NSAIDS Flashcards
What are the therapeutic effects of NSAIDS?
The 5 A's Anti inflammatory Analgesic Antipyretic Anti cancer Anti coagulant
What are the possible mechanisms of beneficial action of aspirin like anti inflammatory drugs
- displace Ligands from plasma proteins
- Inhibit action of prostanoids
- reduce PG production by inhibition of arachidonic acid release
- Inhibit cyclo-oxygenase
Adverse effects of NSAIDs?
Gastric bleeding Gastric ulceration Skin reactions Renal toxicity Liver damage
What are the Cyclo-oxygenase independent adverse effects?
Allergy
Irritation
Kernictorus (displacement of billirubin from plasma binding protein, cross blood brain barrier, damage to basal ganglia)
Adverse effects dependent on inhibition of cyclo oxygenase
Gastric ulceration
Prolonged clotting line
Renel damage
What’s the process from membrane phospholipids to cox drugs
Membrane phospholipids to arachidonic acid
to COX1 and COX 2 drugs
What are the iso enzymes of cyclo oxygenase
COX1 and COX 2
Describe COX 1
Normally present and active in most cells Involved in normal physiological functions Generates prostaglandins (have a protective function in the stomach)
Describe COX 2
Not normally in cells
Can be induced and activated in inflammatory cells after injury
Generate prostaglandins involved in inflammation
What the function of COX 2?
Generates prostaglandin(involved in regulation of inflammation
What’s the location of COX 2?
Monocytes, macrophages, synovial cells. Induced by Endotoxin, interferon
Down regulated by interleukin 10 (anti inflammatory mediator)
What can inhibit COX 1 and COX 2?
NSAIDs
Examples of COX 2 inhibitors?
piroxican
Meloxican
Sulindae
Example like anti inflammatory drugs (NSAIDS)
Paracetamol
Aspirin
Naproxen
Ibruprofen
Advantages of COX 2 inhibitors
Enhances production of prostaglandins which triggers inflammation
COX 2 dilates blood vessels and therefore protects platelet aggregation
