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EICASANOIDS AND NSAIDs (PROSTANOIDS (PGE2 (membrane PGE2 induced with…
EICASANOIDS AND NSAIDs
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Phosholipase A2
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initial rate-limiting step in eicosanoid synthesis is the liberation of intracellular arachidonate-catalyzed by PLA2
PROSTANOIDS
both COX-1 and -2 catalyse incorporation of 2 molecules O2 into 2 unsaturated double bonds in each arachidonate molecule
form highly unstable endoperoxides PGG2 and PGH2-rapidly transformed into PGE2, PGI2,PGD2, PGF2L and TXA2
PGD2
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DP receptor cause vasodilation in vascular beds, inhibition of aggregation and relaxation of GI and uterine smooth muscle
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PGI2
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IP receptors: vasodilatation, inhibit platelet aggregation and renin release
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TXA2
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TP receptors: vasocontriction, platelet aggregation and bronchoconstriction
PGE2
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EP2: bronchodilatation, vasodilatation, stimulation of intestinal fluid secretion and relaxation of GI smooth muscle
EP3: contraction of intestinal smooth muscle, inhibition of gastric acid secretion, increased gastric mucus secretion, inhibition of lypolysis, inhibition of autonomic NR release and stimulation of contraction of uterus
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Oedema not directly induce vascular permeability, potentates action of other inflammatory mediators
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Analogues
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Iloprost: PGI2 analogue- used for pulmonary arterial hypertension, scleroderma, Raynaud's (areas of body feel numb due to cold temperatures or stress)
Classical NSAIDs
Physiological-inhibits gastric acid,contract uterus and increase renal blood flow
Pathological-pyretic, pro-inflammatory and hyperalgesic
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PLATELET ACTIVATION
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intact endothelial lining inhibits platelet activation by producing NO,endothelial ADPase and PGI2
promotes efflux of calcium, reduce intracellular Ca availability for platelet activation
LEUKOTRIENES
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can be converted into LTB4 oe LTC4,LTD4 and LTE4
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RECEPTORS
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Cys-LT1 receptor (LTD4,LTE4): bronchospasm, plasma exudation and eosinophil recruitment
CysLT receptor for cysteinyl leukotrienes: mast cells, basophils and eosinophils
BLT receptor: leukocyte chemotaxis, leukocytes and cytokine secretion, IgE synthesis
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soluble cytosolic enzymes found in lung, platelets, mast cells and wBCs