IC9

Question 1

MOA of paracetamol

Answer 1

inhibition of prostaglandins in the CNS; possibly COX-3 in the CNS.

Question 2

Hepatotoxic metabolite of paracetamol is called ____

Answer 2

N-acetylimidoquinone (NAPQI)

Question 3

Does paracetamol have anti-inflammatory ppty?

Answer 3

No, but it has analgesic effects

Question 4

MOA of salicylic acid-based NSAID

Answer 4

Covalently acetylates Ser530 in COX-1, thereby blocking PG synthesis

Question 5

MOA of aspirin

Answer 5

a suicidal enzyme inhibitor as it permanently inactivates COX-1 as it interact with the active site

Question 6

Essential group for aspirin activity

Answer 6

OH group ortho to COOH

Question 7

What helps to increase anti-inflammatory activity of aspirin?

Answer 7

A second phenyl ring conjugated with the phenyl in salicylic acid increases anti-inflammatory activity.

Question 8

Salicylic acid originated from _____

Answer 8

bark of willow tree

Question 9

For chiral NSAIDs, which enantiomer is the active stereoisomer?

Answer 9

generally the S-enantiomer

Question 10

A large proportion of NSAIDs belongs to the group of ______

Answer 10

Arylalkanoic Acids

Question 11

How is nabumetone activated?

Answer 11

Catalysis by beta-oxidase into 6-MNA

Question 12

How is nabumetone eliminated?

Answer 12

Reduction of keto group into alcohol, which undergoes glucuronidation -> eliminated

Question 13

Does ibuprofen have a short or long DOA?

Answer 13

Short, as it can be metabolised into many inactive metabolites

Question 14

Selective COX-2 inhibitors

Answer 14

Celecoxib and etoricoxib

Question 15

Colchicine is a natural product obtained from _____

Answer 15

Colchicine autumnale

Question 16

What is colchicine used for?

Answer 16

Prophylaxis / treatment of gout; retards inflammation caused by uric acid crystals

Question 17

MOA of allopurinol

Answer 17

Xanthine mimic; competitively inhibits xanthine oxidase -> reduce uric acid levels -> reduce gout attack

Question 18

MOA of febuxostat

Answer 18

Non-purine selective, non-competitive inhibitor of xanthine oxidase (both oxidized and reduced forms)

Question 19

Indication of febuxostat

Answer 19

• chronic management of hyperuricemia in patients with gout
• patients who cannot tolerate allopurinol

Question 20

Which chemical has renal and hepatic toxicities hence are used as rodenticides instead of anticoagulant?

Answer 20

1,3-indandione

Question 21

How to differentiate btw COX1 and COX2 selective inhibitor?

Answer 21

COX-2 is non-acidic and larger compared to COX-1 selective inhibitor

Question 22

Difference btw Desirudin and bivalirudin VS Dabigatran

Answer 22

All are DTI, but Desirudin and bivalirudin are peptidic while dabigatran is non-peptidomimetic