Kelli Exam 3

Question 1

Arylpropionic acid analog examples

Answer 1

ibuprofen, naproxen, fenoprofen, ketoprofen, flurbiprofen

Question 2

Arylpropionic acid analog MoA/info

Answer 2

non-selective COX inhibitor

only active in the S form

Question 3

Oxicam (enolic acid) examples

Answer 3

meloxicam, piroxicam

Question 4

Oxicam (enolic acid) MoA/info

Answer 4

enolic hydroxyl group interacts with Tyr385 and Ser530
Long half life
Bulky so COX 2 is targeted more

Question 5

Diaryl heterocyclic examples

Answer 5

celecoxib, rofecoxib, valdecoxib

Question 6

Diaryl heterocyclic MoA/info

Answer 6

bulky so targets COX 2
Sulfur containing group binds to additional binding pocket
Increased risk of cardiovascular events

Question 7

N-arylanthranilic acid examples

Answer 7

mefenamic acid, flufenamic acid, meclofenamic acid

Question 8

N-arylantranilic acid MoA/info

Answer 8

The oxygen in salicylic acid is switched out for a nitrogen

non-selective COX inhibitor

Question 9

P-aminophenol derivative example

Answer 9

acetaminophen

Question 10

P-aminophenol derivative MoA/info

Answer 10

may act on COX 3 as an anti-inflammatory in the CNS

not considered a traditional NSAID

Question 11

nitrogen-containing salicylate examples

Answer 11

mesalamine, olsalazine, sulfasalazine

Question 12

nitrogen-containing salicylate MoA

Answer 12

not inhibition of COX - maybe other mediators?

Question 13

indole-3-acetic acid derivative example

Answer 13

indomethacin

Question 14

indole-3-acetic acid derivative MoA/info

Answer 14

binds tightly to COX 1 and can be functionally irreversible. It loses its affinity if the methyl is taken off
widespread intolerable side effects

Question 15

arylacetic and arylpropionic acid derivative examples

Answer 15

sulindac, ketorolac, tolmetin, diclofenac, etodolac

Question 16

arylacetic and arylpropionic acid derivative MoA/info

Answer 16

competes with arachidonic acid

Question 17

arylacetic and arylpropionic acid derivatives selective for COX 2

Answer 17

diclofenac and etodolac bind to Tyr385 and Ser530

Question 18

arylacetic and arylpropionic acid derivatives selective for COX 1

Answer 18

ketorolac and tolmetin

Question 19

Active sites of COX binding pocket and what they do

Answer 19

Arg120: interacts with the carboxylate of the fatty acid
Ser530: the residue acetylated by aspirin
Tyr385: abstracts the pro-S hydrogen to initiate the COX reaction

Question 20

PGI location and effects

Answer 20

endothelial cells

vasodilation and decreased platelet aggregation

Question 21

TXA location and effects

Answer 21

platelets

vasoconstriction and platelet aggregation

Question 22

PGF location and effects

Answer 22

uterus

vasoconstriction

Question 23

PGE location and effects

Answer 23

most cells

erythema, edema, pain, fever

Question 24

PGD location and effects

Answer 24

mast cells and brain

erythema, edema, pain, decreased platelet aggregation

Question 25

Zileuton MoA

Answer 25

inhibits the 5-lipoxygenase that converts arachidonic acid to 5-HPETE, preventing formation of subsequent leukotrienes

Question 26

Zafirleukast and Montelukast MoA

Answer 26

reversible and competitive inhibitor of the cysteinyl-leukotriene receptor

Question 27

Cromolyn and Nedocromil MoA

Answer 27

likely inhibits chloride channels, which may in turn inhibit calcium availability

Question 28

Lodoxamide and Olopatadine MoA

Answer 28

prevention of antigen-stimulated release of histamine and other inflammatory mediators, and may also prevent calcium influx into mast cells