NSAIDS

Question 1

what is an Inflammatory Response?

Answer 1

response of body to injurious stimuli - includes wide variety of noxious agents.

Physical /Chemical Injury - Structural Strain - Infections- Many Diseases - Autoimmune Conditions

• Normally a protective response to reduce risk of further damage to organism

Question 2

what are Autacoids? why r there so many types? what r their key feautres?

Answer 2

are biological factors which act like local hormones, have a brief duration, and act near the site of synthesis.

• 3ashan itha mshkla in the production of one, at least feeh others

SHORT HALF LIFE!

saves u from wasting any more energy than u need to in response to the injury

Question 3

where r Eicosanoid classes derived from?

Answer 3

All Eicosanoid classes derived from Arachidonic Acid which is cleaved from cell membrane phospholipids

Question 4

central role of arachidonic acid in prostanoid synthesis

which prostaglandin is most important in mediating inflammatory response?

Answer 4

Question 5

COX-1

• roles of the PG made by COX-1
• half life?

Question 6

COX-2

• when is it expressed?
• where is it found?

Answer 6

localized injury>COX 2 gets expressed on top of the COX 1,

Question 7

what r most of the ADRs caused by NSAIDs result from?

Answer 7

bc of its contious expression! >> most ADRs caused by NSAIDs effects are due to COX-1 inhibition

Question 8

Understand therapeutics / ADRs in terms of action on COX-1 and COX-2

Answer 8

• Main therapeutic effects of NSAIDs occur via COX-2 inhibition
• Due to its constitutive expression, most ADRs caused by NSAIDs effects are due to COX-1 inhibition

Question 9

differences in COX-1 and COX-2 tunnel for selective inhibition by different NSAIDS

Answer 9

Question 10

Prostaglandins: General Pharmacology

• binds to?
• how many types?
• actions?

Answer 10

Prostaglandins Specific For GPCRs

actions depend on PG recepter type

for PG E>> theres 4 types

Synergise with other autacoids – Bradykinin/Histamine

• PGs act as potent vasodilators - but don’t increase capillary permeability directly - synergise permeating effects of Bradykinin/Histamine

Often action includes synergising effects of other autacoids – to enhance the inflammatory signalling response!

eg. Bradykinin/Histamine

Question 11

how do PGs act as potent vasodilators ?

Answer 11

don’t increase capillary permeability directly

BUT

byincreasing dilation> increased SA> more inflammatory mediators can pass through!

Question 12

what induces the expression of COX 2?

Answer 12

Autacoid release also induces expression of COX-2

Question 13

NSAIDs: Therapeutic Effects?

(main therapeutic effect?)