NSAIDs Flashcards
What does NSAID stand for?
Non-steroidal Anti-Inflammatory Drug
What are commonly used small animal NSAIDs?
Meloxicam
Carprofen
Robenacoxib
Firocoxib
Grapiprant
What are commonly used equine NSAIDs?
Phenylbutazone (suxibuzone)
Flunixin meglumine
Meloxicam
What are commonly used Farm Animal NSAIDs?
Meloxicam
Ketoprofen
What occurs in normal injury?
Release of phospholipids which are broken down into arachidonic acid
COX 1 or COX2 enzymes act on arachidonic acid
Leads to production of prostaglandins and thromboxane
How do NSAIDs work? (Pharmacodynamics)
Inhibit action of COX enzymes
Therefore inhibit prostaglandin synthesis
Which isoform is more important in NSAIDs?
COX2 - unregulated during injury
What effects do COX2 selection have?
Anti-inflammatory effect
Analgesic effect
Anti-pyretic effect
How does selection for COX2 have an anti-inflammatory effect?
The decrease in PGE2 and PGI reduces vasodilation
Indirectly reduces oedema
How does selection for COX2 have an analgesic effect?
Decreased PG generation means reduced sensitisation of nociceptive nerve ending to inflammatory mediators such as bradykinin
Relief of headache is probably due to decreased PG-mediated vasodilation
How does selection for COX2 have antipyretic effect?
Interleukin 1 releases PG in the CNS, where they elevate the hypothalamic set point for temperature control, thus causing fever
NSAIDs prevent this
General pharmacokinetic properties of NSAIDs
Weak acids
Well absorbed after oral administration
formulations for IV, IM and SC
Very high plasma protein binding
Most bio-transformed in the liver to inactive metabolites
There is variation in elimination half-life between NSAIDS and species
Types of NSAIDs
Salicylates
Phenylbutazone
Carprofen
Ketoprofen
Flunixin
Oxicam derivatives
Coxib
Salicylate action
Non-selective
Methyl group causes irreversible interaction with COS
Salicylate usage
Mild to moderate pain
Salicylate example/licensing
Aspirin
None licensed in veterinary medicine