Skip to main content

Differential target tissue presentation and COX-2/COX-1 inhibition by non-steroid anti-inflammatory drugs: a rationale for a new classification

  • Chapter
New Targets in Inflammation

Abstract

‘Selecting a non-steroid anti-inflammatory drug (NSAID) for an individual patient remains more an art than a science’1. Prescribing of NSAIDs has been influenced by a lack of reliable scientific data on individual agents with respect to gastrointestinal (GI) tolerability or detrimental effects on cartilage metabolism. This has led to a number of unsubstantiated marketing claims about NSAIDs.

This is a preview of subscription content, log in via an institution to check access.

Access this chapter

Chapter
USD 29.95
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
eBook
USD 84.99
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD 109.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Institutional subscriptions

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. Gottlieb NL. The art and science of non-steroidal anti-inflammatory drug selection. Semin Arthritis. 1985;15(suppl 2):1.

    Article  CAS  Google Scholar 

  2. Furst DE. Are there differences among nonsteroidal antiinflammatory drugs? Arthritis Rheum. 1994;37:1–9.

    Article  PubMed  CAS  Google Scholar 

  3. Day RO, Graham GG, Williams KM, Brooks PM. Variability in response to NSAIDs: Fact or fiction? Drugs. 1988;36:643–51.

    Article  PubMed  CAS  Google Scholar 

  4. Brooks PM, Day RO. Nonsteroidal antiinflammatory drugs - differences and similarities. N Engl J Med. 1991;324:1716–25.

    Article  CAS  Google Scholar 

  5. Engelhardt G, Homma D, Schlegel K, Utzmann R, Schnitzler C. Anti-inflammatory, analgesic, antipyretic and related properties of meloxicam, a new non-steroidal anti-inflammatory agent with favourable gastrointestinal tolerance. Inflamm Res. 1995 44:423–33.

    Article  PubMed  CAS  Google Scholar 

  6. Wiesenberg-Boettcher I, Schweizer A, Green JR, Mueller K, Maerki F, Pfeilschifter J. The pharmacological profile of COP 28238, a novel highly potent anti-inflammatory compound. Drugs Exp Clin Res. 1989;15;501–9.

    PubMed  CAS  Google Scholar 

  7. Fowler PD, Shadforth MF, Crook PR, John VA. Plasma and synovial fluid concentrations of diclofenac sodium and its major hydroxylated metabolites during long-term treatment of rheumatoid arthritis. Eur J Clin Pharmacol. 1983;25:389–94.

    Article  PubMed  CAS  Google Scholar 

  8. Fowler PD, Dawes PT, John VA, Shotton PA. Plasma and synovial fluid concentrations of diclofenac sodium and its hydroxylated metabolites during once-daily administration of a 100 mg slow-release formulation. EurJ Clin Pharmacol. 1986;31:469–72.

    Article  CAS  Google Scholar 

  9. Emori WE, Champion GD, Bluestone R, Paulus HE. Simultaneous pharmacokinetics of indomethacin in serum and synovial fluid. Ann Rheum Dis. 1983;32:433–5.

    Article  Google Scholar 

  10. Gallo JM, Gall EP, Gillespie WR, Albert KS, Perrier D. Ibuprofen kinetics in plasma and synovial fluid of arthritic patients. J Clin Pharmacol. 1986;26:65–70.

    CAS  Google Scholar 

  11. Day RO, Francis H, Vial J, Geisslinger G, Williams KM. Naproxen concentrations in plasma and synovial fluid and effects on prostanoid concentrations. J Rheumatol. 1995;22:2295–303.

    PubMed  CAS  Google Scholar 

  12. Degner F, Heinzel G, Busch U. Transsynovial kinetics of meloxicam. Scand 7 Rheumatol. 1995; 98(suppl 98):121.

    Google Scholar 

  13. Kurowski M, Dunky A. Transsynovial kinetics of piroxicam in patients with rheumatoid arthritis. Eur J Clin Pharmacol. 1988;34:401–6.

    Article  PubMed  CAS  Google Scholar 

  14. Engelhardt G, Bögel R, Schnitzler C, Utzmann R. Meloxicam: Influence on arachidonic acid metabolism. In vitro findings - Part I. Biochem Pharmacol. 1996;51:21–8.

    Article  PubMed  CAS  Google Scholar 

  15. Churchill L, Graham AG, Shih C-K, Pauletti D, Farina PR, Grob PM. Selective inhibition of human cyclo-oxygenase-2 by meloxicam. Inflammopharmacology. 1996;4:125–35.

    Article  CAS  Google Scholar 

  16. Patrignani P, Panara MR, Greco A et al. Biochemical and pharmacological characterization of the cyclooxygenase activity of human blood prostaglandin endoperoxide synthases. J Pharmacol Exp Ther. 1994;271:1705–12.

    PubMed  CAS  Google Scholar 

  17. Pairet M, Engelhardt G. Differential inhibition of COX- 1 and COX-2 in vitro and pharmacological profile in vivo of NSAIDs. In: Vane J, Botting J, Botting R (eds): Improved Non-steroid Anti-inflammatory Drugs — COX-2 Enzyme Inhibitors. Dordrecht/Boston/London: Kluwer Academic Publishers; 1996;103–19.

    Chapter  Google Scholar 

  18. Distel M, Mueller C, Bluhmki E, Fries J. Safety of meloxicam: A global analysis of clinical trials. Br J Rheumatol. 1996;35(1):68–77.

    Article  PubMed  CAS  Google Scholar 

  19. Lanza FL. Gastrointestinal toxicity of new NSAIDs. Am J Gastroenterol. 1993;88:1318–23.

    PubMed  CAS  Google Scholar 

  20. Geis GS, Stead H, Wallemark CB, Nicholson PA. Prevalence of mucosal lesions in the stomach and duodenum due to chronic use of NSAID in patients with rheumatoid arthritis or osteoarthritis, an interim report on prevention by misoprostol of diclofenac associated lesions. J Rheumatol Suppl. 1991;28:11–14.

    PubMed  CAS  Google Scholar 

  21. A report from the SPALA Project. The Design of SPALA (Safety Profile of Antirheumatics in Long-term Administration): an intensive monitoring system for NSAIDs. Eur J Clin Pharmacol. 1988;34:529–30.

    Article  Google Scholar 

  22. Longman MJS. Anti-inflammatory drugs and the gut: ulcerative damage and protection from cancer. Proceedings of Symposium: New Insights into Anti-inflammatory Therapy and its Benefits, Cannes, October 1994. Macclesfield, UK: Adelphi Communications Ltd.

    Google Scholar 

  23. Garcia Rodriguez LA, Jick H. Risk of upper gastrointestinal bleeding and perforation associated with individual non-steroidal anti-inflammatory drugs. Lancet. 1994;343:769–72.

    Article  Google Scholar 

  24. Henry D, Dobson A, Turner C. Variability in the risk of major gastrointestinal complications from non aspirin non steroidal anti-inflammatory drugs. Gastroenterology. 1993;105:1978–88.

    Google Scholar 

  25. Savage RL, Moller PW, Ballantyne CL, Wells JE. Variation in the risk of peptic ulcer complications with non steroidal anti-inflammatory drug therapy. Arthritis Rheum. 1993;36:84–90.

    Article  PubMed  CAS  Google Scholar 

Download references

Authors

Editor information

Editors and Affiliations

Rights and permissions

Reprints and permissions

Copyright information

© 1996 Springer Science+Business Media Dordrecht

About this chapter

Cite this chapter

Fenner, H. (1996). Differential target tissue presentation and COX-2/COX-1 inhibition by non-steroid anti-inflammatory drugs: a rationale for a new classification. In: Bazan, N., Botting, J., Vane, J. (eds) New Targets in Inflammation. Springer, Dordrecht. https://doi.org/10.1007/978-94-011-5386-7_11

Download citation

  • DOI: https://doi.org/10.1007/978-94-011-5386-7_11

  • Publisher Name: Springer, Dordrecht

  • Print ISBN: 978-94-010-6265-7

  • Online ISBN: 978-94-011-5386-7

  • eBook Packages: Springer Book Archive

Publish with us

Policies and ethics