Anti-inflammatories Flashcards
What does COX do?
Acts on Arachidonic acid and creates an intermediate which is further acted on by different prostaglandins
What does prostaglandin B2 do?
Platelet aggregation
How does blood temperature increase?
IL-1 which induces COX enzyme in hypothalamus to produce prostaglandin which raised blood temperature
What does TxA2 do?
Endothelium vasoconstriction
What does PGE2 do?
Inflammation, bronchoconstriction, vasodilation
What are the 2 sites on COX?
Cycloxygenate site and then peroxidase
Where is COX docked?
The ER
Where do drugs bind to COX?
To the active site
Where does aspirin bind to COX?
Serine residue
What is aspirins duration?
10-20 minutes to be absorbed, 4 hours to go
What do amino acid to NSAIDs interact with on COX1 and COX2?
COX1-iosleucine, COX2-Valine
What does Dicholenic show some selectivity towards?
COX2- for musculoskeletal pain
What does ibuprofen show some selectivity towards?
COX1
What are side effects of NSAIDs?
Renal function, gut problems, bronchospasm, liver damage, skin rashes
Why do NSAIDs cause kidney function problems?
Prostaglandins normally maintain renal blood flow
Why do NSAIDs cause liver damage?
Toxic intermediates
What are the advantages and disadvantages for NSAIDs selective for COX1?
Advantages- reduce strokes due to involvement in platelet aggregation
Disadvantages- bad for gut
What are the advantages and disadvantages for NSAIDs selective for COX2?
Advantages- anti inflammatory and analgesics
Disadvantages- kidney - salt retention so raised bp