Flashcards in Anti- inflammartories I Deck (65)
3 examples of anti-inflammatory and immunosuppressant drugs?
1) NSAIDs (inc. coxibs)
2) Antirheumatic drugs
3) Biologicals (biopharmaceuticals)
What are NSAIDs?
Non-steroidal anti-inflammatory drugs
What is special about the bark of the willow tree?
Fever lowing (antipyretic) and pain lowering (analgesic)
What is the precursor of aspirin and isolated it discovered it and when?
Isolated by Henry Leroux in 1828
What did Felix Hoffmann do?
Added an ester group to salicylic acid - making acetyl salicylic acid
- Gave the drug to his grandfather
Which was more tolerated, salicylic acid or acetyl salicylic acid?
Acetyl salicylic acid
What do NSAIDs provide? (3)
- Pain relief
- Lower fever
- Some reduce swelling
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
What are inflammatory mediators an example of?
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
What are prostanoids?
Prostanoids are a subclass of molecules consisting of:
What are prostaglandins mediators of?
Inflammatory and anaphylatic reactions
What are thromboxanes mediators of?
Vasoconstriction and clot formation
What are prostacyclins and what are they mediators of?
They are a PROSTAGLANDIN member
- Inhibition of platelet aggregation
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)
What determines what mediators are made?
Which ENZYMES are expressed in a particular tissue
What is COX?
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
What prostacyclins are made as a result of the COX pathway?
What is its function?
- Inhibit platelet aggregation
- Hyperalgesic (increase pain sensitivity)
What thromboxanes are made as a result of the COX pathway?
What is its function?
- Thrombotic (cause clot formation)
What happens if cyclo-oxygenase is inhibited by NAIDs?
Inhibit the functions of the prostanoids (prostaglandins, prostanoids, thromboxanes):
What does algesic relate to?
Sensitivity of pain
What does pyretic relate to?
How are NSAIDs anti-inflammatory?
- Inhibit prostanoids (PGI2, PGE2)
- Inhibit VASODILATION and ODEMA (swelling an bruising)
What are NSAIDs ineffective against?
Mediators that contribute to tissue damage associated with CHRONIC INFLAMMATION
These mediators AREN'T prostanoids (NSAIDs are only affective with prostanoids)
How do NSAIDs reduce pain sensitivity?
Inhibit prostanoids (PGI2 and PGE2)
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
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
How are headaches controlled?
Caused by vasodilation of the blood vessels of the brain