Lecture 12/ 13

Question 1

Acetylsalicylic acid

Answer 1

ASA, Derivative of salicylic acid by adding ester, better tolerated

Question 2

NSAIDs action

Answer 2

Inhibit production of certain inflammatory mediators

Decrease prostaglandins and thromboxane production

Question 3

PGI2

Answer 3

Vasodilator, hyperalgesia, stops platelet aggregation

Question 4

TXA2

Answer 4

thrombotic, vasoconstrictor

Question 5

PGF2X

Answer 5

Bronchoconstrictor, myometrial contraction

Question 6

PGD2

Answer 6

Inhibits platelet aggregation, vasodilation

Question 7

PGE2

Answer 7

Vasodilator, hyperalgesic

Question 8

LTC4, LTD4 and LTE4

Answer 8

Bronchoconstrictors, increase vascular permeability

Question 9

PAF

Answer 9

Vasodilator, increases vascular permeability, bronchoconstrictor, chemotoxin

Question 10

Cyclo-oxygenases

Answer 10

The second enzymes in a cascade that leads to production of many mediators called prostanoids

Question 11

Phospholipase A2

Answer 11

enzymes that create reactive intermediates from phospholipids in the plasma membrane of all cells

Question 12

Arachadonate

Answer 12

Substrate for all cyclo-oxygenases

Question 13

Thromboxine

Answer 13

Prevalent in platelets, normal function is to cause/facilitate clot formation

Question 14

Analgesic properties

Answer 14

reduces certain pains

Question 15

Anti-pyretic

Answer 15

Lowers raised temperatures

Question 16

COX enzymes

Answer 16

Has a peroxidase site and a cyclo-oxygenase site
Made up of two identical subunits with 2 catalytic sites
Anchored into ER membrane
Channel by which arachadonate has to enter

Question 17

COX-1

Answer 17

Splice variant (often referred t as COX3)
Constitutively expressed -> on all the time in vast majority of body cells

Question 18

COX enzymes in stomach endothelial cells

Answer 18

Trigger secretion of mucus to produce critical lining to protect cells from acidic pH
Therefore too much aspirin inhibits mucus production and can lead to ulceration

Question 19

COX3

Answer 19

Largely expressed in the CNS and the brain
Not much known about its action
thought to be where paracetamol exerts most of its action

Question 20

COX2

Answer 20

Inducible enzyme triggered by inflammation, growth factors and tumour promoters, leads to prostaglandin production

Question 21

Aspirin selectivity

Answer 21

Some selectivity towards COX1

Question 22

Ibuprofen selectivity

Answer 22

Doesn’t distinguish well but slight preference to COX1

Question 23

Paracetamol selectivity

Answer 23

COX3 preference

Question 24

Coxibs selectivity

Answer 24

New NSAIDs with imrpoved selectivity for COX2