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asprin
- composed of acetylsalicylic acid
- inhibits synthesis of prostaglandins
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enteric coated asprin
- spares stomach irratation but not small intestine
- delayed onset of analgesic effects
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misoprostol
- (cytotec)
- taken with NSAID
- inhibits gastric secretion therby reducing damage
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omeprazole
- (prilosec)
- taken with NSAID
- inhibits proton pump that is responsible for secreteing gastric acid from muscosal cells into the lumen of the stomach.
- increases healing and reduces ulcers
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ranitidine
- (zantac)
- taken with NSAID
- H2 receptor blockers that decrease GI damage
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cimetidine
- (tagamet)
- taken with NSAID
- H2 receptor blockers that decrease GI damage
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reye syndrome
- affects children and teenagers
- fever, vomiting, liver dysfunction and unresponsiveness
- *acetomenophen and ibuprofen not associated with reye syndrome
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celecoxib
- (celebrex)
- NSAID and Cox 2 inhibitor
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rofecoxib
- (vioxx)
- NSAID and Cox 2 inhibitor
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acetomenophen
- aka paracetamol
- has equal analgesic and antipyretic effects as NSAIDs
- does not have antiinflammatory and anticoagulant effects
- does not irritate upper GI tract
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List (4) Pharmalogical properties of NSAIDS
- 1. for relief of mild to moderate pain
- 2. decrease inflammation
- 3. decrease body temp. (assoc. w/ fever)
- 4. decrease blood clotting (via inhibiting platelet aggregation
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Group of lipid like compounds produced by every cell except the RBC that act locally to regulate cell function
Prostaglandins
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Together with PG's they are reffered as eicosanoids.
Thromboxanes and Leukotrienes
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Eicosanoids are derived from what?
fatty acids knowns as arachidonic acid, which is stored as a phospholipid in the cell membrane
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Arachidonic acid is cleaved from the cell membrane by what enzyme?
Phospholipase A2
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Cyclooxygenase (cox) converts arachidonic acid into what? (2)
- Prostaglandins
- Thromboxanes
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Lipoxygenase converts arachidonic acid into what? (1)
Leukotrienes
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T/F NSAIDs are COX inhibitors but not LOX.
True
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Name (2) PG's involved in inflammation.
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Increases local blood flow and permeability via potentiating histamine and bradykinin.
PGE2
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Contributes to inflammation and increases vascular permeability
LTB4
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Causes blood clots via platelet aggregation
TXs, especially TXA2
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What are eicosanoids associated with? (7)
- trauma
- inflammation
- pain
- fever
- dysmenorrhea
- thrombus formation
- other pathologies- CVD, tumors, respiratory dys.
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List 2 subtypes (isozymes) of the COX enzyme system.
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PG's made from COX-1 enzyme are involved with what? (4)
- normal cell activity/ homeostasis
- protecting stomach lining from gastic acid
- maintaing normal renal function
- regulating platelet activity (thromboxanes)
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Produced primarily in injured cells
COX-2 enzyme
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PG's made from COX-2 enzyme do what?
mediate pain and inflammation
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List (4) clinical applications of asprin like drugs
Treatment of pain and inflamation, fever, vascular disorders and prevention of cancer.
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protects gastric mucosa by:
inhibiting gastric acid secretion
increasing stomach mucous
maintaing blood flow to gastric mucosa
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T/F COX 2 drugs inhibit platelet function
false, these PGs are under control of COX-1
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Why are COX-2 Drugs associated w/ increased risk of CV events? (2)
- B/c COX-2 impairs prostacylin production
- COX-2 does not inhibit thromboxane production
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A highly reactive byproduct of NSAIDs.
N- acetyl-p-benzoquinoneimine (NAPQI)
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This detoxifies NAPQI by coupling with it.
glutathione (GHS)
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glutathione coverts NAPQI into a nonreactive by product called...?
mercapturic acid (execreted by the kidneys)
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