Third Flashcards
Inflammatory compounds are all derived from_____________ which is broken down by _____________
membrane phospholipids
phospholipase
Phospholipase breaks down phospholipids to produce _____________
arachidonic acid
Arachidonic acid can enter two cycles…what are they?
lipoxygenase
cyclo-oxygenase
Leukotrienes are derived from what pathway?
lipoxygenase
Prostaglandins are derived from what pathway?
cyclo-oxygenase
Thomboxane are derived from what pathway?
cyclo-oxygenase
Prostacyclin are derived from what pathway?
cyclo-oxygenase
Prostacyclins counteract the action of _____________
thromboxanes
LTB4 is involved in ___________
chemotaxis
hyperalgesia
LCT4, LTD4, LTE4 are involved in _______________
bronchoconstriction
edema
*produced in asthma
Zafirlukast, montelukast block activity of which leukotrienes?
LCT4, LTD4, LTE 4
Acetaminophen is _______________ an NSAID
NOT
*tylenole ?
Is aspirin an NSAID?
yep
Is acetaminophen an NSAID?
nope
MOA of NSAIDs
blocks cyclo-oxygenase pathway
*cox 1 and cox 2
What are the selective COX2 inhibitors?
celecoxib
rofecoxib
Why would you prefer selective cox2 inhibitors over common nsaids?
COX1 remains intact, allowing for the production of gastric cytoprotection
COX1 pathway is known as the ___________ pathway
constitutive physiologically active (always on) -gastric protection
COX2 pathway is known as the ____________pathway
inducible
Why would the COX2 pathway be turned on?
it kickstarts the inflammatory process, including pain
makes you mores sensitive to pain
What turns of COX2 pathway?
glucocorticoids
NSAIDs
growth factors, gut peptides
COX 2 inhibitors
_____________is located predominantly located in the vascular endothelium
prostacyclin
PGI2
TxA2 is found ________________
in the platelets
What are the main effects of PGI2?
vasodilation
inhibition of platelet aggregation
What are the main effects of TxA2?
platelet aggregation
vasoconstriction
PGE2 causes________________
inhibitirion of gastric acid secretion
contraction of uterus
contraction of GI smooth muscles
PGF2-a main effects are ________________
contraction of bronchi
contraction of myometrium in uterus
The cyclooxygenase (COX) is found ____________________________
bound to the endoplasmatic reticulum
__________ acts in physiological conditions
COX1
___________ is induced by inflammatory cells by pathological stimulus
COX2
____________ is located only in the brain
COX3
Which COX provides gastric protection?
COX1
What are the nonselective NSAIDs?
salicylates pehnylacetates ndolacetates enolates fenamates propionates butylpyrazo----- ugh
Phenylacetates:______________
diclofenac
indolacetates:__________________
indomethacin, sulindac
Enolates:____________________
piroxicam….. I dont think we need to know these.
___________connected with influence of thermoregulatoy centre in the hypothalamus
antipyresis
*benefit of NSAID
_________________mainly anti-exudative effect
anti-inflammatory
*benefit of NSAID
_______________ in very low daily doses
anti-thrombotic action
*benefit of NSAID
__________ of ductus arteriosus
Closure
*benefit of NSAID-specifically INDOMETHACIN
Which NSAID can be used to close the ductus arteriosus?
indomethacin
Toxicities of NSAIDs
gastric mucosal damage bleeding limitation of renal blood flow delay/prolongation of labor asthma and anaphylactoid reactions
__________ arises from the inhibition of platelet function (TxA2 synthesis)
bleeding
Limitation of renal blood flow results in what?
Na and water retention
Asthma and anaphylactoid reactions associated with NSAIDS are connected with __________ inhibition
PGF2-a