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

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• • • • Biochemical comparisons of the Cox-1 and Cox-2 COX-1 and COX-2 are membrane-bound proteins … in the endoplasmic reticulum. COX-1 and COX-2 share 60% homology at the amino acid level; both catalyze from arachidonic acid the formation of prostaglandin (PG) G2 followed by PGH2 via a peroxidase function COX-1 and COX-2 have important differences in the catalytic regions, particularly the exchange of Ile in COX-1 for Val in COX-2 at position 523. This substitutions results in a larger and more flexible substrate channel in COX-2 than in COX-1 and in the inhibitor binding site in COX-2, being 25% larger than that in COX-1. Warner TD, Mitchell JA. Cyclooxygenases: new forms, new inhibitors, and lessons from the clinic. FASEB J. 2004 May;18(7):790-804. 2009-2010 AINS et paracetamol 36
heme Kurumbail RG et al. Nature 1996;384:644-8. Structures of COX-1 and COX-2 COX-1 hydrophobic channel tyrosine at 385 + arginine at 120 COX-2 hydrophobic channel hydrophilic “side pocket” tyrosine at 385 arginine at 120 2009-2010 AINS et paracetamol 37 +
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 and 34: *NSAIDs - Relative Risk of GI Compl
Page 35: COX-2: a new anti-inflammatory drug
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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