L11-12 Anti-inflammatories Flashcards Preview

BMS242 Core Phys Pharm > L11-12 Anti-inflammatories > Flashcards

Flashcards in L11-12 Anti-inflammatories Deck (89)
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1

What does NSAID stand for

Non-steroidal anti-inflamatory drug

2

When was the natural precurrsor to aspirin disocered

5th century

3

What does coxib stand for

COX2 - Inhibitors

4

What was significant in 18228

Leroux isolated the active ingredient for aspirin from the willow tree

5

What is the active ingredient in aspirin

Salicyclic acid

6

What was done in 1897 to produce the first synthetic drug, who was this done by

Hoffman
Ester group was added to form acetyl-salcylic acid

7

What was acetyl-salicyclic acid used to treat, why was this better than other treatments

Arthritus
Tolerated better by the GI system

8

What is different between all of the various NSAIDS

Phramacokinetics, derivation and side effects

9

What are NSAIDs generally prescribed for

Rheumatic musculoskeletal problems

10

What group of people are especially at risk when taking NSAIDs

Elderly

11

Two NSAID examples

Paracetamol

12

What are coxibs

Group of drugs which act to inhibit COX-2

13

What does phospholipase A catalyse

The conversion of phospholipid to aracidonate

14

What catalyses the conversion of phospholipid to aracidonate

Phospholipase A

15

What group of enzymes catlayse the conversion of aracidonate to thromboxane and prostaglandins

Cyclo-oxygenases

16

What does the COX enzyme (cyclo-oxygenase) catalyse

The conversion of aracidonate to thromboxane and prostaglandins

17

What is the action of NSAIDs on cyclo-oxygenases
What effect does this have on prostaglandins and thromboxane

Inhibits
Decreases the levels of prostaglandins and thromboxanes

18

Effects of PGI2

Vasodilator
Hyperalgesic
Stops platelet aggregation

19

Effects of PGD2

Vasodilator
Inhibits the aggregation of platelets

20

Effects of PGE2

Vasodilator
Hyperalgesic

21

Effect of thromboxane A2

Thrombotic : it stimulates activation of new platelets as well as increases platelet aggregation
Vasoconstrictor

22

What effect would thromboxane A2 have on clot formation

Would cause the formation of blood clots

23

What is the effect on PGs and thromboxane of NSAIDS

Decrease both

24

Describe the anti-inflammatory effects of NSAIDs

Decrease vasodilation --> reduce oedema
Ineffective against mediators that contribute to tissue damage associated with chronic inflammatory conditions

25

Describe the analgesic effects of NSAIDs

Decrease the prostaglandin production in damaged/inflamed tissue
PG is responsible for the sensitisation of nociceptors to inflammatory mediators (e.g. bradykinin)

26

What does analgesic mean

Reduction of pain

27

Describe the anti-pyretic effects of NSAIDs

Thermostat in the hypothalamus is activated by IL-1
COX2 induction causes production of PGE-2 signals to IL-1
Inhibition of COX2 here leads to less signalling of PGE2 to IL-1 which leads to a reduction of activation of the hypothalamus

28

Why are NSAIDS used after surgery

As can reduce the need for opiate drugs when given in the right combination

29

Why are NSAIDs effective at treating headaches

May be due to the ability to deecrease vasodilation
Vasodilation of the cerebral vasculature is what is thought to be behind headaches

30

Expression of COX1

Constitutive