A series of 1,2,5-trisubstituted 4(1H)-pyridinone derivatives (7-14) were synthesised by using 4-pyrone derivatives with primary amines in ethanol. The structures of the synthesised compounds were confirmed by analytical and spectral data (UV, IR and 1H-NMR and microanalysis). Analgesic and antiinflammatory activities of the synthesised compounds were investigated by acetic acid-induced writhing syndrome and carrageenan rat paw edema tests. All of the test compounds exhibited higher analgesic activities than acetyl salicylic acid and showed higher antiinflammatory activities than indomethacin. The anti-inflammatory activity and gastric ulceration potential of the compounds were tested using indomethacin as reference drug.
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http://dx.doi.org/10.1016/s0223-5234(02)01390-9 | DOI Listing |
The opioid crisis has been an issue in the United States since the mid-1990s, claiming numerous lives and presenting a significant challenge to health care clinicians. Various preoperative, intraoperative, and postoperative strategies aimed at reducing opioid consumption can be used by orthopaedic surgeons to help minimize this crisis. Preoperative screening tools can help identify patients at risk for prolonged opioid use, allowing for tailored interventions and counseling.
View Article and Find Full Text PDFMultimodal analgesia and anesthesia have become the gold standard in total joint arthroplasty to reduce postoperative pain and opioid consumption and minimize complications associated with opioid use. There are several elements in an effective multimodal protocol, including oral medications, periarticular injection, regional nerve blocks, and spinal and general anesthesia. Many nonopioid medications are often used, such as acetaminophen and NSAIDs.
View Article and Find Full Text PDFVet Med Sci
January 2025
Department of Medical Pharmacology, Faculty of Medicine, Ataturk University, Erzurum, Turkey.
The present study aimed to unveil the gastroprotective potential of Vaccinium macrocarpon (VM) extract and its mechanism of action against indomethacin (INDO)-induced gastric ulcers in rats. To achieve this goal, rats were pretreated with either omeprazole (20 mg/kg) or VM (100 mg/kg) orally for 14 consecutive days. Gastric tissue samples were collected and various parameters were evaluated to understand the mechanism of VM's action, including the levels of superoxide dismutase, malondialdehyde, glutathione, CAT and transforming growth factor beta (TGF-β), as well as the mRNA expression levels of tumour necrosis factor alpha, interleukin 1 beta, nuclear factor kappa B (NF-κB) and inhibitor kappa B (IκB).
View Article and Find Full Text PDFAnn Agric Environ Med
December 2024
Department of Experimental Pharmacology, Institute of Rural Health, Lublin, Poland.
Introduction And Objective: The aim of the study was to investigate the effect of bee venom on the activity of two analgesics: ketoprofen (a non-steroidal anti-inflammatory drug) and tramadol (an opioid drug) in the acute thermal pain model (hot-plate test) in mice.
Material And Methods: Linear regression analysis was used to evaluate the dose-response relationship between logarithms of drug doses and their resultant maximum possible anti-nociceptive effects in the mouse hot-plate test. Doses that increased the anti-nociceptive effect by 20% (ED values) for bee venom, ketoprofen and tramadol, and their combination were calculated from linear equations.
Allergy Asthma Proc
January 2025
From the Division of Allergy and Immunology, Department of Medicine, University of California San Diego, La Jolla, California and.
Idiopathic non-mast cell angioedema (INMA) is a rare disease typified by recurrent attacks of cutaneous and subcutaneous swelling. Every attack carries the potential for severe morbidity and, in the case of laryngeal involvement, mortality. Whereas therapies approved for hereditary angioedema (HAE) have been used in the care of patients with INMA, little is known with regard to their efficacy for the treatment of this disease.
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