Anti- inflammartories I Flashcards Preview

BMS 242 - Core Phys/pharm > Anti- inflammartories I > Flashcards

Flashcards in Anti- inflammartories I Deck (65)
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1

3 examples of anti-inflammatory and immunosuppressant drugs?

1) NSAIDs (inc. coxibs)
2) Antirheumatic drugs
3) Biologicals (biopharmaceuticals)

2

What are NSAIDs?

Examples?

Non-steroidal anti-inflammatory drugs

Including:
- Aspirin
- Paracetamol
- Ibuprofen

3

What is special about the bark of the willow tree?

Fever lowing (antipyretic) and pain lowering (analgesic)

4

What is the precursor of aspirin and isolated it discovered it and when?

Salicylic acid

Isolated by Henry Leroux in 1828

5

What did Felix Hoffmann do?

Added an ester group to salicylic acid - making acetyl salicylic acid

- Gave the drug to his grandfather

6

Which was more tolerated, salicylic acid or acetyl salicylic acid?

Acetyl salicylic acid

7

What do NSAIDs provide? (3)

- Pain relief

- Lower fever

- Some reduce swelling

8

What is the action of NSAIDs?

They inhibit the production of certain inflammatory meditators by inhibiting the CYLCOOXYGENASE enzymes which lead to the production of PROSTANOIDS

This inhibits the production of PROSTAGLANDINS and THROMBOXANES

9

What are inflammatory mediators an example of?

Paracrine mediators

10

What are paracrine mediators?

Produced by one cell and interact with other cells
Can interact with:
- The same type of cell
- Different types of cell

11

What are prostanoids?

Prostanoids are a subclass of molecules consisting of:

1) Prostaglandins

2) Thromboxanes

3) Prostacyclins

12

What are prostaglandins mediators of?

Inflammatory and anaphylatic reactions

13

What are thromboxanes mediators of?

Vasoconstriction and clot formation

14

What are prostacyclins and what are they mediators of?

They are a PROSTAGLANDIN member

Mediators of:
- Inhibition of platelet aggregation
- Vasodilation

15

What is the process for formation of inflammatory mediators?

1) Phospholipase A2 enzyme in the plasma membrane creates an intermediates from phospholipids - ARACHIDONATE

2) Aracadonate is the substrate of CYCLOOXYGENASE

3) Leads to the production of prostaglandins, prostacyclins and thromboxanes (PROSTANOIDS)

16

What determines what mediators are made?

Which ENZYMES are expressed in a particular tissue

17

What is COX?

Cyclo-oxygenase

18

What prostaglandins are made as a result of the COX pathway?

What are their functions?

PGD2 - Vasodilator and inhibitor of platelet aggregation

PGE2 - Vasodilator and hyperalgesic (increase pain signalling) and HYPERPYRETIC

19

What prostacyclins are made as a result of the COX pathway?

What is its function?

PGI2

- Vasodilator
- Inhibit platelet aggregation
- Hyperalgesic (increase pain sensitivity)

20

What thromboxanes are made as a result of the COX pathway?

What is its function?

TXA2

- Thrombotic (cause clot formation)
- Vasoconstrictor

21

What happens if cyclo-oxygenase is inhibited by NAIDs?

Inhibit the functions of the prostanoids (prostaglandins, prostanoids, thromboxanes):

1) Anti-inflammatory

2) Analgesic

3) Antipyretic

22

What does algesic relate to?

Sensitivity of pain

23

What does pyretic relate to?

Fever (temperature)

24

How are NSAIDs anti-inflammatory?

- Inhibit prostanoids (PGI2, PGE2)
- Inhibit VASODILATION and ODEMA (swelling an bruising)

25

What are NSAIDs ineffective against?

Why?

Mediators that contribute to tissue damage associated with CHRONIC INFLAMMATION

These mediators AREN'T prostanoids (NSAIDs are only affective with prostanoids)

26

How do NSAIDs reduce pain sensitivity?

Inhibit prostanoids (PGI2 and PGE2)

27

How does PGI2 (prostacyclin) usually cause pain sensitivity?

1) Released in area of tissue damage

2) Feeds onto nerve endings - activating GPCR

3) Sensitises nociceptive receptors to inflamaory mediators such as bradykinins and 5-HT

28

How doe NSAIDs reduce temperature/fever?

Prevent production of IL-1 which causes the release of PGE2 which activates the thermostat in the hypothalamus and increases the temperature of the body

29

How are headaches controlled?

Why?

Anti-inflammatory mechanisms!!

Caused by vasodilation of the blood vessels of the brain

30

What is the structure of COX (cyclo-oxygenase)?

- 2 identical subunits, each with a catalytic active site
- Forms a CHANNEL where arachidonate goes through