NSAID drugs Flashcards Preview

Therapeutics Spring 2015 > NSAID drugs > Flashcards

Flashcards in NSAID drugs Deck (105)
Loading flashcards...
1

What is the mechanism of Salicylic Acid?

Inhibits COX-1 and COX-2 reversibly
May suppress COX-2 induction

2

How are salicylates absorbed?

Ionically through the small intestine
In acid form less from the stomach

3

What are 3 kinds of salicylic acid drugs?

Salicin
Salicylic acid
aspirin (ASA)

4

Generic name of aspirin?

acetylsalicylic acid

5

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

6

What kind of enzyme hydrolyzes aspirin?

plasma esterase

7

which is more potent, aspirin or salicylic acid?

asprin is 2x more potent as an analgesic and andipyretic

8

What is a an exploited side effect of aspirin?

it blocks platelet aggravating factor thromboxane A2

9

Is aspirin stable in solution?

NO

10

Brand name of salsalate?

Disalcid

11

What is the structure of salsalate?

salicylic acid dimer connected by an ester bond

12

How is salsalate absorbed?

hydrolyzed in the small intestine and absorbed

13

What is an advantage of salsalate?

it does not cause GI bleeding, less active in stomach

14

What NSAID category does salsalate belong too?

Salicylates

15

what is the brand name of diflunisal?

Dolobid

16

which is more potent, aspirin or diflunisal?

diflunisal is a more potent analgesic but has less antipyretic activity

17

What is the unique structural property of diflunisal?

diflurobenzene ring

18

Which has a longer half life, aspirin or diflunisal?

Diflunisal

19

which NSAID category does diflunisal belong too?

salicylates

20

which category does indomethacin belong too?

arylacetic acids

21

is indomethacin suitable for long term use?

No, very high incidence of side effects

22

Is indomethacin stable in solution?

No, amide bond hydrolyzed in solution

23

True of false, indomethacin is one of the most potent NSAIDs in use?

True

24

What NSAID category does sulindac belong too?

Arylacetic acids

25

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

26

what is the brand name of etodolac?

Lodine

27

how potent is etodolac?

as potent as indomethacin

28

What is an advantage of etodolac?

less GI bleeding

29

What is the primary use of etodolac?

Long term management of osteoarthritis

30

What is the unique structural property of etodolac?

pyranocarboxylic acid