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Why are RA and OA considered similar?
Increases inflammatory mediators → Increases inflammatory pain
What is the precursor of all eicosanoids?
Arachidonic acid
What three kinds of signals are released after AA is transformed from COX?
Thromboxane A2, PGE2, PGI2,
What does thromboxane A2 syntheses?
Platelet aggregation and vasoconstriction
How does PGE2 amplify the pain signal?
Decreases nociceptors activation threshold which increases the ability to excite
What does PGI2 syntheses?
Vascular endothelium = inhibition of platelet aggregation
What does PGE2 syntheses?
Mucosal protection & Inflammatory cells → nociceptor sensitization + pro-inflammatory signaling
What is the difference between COX-1 and COX-2?
COX-2 promotes inflammation
COX-1 maintains homeostasis used more with gastric mucosa
What kind of inhibition does ibuprofen do?
Noncovalent inhibition
What kind of inhibition does aspirin do?
Irreversible covalent modification
What is converted into PGE2?
PGH2
Define this:
How much more potently a drug inhibits one target than another
Selectivity
Define this:
Less drug required to inhibit that target by 50%
Lower IC50