The murky world of the COX-2-selective agents

Inflammopharmacology

Volumn 13, Issue 4, 2005, Pages 381-393

  Bjarnason, Ingvar ^a   Thjodleifsson, Bjarni ^b  

^a KING'S COLLEGE LONDON   (United Kingdom)

^b LANDSPITALI UNIVERSITY HOSPITAL   (Iceland)

Author keywords

(COX 2) selective agents; Analgesics; Cyclo oxygenase 2 (COX 2)

Indexed keywords

CELECOXIB; CYCLOOXYGENASE 2 INHIBITOR; FLOSULIDE; LUMIRACOXIB; MISOPROSTOL; NONSTEROID ANTIINFLAMMATORY AGENT; ROFECOXIB;

ANALGESIC ACTIVITY; ANTIINFLAMMATORY ACTIVITY; DIGESTIVE SYSTEM PERFORATION; DRUG FATALITY; DRUG MECHANISM; DRUG MONITORING; DRUG SELECTIVITY; DRUG TOLERABILITY; DRUG WITHDRAWAL; DYSPEPSIA; GASTROINTESTINAL SYMPTOM; GASTROINTESTINAL TOXICITY; HUMAN; IN VITRO STUDY; MUSCULOSKELETAL DISEASE; PEPTIC ULCER BLEEDING; PRESCRIPTION; PRIORITY JOURNAL; REVIEW; STOMACH INJURY; STOMACH ULCER; TREATMENT OUTCOME;

ANIMALS; ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; CYCLOOXYGENASE 2; CYCLOOXYGENASE 2 INHIBITORS; DYSPEPSIA; HISTORY, 20TH CENTURY; HUMANS; STOMACH ULCER; SUBSTRATE SPECIFICITY;

EID: 27744436547     PISSN: 09254692     EISSN: None     Source Type: Journal    
DOI: 10.1163/156856005774415592     Document Type: Review

References (76)

1. Aabakken, L., Weberg, R., Lygren, I., et al. (1991). Gastrointestinal bleeding: dyspeptic symptoms and clinical course in relation to use of non-steroidal antiinflammatory drugs, Scand. J. Rheumatol. 20, 366-369.
2. Adams, S. S. and Cobb, R. (1958). A possible basis for the anti-inflammatory activity of salicylates and other non-hormonal anti-rheumatic drugs, Nature 181, 773-774.
3. Adams, S. S., Bough, R. G., Cliffe, E. E., et al. (1970). Some aspects of the pharmacology, metabolism, and toxicology of ibuprofen. I. Pharmacology and metabolism, Rheumatol. Phys. Med. 10 (Suppl. 10), 9-26.
4. Adams, S. S., McCullough, K. F. and Nicholson, J. S. (1975). Some biological properties of flurbiprofen, an anti-inflammatory, analgesic and antipyretic agent, Arzneimittelforschung 25, 1786-1791.
5. Allison, M. C., Howatson, A. G., Torrance, C. J., et al. (1992). Gastrointestinal damage associated with the use of nonsteroidal anti-inflammatory drugs, N. Engl. J. Med. 327, 749-754.
6. Armstrong, C. P. and Blower, A. L. (1987). Nonsteroidal anti-inflammatory drugs and life threatening complications of peptic ulcer disease, Gut 28, 527-532.
7. Atherton, C., Jones, J., McKaig, B., et al. (2004). Pharmacology and gastrointestinal safety of lumiracoxib, a novel cyclooxygenase-2-selective inhibitor: an intigrated study, Clin. Gastroenterol. Hepatol. 2, 113-120.
8. Bjarnason, I., Hayllar, J., Macpherson, A. J., et al. (1993). Side effects of nonsteroidal anti-inflammatory drugs on the small and large intestine, Gastroenterology 104, 1832-1847.
9. Bjarnason, I., Macpherson, A., Rothman, H., et al. (1997). A randomised, double blind, crossover comparative endoscopy study on the gastroduodenal tolerability of a highly specific cyclooxygenase-2 inhibitor, flosulide, and naproxen, Scand. J. Gastroenterol. 32, 126-130.
10. Bjarnason, I., Scarpignato, C., Takeuchi, J., et al. (2005). Determinants of the short-term gastric damage caused by NSAIDs in man, submitted.
11. Bombardier, C., Laine, L., Reicin, A., et al. (2000). Comparison of upper gastrointestinal toxicity of rofecoxib and naproxen in patients with rheumatoid arthritis. VIGOR Study Group, N. Engl. J. Med. 343, 1520-1528.
12. Chan, F. K. L., Hung, L. C. T., Suen, B. Y., et al. (2002). Celecoxib versus diclofenac and omeprazole in reducing the risk of recurrent ulcer bleeding in patients with arthritis, N. Engl. J. Med. 347, 2104-2110.
13. Chan F. K., Hung, L. C., Suen, B. Y., et al. (2004). Celecoxib versus diclofenac plus omeprazole in high-risk arthritis patients: results of a randomized double-blind trial, Gastroenterology 127, 1038-1043.
14. Emery, P., Zeidler, H., Kvien, T. K., et al. (1999). Celecoxib versus diclofenac in long-term management of rheumatoid arthritis: randomised double-blind comparison, Lancet 354, 2106-2111.
15. Fiorucci, S., Santucci, L., Wallace, J. L., et al. (2003). Interaction of a selective cyclooxygenase-2 inhibitor with aspirin and NO-releasing aspirin in the human gastric mucosa, Proc. Natl. Acad. Sci. USA 100, 10937-10941.
16. Fries, J. F., Miller, S. R., Spitz, P. W., et al. (1989). Toward an epidemiology of gastropathy associated with non-steroidal anti-inflammatory drug use, Gastroenterology 96 (Suppl.), 647-655.
17. Fries, J. F., Williams, C. A., Bloch, D. A., et al. (1991). Nonsteroidal anti-inflammatory drug-associated gastropathy: incidence and risk factor models, Am. J. Med. 91, 213-222.
18. Goldstein, J. L., Correa, P., Zhao, W. W., et al. (2001). Reduced incidence of gastroduodenal ulcers with celecoxib, a novel cyclooxygenase-2 inhibitor, compared to naproxen in patients with arthritis, Am. J. Gastroenterol. 96, 1019-1027.
19. Goldstein, J. L., Eisen, G. M., Burke, T. A., et al. (2002). Dyspepsia tolerability from the patients' perspective: a comparison of celecoxib with diclofenac, Aliment. Pharmacol. Ther. 16, 819-827.
20. Graham, D. Y. (1996). Famotidine to prevent peptic ulcer caused by NSAIDs, N. Engl. J. Med. 335, 1322-1323.
21. Griffin, M. R., Ray, W. A. and Schaffner, W. (1998). Non-steroidal anti-inflammatory drug use and death from peptic ulceration, Ann. Int. Med. 109, 359-363.
22. Harris, S. I., Kuss, M., Hubbard, R. C., et al. (2001). Upper gastrointestinal safety evaluation of parecoxib sodium, a new parenteral cyclooxygenase-2-specific inhibitor, compared with ketorolac, naproxen, and placebo, Clin. Ther. 23, 1422-1428.
23. Hawkey, C. J. (1990). Non steroidal anti-inflammatory drugs and peptic ulcers, Br. Med. J. 300, 278-284.
24. Hawkey, C. J. (1999). COX-2 inhibitors, Lancet 353, 301-314.
25. Hawkey, C., Laine, L., Simon, T., et al. (2000). Comparison of the effect of rofecoxib (a cyclooxygenase 2 inhibitor), ibuprofen, and placebo on the gastroduodenal mucosa of patients with osteoarthritis: a randomized, double-blind, placebo-controlled trial, Arthritis Rheum. 43, 370-377.
26. Hawkey, C. J., Laine, L., Simon, T., et al. (2003). Incidence of gastroduodenal ulcers in patients with rheumatoid arthritis after 12 weeks of rofecoxib, naproxen, or placebo: a multicentre, randomised, double blind study, Gut 52, 820-826.
27. Hawkey, C. J., Farkouh, M., Gitton, X., et al. (2004a). Therapeutic arthritis research and gastrointestinal event trial of lumiracoxib - study design and patient demographics, Aliment. Pharmacol. Ther. 20, 51-63.
28. Hawkey, C. J., Svoboda, P., Fiedorowicz-Fabrycy, I. F., et al. (2004b). Gastroduodenal safety and tolerability of lumiracoxib compared with Ibuprofen and celecoxib in patients with osteoarthritis, J. Rheumatol. 31, 1804-1810.
29. Henry, D., Dobson, A. and Turner C. (1993). Variability in the risk of major gastrointestinal complications from nonsteroidal anti-inflammatory drugs, Gastroenterology 105, 1078-1088.
30. Henry, D., Lim, L. L.-Y., Rodrigues, L. A. G., et al. (1996). Variability in risk of gastrintestinal complications with individual non-steroidal anti-inflammatory drugs: results of a collaborative meta-analysis, Br. Med. J. 312, 1563-1566.
31. Henry, D., Drew, A. and Beuzeville, S. (1997). Adverse drug reactions in the gastrointestinal system attributed to ibuprofen, in: Safety and Efficacy of Non-Prescription (OTC) Analgesics and NSAIDs, Rainsford, K. D. and Powanda, M. C. (Eds), pp. 19-46. Kluwer, Dordrecht.
32. Holvoet, J., Terriere, L., Van Hee, W., et al. (1991). Relation of upper gastrointestinal bleeding to non-steroidal anti-inflammatory drugs and aspirin: a case-control study, Gut 32, 730-734.
33. Hunt, R. H., Harper, S., Watson, D. J., et al. (2003a). The gastrointestinal safety of the COX-2-selective inhibitor etoricoxib assessed by both endoscopy and analysis of upper gastrointestinal events, Am. J. Gastroenterol. 98, 1725-1733.
34. Hunt, R. H., Harper, S., Callegary, P., et al. (2003b). Complementary studies of the gastrointestinal safety of the cyclo-oxygenase-2-selective inhibitor etoricoxib, Aliment. Pharmacol. Ther. 17, 201-210.
35. Jacob, M., Simpson, R. and Bjarnason, I. (1998). Nonsteroidal anti-inflammatory drugs, cyclooxygenase selectivity and gastrointestinal toxicity, Ital. J. Gastroenterol. Hepatol. 30, 12-18.
36. Juni, P., Rutjes, A. W. S. and Dieppe, P. A. (2002). Are selective COX-2 inhibitors superior to traditional nonsteroidal anti-inflammatory drugs?, Br. Med. J. 342, 1287-1288.
37. Kay, L. and Jorgensen, T. (1994). Epidemiology of upper dyspepsia in a random population. Prevalence, incidence, natural history, and risk factors, Scand. J. Gastroenterol. 29, 2-6.
38. Ladwa, M., Takeuchi, K. and Bjarnason, I. (2005). NSAIDs request parity with Helicobacter pylori, Scand. J. Gastroenterol., in press.
39. Laine, L., Connors, L. G., Reicin, A., et al. (2003). Serious lower gastrointestinal clinical events with nonselective NSAID or coxib use, Gastroenterology 124, 288-292.
40. Laine, L., Maller, E. S., Yu, C., et al. (2004). Ulcer formation with low-dose enteric-coated aspirin and the effect of COX-2-selective inhibition: a double-blind trial, Gastroenterology 127, 395-402.
41. Langenbach, R., Morham, S. G., Tiano, H. F., et al. (1995). Prostaglandin synthase 1 gene disruption in mice reduced arachidonic acid-induced inflammation and indomethacin-induced gastric ulceration, Cell 83, 483-492.
42. Langman, M. J. S. (1998). Epidemiological evidence on the association between peptic ulceration and antiinflammatory drugs, Gastroenterology 96, 640-646.
43. Langman, M. J. S., Weil, J., Wainwright, P., et al. (1994). Risk of bleeding peptic ulcers associated with individual non-steroidal anti-inflammatory drugs, Lancet 343, 1075-1078.
44. Lanza, F. L., Rack, M. F., Simon, T. J., et al. (1999). Specific inhibition of cyclooxygenase-2 with MK-0966 is associated with less gastroduodenal damage than either aspirin or ibuprofen, Aliment. Pharmacol. Ther. 13, 761-767.
45. Larkai, E. N., Smith, J. L., Lidsky, M. D., et al. (1987). Gastroduodenal mucosa and dyspeptic symptoms in arthritis patients during chronic nonsteroidal anti-inflammatory drugs, Am. J. Gastroenterol. 82, 1153-1158.
46. Larkai, E. N., Smith, J. L., Lidsky, M. D., et al. (1989). Dyspepsia in NSAID users: the size of the problem, J. Clin. Gastroenterol. 11, 158-162.
47. McKenna, F., Borenstein, D., Wendt, H., et al. (2001). Celecoxib versus diclofenac in the management of osteoarthritis of the knee, Scand. J. Rheumatol. 30, 11-18.
48. Morham, S. G., Langenbach, R., Loftin, C. D., et al. (1995). Prostaglandin synthase 2 gene disruption causes severe renal pathology in the mouse, Cell 83, 473-482.
49. National Institute for Clinical Excellence (2001). NICE issues guidance on Cox II inhibitors for osteoarthritis and rheumatoid arthritis. Accessible at http://www.nice.org.uk/page.aspx?o=37980.
50. Ofman, J., Maclean, C. H., Straus, W. L., et al. (2003). Meta-analysis of dyspepsia and nonsteroidal antiinflammatory drugs, Arthritis Rheum. 49, 508-518.
51. Pavelka, K., Recker, D. P. and Verburg, K. M. (2003). Valdecoxib is as effective as diclofenac in the management of rheumatoid arthritis with a lower incidence of gastroduodenal ulcers: results of a 26-week trial, Rheumatology 42, 1207-1215.
52. Riendeau, D., Percival, M. D., Brideau, C., et al. (2001). Etoricoxib (MK-0663): preclinical profile and comparison with other agents that selectively inhibit cyclooxygenase-2, J. Pharmacol. Exp. Ther. 296, 558-566.
53. Rodrigues, L. A. G. and Jick, H. (1994). Risk of upper gastrointestinal bleeding and perforation associated with individual non-steroidal anti-inflammatory drugs, Lancet 343, 769-772.
54. Rordorf, C., Kellett, N., Mair, S., et al. (2003). Gastroduodenal tolerability of lumiracoxib vs placebo and naproxen: a pilot endoscopic study in healthy male subjects, Aliment. Pharmacol. Ther. 18, 533-541.
55. Scheiman, J. M., Cryer, B., Kimmey, M. B., et al. (2004). A randomized, controlled comparison of ibuprofen at the maximal over-the-counter dose compared with prescription-dose celecoxib on upper gastrointestinal mucosal injury, Clin. Gastroenterol. Hepatol. 2, 290-294.
56. Schnitzer, T. J., Burmester, G. R., Mysler, E., et al. (2004). Comparison of lumiracoxib with naproxen and ibuprofen in the Therapeutic Arthritis Research and Gastrointestinal Event Trial (TARGET), reduction in ulcer complications: randomised controlled trial, Lancet 364, 665-674.
57. Schoen, R. T. and Vender, R. J. (1989). Mechanisms of nonsteroidal anti-inflammatory drug-induced gastric damage, Am. J. Med. 86, 449-458.
58. Shah, A. A., Thjodleifsson, B., Murray, F. E., et al. (2001). A randomised, double blind, double dummy, crossover study of the effects of nimesulide and naproxen on the gastrointestinal tract and an in vivo assessment of their selectivity for cyclooxygenase 1 and 2, Gut 48, 339-348.
59. Sigthorsson, G., Simpson, R. J., Walley, M., et al. (2002). COX-1 and 2, intestinal integrity and pathogenesis of NSAID-enteropathy in mice, Gastroenterology 122, 1913-1923.
60. Sikes, D. H., Agrawal, N. M., Zhao, W. W., et al. (2002). Incidence of gastroduodenal ulcers associated with valdecoxib compared with that of ibuprofen and diclofenac in patients with osteoarthritis, Eur. J. Gastroenterol. Hepatol. 14, 1101-1111.
61. Silverstein, F. E., Graham, G. Y., Senior, J. R., et al. (1995). Misoprostol reduces serious gastrointestinal complications in patients with rheumatoid arthritis receiving nonsteroidal anti-inflammatory drugs, Ann. Int. Med. 123, 241-249.
62. Silverstein, F. E., Faich, G., Goldstein, J. L., et al. (2000). Gastrointestinal toxicity with celecoxib vs nonsteroidal anti-inflammatory drugs for osteoarthritis and rheumatoid arthritis: the CLASS study: A randomised controlled trial. Celecoxib Long-term Arthritis Study, J. Am. Med. Ass. 284, 1247-1255.
63. Simon, L. S., Lanza, F. L., Lipsky, P. E., et al. (1998). Preliminary study of the safety and efficacy of SC-58635, a novel cyclooxygenase 2 inhibitor: efficacy and safety in two placebo-controlled trials in osteoarthritis and rheumatoid arthritis, and studies of gastrointestinal and platelet effects, Arthritis Rheum. 41, 1591-1602.
64. Simon, L. S., Weaver, A. L., Graham, D. Y., et al. (1999). Anti-inflammatory and upper gastrointestinal effects of celecoxib in rheumatoid arthritis: a randomised controlled trial, J. Am. Med. Ass. 282, 1921-1928.
65. Singh, G. and Triadafilopoulos, G. (1999). Epidemiology of NSAID induced gastrointestinal complications, J. Rheumatol. 56 (Suppl.), 18-24.
66. Singh, G., Ramey, D. R., Morfeld, D., et al. (1996). Gastrointestinal tract complications of nonsteroidal anti-inflammatory drug treatment in rheumatoid arthritis. A prospective observational cohort study, Arch. Intern. Med. 156, 1530-1536.
67. Talley, N. J., Evans, L. M., Fleming, K. C., et al. (1995). Nonsteroidal antiinflammatory drugs and dyspepsia in the elderly, Dig. Dis. Sci. 40, 1345-1350.
68. Tramer, M. R., Moore, R. A., Reynolds, D. J., et al. (2000). Quantitative estimation of rare adverse events which follow a biological progression: a new model applied to chronic NSAID use, Pain 85, 169-182.
69. Vane, J. R. (1994). Towards a better aspirin, Nature 367, 215-216.
70. Vane, J. R. (1995). NSAIDs, Cox-2 inhibitors, and the gut, Lancet 346, 1105-1106.
71. Vane, J. R. and Botting, R. M. (1996). Overview -mechanisms of action of anti-inflammatory drugs, in: Improved Non-Steroidal Anti-Inflammatory Drugs: COX-2 Enzyme Inhibitors, Vane, J., Botting, J. and Botting, R. M. (Eds), pp. 1-27. Kluwer, Dordrecht.
72. Vane, J. R. and Botting, R. M. (2001). Formation and actions of prostaglandins and inhibition of their synthesis, in: Therapeutic Roles of Selective COX-2 Inhibition, Vane J. R. and Botting, R. M. (Eds), pp. 1-47. William Harvey Press, London.
73. Warner, T. D., Giuliano, F., Vojnovic, I., et al. (1999). Nonsteroid drug selectivities for cyclooxygenase-1 rather than cyclo-oxygenase-2 are associated with human gastrointestinal toxicity: a full in vitro analysis, Proc. Natl. Acad. Sci. USA 96, 7563-7568.
74. Watson, D. J., Harper, S. E., Zhao, P. L., et al. (2000). Gastrointestinal tolerability of the selective cyclooxygenase-2 (COX-2) inhibitor rofecoxib compared with nonselective COX-1 and COX-2 inhibitors in osteoarthritis, Arch. Intern. Med. 160, 2998-3003.
75. Wight, N. J., Gottesdiener, K., Garlick, N. M., et al. (2001). Rofecoxib, a COX-2 inhibitor, does not inhibit human gastric mucosal prostaglandin production, Gastroenterology 120, 867-873.
76. Wolfe, M. M., Lichtenstein, D. R. and Singh, G. (1999). Gastro intestinal safety of nonsteroidal antiinflammatory drugs, N. Engl. J. Med. 340, 1888-1899.