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24 Cards in this Set

  • Front
  • Back

How do the NSAIDs have their anti-inflammatory effect?

Via inhibition of cyclo-oxygenase (COX)

What are the two isoforms of COX and how do they differ?

COX-1 (Good COX) - involved in numerous protective roles in the body, PGE2, PGI2




COX-2 (Bad COX) - induced after pro-inflammatory insult to create mediators of inflammation.

Why do we use drugs to reduce inflammation which exists to remove noxious stimuli?

Because inflammatory response can be overzealous.

What is the significance of COX selectivity of NSAIDs?

Allows use of drugs with more targeted affects and helps to reduce the negative side effects.

What are the main side effects of the NSAIDs and what does it relate to?

COX-1 inhibition:




- GI tract


- Platelets


- Kidneys





What is the MOA of NSAID GI tract side effects?

Inhibit PGE2 and PGI1 (good protoglandins) which are responsible for:




- Inhibiting acid secretion


- Increasing mucosal blood flow


- Increasing mucus production




Leads to erosion, ulceration and haemorrhage

What is the MOA of the NSAID platelet side effects?

inhibits thromboxane (pro-platlet aggregator) irreversibly and PGI2 (anti-platelet aggregator) temporarily.




Leads to net decrease in platelet aggregation

What is the MOA of the NSAID kidney side effects?

Inhibits good protaglandins:


PGE2 - Increases salt and water excretion


PGI2 - Increases salt and water excretion and increases renal vasodilation




Causes increased water retention leading to hypertension and decreases renal blood flow leading to necrosis

What is relevant about NSAID pharmacokinetics?

Good oral bioavailability


Can readily be given as tablets


Highly bound to blood protein


would normally not leave blood and enter tissue unless their has been an increase in permeability (inflammation)

What are the main NSAIDs used in small animals?

Meloxicam


Carprofen


The 'coxibs:


Firocoxib, deracoxib, robenacoxib, mavacoxib

What is meloxicam's MOA and what is it used for?

NSAID used for analgesia




Suitable for exotic and cats due to lower concentration preparations available.

What is carprofen's MOA and what is it used for?

NSAID used for analagesia

What are firocoxib and deracoxib's MOA and what are they used for?

COX-1 sparing NSAID leading to decreased side-effects associated with non-selective NSAIDs.




Only registered in dogs





What is robenacoxib's MOA and what is it used for?

COX-1 sparing NSAID leading to decreased side-effects associated with non-selective NSAIDs.




Registered in both cats and dogs and has good palatability.

What is mavacoxib's MOA and what is it used for?

EXTREMELY LONG-ACTINGCOX-1 sparing NSAID leading to decreased side-effects associated with non-selective NSAIDs.




Long DOA (7 doses in 6 months) due to slow clearance


Side-effects not as long acting as benefits.

What are the main NSAIDs used in horses?

Phenylbutazone


Flunixin


Meloxicam (rarely used)

What is phenylbutazone's MOA and what is it used for?

Non-selective NSAID for musculoskeletal analgesia




Increased risk of side-effects due to lack of selectivity.

What is flunixin's MOA and what is it used for?

Non-selective NSAID used for visceral analgesia.




Increased risk of side-effects due to lack of selectivity.

What is meloxicam's significance in large animals?

Rarely used but large animals although large animal preparation does exist.

What are the main NSAIDs used in production animals?

Flunixin


Tolfenamic acid


Meloxicam



What is flunixin used for in production animals?

Dairy cattle mastitis with well established withholding periods

What is tolfenamic acid's MOA and what is it used for?

COX-1 sparing NSAID leading to decreased side-effects associated with non-selective NSAIDs.




More expensive than flunixin so rarely used.


Established withholding periods.

Why is phenylbutazone not routinely used in production animals?

No established withholding periods.

What is the concern with using NSAIDs in sheep?

None of the main drugs are registered in sheep and so have to be used off-label.




Off-label use in production animals discouraged as withholding periods have not been established.