58-NSAIDS and Gout

Question 1

What are the differences in the two COX enzymes?

Answer 1

COX-1 is “houskeeping” that is constitutively expressed and widely distributed
COX-2 is inducible and produces inflammatory molecules
(you want to block COX-2 no necessarily COX-1 for anti-inflammatory)

Question 2

Aspirin

Answer 2

non-selective COX inhibitor
low dose has analgesic, antipyretic (body temp at hypothalamus and dilation of superficial blood vessels) effects, but takes high dose to reach anti-inflammatory effects

Question 3

Adverse effects of aspirin?

Answer 3

GI upset, GI irritation (no protective COX-1), platelet inhibition

Question 4

Non-selective COX inhibitors?

Answer 4

Aspirin, ibuprofen, indomethacin, ketorolac, naproxen, oxaprozin, piroxicam, sulindac

Question 5

Advantage of COX-2 selective drugs? Problems?

Answer 5

analgesic, antipyretic, and anti-inflammatory with LESS GI effects
Thrombotic events associated with use

Question 6

COX-2 selective?

Answer 6

Celecoxib, etoricoxib, meloxicam

Question 7

Acetaminophen

pros, cons

Answer 7

no anti-inflammatory effects. Safe for all ages

hepatotoxicity, liver necrosis/failure because narrow therapeutic index; CYP450 metabolism–interactions

Question 8

common side-effects of NSAIDS

Answer 8

gascric ulcers, anemia, GI bleed, perforation, platelet inhibition, bruising, hemorrhage

Question 9

goals of gout treatment?

Answer 9

control pain and inflammation

Question 10

Primary NSAID for gout?

Answer 10

indomethacin (NOT aspirin)

Question 11

Colchicine

use, MOA, adverse

Answer 11

gout treatment
inhibits leukocyte migration and phagocytosis
diarrhea

Question 12

allopurinol, febuxostat

Answer 12

Xanthine Oxidase inhibitors

block formation of uric acid

Question 13

Probenecid or sulfinpyrazone

Answer 13

increase renal clearance of uric acid (uricosuric drugs)