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NSAIDS: COX – 2 Inhibitors

NSAIDS: COX – 2 Inhibitors. Stephanie Cole- Peine October 31, 2007. NSAIDS – “Non-Steroidal Anti- Inflammatory Drugs”. NSAIDS are a very widely used class of drugs for the treatment of arthritis and other conditions that cause chronic pain. . NSAIDS – Mechanism of Action.

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NSAIDS: COX – 2 Inhibitors

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  1. NSAIDS: COX – 2 Inhibitors Stephanie Cole-Peine October 31, 2007

  2. NSAIDS – “Non-Steroidal Anti- Inflammatory Drugs” NSAIDS are a very widely used class of drugs for the treatment of arthritis and other conditions that cause chronic pain.

  3. NSAIDS – Mechanism of Action NSAIDS inhibit the synthesis of prostaglandins that occur naturally upon tissue damage and cause inflammation.

  4. Prostaglandins -First discovered in 1930s -Present in all cells of the body -Function similar to hormones -Synthesized from Arachidonic Acid from cell membranes

  5. Arachidonic Acid Prostaglandins Thromboxanes Leukotrienes

  6. Phospholipase A2 – Enzyme involved in the release of Arachidonic Acid from cell membrane; steroidal drugs inhibit this enzyme.

  7. Clyclo-Oxygenase – Enzymes responsible for conversion of Arachidonic Acid to prostaglandins.

  8. Cyclo-Oxygenase COX -1 - Constitutive Enzyme - “Housekeeping” Functions - Maintenance of Mucosa Layer of GI Tract COX – 2 - Inducible enzyme; Not detectable in healthy tissues - Found abundantly in damaged tissues and activated macrophages - Responsible for inflammation COX – 3 - “Variant” of COX – 1 - Role in acetaminophen’s mechanism of action?

  9. Vioxx (Rofecoxib) • -FDA approved May 1999 • Voluntarily withdrawn from market by Merck • September 2004 due to concerns of CV events • One of the most widely-used drugs ever to be • withdrawn

  10. Mechanism by which adverse effects are thought • occur: suppression of anti-blood-clotting • prostaglandins • Merck has currently not made a decision whether • or not to seek approval to bring Vioxx back to the • market

  11. Celebrex (Celecoxib) • Marketed by Pfizer; one-million prescriptions • filled each month, on average • Controversy regarding risk of CV events

  12. Never been removed from market; in 2005 FDA • concluded benefits outweigh risks for some patients • Should be used exactly as directed, at lowest • possible dose, for shortest time possible

  13. COX – 2 Inhibiting NSAIDS Today • Current data suggests COX – 2 selective NSAIDS and • non-selective NSAIDS have similar CV risk profiles • FDA has issued public health advisory warning • concerning all NSAIDS, required more labeling

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