Patients with osteoarthritis make up the largest group of users of nonsteroidal anti-inflammatory drugs (NSAIDs), but the effects of these agents on the gastrointestinal mucosa of such patients have not been well studied. This article describes a short-term comparison of two widely used NSAIDs, diflunisal and ibuprofen, in patients requiring these medications for their osteoarthritis. Efficacy, tolerability, and endoscopically documented effects of these drugs on the gastric and duodenal mucosa were assessed. Consenting, eligible patients were randomly assigned to one of the two study drugs for a two-week course. Clinical assessments were made after each week of treatment. Fiberoptic endoscopy and laboratory tests were performed before and after the treatment period. Thirty patients completed the study: 16 received diflunisal and 14 received ibuprofen. Similar improvements in pain, joint mobility, functional capacity, and joint swelling and tenderness were observed in both treatment groups. Transient, mild abdominal cramping was reported by two patients in each group; one patient receiving ibuprofen complained of transient dizziness. No patient withdrew from the study because of side effects. Follow-up endoscopy revealed slight (grade 1) changes in the gastric mucosa of two patients in each treatment group. An additional patient in the ibuprofen group had gastric erosions (grade 2) at the end of the study. Endoscopic changes were not correlated with symptoms. Diflunisal and ibuprofen were found to be similarly effective and well tolerated in the treatment of osteoarthritis. Their use may be associated with some gastrointestinal side effects even during short-term use.
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Int J Biol Macromol
December 2024
Department of Chemistry, Coimbra Chemistry Centre-Institute of Molecular Sciences (CQC-IMS), University of Coimbra, Rua Larga, 3004-535 Coimbra, Portugal. Electronic address:
Lapachol (LAP), a natural 1,4-naphthoquinone used in popular medicine in South America, is an antioxidant and antimicrobial compound in teas and infusions and used as a food additive; however, its interactive profile with the main protein carrier of compounds in the human bloodstream (human serum albumin, HSA) was not still characterized. Additionally, the impact of LAP in binding clinically drugs to albumin is still unknown. Thus, the present work describes the interaction HSA:LAP using different biophysical techniques, i.
View Article and Find Full Text PDFMol Pharm
May 2024
Department of Chemistry, Faculty of Sciences, UNESP─São Paulo State University, Bauru 17033-360, São Paulo, Brazil.
The molecular structures of nonsteroidal anti-inflammatory drugs (NSAIDs) vary, but most contain a carboxylic acid functional group (RCOOH). This functional group is known to be related to the mechanism of cyclooxygenase inhibition and also causes side effects, such as gastrointestinal bleeding. This study proposes a new role for RCOOH in NSAIDs: facilitating the interaction at the binding site II of serum albumins.
View Article and Find Full Text PDFPharmaceuticals (Basel)
March 2021
Department of Chemical Engineering and Analytical Chemistry, Faculty of Chemistry, University of Barcelona, Martí i Franquès 1-11, 08028 Barcelona, Spain.
The interaction between drugs and transport proteins, such as albumins, is a key factor in drug bioavailability. One of the techniques commonly used for the evaluation of the drug-protein complex formation is fluorescence. This work studies the interaction of human serum albumin (HSA) with four non-steroidal anti-inflammatory drugs (NSAIDs)-ibuprofen, flurbiprofen, naproxen, and diflunisal-by monitoring the fluorescence quenching when the drug-albumin complex is formed.
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