NSAIDs

Question 1

COX-1 selectivity?

Answer 1

Aspirin (only irreversible one)

Question 2

Most COX-2 selective?

Answer 2

Celecoxib, Etoricoxib

Question 3

Selective for COX-1/2?

Answer 3

Ibruprofen, Naproxen

Question 4

Analgesic effect?

Answer 4

Blocks PGE2

Question 5

Anti-inflammatory effect?

Answer 5

Reduced prostaglandin synthesis
Reduced vasodilation (reduced PGI2)
Reduced vascular permeability

Question 6

Antipyretic?

Answer 6

Reduced PGE2 production

Question 7

GI ADR?

Answer 7

Less circulating prostaglandins

Reduced mucosal blood flow
Reduces mucus/HCO3- secretion
Increased acid secretion

Question 8

Renal ADR?

Answer 8

Reduce GFR

Prostaglandins usually vasodilate afferent arteriole to increase GFR

Question 9

NSAID other ADRs?

Answer 9

Hypertension
Hypernatraemia
Fluid retention

Question 10

NSAIDs effect on protein bound drugs?

Answer 10

Dispace protein bound drugs
^free drug of other drug

Methothrexate - hepatotoxicity
Warfarin - ^bleed risk

Question 11

Paracetamol MoA?

Answer 11

COX-2 selective inhibition in CNS

Analgesic, Antipyretic

Question 12

Paracetamol OD MoA?

Answer 12

Paracetamol metabolised to NAPQI

Conjugated with glutathione for excretion

NAPQI builds up (hepatitc glutathione overwhelmed)

Question 13

Paracetamol OD treatment?

Answer 13

N-Acetylcystiene to ^glutathione levels

Activated charcoal if taken recently

Question 14

NSAID DDI?

Answer 14

Aspirin/anticoagulants - ^bleeding