Pharm of NSAIDS (Fitz)

Question 1

action of PGI2 (prostacyclin) in vasculature endothelium?

Answer 1

Vasodilation

decrease platelet aggreg

Question 2

action of PGE2 in vasculature?

Answer 2

Permeability

Question 3

Action of PGE2 in CNS?

Answer 3

Fever

Question 4

action of PGE2 in PNS?

Answer 4

pain sensitization

Question 5

how is aspirin metabolized? what is High-dose ASA?

Answer 5

extensively metabolized to Salicylate by de-acetylation in liver

high-dose ASA is a pro-drug for anti-inflamm doses of salicylate

Question 6

COX-independent toxicities of salicylates, aspirin?

Answer 6

• acid-base disturbance
• tinnitus
• hypersensitivity
• REYES SYNDROME

Question 7

salicylate effect (toxicity) with ASA dose of 6-20 gms?

Answer 7

Early=Resp Alkalosis
Late=Met acidosis

fever, dehydration

Question 8

ASA contraindication:

FDA warns against aspirin use by __

Answer 8

anyone <19 with a fever –> risk of Reyes syndrome

don’t give if <19 for flu-like illnesses, chicken pox, colds, etc

Question 9

preferred alternative(s) to ASA for age <19 with flu-like illnesses, chicken pox, colds, etc?

Answer 9

acetaminophen=preferred alternative

non-salicylates (ibuprofen)=safe

Question 10

ibuprofen, naproxen, diclofenac, and indomethacin are under what drug type? What about celecoxib?

Answer 10

all tNSAIDs and celecoxib is a coxib

Question 11

the anti-inflamm, analgesic, and anti-pyretic actions of NSAIDs originate from inhibition of what enzyme?

Answer 11

COX –> reduced PG formation

Question 12

which COX is constitutive? which is induced?

Answer 12

COX1-constitutive, expressed in all tissues, all the time

COX2-induced, distinctive pays role in kidney; prominent role responding to pathologic stimuli

Question 13

t1/2 of diclofenac? t1/2 of ibuprofen? t1/2 of naproxen?

Answer 13

diclofenac=1 hr
ibuprofen=2 hrs
naproxen=14 hrs

Question 14

NSAID indications for MSK?

Answer 14

osteoarthritis and other arthritides
bursitis
gout ‘flare’
ankylosing spondylitis

others: dysmenorrhea, headache

Question 15

mucosal complications of tNSAIDs? hemostasis-related complications of tNSAIDs? renal-related complications of tNSAIDs?

Answer 15

mucosa-Ulcer
hemostasis-bleeding
renal-peripheral edema, increased BP

Question 16

NSAIDs are not indicated/contraindicated/caution in which respiratory condition? GI?

Answer 16

asthma

gut inflamm–> gastritis, colitis, pancreatitis, hepatitis

Question 17

what is the selectivity of coxibs?

Answer 17

COX2-selective, COX1-sparing

Question 18

t1/2 of celecoxib?

Answer 18

11 hr

Question 19

what happens to a pt with sulfa allergy who takes celecoxib?

Answer 19

Hypersensitivity to sulfonamides

Can cause exfoliative dermatitis, STEVENS-JOHNSON SYNDROME, and toxic epidermal necrolysis

Question 20

other complications from COXIBS?

Answer 20

peripheral edema, increased BP

Question 21

at anti-inflamm doses, aspirin is a __

Answer 21

pro-drug –> salicylate (reversible COX inhibitor)

Question 22

Aspirin itself is a __ inhibitor because it acetylates COX

tNSAIDs are __ COX inhibitors with distinctive chem and pharmacokinetic traits

Answer 22

irreversible

reversible

Question 23

black box warning for ALL NSAIDs, except aspirin?

Answer 23

Since 2005, all NSAIDS have had a black box warning for CV risks –> avoid or use with extreme caution in pts with existing CV disease, or risk factors for CV disease