Pain Overview and COX inhibitors (2)

Question 1

Why do NSAIDs cause GI ulcers?

Answer 1

NSAIDs inhibit COX-1, inhibiting prostaglandins which increases gastric secretions

Question 2

Eicosanoids include _______ and ______ which mediate what?

Answer 2

Prostaglandins
Leukotrienes

mediate inflammatory rxn (vasodialtion, vasc permeability, platelete agregation, leukocyte chemotaxis)

Question 3

For acute mild/moderate pain use _______ or ______ first.

Answer 3

NSAIDs

APAP

Question 4

Fore severe acute pain use ______ 1st

Answer 4

opioids

Question 5

Visceral pain 1st line for severe and 2nd line

Answer 5

opioids for severe, add adjuvants TCA or AED

Question 6

Inflamm pain 1st line

Answer 6

apa or nsaids

Question 7

neuropathic pain 1st line central

Answer 7

clonidine or baclofen

Question 8

peripheral neuropathic pain 4

Answer 8

TCA/AED
Lidocaine
SSRI/SNRI
Long acting opioid

Question 9

Chronic functional pain 1st line

Answer 9

TCA or Tramadol

2nd line SSRI/SNRI or pregabalin

Question 10

what are MOAIs?

Answer 10

Nonsteroidal anti-iflam

Inhibit COX to stop prostoglandin synth

Question 11

3 main clinical results of MOA

Answer 11

antipyretic, analgesia, anti-inflam

Question 12

Asprin is an MOA with _____ inhibition

Answer 12

irreversible acetylation of active site

Question 13

Ibuprofen is an MOA with _____ inhibition

Answer 13

competative

Question 14

NSAIDs are analgesic and are most effective when ________ is involved

Answer 14

inflammation

bc inhib prostaglandin synthesis

Question 15

3 indications for NSAIDs

Answer 15

MSK/joint dz (sprains, gout, arthritis, rheum)
analgesic for mild-mod pain releif of HA, dysmenorrhea, sunburn
sympt releif of fever

Question 16

Misoprostol is a …..

Answer 16

PGE analog used to treat NSAID induced GI damage (PPI also effective(used for GERD))

Question 17

contraindications of misoprostol

Answer 17

pregnancy

Question 18

Don’t use NSAIDs in pts with _________, _______, ________, or ________

Answer 18

GI ulcers
cardiac dz
renal dz (edema and hypercalemia)
asthma

Question 19

Asprin is the prototype of traditional _______(drugs) (4 effects)

Answer 19

NSAIDs

inhibits COX: anti-coag, antipyretic, analgesic, anti-inflamm

Question 20

Asprin can lead to ________ poisoning (list 7 sx)

Answer 20

salicylism

causes NV, hypervent, HA, confusion, delerium, convulsions, acidosis

Question 21

Asprin is NOT recommended for children <12 b/c they may develop….

Answer 21

Reye’s syndrome

post viral infxn, admin of asprin leads to hepatitis and cerebral edema that can be fatal

Question 22

Asprin should not be taken with (6)

Answer 22

heparin or oral anticoag -bleeding
probenecid or sulfinpyrazone- dec urate excretion(gout pt)
antacids -dec rate of absorption
ibuprofen - inc clotting

Question 23

Diflunisal is a derivative of _____. It’s more potent than ______ but has no _____ activity

Answer 23

salicyclic acid (but no risk of poisoning)
more potent than asprin
no antipyretic activity bc doesnt cross BBB

Question 24

Name the 6 classes of NSAIDs

Answer 24

Propionic acid
indoleacetic acids
oxicoms
phenylbutazone
fenamates
salicyclates

Question 25

Name the propionic acid NSAIDs

Answer 25

Ibuprofen

Question 26

propionic acid NSAIDs all possess 3 activities but have less intense effects on _____

Answer 26

anti-inflam, analgesic, anipyritic | less intense GI effects than asprin

Question 27

Indoleacetic acid NSAIDs are good for tx of _________; these are very potent anti-inflamms but Sfx limit use, including dec effectiveness of ___ drugs

Answer 27

arthritis | dec effect of CV drugs

Question 28

Etodolac has less ___ issues but more _____ issues

Answer 28

less GI issues | more kidney issues (esp w/digoxin, lithium, MTX)

Question 29

Diclofenac approved for ___, ___, and ______. | and a ______ preparation is available

Answer 29

RA, OA, and ank sponylitis | opthalmic prep

Question 30

Nabumatone (3)

Answer 30

prodrug as potent as asprin for RA and OA fewer sf

Question 31

Piroxicam and meloxicam (3)

Answer 31

COX2 sel at low doses, nonsel at high doses GI ADRs Interferes with lithium excretion(bipolar pt)

Question 32

Mefenamic acid and Meclofenamate (2)

Answer 32

no advantages over other NSAIDs severe diarrhea and hemolytic anemia

Question 33

Phenylbutazone (3)

Answer 33

powerful antiinflam limited use bc agranulocytosis and aplastic anemia, GI, fluid retention displaces warfarin, oral hypoglycemic, and sulfonamides from protein binding

Question 34

Ketotolac

Answer 34

GOOD for inflam pain (pyrrolizine carboxylic acid derivative) this is the ONLY injectable NSAID (IM or IV) High rate of GI bleed 5 day max use dec dose in elderly and kidney pts; cleared more slowly

Question 35

COX 2 inhibitors

Answer 35

fewer sfx, fewer gi bleed, still need caution for heart and kidney celecoxib - black box warning!!! Inc MI and stroke risk

Question 36

celecoxib

Answer 36

BLACK BOX WARNING - Inc MI and Stroke