NSAIDS, RA, and gout

Question 1

effect of inflammation?

Answer 1

can be beneficial or deleterious

Question 2

classic inflammatory sx

Answer 2

redness (rubor), swelling (tumor), heat (calor), pain (dolor)

Question 3

what are some of the molecular inflammatory mediators?

Answer 3

bradykinins, substance P, histamine, prostaglandin, thromboxanes, prostacyclin, TNF-alpha

Question 4

what is the fxns of DMARDS?

Answer 4

delay or arrest of diease process

Question 5

fxnal characteristics of NSAIDS

Answer 5

1. analgesia
2. antipyretic
3. anti-inflammatory

Question 6

is acetaminophen an nsaid?

Answer 6

NOOOO, but it does have analgesic and antipyretic properties

Question 7

downstream effects o PGE2 and PGI2?

Answer 7

incr edema, incr vascular permeability

Question 8

which COX is constitutively expressed, protective, is a housekeeping isozyme?

Answer 8

COX1

Question 9

which COX is inducible, production of inflammatory molec, expressed in vascular endothelium?

Answer 9

COX-2

Question 10

which COX promotes synthesis of PG in stomach mucosa that protect stomach lining from gastric acid?

Answer 10

COX-1

Question 11

which NSAIDS are non-selective (both COX1 & 2)

Answer 11

ASA, ibuprofen, indomethacin

Question 12

which NSAIDS are COX-2 selective?

Answer 12

celecoxib

Question 13

is acetylation & inhibition of COX by ASA reversible or irreversible?

Answer 13

irreversible

Question 14

how does ASA irritate the GI?

Answer 14

inhibit protective PG–>PGe, PGI normally decr gastric acid secretion, maintain mucosal resistance/enhance repair

Question 15

how does ASA potentially decr kidney fxn?

Answer 15

1. inhibition of PG–>decr renal blood flow (tubular necrosis)
2. PG inhibition may allow fro enhanced Na/Water reabsorption

Question 16

what is the major difference b/w ASA and other non-specific NSAIDS?

Answer 16

1. duration of action

2. potency

Question 17

do COX-2 selective inhibitors impact platelet aggregation?

Answer 17

no (this is mediated by COX1)

Question 18

effects of COX-2 selective inhibitors?

Answer 18

analgesic, antipyretic, anti-inflammatory

Question 19

major issue assc’d with COX-2 inhibitors?

Answer 19

CV thrombotic events

Question 20

what is the bad SE effect associated with acetaminophen?

Answer 20

acute liver toxicity

p450 metab–>beware of interactions w/ ethanol, INH

Question 21

therapeutic goals with gout tx?

Answer 21

1. terminate acute gout attacks
2. provide control of pain and inflammation
3. prevent future attacks

Question 22

what is the 1st line tx for gout?

Answer 22

indomethacin (NSAID)

Question 23

which NSAIDS can be used for tx of gout?

Answer 23

indomethacin, ibuprofen, naproxen, sulindac

Question 24

can you use ASA to tx gout?

Answer 24

NO, it causes renal retention of uric acid at low dose

Question 25

when to use corticosteroids as tx for gout?

Answer 25

when patients can't tolerate NSAIDS

Question 26

what are the 3 stages of RA?

Answer 26

1. initiation phase (nonspecific inflammation) 2. amplification phase (T cell activation) 3. chronic inflammation (tissue injury)

Question 27

which drugs for RA reduce inflammation, improve sx, slow bone damage, but have a slow onset of action?

Answer 27

DMARDS

Question 28

what is the 1st line DMARD tx for RA?

Answer 28

methotrexate

Question 29

what was the First agent for RA indicated for both sympt improvement and retardation of structural joint damage?

Answer 29

leflunomide

Question 30

Anti-TNFa agent; cytokine receptor fusion protein

Answer 30

Etanercept

Question 31

Anti-TNFa agent; chimeric monoclonal ab

Answer 31

Infliximab

Question 32

IL-1 inhib (IL-1 cytokine receptor decoy)

Answer 32

Anakinra

Question 33

which RA drug is an Antimetaboite & antifolate agent

Answer 33

methotrexate

Question 34

which RA drug inhibs ribonucleotide synthesis?

Answer 34

leflunomide

Question 35

how does ASA exert anti-pyretic effects?

Answer 35

blocks production of PG in CNS to reset temperature control at hypothaalmus-->dilation of superfifical blood vessels-->drop in temp

Question 36

does acetaminophen have anti-inflammatory properties?

Answer 36

nope, just used as pain relief and fever reducer

Question 37

hepatotoxicity with acetaminophen needs to be monitored with?

Answer 37

high doses, alcohol abuse, CYP450 inducers, elderly

Question 38

capaisin can be used for what?

Answer 38

RA, osteoartiritis, neuralgia