NSAIDs

Question 1

Describe GI ADRs

Answer 1

dyspepsia, nausea, peptic ulceration, bleeding, perforation

decreased mucus, bicarb secretion and blood flow, increased acid secretion

Question 2

Describe renal ADRs

Answer 2

they cause reversible decreased GFR
more likely in underlying CKD/HF where there is greater reliance for prostaglandins for vasodilation and perfusion.
prostaglandins inhibition na absorption in collecting duct, so this is inhibited causing increased Na, H2O and BP

Question 3

Selective cox2 inhibitors - names, action

Answer 3

celecoxib, etoricoxib
less inhibitory action on cox1 so cox1 mediated homeostatic mechanisms less affected.
decreased GI ADRs, renal ADRs similar.

Question 4

What is the relationship between NSAIDs and protein binding?

Answer 4

NSAIDs displace other bound drugs which increases the free drug concentration

Question 5

paracetamol - uses, actions

Answer 5

for analgesia and pyrexia

cox2 selective inhibition in CNS which decreases pain signals to higher centres

Question 6

NAPQI - normal conditions, overdose

Answer 6

normally conjugates with glutathione
napqi is highly nucleophilic and ultimately leads to cell death by necrosis and apoptosis
n acetyl cysteine replaces glutathione

Question 7

list NSAIDs in order of cox1 to cox2 selectivity

Answer 7

aspirin, ibuprofen, naproxen, diclofenac, celecoxib, etoricoxib