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NSAIDS
VM 609 Final
29
Veterinary Medicine
Professional
09/25/2012

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Term
NSAIDs Mechanism of Action
Definition
inhibits production of prostaglandins which are inflammatory mediators
inhibits cyclooxygenase enzyme which converts arachidonic acid to prostaglandins
Term
Prostaglandins
Definition
synthesized at constant rate
short half life
play important role in homeostasis
during pathology can incite inflammation and pain
Term
PGE2 Functions
Definition
repro, neuro, metabolic, immune
bone formation and healing
temperature regulation, vasomotor response of vasculature
classic pro-inflammatory mediator (redness, swelling, pain)
promotes hyperalgesia
Term
PGI2 Functions
Definition
regulatory funciton
vascular and thrombotic balance
Term
PGD2 Functions
Definition
mast cells, macrophages
bronchoconstriction, vasodilation, increased capillary permeability, mucous production
elevated in asthmatics
Term
PGF2a Functions
Definition
repro
active in acute and chronic inflammation
Term
COX-2 Functions
Definition
upregulated in inflammation
makes prostaglandins that are useful for protection of the GI tract and for vascular homeostasis
Term
COX-3 Functions
Definition
thought to be mechanism by which acetominophen works
doesn't play a role in prostaglandin mediated fever
Term
COX Selectivity
Definition
COX selection has no bearing on NSAID efficacy
may be more/less effective on individual patient basis
Term
Clinical Use of NSAIDs
Definition
pain relief associated with inflammation
anti-pyretic effects
anti-endotoxic effects
anti-coagulation effects
anti-neoplastic effects
synergistic with opioids
Term
NSAIDs Contraindications
Definition
narrow therapeutic margin of safety
associated with GI toxicity, renal toxicity, hepatic toxicity
Term
GI Side Effects
Definition
COX selectivity does not confer safety
anorexia, vomiting, gastritis, GI irritation, ulceration, melena, perforation, peritonitis, sepsis
Term
Renal Side Effects
Definition
COX-1 and COX-2 both mediate renal perfusion in cases of hypovolemia
avoid NSAIDS in animals with hypovolemia or underlying renal disease
adequately hydrate animals prior to anesthesia
Term
Hepatotoxicity
Definition
obtain baseline ALT and AST values before tx
retest in 3-4 weeks and periodically after
3-5 fold liver enzyme increase are indicators
need to stop tx
most occur in first 3 weeks
Term
Bone Healing
Definition
long-term administration of carprofen decreases bone healing
Term
Which surgeries get NSAIDs
Definition
spays/castration, dentals, minor procedures where the patient is normally healthy
Term
Aspirin
Definition
COX-1 preferential
irreversibly acetylates COX enzymes
chronic use results in gastric mucosa adaptation
used for osteoarthritis pain in dogs
anti-pyretic and anticoagulant
Term
Ketoprofen
Definition
COX-1 and COX-2 inhibitor
controls post-operative pain
should not be used in patients at risk for hemorrhage
approved for horses
Term
Flunixin Meglumine
Definition
COX-1 and COX-2 inhibitor
approved for use in horses and ruminants
used to treat colic
anti-inflammatory, analgesic, anti-endotoxin, anti-pyrteic
used in bovine respiratory disease
better for visceral pain than somatic pain
Term
Diclofenac
Definition
COX-1 and COX-2 inhibitor
used in cream form for joint pain management
multiple joint application can result in high serum concentrations
Term
Meloxicam
Definition
COX-2 Preferential
no antithromboxane activity
does not interfere with hemostasis
GIT ulceration if combined with steroids or aspirin
excellent analgesic when combined with opioids
approved for cats to use high dose once ever
Term
Carprofen
Definition
COX-2 preferential
approved for perioperative and chronic pain management in dogs
antithromboxane is minimal
acute hepatotoxicity and death have been reports in Labs
good analgesia for 12-18 hours post-op
Term
Etodolac
Definition
COX-2 preferential
approved for use in dogs for management of pain and inflammation associated with osteoarthritis
adverse GI effects
Term
Deracoxib
Definition
COX-2 specific
approved for post op pain and inflammation associated with orthopedic sx and chronic osteoarthritis in dogs
GIT lesions tend to be worse compared to other NSAIDs
Term
Firocoxib
Definition
COX-2 specific
approved for control of osteoarthritis in dogs
only COX-2 specific for horses
Term
Robenacoxib
Definition
For the contorl of post operative pain and infalmmation associated with orthopedic surgary, OHE, castration in cats weighing at least 5.5 lb and at least 6 months of age
Term
Acetaminophen
Definition
COX-3 inhibitor with minimal COX-1 and COX-2 effects
antipyretic and mild analgesic for dogs
synergistic with opioids
lethal for cats
Term
Dipyrone
Definition
COX-3 inhibitor
anti-pyretic for horses where other NSAIDs are contraindicated (foals)
don't see much nephro or gastro toxicity
Term
NSAID Washout
Definition
period between switching drugs from NSAID to NSAID or to/from steroids
4-14 days
longer following aspirin or glucocorticoids
takes 14 days for COX to regenerate itself
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