NSAIDs Flashcards
what are 4 uses of NSAIDs?
- Mild to moderate pain relief
- Anti-inflammatory
- Analgesic
- Anti-pyretic
What is the largest group of drugs having adverse effects?
NSAIDs
The use of lower doses of multiple drug classes provides higher safety and less negative side effects is known as what?
Multi-modal analgesia
NSAIDs have sparing effects on what other category of drug?
Opioids
What is the rate-limiting step of the arachidonic acid cascade?
Release of AA from membrane phospholipid catalyzed by enzyme phospholipase A2.
Cyclooxygenase (COX) oxidizes arachidonic acid (AA) to what?
Prostaglandins (PGs)
Lipoxygenase (LOX) oxidizes AA to what?
Leukotrienes
Are prostaglandins continually synthesized?
Yes
Are prostaglandins stored?
No
Where do prostaglandins act?
Locally at site of production.
T/F: Prostaglandins have only a few physiological functions.
False - Prostaglandins have many physiological functions.
What can inhibition of prostaglandins result in?
Serious side effects.
What are 2 functions of COX 1?
- Mucosal defense
- Platelet function (TxA2)
What effect does COX 2 have on mucosa?
Prevents erosions & promotes healing.
Which COX acts as an anti-inflammatory?
How?
- COX 2
- Inhibits leukocyte adherence
Which COX offers renal protection?
COX 2
Which COX is involved with fever initiation?
COX 3
What are 4 functions COX inhibition affects?
- Primary plug formation of platelets
- Renal & gastric mucosa vascular tone
- Smooth muscle contraction
- Temperature regulation
T/F: Different drugs inhibit COX 1, 2 & 3 variably.
True
Which COX is involved with vicero-nociception and thermal stimulation?
COX 1
T/F: COX 1 is involved in constitutive functions with COX 2.
True
Which COX is inducible?
COX 2
Which COX is up-regulated during inflammatory states?
COX 2
There is over a 20 times greater presence of which COX at injured sites?
COX 2
Which COX has a key role in nociception?
COX 2
What are 2 functions of COX 3?
- Pyrexia
- Analgesia
Does COX 3 have better or poorer anti-inflammatory properties than COX 1 & 2?
Poorer
COX 3 is derived from what?
COX 1 gene
What are 5 drugs that inhibit both COX 1 & 2?
- Aspirin
- Phenylbutazone
- Ketoprofen
- Ketorolac
- Flunixin meglumine
What are 5 drugs that are COX 2 preferential and have weak COX 1 inhibition?
- Meloxicam
- Carprofen
- Etodolac
- Vedaprofen
- Tolfenamic acid
What are 3 drugs that are COX 2 selective?
- Deracoxib
- Firocoxib
- Robenacoxib
What are 2 drugs that are COX 3 preferential and have weak COX 1 & 2 inhibition?
- Acetaminophen
- Diclofenac
What is an example of a COX & LOX inhibitor?
Tepoxalin
What do prostaglandins mediate?
- Pain
- Inflammation
Prostaglandins have what type of central effects?
Central anti-nociceptive effects
Are NSAIDs highly protein bound?
How might this affect other drugs?
- Yes
- May displace other drugs and increase their plasma concentration.
What are 2 concerns with giving NSAIDs?
- Patient with underlying organ dysfunction.
- Patient receiving other highly protein-bound drugs with narrow therapeutic index.
Do NSAIDs have a wide or narrow safety margin?
Narrow
Can the upper dose limit be exceeded with NSAIDs?
No
What dose of NSAIDs should be used?
Lowest effective dose
How much time should be waited in between drugs?
Minimum of 7 days
How old do patients have to be for NSAIDs?
Over 6 weeks old
What should the hydration status be?
Well-hydrated
What are 3 contraindications for the use of NSAIDs?
- Concern for or evidence of GI ulceration
- Concurrent corticosteroid use
- Concurrent administration of other NSAID
What type of renal and hepatic function is needed?
Normal
Surgical preemptive use of NSAIDs should be avoided in what for cases?
- Expected hemorrhage
- Hypotension
- Prolonged procedure
- Any contraindications
How long does it take for therapeutic effects of NSAIDs to be seen with post-operative administration?
Does route of administration matter?
- 45 minutes or greater
- No
Should NSAIDs be given with food?
Yes
What should be avoided with NSAIDs?
Direct contact with gastric mucosa
What are 2 types of surgeries NSAIDs can provide post-operative pain management for?
- Orthopedic surgeries
- Soft tissue surgeries
What should NSAIDs be co-administered with for post-operative pain management?
Opioid
What needs to be done with long-term NSAID use?
Monitor the patient
Are coagulopathies a contraindication for NSAID use?
Yes
Are breeding/pregnancy a contraindication for NSAID use?
Yes
What are 2 side effects seen with aspirin?
- GI ulceration
- Decreased platelet activity
What formulation does aspirin come in?
Tablet
What type of COX inhibitor is aspirin?
Non-selective COX inhibitor (Inhibits 1 & 2)
Phenylbutazone is commonly used in what 2 species?
What species is it not recommended in?
- Horses & cattle
- Dogs
What are 3 formulations that phenylbutazone comes in?
- Powder
- Paste
- Parenteral
What is the duration of phenylbutazone?
12 hours
There is a high risk of what 2 side effects with phenylbutazone?
- GI ulceration
- Nephrotoxicity
Residues of phenylbutazone are toxic to what species?
Should be avoided in cattle of what age?
- Humans
- Greater than 20 months old
What type of COX inhibitor is phenylbutazone?
COX 1 & 2
What 2 species is flunixin meglumine used in?
What species in Europe?
- Ruminants
- Horses
- Dogs in Europe
What is the DOA for flunixin meglumine?
12-24 hours
What are 4 side effects seen with flunixin meglumine?
- Local swelling
- GI ulceration
- Nephrotoxicity
- Hepatotoxicity
What type of COX inhibitor is flunixin meglumine?
COX 1 & 2
What species is carprofen widely used in?
What species in Europe?
In UK?
- Dogs
- Cats
- Horses
What are 2 formulations for carprofen?
- Tablet
- Parenteral
What is the DOA of carprofen?
12-24 hours
What are 4 side effects seen with carprofen?
- Nephrotoxicity
- Hepatotoxicity
- GI ulceration
- Hemostatic deficiencies
Hepatotoxicity from carprofen is seen particularly in what dog breed?
Labs
What type of COX inhibitor is carprofen?
COX 2 preferential
What are 4 species meloxicam can be used in?
- Dogs
- Cats
- Horses
- Cattle
What are 3 formulations for meloxicam?
- Oral liquid
- OTM spray
- Parenteral
What is the DOA for meloxicam?
12-48 hours
What are 4 side effects seen with meloxicam?
- Vomiting
- Diarrhea
- Increase in liver/kidney enzymes
- Decrease in appetite
What type of COX inhibitor is meloxicam?
COX 2 preferential
What formulation does deracoxib come in?
Tablet
What is the DOA for deracoxib?
24 hours
What are 5 side effects of deracoxib?
- Vomiting/diarrhea
- Hematochezia
- Melena
- Anorexia
- Renal issues
What type of COX inhibitor is deracoxib?
COX 2 selective
What formulation does firocoxib come in for dogs?
What 2 forms for horses?
- Dog: tablet
- Horse: paste & parenteral
What is the DOA for firocoxib?
24 hours
What are 5 side effects seen with firocoxib?
- Abdominal pain
- Diarrhea
- Urticaria
- PU/PD
- Renal
What type of COX inhibitor is firocoxib?
COX 2 selective
What 2 formulations does robenacoxib come in?
- Tablet
- Parenteral
What is the DOA of robenacoxib?
24 hours
What are 3 side effects seen with robenacoxib?
- Vomiting/diarrhea
- GI ulceration
- Renal toxicity
What type of COX inhibitor is robenacoxib?
COX 2 selective
What 2 formulations does acetaminophen come in?
- Tablet
- Oral suspension
Is acetaminophen approved for use in veterinary patients?
No
What is the DOA?
8 hours
What species should acetaminophen not be used in?
Cats
What are 3 side effects seen with acetaminophen?
- Hepatic damage
- Renal damage
- GI ulceration
What type of COX inhibitor is acetaminophen?
COX 3 preferential
What species is tepoxalin used in?
Dogs
What formulation does tepoxalin come in?
Dissolvable wafer
What is the DOA of tepoxalin?
24 hours
Is tepoxalin commercially available?
No
What type of inhibitor is tepoxalin?
COX 1, 2 and LOX
What does LETD stand for?
Locally enhanced topical delivery
What is an example of a topical NSAID?
Use?
- Surpass (diclofenac)
- Equine osteoarthritis
Are there any ophthalmic topical NSAIDs approved for veterinary use?
No
