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8 Cards in this Set
- Front
- Back
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COX-1
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constitutive enzyme that is expressed in most tissues
makes prostanoids for "housekeeping" notables: PGE2, PGFα2 = gastric mucosal protection TXA2= platelet aggregation, vasoconstriction PGI2= inhibitor of platelet aggregation and vasodilation |
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COX-2
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Inducible- upregulated by stress, growth factors and cytokines
-constitutive in kidneys and brain source of prostanoids in inflammation and cancer notables: prostacyclin= dev. and function of kidneys PGE2= pain, patent ductus arteriosus PGI2= inhibits gastric acid secretion, keeps TXA2 in balance |
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NSAID actions
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anti-inflammation
anti-pyrexia analgesia increases alveolar ventilation(salicylates) decrease renal blood blow inhibit platelet aggregation, increase bleeding time |
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NSAID uses
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1.prophylaxis for cardiovascular events
2.antipyretic, analgesia 3.antiinflammatory 4. reduces risk of colon cancer |
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NSAID doses
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analgesia:
two 325mg tablets 4x per day antiinflammatory: 45mg/kg/d in divided doses salicylates= analgesic in low doses, anti-inflammatory in high doses |
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NSAID Adverse Effects
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GI- gastritis
Blood- prolonged bleeding time Resp- resp acidosis and metabolic acidosis -in acute= resp alkalosis, metabolic acidosis Liver- may elevate enzymes, hepatitis Hypersensitivity rxns Reye's syndrome in children- use acetaminophen instead. dose of less than 2g= inc. in uric a. dose of more than 4g= dec in urate levels. -salicylate compete with uric a. |
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Celecoxib, etoricoxib, meloxicam
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COX-2 selective inhibitors
less GI adverse effects no cardiocascular effects since TXA2 from COX-1 -associated with prothrombotic state because TXA2, PGI2 balance altered since COX-2 inhibition= no PGI2 only celecoxib in USA etoricoxib most selectivity meloxicam least selectivity U: inflammatory disorders AD: GI, renal, celecoxib= hypersensitivity rxns |
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Acetaminophen
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NOT an NSAID
-weak inhibition of COX-1/2 no anti-inflammatory effects; only analgesia and anti-pyrexia -via unknown mechanism (COX-3?) AD: large doses= hepatotoxin -antidote=acetylcysteine |
