Cyclo-oxygenase inhibitors (NSAIDs)

learning objective


·
describe mechanism of action of cyclo-oxygenase (cox) inhibitors


· explain why selectivity for cox-2 is of therapeutic benefit

·
give examples of clinically important side effects ofCox inhibitors




Uses




-

anti-inflammatory

-

Analgesic (pain reliefs


-
antipyretic (fever relief)




Traditional non steroidal and anti-inflammatory drugs INSAIDs) and coxibs




Ring structure
(similarity they exactly
·
aren't all the same



·
carboxylic group



Why are NSAIDs called cyclo-oxygenase inhibitors ?




starts here. Need them
in the cell membrane

↑
important precursor for

generation of pro
inflammatory prostaglanding
derived
this
from

L
conversion of arachidonate
Inhibit


via Cyclic endoperoxides

to lots end
of products
> inhibiting
-
Cox will reduce these

and functions




Cox enzymes are bifunctional , catalysing a dioxygenase step followed by a peroxidase reaction