NSAIDs

Question 1

major sites of COX-1 that can result in NSAID toxicity

Answer 1

platelets, blood vessels, stomach, kidney

Question 2

expressed during inflammation

Answer 2

Cox-2

Question 3

typical NSAID theraputic uses

Answer 3

analgesic, anti-inflammatory, antipyretic

Question 4

decrease the pain threshold

Answer 4

prostaglandins

Question 5

mediate edema response

Answer 5

PGE2/PGI2

Question 6

ways NSAIDS reduce inflammation

Answer 6

inhibit PGE2/PGI2 and reduce neutrophil migration

Question 7

alters body temp set point

Answer 7

PGE2

Question 8

clinical uses of NSAIDS

Answer 8

Pain, primary dysmonorrhea, Joint inflammation, fever

Question 9

GI Side effects of NSAIDS

Answer 9

distress, damage, bleeding

Question 10

way that NSAIDS increase stomach acid

Answer 10

inhibit PGE2/PGI2 which normally inhibit the H+/K+ ATPase, and increase bicarb production in the paritel cells. This leads to more proton release and less buffering

Question 11

renal side effects of NSAIDS

Answer 11

fluid retention , decresed sodium excretion, decreased GFR, instersitial nephritis

Question 12

How NSAIDS can increase bleeding

Answer 12

in pts with reduced clotting factors, TXA2 may be needed more to clot - NSAIDS reduce TXA2

Question 13

ways NSAIDS can increase BP

Answer 13

reduces PGI2, which oppose vascular contractions. inhibition of COX-1/2 decreases Na+ and H2O excretion

Question 14

salicylate prototypes (3)

Answer 14

asprin, aslicylic acid, difunisal

Question 15

Acetic acid derivitaves (2)

Answer 15

indomethacin, ketorolac

Question 16

proprionic acid derivitives (2)

Answer 16

ibuprophen, naproxen

Question 17

enolic acid derivtive

Answer 17

meloxicam

Question 18

COX-2 selective inhibitor

Answer 18

celecoxib

Question 19

MOA of salicylates

Answer 19

binds to COX irreversably, alters ratio of PGI2/TXA2 in vasculature

Question 20

Sx of salicylate toxicity

Answer 20

theraputic doses: GI bleedin, decreased uric acid excretion, hypersenstivy reactions

mild intox (salicylism): tinnitus, vomiting, vertigo, hyperventalation due to resp alkalosis

moderate tox: increased metabolic rate, fever, metabolic acidosis

severe tox: resp depression, dehydration, come, organ failure

Question 21

theraputic dose of salicylate

Answer 21

2-4 g.day

Question 22

lethal dose of salicylate

Answer 22

160 g/day

Question 23

tx for salicylate tox

Answer 23

1) cool, rehydrate, correct acid.base imbalances
2) prevent further absorption via emesis and lavage
3) alkalinize urine
4) hemodyalsis
5) diazepam for convulsions

Question 24

Contraindications for salicylates

Answer 24

renal disease, bleeding disorders, gout, young kids, 3rd trimester preg

Question 25

advantages of naproxen

Answer 25

long t 1/2, intermediate potency

Question 26

most potent NSAID

Answer 26

indomethacin

Question 27

uses of indomethacin

Answer 27

acute gout, arthritis, closing PDA

Question 28

SE of indomethacin

Answer 28

GI distress and aplastic anemia

Question 29

IV NSAID often uses with opiate

Answer 29

ketoralac

Question 30

partially selective COX-2 inhbitor used fir RA and OA in adults

Answer 30

meloxicam

Question 31

reason most COX-2 inhibitors taken off market

Answer 31

high risk of CV events

Question 32

population that is advised not to take non-asprin NSAIDS at all

Answer 32

people with known CV disease

Question 33

triggers inflamation in gout

Answer 33

granulocytes trying to remove urate crystals in joints

Question 34

DOC for acute gout

Answer 34

colchicine

Question 35

MOA of colchicine

Answer 35

inhibits release of chemotactic and inflammatory factors

Question 36

disadvantage of colchicine

Answer 36

highly toxic - very low TI

Question 37

side efects of colchicine

Answer 37

n/v, diarrhea

Question 38

DOC for prevention of gout

Answer 38

probenecid and sulfinpyrazone, allopurinol, feboxustat

Question 39

MOA of probenecid and sulfinpyrazone

Answer 39

inhibits renal reabsorption of urate

Question 40

MOA of allopurinol

Answer 40

suicide inhibitor of xanathine oxidase - blocks urate synthesis

Question 41

SE of allopurinol

Answer 41

GI irritation and skin reactions, inhibits other enzymes in purine pathway

Question 42

febuxostat MOA

Answer 42

nonpurine inhibitor of xanthine oxidase - blocks urate synthesis

Question 43

SE of febuxostat

Answer 43

liver tox and GI irritation