Case 1 Unveil Independent Learning Flashcards
What do NSAIDs do
Inhibit PGHS-2 dervied prostaglandins (e.g. PGE2) which reduces the extend and duration of local inflammation caused by vasodilation and increased vascular permeability
What two effects do NSAIDs have
Analgesic and anti-pyretic
What does analgesic mean
Decrease in pain and swelling
What does anti-pyretic mean
Decrease in temperature
How do NSAIDs exert their anti-pyretic property
NSAIDs inhibit hypothalamic PGHS-2 which normally generates PGE2 in response to circulating pyrogens. So by blocking PGE2 you stop pyrexia
How do NSAIDs decrease pain and swelling
Largely due to PGH2. PGH2 supercharged the pain response
What is the full name form aspirin
Acetyl salicylic acid
What is the only irreversible inhibitor of PGHS-1 and PGHS-2
Aspirin
Describe the mechanism of action of aspirin
Acetylation of serine reside in the COX domain active site
What is the origin of aspirin
Willow tree bark containing salcin
Describe ibuprofen
It is produced as a racemate, the S-enantiomer is the active NSAID
Describe the mechanism of action of ibuprofen
It competes with AA for the COX domain site of PGHS-1 and PGHS-2. It is a reversible, competitive inhibitor
Describe the origin of ibuprofen
Derived from propanoic acid
Why may paracetamol be chosen over NSAIDs
It can have better analgesic and anti-pyretic effects
What is one thing paracetamol doesn’t do that NSAIDs do
Little anti-inflammatory activity