1 / 14

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.

kylee
Download Presentation

NSAIDS: COX – 2 Inhibitors

An Image/Link below is provided (as is) to download presentation Download Policy: Content on the Website is provided to you AS IS for your information and personal use and may not be sold / licensed / shared on other websites without getting consent from its author. Content is provided to you AS IS for your information and personal use only. Download presentation by click this link. While downloading, if for some reason you are not able to download a presentation, the publisher may have deleted the file from their server. During download, if you can't get a presentation, the file might be deleted by the publisher.

E N D

Presentation Transcript

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 Vioxx (Rofecoxib) • -FDA approved May 1999 • Voluntarily withdrawn from market by Merck • September 2004 due to concerns of CV events • One of the most widely-used drugs ever to be • withdrawn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

More Related