Anti inflammatory agents: Fitz

Question 1

another name for PGI2

Answer 1

prostacyclin

Question 2

Action of prostacyclin

Answer 2

• vasodilation

- decrease in platelet aggregation

Question 3

PGE2 does hat in vasculature?
CNS?
PSN?

Answer 3

• permeability
• Temperature
• Pain sensitization

Question 4

what cleaves lipids from membrane into arachidonic acid?
then to what by what?
then what enzymes?

Answer 4

• phospholipase A2
• AA to PGH2 by COX
• then tissue specific isomerases

Question 5

High dose ASA (Aspirin) is a pro druge for anti inflammatory doses of what

Answer 5

salicylate

Question 6

what are complications of High dose Aspirin (Cox Independent toxicities)?

Answer 6

• Acid base disturbances
• Tinnitus
• Hypersensitivity
• Reye’s Syndrome

Question 7

Aspirin does for antiplatelet effect?
analgesic, antipyretic?
anti-inflammatory, tinnitus?
-Respiratory alkalosis then metabolic acidosis, fever, dehydration?
-above plus shock and coma?

Answer 7

• 80-160 mg
• 325-1000 mg
• 325mg - 6 g
• 6-20 g
• > 20 g

Question 8

describe the progression of aspirin/salicylate Toxicity?

Answer 8

• Salicylates uncouple mitochondrial oxidative phosphorylation in the CNS
• Respiratory center registers low ATP as hypoxemia and responds with hyperventilation
• this blows of CO2, drop in CO2 causes respiratory alkalosis eventually prompting kidney to deplete bicarb
• Organic acids accumulate because ATP no longer generated through Krebs cycle
• metabolic acidosis becomes life threatening

Question 9

Aspirin contraindication

Answer 9

• don’t use in anyone <19 with a fever for treating symptoms of flu like illnesses, chicken pox, colds, etc due to risk of Reye’s syndrome
• used acetaminophen instead

Question 10

what are the Salicylate NSAIDs?

Answer 10

• Salicylate
• Aspirin
• Diflunisal

Question 11

What are the Coxib NSAIDs

Answer 11

celecoxib

Question 12

What are the traditional tNSAIDs?

Answer 12

• Ibuprofen
• Naproxen
• Diclofenac
• Indomethacin

Question 13

Describe the expression difference b/t COX 1 and 2

Answer 13

• COX1: constitutive expression in all tissues all the time . . responds to physiologic stimuli
• COX-2: induced in some tissue . . PATHOLOGIC stimuli . . ie inflammation

-so COX-1 will produce PGE2 which will cause symptoms to induce COX-2 and exacerbate the symptoms more

Question 14

what are complications of tNSAIDs because they non selectively inhibit COX

Answer 14

• increase PERIPHERAL edema
• bleeding
• decrease mucosal integrity

Question 15

contraindications of NSAIDS

Answer 15

• Asthma
• Gut inflammation
• Infectious inflammation

Question 16

Coxibs selectively inhibit which COX

Answer 16

2

Question 17

what is the benefit of coxib COX 2 selectivity

Answer 17

gut sparing

Question 18

contrainidications/complications of coxibs?

Answer 18

• Hypersensitivity to sulfonamides (Stevens Johnson syndrome)
• Still can cause peripheral edema and increase BP

Question 19

what is the black box warning for all NSAIDs except Aspirin?

Answer 19

cardiovascular risks . . even Coxibs