Clinical pharmacology of celecoxib, a COX-2 selective inhibitor

Expert Opin Pharmacother. 2007 Aug;8(11):1719-32. doi: 10.1517/14656566.8.11.1719.

Abstract

NSAIDs are extensively used worldwide; nonetheless, they are associated with adverse gastrointestinal (GI) effects. COX-2 inhibitors (coxibs) have been developed to reduce pain and inflammation without associated GI and bleeding risks. Celecoxib was the first COX-2 inhibitor introduced on the market, and it still remains so, whereas rofecoxib and valdecoxib were withdrawn due to excess cardiovascular (CV) risk. There is consequently a concern that CV toxicity reflects a class effect of all COX-2 inhibitors. Celecoxib possesses anti-inflammatory and analgesic properties, and the evidence for CV risk is rather small and comparable to that of other traditional NSAIDs in short-term treatments (of < 4 weeks). It could be suggested that the use of low doses of celecoxib (100 mg b.i.d.) in short-treatment, especially in patients with previous experience of GI events and the recommendation of avoiding use of celecoxib in patients with CV history or risk, contribute in the decision-making process of prescribing COX-2 or NSAIDs.

Publication types

  • Review

MeSH terms

  • Animals
  • Celecoxib
  • Cyclooxygenase 2 / metabolism
  • Cyclooxygenase 2 Inhibitors / adverse effects
  • Cyclooxygenase 2 Inhibitors / pharmacology*
  • Cyclooxygenase 2 Inhibitors / therapeutic use
  • Humans
  • Membrane Proteins / antagonists & inhibitors*
  • Membrane Proteins / metabolism
  • Pyrazoles / adverse effects
  • Pyrazoles / pharmacology*
  • Pyrazoles / therapeutic use
  • Sulfonamides / adverse effects
  • Sulfonamides / pharmacology*
  • Sulfonamides / therapeutic use

Substances

  • Cyclooxygenase 2 Inhibitors
  • Membrane Proteins
  • Pyrazoles
  • Sulfonamides
  • Cyclooxygenase 2
  • PTGS2 protein, human
  • Celecoxib