COX-2 inhibitors

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<languages /><translate> Abbreviation for cyclooxygenase-2 inhibitors, medications that reduce pain and swelling by targeting a particular enzyme known as cyclooxygenase-2 (COX-2).

Anitrazafen structure - Cox-2 inhibitor.
Anitrazafen structure - Cox-2 inhibitor.
  • COX-2 inhibitors include drugs such as celecoxib (Celebrex) and rofecoxib (Vioxx).
  • Although rofecoxib was withdrawn from the market in late 2004 due to adverse side effects associated with coronary problems, celecoxib remains on the market and is widely prescribed.
  • COX-2 inhibitors are reported to induce fewer adverse gastrointestinal side effects compared with other traditional NSAIDs such as ibuprofen and naproxen.
  • As a class, NSAIDs are used to treat pain and are commonly prescribed for treatment of arthritis.

Anti-inflammatory actions[edit | edit source]

Non-selective non-steroidal anti-inflammatory drugs (NSAIDs) have anti­inflammatory, analgesic and antipyretic effects.

Mechanism of action[edit | edit source]

These medications work as inhibitors of the cyclo-oxygenase isoenzymes COX-1 or COX-2.

What are COX-1 and COX-2?[edit | edit source]

The enzyme cyclooxygenase 1 and cyclooxygenase 2 are involved in the production of prostaglandins and thromboxanes

Less GI side effects[edit | edit source]

Gastrointestinal (GI) side effects occur commonly with all NSAIDs. These events are mediated by inhibition of COX-1, responsible for synthesis of the prostaglandins that inhibit acid secretion. COX-2 selectivity reduces the risk of GI adverse events

Cross reactivity between COX-1 and COX-2[edit | edit source]

  • COX-2 inhibitors still have a low affinity for COX-1.

How to reduce risk of GI bleeds?[edit | edit source]

  • Using the lowest effective dose
  • Shortest duration possible.
  • Avoiding the concomitant use of more than one NSAID
  • Avoiding the concomitant use of aspirin a
  • Avoid use anticoagulant where possible
  • Consider use of proton pump inhibitor.
Celecoxib-3D-balls
Celecoxib-3D-balls

List of COX-2 inhibitors[edit | edit source]



COX-2 inhibitors Resources
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