Anti-inflammatoires non-stéroïdiens (AINS) et paracétamol:

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• • • Discovery of two forms of cyclooxygenase 1989 ... IL-1 induces COX activity in fibroblasts 1 1990 … the inducible COX activity is inhibited by steroids 2 BUT steroids have no effect on basal cyclooxygenase activity 1991 … the inducible cycloxygenase (COX-2)is cloned 3 – – – 60% identical to COX-1 certain important amino acid differences cytokine-induced and regulated by glucocorticoids 1 : Raz et al, PNAS, 1989, 86, 1657-1661 2 : Fu et al, J Biol Chem, 1990, 265. 16737-40 3 : Xie et al, 1991, PNAS, 88, 2692-6 2009-2010 AINS et paracetamol 34
COX-2: a new anti-inflammatory drug target COX-1 (constitutive) Stomach Intestine Kidney Platelet Arachidonic Acid (–) conventional NSAIDs COX-2 (inducible) Inflammatory Site • Macrophages • Synoviocytes • Endothelial cells 2009-2010 AINS et paracetamol 35 (–) • • • Glucocorticoids (block mRNA expression) Brain Kidney Female U/G tract
Page 1 and 2: Anti-inflammatoires non-stéroïdie
Page 3 and 4: • • • • • • • • •
Page 5 and 6: • • • Douleur ... propagation
Page 7 and 8: • • • Types de sensations dou
Page 9 and 10: Mécanismes de transduction des voi
Page 11 and 12: Contrôle du passage l'information
Page 13 and 14: • • Causes de l'inflammation Fa
Page 15 and 16: COX Activity 1600 1200 800 400 0 Ef
Page 17 and 18: O O O O Métabolisme OOH OH de l'ac
Page 19 and 20: • • • • Découverte des ant
Page 21 and 22: Filling up the enzyme with salicyli
Page 23 and 24: Mapping of the cyclooxygenase COX-1
Page 25 and 26: • • • • • • Classes d'A
Page 27 and 28: Upper - GI Renal Adverse Effects of
Page 29 and 30: X Support Renal and Platelet Functi
Page 31 and 32: • • • • • NSAID Ulcers an
Page 33: *NSAIDs - Relative Risk of GI Compl
Page 37 and 38: heme Kurumbail RG et al. Nature 199
Page 39 and 40: H3 CO hydrophilic group Pharmacoche
Page 41 and 42: Importance of the Ile Val change i
Page 43 and 44: Cox-1 vs flurbiprofene Picot et al.
Page 45 and 46: Clinical efficacy ? 2009-2010 AINS
Page 47 and 48: Celecoxib vs Diclofenac plus omepra
Page 49 and 50: Localization of COX-1 and COX-2 in
Page 51 and 52: The hypertension story starting in
Page 53 and 54: • F • F F Y-a-t-il un avenir po
Page 55 and 56: Making an irreversible linkage by a
Page 57 and 58: AINS et principales interactions m
Page 59 and 60: Metabolisme O O > 5-10 g hépatique
Page 61 and 62: Le paracétamol "en notice" … Pra
Page 63 and 64: • • • Principaux usages clini
Page 65: • • • • • Autres médicam

Anti-inflammatoires non-stéroïdiens (AINS) et paracétamol:

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