Term
| therapeutic uses of NSAIDs = |
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Definition
anti-inflam
anti-pyrexic
analgesic |
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Term
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Definition
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Term
| How are NSAIDs better than glucocorticosteroids? |
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Definition
steroids inhibit PLA2 = inhibits leukotrienes as well as inflam mediators = decr WBCs - not gd if got severe infection where want WBCs to be activated and functioning efficiently.
NSAIDs only inhibit COX = only decr imflam mediators = more specific :) |
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Term
| half life of eicosanoids = |
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Definition
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Term
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Definition
constitutive enzyme, always there in most cells, = produce homeostatic PGs
maintains tissue homeostasis
some cox1 upreg in inflam |
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Term
| COX 1 enzymes homeostatic functions = |
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Definition
regulate kidney perfusion (vasodilation)
gut protection (local BF, cell turnover, mucous production, HCO3-production)
platelet aggregation by TXA2 |
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Term
| inhibit cox 1 get what side effects? |
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Definition
1. acute renal failure (decr perfusion of kidneys)
2. gastric ulcer & bleeding(decr PG)
3. bleeding as got decr clotting (decr TXA2)
4. skin reactions
5. liver disorders
6. BM disturbances |
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Term
|
Definition
inducible in inflam cells
large upreg in inflam
produce protanoid mediators of inflam
drugs want to target COX2 |
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Term
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Definition
recently found
not present in all sp
splice varient of cox1 (v similar) |
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Term
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Definition
| specific cox2 inhibitor taken off market due to dangerous CVS side effects (heart attack and stroke) |
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Term
| meaure cox slectivity via... |
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Definition
| ...in vitro isolated cells or whole blood, therefore cant compare NSAIDs as may not refelct in vivo safety! |
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Term
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Definition
| [NSAID] that inhibits 50% of cox enzymes |
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Term
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Definition
| [NSAID] that inhibits 90% of cox enzymes |
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Term
Ideally want IC50 of cox1 to be...(a)
and IC50 of cox2 to be...(b) |
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Definition
(a) high
(b) low
want cox2 selectivity! |
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Term
| NSAIDs side effects with peri-op use = |
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Definition
kidney damage
blood clotting (incr by inhibition of PG and PGI)
GIT ulcers & bleeding |
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Term
| NSAIDs side effects with long term use = |
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Definition
GIT (ulcers & bleeding)
effects on s=arthritic cartilage - decr healing
hepatopathy |
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Term
diameter of
a)cox1
b)cox2
enxyme tunnel = |
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Definition
a) narrow
b)wide
(so small aspirin gets into cox1 but bigger carprofen wont fit, and aspirin too small for cox2 but carprofen =right fit for cox2 to reach both sides) |
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Term
| more cox1 selective NSAIDs = |
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Definition
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Term
| more cox2 selective NSAIDs = |
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Definition
carprofen
deracoxib
tepoxalin
meloxicam
nimuselide |
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Term
| what prostanoids cause inhibition of platelet aggregation? |
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Definition
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Term
| what prostanoids cause vasodilation? |
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Definition
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Term
| what prostanoids cause hyperalgesia? |
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Definition
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Term
| what prostanoids cause myometrial contraction and bronchoconstriction? |
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Definition
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Term
| what prostanoids causes vasoconstriction and platelet aggregation? |
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Definition
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Term
| balance of what two prostanoids is v imp? |
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Definition
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Term
| only irreversible NSAID = |
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Definition
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Term
| mainly cox 1 selective but less so than aspirin = |
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Definition
ibruprofen
flubiprofen
nabumetone |
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Term
| NSAID toxicity related to... |
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Definition
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Term
| NSAID with strong anti-inflam effect = |
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Definition
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Term
| NSAIDs commonly used in vetmed= |
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Definition
relatively cox 1 selective:
aspirin
flunixin
ketoprofen
reletively cox2 selective:
carprofen
meloxicam
phenylbutazone
deracoxib |
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Term
| why is tepoxalin not a v gd NSAID? |
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Definition
| cox1 selective and LOX inhibitor (decr WBCs) :( |
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Term
| some cox2 enzymes have homeostatic roles therefore can get the following side effects with inhibition of cox 2 :( |
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Definition
decr healing of GIT & bone
thrombosis
renal dz |
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Term
| antipyrexic effects of NSAIDs |
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Definition
inhibit production PG in hypothalamus which cause an incr in the body temp set point causing pyrexia)
Only has this efefct in pyrexic animals, doesnt decr temp in normal animal |
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Term
| analgesic effects of NSAIDs |
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Definition
| NSAIDs inhibit PGE2 and PGI2 which would otherwise sensitize nociceptive neurones to actions of mediators of inflam such as bradykinin = pain. |
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Term
| analgesic effect of NSAID most effective against pain associated with... |
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Definition
| ...inflam and tissue damage |
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Term
| anti-inflam effects of NSAIDs... |
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Definition
inhibit synth of prostanoids (= mediators of inflam)
in particular:
decr vasoldilation
decr bv perm = decr oedema
decr pain |
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Term
| has does aspirin irreversibly inhibit cox1? |
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Definition
| by acetylating Serine-350 in active site of cox1 |
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Term
| commonly used NSAIDs in vetmed = |
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Definition
salicylates (aspirin)
carprofen
phenylbutazone |
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Term
| what blood cells release TXA2? |
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Definition
|
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Term
| how does aspirin (at low doses) inhibit platelet aggregation? |
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Definition
| targets and inhibits platelets releasing TXA2 |
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Term
| how does aspirin (at high doses) activate platelet aggregation? |
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Definition
| inhibits PG release (PGE2 and PGD2) from epi (PGs inhibit platelet aggregation so by inhibiting PGs =activate platelet aggregation) |
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Term
| DONT want platelet aggregation if... |
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Definition
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