NSAIDs Flashcards

1
Q

What does NSAID stand for?

A

Non-steroidal Anti-Inflammatory Drug

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2
Q

What are commonly used small animal NSAIDs?

A

Meloxicam
Carprofen
Robenacoxib
Firocoxib
Grapiprant

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3
Q

What are commonly used equine NSAIDs?

A

Phenylbutazone (suxibuzone)
Flunixin meglumine
Meloxicam

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4
Q

What are commonly used Farm Animal NSAIDs?

A

Meloxicam
Ketoprofen

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5
Q

What occurs in normal injury?

A

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

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6
Q

How do NSAIDs work? (Pharmacodynamics)

A

Inhibit action of COX enzymes
Therefore inhibit prostaglandin synthesis

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7
Q

Which isoform is more important in NSAIDs?

A

COX2 - unregulated during injury

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8
Q

What effects do COX2 selection have?

A

Anti-inflammatory effect
Analgesic effect
Anti-pyretic effect

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9
Q

How does selection for COX2 have an anti-inflammatory effect?

A

The decrease in PGE2 and PGI reduces vasodilation
Indirectly reduces oedema

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10
Q

How does selection for COX2 have an analgesic effect?

A

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

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11
Q

How does selection for COX2 have antipyretic effect?

A

Interleukin 1 releases PG in the CNS, where they elevate the hypothalamic set point for temperature control, thus causing fever
NSAIDs prevent this

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12
Q

General pharmacokinetic properties of NSAIDs

A

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

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13
Q

Types of NSAIDs

A

Salicylates
Phenylbutazone
Carprofen
Ketoprofen
Flunixin
Oxicam derivatives
Coxib

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14
Q

Salicylate action

A

Non-selective
Methyl group causes irreversible interaction with COS

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15
Q

Salicylate usage

A

Mild to moderate pain

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16
Q

Salicylate example/licensing

A

Aspirin
None licensed in veterinary medicine

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17
Q

Phenylbutazone action

A

Non-selective
Main metabolite also has similar properties
Low therapeutic index

18
Q

Phenylbutazone usage

A

Mild to moderate pain and inflammation
DO NOT USE IN CATS

19
Q

Phenylbutazone licensing

A

Horses

20
Q

Carprofen action

A

COX2 preferential but not selective

21
Q

Carprofen usage

A

Post-operative pain and inflammation
Reduction of chronic inflammation
Adjunct to reduce pain with acute infectious respiratory disease and mastitis

22
Q

Carprofen licensing

A

Dogs
Cats

23
Q

Ketoprofen action and usage

A

Non-selective

24
Q

Ketoprofen usage

A

Acute pain and chronic pain from osteoarthritis
Alleviation of inflammation and pain associated with MSK and GI disorders

25
Q

Ketoprofen licensing

A

Cattle
Horses
Pigs
Not licenced for peri-operative indication

26
Q

Flunixin usage

A

Alleviation of inflammation and pain associated with MSK, respiratory and GI disorders

27
Q

Flunixin Licensing

A

Cattle
Horses
Pigs

28
Q

Oxicam derivatives action

A

COX2 selective

29
Q

Oxicam derivatives usage

A

Alleviation of inflammation and pain in chronic MSK disorders and post-operative pain

30
Q

Oxicam derivatives example and licensing

A

Meloxicam - Small animal, Farm Animal, Horses

31
Q

Coxib action

A

Highly COX2 selective
>100 fold selectivity for COX2 over COX1

32
Q

Coxib uses

A

Pain and inflammation associated with osteoarthritis and peri-operative

33
Q

Coxib examples

A

Robenacoxib
Firocoxib
Mavacoxib
Cimicoxib

34
Q

Coxib licensing

A

Robenacoxib - Small animal
Firocoxib - Small animal, horses
Mavacoxib - dogs
Cimicoxib - dogs

35
Q

Grapiprant Action

A

NOT COX INHIBITOR - still affects prostaglandin
* Selective antagonist of the EP4 receptor
○ Receptor that mediates PGE2-induced nociception

Rapid absorption after oral treatment

36
Q

Grapiprant licensing

A

small animals

37
Q

Grapiprant cautions

A

Dogs suffering from pre-existing liver, cardiovascular or GI disease

38
Q

Why are there contraindications to COX inhibitors

A

Unwanted side effects come from inhibition of COX1
Usually in older patients

39
Q

What are the contraindications of COX inhibitors?

A

GI disturbances:
○ Due to reduction in protective prostaglandins in gastric mucosa
○ Gastric and intestinal damage may occur with chronic use with risk of ulceration and bleeding
Adverse cardiovascular effects:
○ Can occur with many NSAIDs including coxib
○ May be related to COX2 inhibition in the kidney leading to hypertension
Reversible renal insufficiency:
○ Mainly seen in patients with compromised renal function when the compensatory PGI2/PGE2-mediated vasodilation is inhibited
Bronchospasm:
○ Seen in aspirin-sensitive asthmatics

40
Q

How long should you wait between administering different NSAIDs

A

24 hours
Do not administer different NSAIDs concurrently

41
Q

When should you not use NSAIDs?

A

Animals suffering from cardiac, hepatic or renal disease
Where there is the possibility of gastrointestinal ulceration or bleeding