Pain Killers

Question 1

What is the MOA of Paracetamol?

Answer 1

MOA not 100% known. Inhibits COX-1 and COX-2 enzymes.

Question 2

What does COX-1 enzyme do? And why is the inhibition of it effective?

Answer 2

Involved in normal cell signalling.
Inhibition blocks chemical messengers telling the brain there is pain.

Question 3

What does COX-2 enzymes do? And why is the inhibition of it effective?

Answer 3

Found is areas of inflammation and produces prostanoids.
Protanoids aid inflammatory response and are powerful vasodilators allowing tissue to be engorged w/ blood and become inflamed.

No protanoids= no pain caused by inflammation.

Question 4

What is the MOA of Ibuprofen?

Answer 4

Works via competitive inhibition of COX-2 enzymes.

Question 5

What is competitive inhibition?

Answer 5

Binds to the active site of the enzymes that allows for cell signalling.
This prevents COX-2 enzyme from binding.
And stops inflammation from occurring.

Question 6

What contra-indications are there for taking painkillers?

Answer 6

Hepatic and renal insufficiency.
Sensitivity to NSAIDs.

Question 7

Ibuprofen dose:

Answer 7

x2 200mg, 4x per day
Best taken with food as can irritate the stomach.

Question 8

Paracetamol dose:

Answer 8

x2 500mg, 4x per day