Flashcards in NSAID drugs Deck (105)
What is the mechanism of Salicylic Acid?
Inhibits COX-1 and COX-2 reversibly
May suppress COX-2 induction
How are salicylates absorbed?
Ionically through the small intestine
In acid form less from the stomach
What are 3 kinds of salicylic acid drugs?
Generic name of aspirin?
what is the mechanism of aspirin?
irreversibly inhibits COX by acetylating a serine residue in the active site
- also has salicylate action because it is rapidly hydrolyzed
What kind of enzyme hydrolyzes aspirin?
which is more potent, aspirin or salicylic acid?
asprin is 2x more potent as an analgesic and andipyretic
What is a an exploited side effect of aspirin?
it blocks platelet aggravating factor thromboxane A2
Is aspirin stable in solution?
Brand name of salsalate?
What is the structure of salsalate?
salicylic acid dimer connected by an ester bond
How is salsalate absorbed?
hydrolyzed in the small intestine and absorbed
What is an advantage of salsalate?
it does not cause GI bleeding, less active in stomach
What NSAID category does salsalate belong too?
what is the brand name of diflunisal?
which is more potent, aspirin or diflunisal?
diflunisal is a more potent analgesic but has less antipyretic activity
What is the unique structural property of diflunisal?
Which has a longer half life, aspirin or diflunisal?
which NSAID category does diflunisal belong too?
which category does indomethacin belong too?
is indomethacin suitable for long term use?
No, very high incidence of side effects
Is indomethacin stable in solution?
No, amide bond hydrolyzed in solution
True of false, indomethacin is one of the most potent NSAIDs in use?
What NSAID category does sulindac belong too?
How is sulindac activated in the body?
It is a prodrug
reduction of the sulfoxide group to the active sulfide intermediate activates into the circulatory system
what is the brand name of etodolac?
how potent is etodolac?
as potent as indomethacin
What is an advantage of etodolac?
less GI bleeding
What is the primary use of etodolac?
Long term management of osteoarthritis