Gastrointestinal effects of COX-2 inhibitors
- 1 July 1999
- journal article
- Published by Informa Healthcare in Expert Opinion on Investigational Drugs
- Vol. 8 (7) , 963-971
- https://doi.org/10.1517/13543784.8.7.963
Abstract
The developing popularity of non-steroidal anti-inflammatory drugs (NSAIDs) over the last 100 years has been paralleled by an increase in associated complications, particularly affecting the gastrointestinal (GI) tract [1]. Over this period, there have been several attempts to develop less toxic NSAIDs, most of which have been unsuccessful. Since the discovery that the enzyme cyclooxygenase (COX) exists as two isoforms, the largely constitutive COX-1 and the mainly inducible COX-2, much interest has centred on the development of drugs capable of selectively inhibiting COX-2. Early studies that investigated specific COX-2 inhibitors (with no effect on the COX-1 isoform over the whole range of concentrations achieved in clinical usage) are encouraging, as they demonstrate that these drugs have fewer effects on gastroduodenal mucosa than standard NSAIDs given at equivalent doses. Further clinical experience with these agents outside trial settings and additional studies to assess the role of COX-2 when induced in the GI tract are needed, before such agents can be safely recommended for widespread prescribing.Keywords
This publication has 40 references indexed in Scilit:
- Characterization of Prostaglandin G/H Synthase 1 and 2 in rat, dog, monkey, and human gastrointestinal tractsGastroenterology, 1996
- Inducible isoforms of cyclooxygenase and nitric-oxide synthase in inflammation.Proceedings of the National Academy of Sciences, 1994
- Gastrointestinal Damage Associated with the Use of Nonsteroidal Antiinflammatory DrugsNew England Journal of Medicine, 1992
- Nature and time‐course of piroxicam‐induced injury to human gastric mucosaAlimentary Pharmacology & Therapeutics, 1989
- Nonsteroidal Anti-Inflammatory Drugs Activate Quiescent Inflammatory Bowel DiseaseAnnals of Internal Medicine, 1987
- RISING FREQUENCY OF ULCER PERFORATION IN ELDERLY PEOPLE IN THE UNITED KINGDOMThe Lancet, 1986
- Enteritis and colitis associated with mefenamic acid.BMJ, 1983
- Upper gastrointestinal disease in rheumatoid arthritisDigestive Diseases and Sciences, 1974
- Inhibition of Prostaglandin Synthesis as a Mechanism of Action for Aspirin-like DrugsNature New Biology, 1971
- GASTROSCOPIC OBSERVATION OF THE EFFECT OF ASPIRIN AND CERTAIN OTHER SUBSTANCES ON THE STOMACHThe Lancet, 1938