PHAR 430 Lecture 11: 11. COX Inhibitors - Melina
Document Summary
Inflammation is a normal & essential response to any noxious stimulus - can be either a local or systemic response. Initial injury causes 1) release of inflammatory mediators (i. e. histamine, serotonin, hydrolytic enzymes, kinins, prostaglandins), which results in 3) vascular leakiness, 4) leukocyte migration, chemotaxis, phagocytosis, 5)connective tissue cell proliferation. Common sources of inflammatory mediators include neutrophils, basophils, mast cells, platelets, macrophages, lymphocytes. Excessive production of prostaglandins & other eicosanoids contributes to the pain, fever, swelling, nausea, vomiting associated with rheumatic (inflammatory) diseases. Naturally occurring, 20-carbon cyclopentano-fatty acid derivatives produced in mammalian tissue from pufas. Belong to a class of bioactive compounds called eicosanoids. Eicosanoids are metabolites of arachidonic acid, found in almost every tissue of the body. Their diverse effects include constriction & dilation of smooth muscle & blood vessels, stimulation of mucus & ion secretion, pain & platelet aggregations. Buncha history blah on slide 3 nomenclature: Cyclooxygenase cyclases arachidonic acid to an intermediate with a 5-membered carbon ring.
