Pharm of NSAIDS (Fitz) Flashcards Preview

MSK 2-Pharmacology > Pharm of NSAIDS (Fitz) > Flashcards

Flashcards in Pharm of NSAIDS (Fitz) Deck (23)
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1
Q

action of PGI2 (prostacyclin) in vasculature endothelium?

A

Vasodilation

decrease platelet aggreg

2
Q

action of PGE2 in vasculature?

A

Permeability

3
Q

Action of PGE2 in CNS?

A

Fever

4
Q

action of PGE2 in PNS?

A

pain sensitization

5
Q

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

A

extensively metabolized to Salicylate by de-acetylation in liver

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

6
Q

COX-independent toxicities of salicylates, aspirin?

A
  • acid-base disturbance
  • tinnitus
  • hypersensitivity
  • REYES SYNDROME
7
Q

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

A

Early=Resp Alkalosis
Late=Met acidosis

fever, dehydration

8
Q

ASA contraindication:

FDA warns against aspirin use by __

A

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

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

9
Q

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

A

acetaminophen=preferred alternative

non-salicylates (ibuprofen)=safe

10
Q

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

A

all tNSAIDs and celecoxib is a coxib

11
Q

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

A

COX –> reduced PG formation

12
Q

which COX is constitutive? which is induced?

A

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

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

13
Q

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

A

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

14
Q

NSAID indications for MSK?

A

osteoarthritis and other arthritides
bursitis
gout ‘flare’
ankylosing spondylitis

others: dysmenorrhea, headache

15
Q

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

A

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

16
Q

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

A

asthma

gut inflamm–> gastritis, colitis, pancreatitis, hepatitis

17
Q

what is the selectivity of coxibs?

A

COX2-selective, COX1-sparing

18
Q

t1/2 of celecoxib?

A

11 hr

19
Q

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

A

Hypersensitivity to sulfonamides

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

20
Q

other complications from COXIBS?

A

peripheral edema, increased BP

21
Q

at anti-inflamm doses, aspirin is a __

A

pro-drug –> salicylate (reversible COX inhibitor)

22
Q

Aspirin itself is a __ inhibitor because it acetylates COX

tNSAIDs are __ COX inhibitors with distinctive chem and pharmacokinetic traits

A

irreversible

reversible

23
Q

black box warning for ALL NSAIDs, except aspirin?

A

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