Eicosanoids PDF
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San Lorenzo Ruiz College of Ormoc, Inc.
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This document describes eicosanoids, a large group of autacoids with potent effects on various tissues. It details their biosynthesis from arachidonic acid and their roles in different body systems like the reproductive, cardiovascular, and gastrointestinal systems. The document also explores the clinical uses of eicosanoid-based drugs.
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146 Eicosanoids large group of autacoids with potent effects on virtually every tissue in the body. derived from the metabolism of 20-carbon, unsaturated fatty acids (arachidonic acids). released locally and act as a local hormone. distributed widely in the body....
146 Eicosanoids large group of autacoids with potent effects on virtually every tissue in the body. derived from the metabolism of 20-carbon, unsaturated fatty acids (arachidonic acids). released locally and act as a local hormone. distributed widely in the body. 147 Biosynthesis of Eicosanoids 148 2. Eicosanoids a. Prostaglandin H synthase pathway a.k.a. ³&\FORR[\JHQDVH´ or COX It produces thromboxane, the primary prostaglandins (PGE, PGF, or PGD), and prostacyclin (PGI2). 149 Clinical Pharmacology of Prostaglandin Female Reproductive System a. Abortion: ¾ Dinoprostone (PGE2) ¾ a synthetic preparation administered vaginally for oxytocic use. ¾ Carboprost Tromethamine (15-methyl- PGF2a) ¾ administered as a single 2.5 mg intra-amniotic injection. ¾ Antiprogestins (Mifepristone) ¾ combined with an oral oxytocic prostaglandin (Misoprostol) to produce early abortion. 150 2. Male Reproductive System a. Erectile Dysfunction: Alprostadil (PGE1) 3. Cardiovascular System a. Pulmonary Hypertension: Prostacyclin b. Peripheral Vascular Disease: PGE & PGI2 c. Patent Ductus Arteriosus: Alprostadil (PGE1) 152 4. Blood a. Platelet Aggregation:TXA2 6. Gastrointestinal System ¾ Misoprostol (PGE1)-available in Europe & the USA for ulcer treatment. 153 8. Glaucoma: ¾ Latanoprost: a stable long acting PGF22aa ¾ Bimatoprost, Travaprost,Unoprostone 154 NSAIDS are a family of eicosanoid inflammatory mediators produced in leukocytes by the oxidation of arachidonic acid by the enzyme arachidonate 5-lipoxygenase One of their roles (specifically, leukotriene D4) is to trigger contractions in the smooth muscles lining the bronchioles; their overproduction is a major cause of inflammation in asthma and allergic rhinitis Leukotriene antagonists are used to treat these disorders by inhibiting the production or activity of leukotrienes (Zafirlukast, Montelukast) 5-Lipoxygenase Inhibitor (Zileuton)