NSAIDS

Question 1

What are the effects that NSAIDs have

Answer 1

Analgesic, antipyretic (fever-reducing), anti-inflammatory effects

Question 2

What is the precursor to aspirin, more bioavailable alternative that is easier on the stomach

Answer 2

Salicylic acid, acetylsalicylic acid

Question 3

What is the precursor for certain inflammation mediators,

Answer 3

Arachidonic acid,

Question 4

what enzyme is inhibited by NSAIDs

Answer 4

cyclooxygenase (COX)

Question 5

Which products from COX are most likely to be affected by NSAIDs

Answer 5

PGE2: inflammation, fever, and pain/ PGI2: anti-aggregatory and hyperalgesic/ TXA: platelet aggregation

Question 6

What are concerns with COX-2 selective inhibition,

Answer 6

Increase the risk of heart attack (promote thrombosis)

Question 7

What products of COX affected

Answer 7

less PGI2 and TXA

Question 8

What is the theory behind APAP not having anti-inflammatory function

Answer 8

APAP is oxidized by peroxides not allowing tyrosine to be oxidized for PGG2 synthesis

Question 9

T/F: APAP is an NSAID

Answer 9

False” APA has little to no binding to the COX-1 and COX-2 enzymes, therefore, having no anti-inflammatory action

Question 10

How do NSAIDs prevent activation of COX

Answer 10

Competitive inhibition

Question 11

how is acetylsalicylic acid different

Answer 11

acetylates the enzyme

Question 12

What are the msot selective COX-2 inhibitors

Answer 12

Meloxicam, Nimesolide, Celecoxib, Etodolac, Rofecobix

Question 13

Asprin Chemistry

Answer 13

acetyl-salicylic acid - hydrolyzes to salicylic acid

Irreversibly inactivate COXs by covalently acetylating enzyme

• salicylate binding COX can reversibly inhibit COX
• covalent acetylation of COX can irreversibly inhibit COX activity in platelets (used to prevent MI)

Question 14

Aspirin Pharmacokinetics

Answer 14

Orally - 325 mg tablets
- distributed throughout the body (CNS included)
- 80% protein-bound- in plasma
- slows accumulation of the free drug
- displaces other drugs
hydrolyzed to free salicylate before reaching other tissues

Question 15

Aspirin Low- Moderate Dose

Answer 15

metabolized in the liver by conjugation w/ glycine or glucuronic acid First-order kinetics & Saturable, analgesic, and anti-pyretic effects

Question 16

Aspirin High Doses

Answer 16

excreted unmetabolized by OATS in the kidney, zero-order kinetics, half-life that increases w/ increasing dose

High enough doses that saturate the liver metabolism & renal elimination capacity are needed for therapeutic inhibition of COX-2 and inflammation