Abstract
Cyclooxygenase-1 (COX-1) derived eicosanoids promote gastroprotective mucosal defenses and induce platelet aggregation. By sparing COX-1, COX-2 specific inhibitors provide effective anti-inflammatory and analgesic activity while substantially reducing the risk of peptic ulcer disease and GI bleeding compared to dual COX inhibitors (traditional NSAIDs). Clinical studies of the COX-2-selective inhibitors have demonstrated efficacy equivalent to nonselective NSAIDs with significantly lower rates of GI toxicity. The incidence of endoscopic ulcers in some studies with coxibs has approximated placebo. However, as the detection of endoscopic lesions is not always correlated with symptomatic ulcers and ulcer complications, outcome studies of GI safety were performed. The results of large outcome studies have evaluated rofecoxib and celecoxib in over 39,000 patients with osteoarthritis or rheumatoid arthritis. Results of these studies showed that patients taking a supratherapeutic dose of rofecoxib or celecoxib had significantly lower rates of GI-related adverse events than those taking a nonselective NSAID. The GI safety of coxibs for patients using low dose aspirin concomitantly with a coxib appears to be reduced, particularly with regard to ulcer complications. Such data provide support for the COX-2 hypothesis and demonstrate that coxibs provide effective treatment of pain and inflammation with a reduced risk of gastropathy.
Keywords: nsaids, peptic ulcer disease, cost-effectiveness evaluation, gastrointestinal bleeding
Current Pharmaceutical Design
Title: Gastroduodenal Safety of Cyclooxygenase-2 Inhibitors
Volume: 9 Issue: 27
Author(s): James M. Scheiman
Affiliation:
Keywords: nsaids, peptic ulcer disease, cost-effectiveness evaluation, gastrointestinal bleeding
Abstract: Cyclooxygenase-1 (COX-1) derived eicosanoids promote gastroprotective mucosal defenses and induce platelet aggregation. By sparing COX-1, COX-2 specific inhibitors provide effective anti-inflammatory and analgesic activity while substantially reducing the risk of peptic ulcer disease and GI bleeding compared to dual COX inhibitors (traditional NSAIDs). Clinical studies of the COX-2-selective inhibitors have demonstrated efficacy equivalent to nonselective NSAIDs with significantly lower rates of GI toxicity. The incidence of endoscopic ulcers in some studies with coxibs has approximated placebo. However, as the detection of endoscopic lesions is not always correlated with symptomatic ulcers and ulcer complications, outcome studies of GI safety were performed. The results of large outcome studies have evaluated rofecoxib and celecoxib in over 39,000 patients with osteoarthritis or rheumatoid arthritis. Results of these studies showed that patients taking a supratherapeutic dose of rofecoxib or celecoxib had significantly lower rates of GI-related adverse events than those taking a nonselective NSAID. The GI safety of coxibs for patients using low dose aspirin concomitantly with a coxib appears to be reduced, particularly with regard to ulcer complications. Such data provide support for the COX-2 hypothesis and demonstrate that coxibs provide effective treatment of pain and inflammation with a reduced risk of gastropathy.
Export Options
About this article
Cite this article as:
Scheiman M. James, Gastroduodenal Safety of Cyclooxygenase-2 Inhibitors, Current Pharmaceutical Design 2003; 9 (27) . https://dx.doi.org/10.2174/1381612033454018
DOI https://dx.doi.org/10.2174/1381612033454018 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Cytotoxicity and Anti-Inflammatory Effects of Polyherbal Formulations, Joint Pain Spl and Rumalaya Forte on Lipopolysaccharide Induced Inflammation in IC-21 Macrophages
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry The Relevance of Supplemental Vitamin D in Malignancies
Anti-Cancer Agents in Medicinal Chemistry p53 Peptide Prevents LITAF-Induced TNF-Alpha-Mediated Mouse Lung Lesions and Endotoxic Shock
Current Molecular Medicine Multitarget Opioid/Non-opioid Ligands: A Potential Approach in Pain Management
Current Medicinal Chemistry Endocarditis Due to Salmonella Enterica Subsp. Arizonae in a Patient with Sickle Cell Disease: A Case Report and Review of the Literature
Cardiovascular & Hematological Disorders-Drug Targets 2-Arylindoles: A Privileged Molecular Scaffold with Potent, Broad-Ranging Pharmacological Activity
Current Medicinal Chemistry Preface
Current Pharmaceutical Design Patient Attitudes Toward Western Medicine and the Future of Chinese Medicine for Spondyloarthritis
Current Rheumatology Reviews Application of Quantum Dots in Drug Delivery
Nanoscience & Nanotechnology-Asia Antiproliferative Efficacy of Angiotensin II Receptor Blockers in Prostate Cancer
Current Cancer Drug Targets Role of Transglutaminase-Catalyzed Reactions in the Post-Translational Modifications of Proteins Responsible for Immunological Disorders
Inflammation & Allergy - Drug Targets (Discontinued) Folate Nutrigenetics: A Convergence of Dietary Folate Metabolism, Folic Acid Supplementation, and Folate Antagonist Pharmacogenetics
Drug Metabolism Letters Fabrication, In vitro and In vivo Characterization of Solid Dispersion- Microsphere Controlled Release System for Lornoxicam
Nanoscience & Nanotechnology-Asia Diagnostic Role of Survivin in Rheumatoid Arthritis: A Systematic Review
Current Rheumatology Reviews Immunotherapy with Peptides in Systemic Lupus Erythematosus
Current Medicinal Chemistry Creating Chemical Diversity to Target Protein Kinases
Combinatorial Chemistry & High Throughput Screening Local Use-Dependent Sleep; Synthesis of the New Paradigm
Current Topics in Medicinal Chemistry Systemic Redox Biomarkers in Neurodegenerative Diseases
Current Drug Metabolism Autophagy Modulators and Neuroinflammation
Current Medicinal Chemistry Colchicine, Biologic Agents and More for the Treatment of Familial Mediterranean Fever. The Old, the New, and the Rare
Current Medicinal Chemistry