed to evaluate the effects of CSIs on blood pressure. CSIs should be used with caution in hypertensive patients and blood pressure monitored closely if a CSI is indicated.

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Hugo F. Miranda, Viviana Noriega, Francisca Moreno, Fernando Sierralta, Ramón Sotomayor-Zárate, and Juan Carlos Prieto. "Nitridergic Modulation of COX-2 Efficacy." World Journal of Advanced Research and Reviews 15, no. 2 (August 30, 2022): 044–51. http://dx.doi.org/10.30574/wjarr.2022.15.2.0784.

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Pain is a common unpleasant sensory and emotional experience, in which are frequently used in their treatment the nonsteroidal anti-inflammatory drugs (NSAIDs). A group of agents with antipyretic, analgesic, and anti-inflammatory properties due to the inhibition of cyclooxygenase enzymes (COXs). Among these drugs there are a group of selective inhibitors of COX-2 named coxib that include to parecoxib, celecoxib, rofecoxib and etoricoxib. Pharmacological information on the mechanism of action of coxibs is insufficient to determine the analgesic and anti-inflammatory efficacy of these agents. There are contradictory reports regarding the antinociceptive effects of the various coxibs at the preclinical level as well as the nitridergic modulation of such actions. The objective of the present study was to evaluate the antinociceptive efficacy of parecoxib, rofecoxib, celecoxib, and etoricoxib using the formalin hind paw assay in mice and the possible contribution of the nitridergic system in the efficacy of COX-2 agents. Antinociception was assessed in a murine formalin assay using dose-response curves to coxibs before and after i.p. administration of 5 mg/kg of L-NAME. Coxibs produced dose-dependent analgesia and anti-inflammation. L-NAME administration reduced the analgesic and anti-inflammatory effectiveness of parecoxib, rofecoxib, celecoxib, and etoricoxib. These findings suggest that the effect of these agents, in addition to COX-2 inhibition, would be mediated by other mechanisms, among which nitridergic modulation would be compromised.

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Llewellyn-Jones, CG, MM Johnson, JL Mitchell, A. Pye, VC Okafor, SL Hill, and RA Stockley. "In vivo study of indomethacin in bronchiectasis: effect on neutrophil function and lung secretion." European Respiratory Journal 8, no. 9 (September 1, 1995): 1479–87. http://dx.doi.org/10.1183/09031936.95.08091479.

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Bronchiectasis is associated with sputum containing high levels of the proteolytic enzyme elastase, which is thought to be involved in the pathogenesis of the disease. Agents which inhibit neutrophil function and interfere with neutrophil elastase release may have a beneficial effect on the development and progression of such diseases. We have studied the effects of the nonsteroidal anti-inflammatory agent indomethacin on neutrophil function in nine patients with clinically stable bronchiectasis. All patients remained clinically stable during the study. We observed a significant reduction in peripheral neutrophil chemotaxis to 10 nmol.L-1 N-formyl-methionyl-leucyl-phenylalanine (FMLP) from a mean of 19.86 (SEM 1.35) to 8.46 (0.68) cells.field-1 after 4 weeks of therapy. There was also a significant reduction in fibronectin degradation both by resting and FMLP-stimulated neutrophils, from a mean of 1.90 (0.19) micrograms x 3 x 10(5) cells at the start of therapy to 0.87 (0.08) micrograms after 4 weeks, and from 3.17 (0.35) micrograms to 1.48 (0.05) micrograms, respectively. There was no effect on spontaneous or stimulated superoxide anion generation by neutrophils. Despite the marked changes in peripheral neutrophil function, no adverse effect was observed on viable bacterial load in the bronchial secretions. In addition, there was no difference in sputum albumin, elastase or myeloperoxidase levels, and only minor changes in the chemotactic activity of the sputum. These results suggest that nonsteroidal anti-inflammatory agents have a major effect on peripheral neutrophil function but do not appear to have an adverse effect on bacterial colonization of the airways.

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Li, Jiayang, Yi Kuang, Junfeng Shi, Yuan Gao, Jie Zhou, and Bing Xu. "The conjugation of nonsteroidal anti-inflammatory drugs (NSAID) to small peptides for generating multifunctional supramolecular nanofibers/hydrogels." Beilstein Journal of Organic Chemistry 9 (May 10, 2013): 908–17. http://dx.doi.org/10.3762/bjoc.9.104.

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Here we report supramolecular hydrogelators made of nonsteroidal anti-inflammatory drugs (NSAID) and small peptides. The covalent linkage of Phe–Phe and NSAIDs results in conjugates that self-assemble in water to form molecular nanofibers as the matrices of hydrogels. When the NSAID is naproxen (1), the resultant hydrogelator 1a forms a hydrogel at a critical concentration (cgc) of 0.2 wt % at pH 7.0. Hydrogelator 1a, also acting as a general motif, enables enzymatic hydrogelation in which the precursor turns into a hydrogelator upon hydrolysis catalyzed by a phosphatase at physiological conditions. The conjugates of Phe–Phe with other NSAIDs, such as (R)-flurbiprofen (2), racemic flurbiprofen (3), and racemic ibuprofen (4), are able to form molecular hydrogels, except in the case of aspirin (5). After the conjugation with the small peptides, NSAIDs exhibit improved selectivity to their targets. In addition, the peptides made of D-amino acids help preserve the activities of NSAIDs. Besides demonstrating that common NSAIDs are excellent candidates to promote aromatic–aromatic interaction in water to form hydrogels, this work contributes to the development of functional molecules that have dual or multiple roles and ultimately may lead to new molecular hydrogels of therapeutic agents for topical use.

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Niedermeyer, Michael E., Masanori Okamoto, Kenneth L. Brigham, and Barbara Meyrick. "The Effect of Steroidal and Nonsteroidal Anti-inflammatory Agents on Granulocyte Migration into Bovine Pulmonary Artery Intimal Explants." Experimental Lung Research 10, no. 3 (January 1986): 313–30. http://dx.doi.org/10.3109/01902148609061500.

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Rantanen, Tuomo, Marianne Udd, Teemu Honkanen, Pekka Miettinen, Vesa Kärjä, Lassi Rantanen, Risto Julkunen, Harri Mustonen, Timo Paavonen, and Niku Oksala. "Effect of Omeprazole Dose, Nonsteroidal Anti-inflammatory Agents, and Smoking on Repair Mechanisms in Acute Peptic Ulcer Bleeding." Digestive Diseases and Sciences 59, no. 11 (August 20, 2014): 2666–74. http://dx.doi.org/10.1007/s10620-014-3242-z.

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Theodosis-Nobelos, Panagiotis, Georgios Papagiouvanis, Maria Pantelidou, Panos N. Kourounakis, Chrysoula Athanasekou, and Eleni A. Rekka. "Design, Synthesis and Study of Nitrogen Monoxide Donors as Potent Hypolipidaemic and Anti-Inflammatory Agents." Molecules 25, no. 1 (December 19, 2019): 19. http://dx.doi.org/10.3390/molecules25010019.

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Inflammation and oxidative stress are involved in cardiovascular diseases. Nitrogen monoxide participates in the regulation of endothelial processes. Thus, derivatives of classic nonsteroidal anti-inflammatory drugs (NSAIDs), trolox or cinnamic acids esterified with 2-(nitrooxy)ethanol were designed and studied. It was found that the nitrogen monoxide (NO) releasing activity was comparable to that of S-nitroso-N-acetylpenicillamine. The nitrooxy derivatives decreased potently lipid indices in the plasma of hyperlipidaemic rats (30–85%). All compounds presented increased anti-inflammatory activity in vivo, inhibiting carrageenan-induced rat paw oedema as high as 76%, up to six times higher than that of the parent acids. Lipoxygenase inhibitory activity was significant for most of them, although the parent molecules exerted a minor effect (IC50 > 0.2 mM). Those compounds incorporating an antioxidant structure inhibited rat microsomal membrane lipid peroxidation strongly and possessed radical scavenging activity. These results indicated that the described compounds could act at different targets in multifactorial diseases, further limiting the possible adverse effects of drug combinations.

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Errasti, María E., Néstor O. Caffini, Lilian E. Pelzer, and Alejandra E. Rotelli. "Evaluation of Anti-Inflammatory Activity of Pseudananas macrodontes (Morr.) Harms (Bromeliaceae) Fruit Extract in Rats." Zeitschrift für Naturforschung C 68, no. 11-12 (December 1, 2013): 445–52. http://dx.doi.org/10.1515/znc-2013-11-1203.

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Several species of the family Bromeliaceae are characterized by the production of proteases in unusual amounts, especially in fruits. Bromelain, an extract rich in cysteine endopeptidases obtained from Ananas comosus L., and a few other proteases have been used as anti-inflammatory agents for some years, but bromelain is still mainly being used as alternative and/or complementary therapy to the treatment with glucocorticoids, nonsteroidal antirheumatics, and immunomodulators. In this study, the anti-inflammatory action of a partially purified extract from Pseudananas macrodontes (Morr.) Harms fruits (PPEPm) is presented, whose main components are cysteine endopeptidases. The effect of PPEPm was assessed in carrageenan-induced and serotonin-induced rat paw edema, as well as in the cotton pellet granuloma model. Doses with equal proteolytic activity of PPEPm and bromelain produced significantly similar anti-inflammatory responses in the acute inflammatory models assayed, supporting the hypothesis that proteolytic activity could be responsible for the anti-inflammatory action. On the contrary, comparable anti-inflammatory effects of PPEPm and bromelain in the chronic inflammatory assay required a much lower proteolytic activity content of PPEPm, which could be due to a differential affinity for the protein target involved in this process.

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Zhou, Yong, Elizabeth J. Dial, Rand Doyen, and Lenard M. Lichtenberger. "Effect of indomethacin on bile acid-phospholipid interactions: implication for small intestinal injury induced by nonsteroidal anti-inflammatory drugs." American Journal of Physiology-Gastrointestinal and Liver Physiology 298, no. 5 (May 2010): G722—G731. http://dx.doi.org/10.1152/ajpgi.00387.2009.

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The injurious effect of nonsteroidal anti-inflammatory drugs (NSAIDs) in the small intestine was not appreciated until the widespread use of capsule endoscopy. Animal studies found that NSAID-induced small intestinal injury depends on the ability of these drugs to be secreted into the bile. Because the individual toxicity of amphiphilic bile acids and NSAIDs directly correlates with their interactions with phospholipid membranes, we propose that the presence of both NSAIDs and bile acids alters their individual physicochemical properties and enhances the disruptive effect on cell membranes and overall cytotoxicity. We utilized in vitro gastric AGS and intestinal IEC-6 cells and found that combinations of bile acid, deoxycholic acid (DC), taurodeoxycholic acid, glycodeoxycholic acid, and the NSAID indomethacin (Indo) significantly increased cell plasma membrane permeability and became more cytotoxic than these agents alone. We confirmed this finding by measuring liposome permeability and intramembrane packing in synthetic model membranes exposed to DC, Indo, or combinations of both agents. By measuring physicochemical parameters, such as fluorescence resonance energy transfer and membrane surface charge, we found that Indo associated with phosphatidylcholine and promoted the molecular aggregation of DC and potential formation of larger and isolated bile acid complexes within either biomembranes or bile acid-lipid mixed micelles, which leads to membrane disruption. In this study, we demonstrated increased cytotoxicity of combinations of bile acid and NSAID and provided a molecular mechanism for the observed toxicity. This mechanism potentially contributes to the NSAID-induced injury in the small bowel.

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Junqueira, Laura A., Hudson Polonini, Sharlene Loures, Nádia R. B. Raposo, Anderson O. Ferreira, and Marcos Antônio F. Brandão. "Permeation Efficacy of a Transdermal Vehicle with Steroidal Hormones and Nonsteroidal Anti-inflammatory Agents as Model Drugs." Current Drug Delivery 16, no. 2 (December 14, 2018): 136–41. http://dx.doi.org/10.2174/1567201815666181024141849.

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Background: Transdermal delivery is an alternative route for the administration of drugs. However, it requires the development of vehicles that allow the drugs to cross the layers of the skin and reach the systemic circulation. Objective: In this study, a new transdermal vehicle was evaluated using progesterone, estradiol, estradiol + estriol (Biest) and ketoprofen administered as model drugs. </P><P> Methods: To evaluate the ex vivo permeation of the drugs, the Franz vertical diffusion cell with human skin was used. Results: After 24 h, the vehicle was able to deliver 18.32 µg/cm2 of progesterone and 92.07 µg/cm2 of ketoprofen through the skin to the receptor medium. The permeation percentages were 91%, 78.8%, 48.5%, 73.2%, and 63.6%, respectively, for estradiol, estradiol (Biest), estriol (Biest), progesterone and ketoprofen. For all drugs, sufficient amounts were delivered to achieve a systemic effect, and it was also possible to decrease the amount of emulsion applied. Thus, the vehicle demonstrated a high performance and the possibility of it being used for drugs that present difficulties in regards to administration by the transdermal route.

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Zakaria, Z. A., A. S. Mohamad, M. S. Ahmad, A. F. Mokhtar, D. A. Israf, N. H. Lajis, and M. R. Sulaiman. "Preliminary Analysis of the Anti-Inflammatory Activity of Essential Oils of Zingiber zerumbet." Biological Research For Nursing 13, no. 4 (November 26, 2010): 425–32. http://dx.doi.org/10.1177/1099800410386590.

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Nonsteroidal anti-inflammatory drugs (NSAIDs) have been widely used for the treatment of inflammation. However, despite their effectiveness, most NSAIDs cause various side effects that negatively affect the management of inflammation and, in part, pain. Thus, there is a need to search for new anti-inflammatory agents with few, or no, side effects. Natural products of plant, animal, or microorganism origin have been good sources of new bioactive compounds. The present study was carried out to evaluate the acute and chronic anti-inflammatory activities of the essential oil of the rhizomes of Zingiber zerumbet (Zingiberaceae) using the carrageenan-induced paw edema and cotton pellet-induced granuloma tests, respectively. The effect of the essential oil on inflammatory- and noninflammatory-mediated pain was also assessed using the formalin test. Essential oil of Z. zerumbet, at doses of 30, 100, and 300 mg/kg, was administered intraperitoneally to rats. The substance exhibited significant anti-inflammatory activity both in acute and chronic animal models. The essential oil also inhibited inflammatory- and noninflammatory-mediated pain when assessed using the formalin test. In conclusion, the essential oil of Z. zerumbet possessed anti-inflammatory activity, in addition to its antinociceptive activity, which may explain its traditional uses to treat inflammatory-related ailments.

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Lien, Hsiu-Man, Yu-Yen Wang, Mei-Zi Huang, Hui-Yu Wu, Chao-Lu Huang, Chia-Chi Chen, Shao-Wen Hung, Chia-Chang Chen, Cheng-Hsun Chiu, and Chih-Ho Lai. "Gastroprotective Effect of Anisomeles indica on Aspirin-Induced Gastric Ulcer in Mice." Antioxidants 11, no. 12 (November 24, 2022): 2327. http://dx.doi.org/10.3390/antiox11122327.

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Gastric ulcers are commonly seen in the upper gastrointestinal tract and may be related to the Helicobacter pylori infection and the use of aspirin, a nonsteroidal anti-inflammatory drug (NSAID). Typically, proton-pump inhibitors (PPIs) are used to treat gastric ulcers; however, adverse effects have emerged following long-term treatment. Natural medicines are used as alternative therapeutic agents in the treatment of gastric ulcers, with few side effects. Despite various reports on the anti-H. pylori and anti-gastric cancer activities of Anisomeles indica, its gastroprotective effect on ulcers remains undetermined. This study investigated the protective effect of A. indica on aspirin-induced gastric ulcers in murine models. Our results show that three fractions of ethanol-extracted A. indica inhibited aspirin-induced gastric injury. Among these, A. indica Fraction 1 was observed to enrich ovatodiolide, which effectively diminished gastric acidity and alleviated aspirin-induced inflammation in the stomach. Our results provide evidence that A. indica could be developed as an effective therapeutic agent for gastroprotective purposes.

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Singh, Sumitra, and Bhagwati Devi. "ETHANOMEDICINAL PLANTS WITH ANTI-INFLAMMATORY EFFECT FROM SOUTHERN HARYANA, INDIA: A REVIEW." International Journal of Advanced Research 8, no. 12 (December 31, 2020): 1013–34. http://dx.doi.org/10.21474/ijar01/12248.

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Inflammation is a physiological host response to external challenges or cellular injury such as pathogens, damaged cells or irritants leading to the release of a complex array of inflammatory mediators and aiding the recovery of tissue structure and function.All inflammatory processes develop along a known sequence: locally increased blood supply, leakage of fluid, small molecule or proteins and infiltration of cells.Inflammation is not a synonym for infection, even in case where inflammation is caused by infection, response includes clinical signs of erythema, edema, hyperalgesia and pain. Since the ancient Greek and Roman era five basic symptoms of inflammation have been known i.e, redness, swelling, heat, pain and deranged function are produced by inflammatory agents such as nitric oxide, prostaglandins, bradykinin, serotonin, leukotrienes and histamine. The inflammatory process is a series of events that can be elicited by numerous stimuli such as infectious and thermal or physical injury through years of ingenious synthesis and structural modifications.

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Durant, S., D. Duval, and F. Homo-Delarche. "Effect of exogenous prostaglandins and nonsteroidal anti-inflammatory agents on prostaglandin secretion and proliferation of mouse embryo fibroblasts in culture." Prostaglandins, Leukotrienes and Essential Fatty Acids 38, no. 1 (October 1989): 1–8. http://dx.doi.org/10.1016/0952-3278(89)90140-3.

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Choi, Eunjoo, Francis Sahngun Nahm, Woong Ki Han, Pyung-Bok Lee, and Jihun Jo. "Topical agents: a thoughtful choice for multimodal analgesia." Korean Journal of Anesthesiology 73, no. 5 (October 1, 2020): 384–93. http://dx.doi.org/10.4097/kja.20357.

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For over a thousand years, various substances have been applied to the skin to treat pain. Some of these substances have active ingredients that we still use today. However, some have been discontinued due to their harmful effect, while others have been long forgotten. Recent concerns regarding the cardiovascular and renal risk from nonsteroidal anti-inflammatory drugs, and issues with opioids, have resulted in increasing demand and attention to non-systemic topical alternatives. There is increasing evidence of the efficacy and safety of topical agents in pain control. Topical analgesics are great alternatives for pain management and are an essential part of multimodal analgesia. This review aims to describe essential aspects of topical drugs that physicians should consider in their practice as part of multimodal analgesia. This review describes the mechanism of popular topical analgesics and also introduces the most recently released and experimental topical medications.

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Shtrygol’, S. Yu, O. O. Koiro, O. V. Kudina, T. K. Yudkevych, and T. V. Gorbach. "Comparative analysis of the effect of diclofenac sodium and etoricoxib on energy metabolism in rat liver in the acute general cooling model." Medicni perspektivi 27, no. 4 (December 29, 2022): 51–57. http://dx.doi.org/10.26641/2307-0404.2022.4.271171.

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When the ambient temperature decreases, physiological mechanisms that prevent heat loss are activated. However, under cold stress hypothermia develops, which significantly disrupts the functioning of the body and can be transformed into life-threatening. Preventive use of nonsteroidal anti-inflammatory drugs, especially diclofenac sodium and etoricoxib, has been found to reduce the severity of cold trauma. Given that their frigoprotective effect can accompany the impact on the synthesis of eicosanoids when exposed to low temperatures, it is advisable to study mechanisms for preventing hypothermia independent of cyclooxygenase, particularly the influence on energy metabolism. The aim of the study was to figure out the effect of diclofenac sodium and etoricoxib on the indicators of energy metabolism in the liver of rats after acute general cooling. Experiments were carried out on 28 sexually mature male rats, which were given diclofenac sodium (7 mg/kg), etoricoxib (5 mg/kg), or solvent 30 minutes before cold trauma intragastrically (in the intact control and pathology control groups). Acute hypothermia was caused by exposure of animals for 2 hours at a temperature of -18°C. Rectal temperature was measured before and after acute general cooling. The content of lactate, pyruvate and adenosine triphosphate in the liver was measured and the lactate/pyruvate ratio was calculated. Diclofenac sodium, unlike etoricoxib, was found to significantly reduce the severity of hypothermia. Both nonsteroidal anti-inflammatory drugs prevent energy metabolism disorders caused by exposure to cold, namely, reducing the concentration of lactic acid and the ratio of lactate/pyruvate, increasing the content of pyruvate and adenosine triphosphate in the liver of animals. Etoricoxib normalizes the content of energy metabolism intermediates to their levels in intact animals. Diclofenac sodium has a similar effect, the expression of which is inferior to the selective cyclooxygenase-2 inhibitor. Therefore, when administered prophylactically before acute general cooling, diclofenac sodium effectively prevents hypothermia in rats, surpassing etoricoxib. Etoricoxib completely prevents a decrease in the content of pyruvate and adenosine triphosphate, as well as the accumulation of lactic acid in the liver. Diclofenac sodium is inferior to etoricoxib in its effect on energy metabolism, which indicates other mechanisms of frigoprotective action of a non-selective cyclooxygenase inhibitor. The frigoprotective and energotropic properties of nonsteroidal anti-inflammatory drugs dissociate.

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Iltar, Utku, Fadime Nurcan Alhan, Ece Vural, Ünal Ataş, Hasan Sözel, Ömer Doğan, Ahmet Boduroğlu, Orhan Kemal Yücel, Ozan Salim, and Levent Ündar. "Recurrent arthritis as an unexpected side effect associated with azacitidine in a patient with myelodysplastic syndrome." Journal of Oncology Pharmacy Practice 28, no. 2 (October 12, 2021): 500–503. http://dx.doi.org/10.1177/10781552211049728.

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Introduction Hypomethylating agents have confirmed efficacy for myelodysplastic syndrome and acute myeloid leukemia and are widely used. Although arthralgia is common side effect associated with hypomethylating agents, arthritis has not been reported previously. Case Report We present the first recorded patient with arthritis after azacitidine treatment. The patient we presented here had severe cytopenias requiring transfusion with erythrocyte and platelet suspensions, and a complete hematological response was obtained for myelodysplastic syndrome after three cycles of azacitidine (AZA) treatment. However, interestingly, after each AZA treatment cycle, the patient had recurrent attacks of arthritis. Management and outcomes The episodes of arthritis were possibly acute flares of pre-existing crystal-induced arthritis, as exhibited with azacitidine treatments and were managed effectively with nonsteroidal anti-inflammatory drugs. Discussion Because it is a rare condition, clinicians should not overlook AZA as a possible cause of arthritis exacerbations when arthritis of unknown etiology develops in patients treated with AZA.

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Salandari, Sajedeh, Tahoora Shomali, Najmeh Mosleh, and Saeed Nazifi. "A comparative study on anti-inflammatory drug combinations in domestic pigeons with experimentally induced acute arthritis." Acta Veterinaria Hungarica 67, no. 4 (December 2019): 588–601. http://dx.doi.org/10.1556/004.2019.058.

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The study compares the effect of one-time administration of nonsteroidal and/or steroidal anti-inflammatory combinations by topical or intramuscular (IM) routes to pigeons with monosodium urate (MSU)-induced arthritis. Forty-five adult domestic pigeons were assigned into nine equal groups: NC, negative control; PC, positive control with arthritis; sham, sham control; T1, meloxicam + hydrocortisone; T2, dexamethasone + piroxicam; T3, meloxicam + dexamethasone; T4, hydrocortisone + piroxicam; T5, dexamethasone + hydrocortisone; T6, meloxicam + piroxicam. Arthritis was also induced in T1 to T6 birds. Meloxicam and dexamethasone were administered by IM injection and the other drugs topically right after the induction of arthritis. Different drug combinations significantly decreased one-leg standing time. Induction of arthritis significantly increased TNF-α and IL-6 levels in synovial fluid and serum corticosterone and epinephrine in the PC group. Administration of drugs to birds of Groups T1 and T5 did not significantly change corticosterone concentration, while all different drug combinations decreased epinephrine level. Drug combinations that demonstrated better analgesic effect more strongly reduced serum epinephrine concentration. Meloxicam + hydrocortisone was the most effective combination in reducing inflammatory cytokines. In conclusion, one-time combination therapy with anti-inflammatory agents was effective in the acute management of inflammatory pain due to MSU-induced arthritis in pigeons, even by the topical route.

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Diana, Frank J., Karen Veronich, and Amrit L. Kapoor. "Binding of Nonsteroidal Anti-Inflammatory Agents and Their Effect on Binding of Racemic Warfarin and Its Enantiomers to Human Serum Albumin." Journal of Pharmaceutical Sciences 78, no. 3 (March 1989): 195–99. http://dx.doi.org/10.1002/jps.2600780304.

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Belhocine, Mansouria, Abdelkader Homrani, Fatima Azzouz Azzouz, and Chahrazed Sakmeche. "Gastro-protective effects of camel milk on indomethacin-induced peptic ulcer in Wistar rats." South Asian Journal of Experimental Biology 7, no. 2 (January 9, 2018): 42–56. http://dx.doi.org/10.38150/sajeb.7(2).p42-56.

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Gastric ulcer associated with the use of nonsteroidal anti-inflammatory drugs (NSAIDs) and low-dose aspirin is a major public health problem. The present study was undertaken to determine the camel milk antioxidant activity, tested on DPPH, and its gastro-protective effect, investigated in Wistar rats sub-jected to gastric ulcer induced by a nonsteroidal anti-inflammatory agent, indomethacin. The study was performed on 20 adult male Wistar rats divided into 4 groups of 5 rats each. The negative control group received distilled water, the positive control group received indomethacin, the standard group received ranitidine and the fourth group was pretreated with raw camel milk, for 15 days respectively. On the 16th day, the indomethacin was ad-ministered to all rats except those of the negative control group. The ulcerogenic effect of indomethacin was highly significant, evidenced by a large number of ulcer lesions, a remarkably high ulcer index, and an important decrease in adherent gastric mucus. Camel milk resulted in significant gastro-protection compared to indomethacin ulcerated rats as manifested by significant decrease in ulcerative lesions number, and the ulcer index with a restored gastric mucus wall. The camel milk protection percentage is close to that of ranitidine. Additionally, in indomethacin-injured rats an increase in white blood cells, granulocytes, serum transaminases, and hemoglobin levels with a lowering in red blood cells were reported. These physiological disturbances were recovered by camel milk. Camel milk seemed to have gastro-protective effect, probably through its strong antioxidant activity, and may be recommended to patients with arthritis.

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Allahverdi, Ertuğrul, Tülay Diken Allahverdi, and Sevil Vural. "Comparison of Ellagic Acid and NSAI Agents in the Treatment of Achilles Tendon Lacerations: An Experimental Study in Rabbits." International Surgery 104, no. 11-12 (November 1, 2019): 575–81. http://dx.doi.org/10.9738/intsurg-d-19-00007.1.

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Objective Although Achilles tendon ruptures can have many causes, they are known to develop most commonly with trauma. Nonsteroidal anti-inflammatory drugs (NSAID) and low doses of corticosteroids are used in the medical treatment of tendon ruptures. Ellagic acid (EA), which also has an anti-inflammatory effect, has been reported to show its effect via cyclooxygenase 2 (COX2) inhibition as well. The effects of EA and diclofenac sodium on tendon healing were compared in this study. Methods We used a total of 18 male New Zealand rabbits in 3 groups with 6 in each. The study was performed under general anesthesia with a xylazine-ketamine combination. After a defect was created in the right Achilles tendon of all the rabbits, group I was administered diclofenac sodium and group II was administered EA for 1 week, whereas the control group (group III) was not administered anything. Postoperative follow-up was provided for all groups. Results Euthanasia was performed in all subjects at the end of the eighth week, and the tendons were compared in terms of macroscopic and histopathologic features and tensile resistance. Although there was no statistically significant difference in the tensile resistance Newton values of group I and group II, these values were higher than in the control group, and the NSAI group values were statistically significantly higher than in the control group. Conclusions We concluded that EA and NSAIs could be effective in the recovery of tendon integrity and tensile strength and increasing the movement capacity in pathology caused by tendon damage because of their anti-inflammatory features.

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Balta, I., H. Simsek, and GG Simsek. "Flurbiprofen-induced generalized bullous fixed drug eruption." Human & Experimental Toxicology 33, no. 1 (May 23, 2013): 106–8. http://dx.doi.org/10.1177/0960327113489048.

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Fixed drug eruption (FDE) is an unusual drug-related side effect that results in recurrent lesions whenever the causative drugs are used. FDEs usually occur as a single, sharply demarcated, round erythematous patch or plaque, occasionally with localized bullae. The most common offending agents include antimicrobials, nonsteroidal anti-inflammatory drugs, and antiepileptics. There are some reports where contact dermatitis and cutaneous vasculitis have been associated with the use of flurbiprofen. We present the case of a 50-year-old man with flurbiprofen-induced generalized bullous FDE. To the best of our knowledge, the most serious form of FDE, the generalized bullous FDE, to be caused by flurbiprofen has not been reported previously.

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Loewen, Peter S. "Review of the selective COX-2 inhibitors celecoxib and rofecoxib: focus on clinical aspects." CJEM 4, no. 04 (July 2002): 268–75. http://dx.doi.org/10.1017/s1481803500007508.

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ABSTRACT:The selective cyclooxygenase-2 (COX-2) inhibitors celecoxib and rofecoxib were designed to have similar efficacy but less gastrointestinal toxicity than traditional nonsteroidal anti-inflammatory drugs (NSAIDs). Their efficacy has been demonstrated in the treatment of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, postoperative dental pain and dysmenorrhea. These agents produce fewer endoscopic ulcers, symptomatic ulcers and gastrointestinal bleeds than traditional NSAIDs; although the absolute benefit is small and the gastropreserving effect is negated by concurrent use of low-dose aspirin for cardiovascular risk reduction. Nephrotoxicity and hyptertension remain concerns with COX-2 inhibitors, as they are with traditional NSAIDs. COX-2 inhibitors may be safe alternatives to traditional NSAIDs for patients with aspirin-sensitive asthma.

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Journal articles on the topic 'Nonsteroidal anti-inflammatory agents Physiological effect'

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