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23 Cards in this Set
- Front
- Back
- 3rd side (hint)
Inhibitors of COX1/COX2 Activity
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NSAIDS
COX2 Inhibitors |
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Cyclic Endoperoxides
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Intermediates from AA
PGG2 PGH2 |
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PGI2
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endothelial of blood vessels
Activates adenylyl cyclase to increase cAMP Decrease intracellular calcium IP receptor vasodilation (potent) INHIBITS platelet aggregation stimulates renin release natriuresis diuresis |
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TXA2
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activates phosphatidylinositol metabolism
increased IP3 and intracellular Ca2+ platelets TP receptor vasoCONSTRICTION platelet aggregation bronchoCONSTRICTION |
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PGF2alpha
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FP recep
Increases uterine tone some broncho- and vasoCONSTRICTION Increase aq humor outflow to decrease intraocular pressure glaucoma |
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PGE2
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EP2 recep
vasoDILATION relaxes GI tone bronchoDILATION cytoprotective prostaglandin EP3 recep INHIBITS gastric acid secretion INCREASES gastric mucus secretion stimulation of pregnancy contractions |
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PGD2
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DP recep
vasoDILATION INHIBITS platelet agg relax GI tone relax uterine smooth muscle |
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Inflammation Prostaglandins
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PGD2
PGE2 PGI2 |
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Pain Prostaglandins
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PGE2
PGI2 |
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Fever Prostaglandins
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PGE2
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Platelet Activity
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PGI2
increased cAMP levels disaggregation TXA2 increased IP3 levels mobilization of intracellular Ca2+ Aggregation |
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COX1
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TXA2
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COX2
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PGI2
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Smooth Muscle Constrictor
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TXA2
PGF2alpha |
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Smooth Muscle Dilator
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PGE2
PGI2 |
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GI
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Stimulation of intestinal motility
Longitudinal muscles contract by PGE2 and PGF2alpha Circular muscle -contracted by PGF2alpha -relaxed by PGE2 |
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Uterine
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increased tone and uterine contractions
Levels of PGE and PGF increase during labor Potent oxytoxic action Can terminate pregnancy at any stage! Incs collagenase activity to soften cervix |
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Cytoprotection
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PGE2 and PGI2
Inhibition of gastric acid secretion Stimulation of mucus secretion Increased bicarb secretion Increased mucosal blood flow enhance resistance of gastric mucosal cells to damage accelerate ulcer healing |
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Renal Effects
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Major products in kidney are PGE2 and PGI2
Protective mech Maintain bp Regulate renal fxn |
Vasodilation
Increase glomerular filtration Modulate renal blood flow Inc medullary blood flow Natriuretic Block ADH eff to increase water clearance |
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Eye
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PGF2alpha
increase aqueous humor outflow decrease intraocular pressure Open angle glaucoma |
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COX1 Inhibition
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GI bleeding
TXA2 inhibition platelet agg inhibition |
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COX2 inhibition
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Stroke
MI PGI2 platelet deagg inhibition |
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PGs Specific Effects
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Inflammation
Pain Fever Platelet activity Smooth muscle GI Reproductive actions Renal effects Eye |
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