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646 SECTION VI Drugs Used to Treat Diseases of the Blood, Inflammation, & Gout
Stimulus
Disturbance of cell membranes
Phospholipids
Phospholipase inhibitors – Phospholipase
Corticosteroids
Fatty acid substitution (diet) Arachidonic acid
Lipoxygenase inhibitors – Lipoxygenase Cyclooxygenase – NSAID, ASA
Leukotrienes
Receptor –
antagonists
LTB 4 LTC /D /E 4 Prostaglandins Thromboxane Prostacyclin
4
4
Phagocyte Alteration of vascular
attraction, permeability, bronchial
activation constriction, increased Leukocyte modulation
secretion
Colchicine –
Inflammation Bronchospasm, Inflammation
congestion,
mucous plugging
FIGURE 36–2 Prostanoid mediators derived from arachidonic acid and sites of drug action. ASA, acetylsalicylic acid (aspirin);
LT, leukotriene; NSAID, nonsteroidal anti-inflammatory drug.
O O
C OH C O Na
O C CH 3 OH
Aspirin O Sodium salicylate
O
O
C O –
HO C CH 3 OH
Acetic acid
Salicylate
Conjugation with Conjugation
glucuronic acid with glycine Oxidation
O H O
Ester and ether C N CH 2 COOH Free HO C OH
glucuronides salicylate
OH OH
Salicyluric acid Gentisic acid
(1%)
FIGURE 36–3 Structure and metabolism of the salicylates. (Reproduced, with permission, from Meyers FH, Jawetz E, Goldfien A: Review of Medical
Pharmacology, 7th ed. McGraw-Hill, 1980. Copyright © The McGraw-Hill Companies, Inc.)