NSAIDs Flashcards
Which of the 7 important NSAIDs belongs to salicyclate class?
Aspirin
Which of the 7 important NSAIDs belongs to Propionic class?
Ibuprofen
Naproxen
How do you identify NSAIDs in the propionic class?
They have “pro” in their name somewhere
Which of the 7 important NSAIDs belongs to Acetic Acid Class?
Indomethacin
Ketorolac
Diclofenac
How do you recognize NSAIDs in the acetic acid class?
They have “ac” in their name, usually toward the end of the name
Which of the 7 important NSAIDs belongs to Sulfonic Acid Class?
Celecoxib
How do you identify NSAID in sulfonic acid class?
Have “coxib” in name
Tylenol is not an NSAID, but it often does similar things as NSAIDs. What class of drug is tylenol?
Aminophenol class
What are the clinical uses for all NSAIDs (3)?
Analgesia
Antipyresis
Anti-inflammation
What are the specific clinical uses of aspirin?
Pain
Fever
Antithrombosis
What are the clinical uses for acetaminophen? (2)
Pain
Fever
What are the clinical uses for ibuprofen, naproxen, and celecoxib?
Arthritis
Gout
Primary Dysmenorrhea
What are the specific clinical uses of indomethacin?
Closing physiologic heart shunt in newborns
What is the clinical use for diclofenac?
Kidney stone pain
What are the specific clinical uses of ketorolac?
Post-surgery analgesia
What effect does acetaminophen have for analgesia when acting in the presence of arachidonic acid?
It increases endogenous canabinoid production –> reduced pain sensitization
Describe the structure of the COX enzyme
The active site is buried deep inside the protein and is reachable by a tunnel that opens out in the ER membrane. It acts like a funnel guiding the arachidonic acid into the enzyme for processing.
How does aspirin interact with the COX enzyme to modify its functionality?
The aspirin enters the tunnel to the catalytic site and covalently binds (IRREVERSIBLE) to the active site via binding to Ser530, blocking the action of the enzyme and thus leading to decreased platelet activation and anti-thrombosis. Platelets don’t have DNA so once aspirin binds to COX enzymes they are unable to synthesize new COX
Complete this table.
How do other NSAIDs react with COX enzymes?
They REVERSIBILY bind to COX thorugh Tyr and Arg residues
How does celecoxib react with COX1 / COX2?
The COX2 catalytic site is slightly wider than COX1 so it does not fit in COX1 but does fit in COX2 for REVERSIBLE inhibition.
