NSAIDS Flashcards
Aspirin MOA
Binds Irreversibly to active site of COX enzymes
Ibuprofen and Naproxen MOA
Same as aspirin, but bind Reversibly instead
What is Naproxen’s usual half life?
14 hours
Which NSAID is said to be specifically for headache pain?
Indomethacin
Why is Acetaminophen not considered a true NSAID?
It only treats pain and fever. It is not an anti-inflammatory.
Which two NSAIDS are only intended for short term use due to extreme side effects.
Clue: One is often used in place of opioids.
Diclofenac and Ketorolac (used in place of Opioids)
Which NSAID does Acetaminophen have a DDI with?
Aspirin
Which two NSAIDS can be used in conjunction with one another and not have overdose risks? Why?
Ibuprofen and acetaminophen; they have different active sites not the target COX enzyme
Which NSAID has the longest half life by far?
Prioxicam; half life is 57 hours
What drug should be given in addition to NSAIDs in the elderly to reduce GI bleeding side effects?
Proton Pump Inhibitors such as Omeprazole.
What is the upper limit of Acetaminophen?
4000mg/day
Ibuprofen and Naproxen have the same side effects, but in decreased severity as to which NSAIDs?
Aspirin
What are two COX-2 selective inhibitors that were taken off the market? Why were they taken off?
Celecoxib and Rofecoxib; they cause deadly heart failure due to clots.
What are the two prostaglandins that regulate platelet aggregation? Which one does what? And which one is downregulated by COX-2 selective inhibitors?
PGI2 decreased thrombolytic effect/clotting and TXA2 increased thrombolytic effects/clotting.
PGI2 is downregulated causing increased clotting and deadly heart clots
Which prostaglandin do Mast Cells secrete?
PGD2
What are the inflammatory mediator prostaglandins?
Eicosanoids, bradykinin, serotonin
What molecule are prostaglandins and thromboxane’s synthesized from?
Arachadonic Acid
Which prostaglandins work on the central nervous system (dorsal horn of spinal cord)?
PGE2, PGI2, and PGF-2alpha
Which prostaglandins work peripherally?
PGI2 and PGE2
Which prostaglandin is involved with the fever phase II?
PGE2: crosses blood brain barrier (BBB) to act on EP3/EP1 on thermosensitive neurons
