Rational Use of NSAIDs Flashcards
How do NSAIDs reduce inflammation?
inhibit the production of prostaglandins released by damaged tissue by inhibiting cyclo-oxygenase
When are NSAIDs indicated?
- controlling pain and inflammation in NON ALLERGIC disorders e.g. degenerative joint disease
- Peri-operative pain management
- Decreasing platelet aggregation e.g. heartworm disease, thromboembolism
What is the name of the pathway that NSAIDs act on and what are the products of these pathways?
Cyclooxygenase pathway
COX-1 (physiologic COX)
COX-2 (the inducible COX)
What is the role of COX-1?
Physiologic roles- mucosal protection, renal blood flow & haemostasis
What is the role of COX-2?
Inducible behaviours- inflammation, pain & fever
How does inhibiting COX-2 helps with tumours?
Tumours produce COX-2 so inhibiting can slow the growth of these tumours
What are the three types of NSAIDs?
- Non selective
- Preferential (mainly inhibit COX-2 with some COX-1 inhibition)
- Selective (inhibit COX-2 without inhibiting COX-1)
How do Corticosteroids reduce inflammation?
Block the production of Phospholipase from the membrane
Phospholipase is usually used to make arachnoid acid which is needed to make COX-1 / COX-2
Therefore Corticosteroids block both COX-1 and COX-2
Why are some NSAIDs more toxic than others?
Their COX-1 : COX-2 ratios differ so have different levels of safety depending on their inhibition of COX-1 (the physiological one)
Give two examples of non selective COX inhibitors?
Aspirin
Phenylbutazone
Ketoprofen
Tolfenamic acid
What are Preferential COX-2 inhibitors good for but what is the risk?
Good for analgesic and anti-inflammatory activity by blocking COX-2
BUT some COX-1 inhibition is possible at elevated doses
Preferential COX-2 inhibitors also includes drugs known as…..
Why?
Coxibs- COX-2 selective in humans but NOT in animals
Give two examples of Preferential inhibitors of COX-2?
Meloxicam / Metacam
Carprofen
Mavacoxib
Cimicoxib
What is the duration of action like for Mavacoxib?
VERY long!- can be given as an NSAID once a month
Give two examples of selective inhibitors of COX-2?
Firocoxib
Robenocoxib