NSAIDs and gout

Question 1

what are the molecular inflammatory mediators?

Answer 1

1. kinins, neuropeptides, vasoactive amines
2. arachadonic metabolites
3. cytokines, free radicals, proteases

Question 2

what are the arachadonic acid metabolites?

Answer 2

PGs, thromboxanes, prostacyclin

Question 3

what are the functional characteristics of NSAIDs?

Answer 3

analgesia
antipyretic
anti-inflammatory
primary target - PG production via COX1 and COX2

Question 4

is acetaminophen an NSAID?

Answer 4

no

Question 5

which COX enzyme is constitutively expressed?

Answer 5

COX1

Question 6

what role do PGE2 and PGI2 play in inflammation?

Answer 6

edema and vascular permeability

Question 7

what is the role of COX1?

Answer 7

homeostasis

PGs in stomach mucosa (protective)

Question 8

what is the role of COX2?

Answer 8

production of inflammatory molecules

essential for normal kidney function

Question 9

what are the nonselective NSAIDs?

Answer 9

acetylsalicylic acid (aspirin) 
ibuprofen 
indomethacin

Question 10

what is the selective NSAID? is it for COX1 or COX2?

Answer 10

celecoxib

COX2

Question 11

once in the blood, aspirin is hydrolyzed to what?

Answer 11

salicylic acid

Question 12

what is the MOA of salicylic acid?

Answer 12

reversible COX inhibitor

Question 13

does aspirin have a potential for drug interactions? why or why not?

Answer 13

yes

80% bound to plasma proteins

Question 14

what are the low dose effects of aspirin?

Answer 14

analgesic, antipyretic

Question 15

what are the high dose effects of aspirin?

Answer 15

antiinflammatory

Question 16

is the acetylation (an inhibition) of COX reversible or irreversible?

Answer 16

irreversible

Question 17

the antiinflammatory effects of aspirin come from inhibition of what COX enzyme?

Answer 17

COX2

Question 18

the analgesic effects of aspirin come from inhibition of what COX enzyme?

Answer 18

COX2

Question 19

what is the MOA of the antipyretic effects of aspirin?

Answer 19

blocks production of PGs in CNS to reset temperature control at hypothalamus

fall in temperature due to dilation of superficial blood vessels

Question 20

what is the effect of aspirin on bleeding time?

Answer 20

prolongs

Question 21

what are the adverse effects of aspirin?

Answer 21

GI tract upset
GI irritation
platelet inhibition

Question 22

GI tract upset from aspirin use is mediated by the inhibition of what COX enzyme?

Answer 22

COX1

Question 23

keterolac, naproxen, oxaprozin, piroxicam, and sulindac are what class of drug?

Answer 23

NSAID

Question 24

which NSAIDs have less GI adverse effects?

Answer 24

COX2 selective inhibitors

Question 25

what is the main adverse effect of the COX2 selective inhibitors?

Answer 25

CV thrombotic events

Question 26

what are the COX2 selective inhibitors?

Answer 26

celecoxib etoricoxib meloxicam

Question 27

which COX2 selective inhibitor is approved for rheumatoid arthritis?

Answer 27

celecoxib (celebrex)

Question 28

what are the actions of acetaminophen? does it have antiinflammatory properties?

Answer 28

analgesic and antipyretic no

Question 29

what are the drug interactions for acetaminophen? why?

Answer 29

ethanol, isoniazid metabolism by cyp450

Question 30

what is the MOA of capsaicin?

Answer 30

release of substance P leading to depletion and prevention of reaccumulation

Question 31

gout is characterized by accumulations of what type of crystals?

Answer 31

monosodium urate (uric acid)

Question 32

what is the primary NSAID used to treat severe gout?

Answer 32

indomethacin

Question 33

what is the role of colchicine? what is the MOA?

Answer 33

used to be primary gout agent inhibits leukocyte migration and phagocytosis

Question 34

what are the xanthine oxidase inhibitors?

Answer 34

allopurinol | febuxostat

Question 35

what are the uricosuric agents?

Answer 35

probenecid | sulfinpyrazone

Question 36

allopurinol and febuxostat are what type of drug for gout?

Answer 36

xanthing oxidase inhibitors

Question 37

probenecid and sulfinpyrazone are what type of drug for gout?

Answer 37

uricosuric