The use of cyclooxygenase-2 (COX-2) selective inhibitors has been recommended to reduce the risk of upper and lower gastrointestinal adverse events. However, it is not clear whether the long-term use of COX-2 inhibitors reduces the risk of gastrointestinal injury. We report the case of a 60-year-old woman with rheumatoid arthritis who had ongoing anemia and intermittent tarry stools after the long-term use of meloxicam, a COX-2 selective inhibitor. Although gastrointestinal injuries were suspected, the findings of gastroduodenoscopy and ileocolonoscopy were normal. However, capsule endoscopy revealed multiple circumferential ulcers with bleeding in the small bowel. With the patient requiring continued meloxicam use, misoprostol, a prostaglandin (PG) analog and rebamipide, an endothelial PG inducer and cytoprotective agents were prescribed for the ulcers. After treatment, her anemia improved promptly, but it relapsed after she stopped regular use of these drugs. However, the anemia improved again after resumption of treatment. In conclusion, the long-term use of a COX-2 selective inhibitor may induce small intestinal injuries and multiple circumferential ulcers. Combination therapy with misoprostol and rebamipide may be useful for treating COX-2 selective inhibitor-induced anemia and small intestinal injuries.
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http://dx.doi.org/10.1007/s12328-012-0286-5 | DOI Listing |
Curr Med Chem
January 2025
Department of Pharmacy, Forman Christian College, Lahore, 54600, Pakistan.
Introduction: Non-steroidal anti-inflammatory drugs are associated with severe gastrointestinal irritation upon prolonged use, largely due to their carboxylic (-- COOH) functional group.
Aim: To address this issue, we aimed to synthesize diclofenac conjugates with glucosamine and chitosan, converting the -COOH group into an amide (-CONH-) via a mechanochemical, environmentally friendly method.
Method: In this study, diclofenac acid was first converted to its acid chloride using thionyl chloride under mechanochemical conditions and subsequently reacted with glucosamine base and chitosan.
BMB Rep
January 2025
Division of Rheumatology, Regional Rheumatoid & Degenerative Arthritis Center, Chungnam National University Hospital, Daejeon 35015, Korea.
Spondyloarthritis (SpA) is a chronic inflammatory disease that leads to ankylosis of the axial skeleton. Celecoxib (cyclooxygenase-2 inhibitor, COX-2i) inhibited radiographic progression in a clinical study of SpA, but in the following study, diclofenac (COX-2 non-selective) failed to show that inhibition. Our study aimed to investigate whether nonsteroidal anti-inflammatory drugs (NSAIDs) inhibited bone progression in SpA, and whether celecoxib had a unique function (independent of the COX-inhibitor), compared with the other NSAIDs.
View Article and Find Full Text PDFInt J Biol Macromol
December 2024
Applied Organic Chemistry Department, National Research Center, Dokki, Cairo 12622, Egypt; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Pharos University in Alexandria, Canal El Mahmoudia St., Alexandria 21648, Egypt. Electronic address:
The current research focuses on the design and synthesis of celecoxib analogues incorporating sulphonamide and pyrazole moieties (4, 5, 6a-e, and 7a-f) with the aim of achieving a broad range of COX-2 selectivity in vitro. Among these, compounds 6b-d, 7a, 7e, and 7d exhibited potent inhibition, with IC values ranging between 0.05 and 0.
View Article and Find Full Text PDFInt J Pharm
December 2024
Department of Biomedical Sciences, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine.
Aim: This study focuses on the design and investigation a transethosomal formulation for enhanced topical delivery and improved analgesic activity of caryophyllene oxide. In addition, this work explores new potential mechanisms of analgesic activity of the active compound including alpha-amino-3-hydroxy-5-methyl-4-isooxazole-propionic acid (AMPA) and Cyclooxygenase 2 (COX-2).
Methods: The transethosomal system containing various caryophyllene concentrations was prepared.
RSC Med Chem
December 2024
Laboratory for Drug Design and Synthesis, Department of Pharmaceutical Sciences and Natural Products, School of Health Sciences, Central University of Punjab Bathinda 151 401 India
A series of 2-(4-bromobenzyl) tethered 4-amino aryl/alkyl-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-]pyrimidines (7a-7u) were designed, synthesized, characterized and screened against a panel of cancer cell lines. Compound 7a, in particular, emerged as a potent antiproliferative agent against FaDu cells (HTB-43) with an IC value of 1.73 μM.
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