NSAIDs

Question 1

NSAIDs

Answer 1

Non Steroidal Anti-Inflammatory Drugs. Weak acids that inhibit cyclooxygenase (COX)

Question 2

traditional NSAIDs

Answer 2

NSAIDs that non selectively inhibit both forms of COX (aspirin, ibuprofen, naproxen)

Question 3

Coxibs

Answer 3

newer NSAIDs that have a greater selectivity for COX2 (don’t have zero effect on COX1 though). names end in coxib

Question 4

mechanism of action of aspirin

Answer 4

acetylates Ser-530 in COX1 and results in irreversible inhibition

Question 5

only NSAID that is irreversible

Answer 5

Aspirin

Question 6

mechanism of other NSAIDs

Answer 6

binds to enzyme’s active site and elicits structural change which inactivates enzyme and is slowly reversible

Question 7

why can’t we use ibuprofen as anti platelet therapy for cardiovascular disease?

Answer 7

platelet aggregation is recoverable whereas with aspirin it is irreversible

Question 8

clinical utility of NSAIDs (4As)

Answer 8

anti-pyretic, analgesic, anti-inflammatory, antiplatelet

Question 9

side effects of NSAIDs

Answer 9

blocking cytoprotection results in gastropathy, blocking platelet activity results in bleeding, reduced renal vasodilation=hypertension, prolongation of gestation

Question 10

gastropathy

Answer 10

inhibit homeostasis of healthy mucosa: increased gastric erosion while at the same time increasing bleeding

Question 11

rofecoxib

Answer 11

selectively inhibited COX2 in order to only target inflammatory effects and reduce toxicities. worked but increased the risk for MI due to homeostasis imbalance of TxA2/PGI

Question 12

low dose vs high dose of aspirin

Answer 12

low: inhibits platelets
high: analgesic, antiinflammatory

Question 13

reyes syndrome

Answer 13

hepatic toxicity syndrome due to aspirin overdose

Question 14

salicylism

Answer 14

salicylate toxicity due to aspirin. headache, tinnitus, dizziness, nausea. common pediatric overdose