NSAIDs 2 Flashcards
Which drug is preferred for the treatment of colic in horses?
Flunixin
Flunixin is COX__-selective in horses.
COX2
Flunixin is COX__-selective in dogs.
COX1
Flunixin is the only NSAID effective verses _____ pain.
Visceral pain
Flunixin is the NSAID with the longest t1/2 in which species?
The horse
In which species is the use of Flunixin FDA-approved?
Bovine & swine
Besides its use verses visceral pain, what are the 3 main effects of Flunixin?
- Analgesia
- Anti-inflammatory
- Anti-pyretic
What is the preferred NSAID versus endotoxicosis?
Flunixin
True or False: Flunixin binds strongly to LPS and endotoxi.
FALSE: Flunixin does NOT bind LPS or endotoxi
True or False: Polymyxin binds to LPS.
TRUE
What two drugs would you combine versus endotoxicosis in the horse?
Ketamine + Flunixin
How does Flunixin work versus endotoxicosis?
Flunixin blocks the PG-related events activated by LPS.
Acetaminophen is selective or non-selective?
Non-selective
To which COX does Acetaminophen bind?
COX2 & COX3
Acetaminophen does NOT inhibit ____ COX2.
Peripheral
Acetaminophen does inhibit ____ COX2 and COX3.
Central
What makes Acetaminophen a weak anti-inflammatory?
Lack of peripheral COX2 inhibition.
What is the primary COX involved in the inflammatory process?
COX2
Anti-COX2 activity of Acetaminophen provides the ____ effect.
Analgesic
Anti-COX3 activity of Acetaminophen provides the ____ effect.
Anti-pyretic
Acetaminophen’s lack of anti-COX1 activity spares the ____ and the ____.
Stomach and platelets
____ at the site of inflammation are able to inactivate Acetaminophen.
Peroxides
What are the two clinical uses for which Acetaminophen would be used?
- Anti-pyresis
2. Analgesia (reduces the pain associated with inflammation without eliminating the cause)
True or False: Acetaminophen has minimal GI effects.
TRUE - lack of COX1 activity
Why is Acetaminophen rarely used in veterinary medicine?
Hepatotoxicity
What is the most nephrotoxic NSAID group?
The “profens”
What are profens?
Propionic acid derivatives
What are the 4 profens?
- Ibuprofen
- Ketoprofen
- Carprofen
- Naproxen
Which of the “profens” are non-selective?
- Ibuprofen
- Ketoprofen
- Naproxen
Which of the “profens” are selective?
- Carprofen
Ketoprofen is a ____ inhibitor and a partial ____ inhibitor.
Ketoprofen is a COX inhibitor and a partial LOX inhibitor.
Which of the “profens” is only approved in the U.S. for use in horses?
Ketoprofen
Ketoprofen is for short or long-term use?
Short-term use
Carprofen is a COX__ inhibitor used in dogs.
COX2
Which two “profens” are contraindicated in pregnant animals?
- Carprofen
2. Ketoprofen
Why are Carprofen and Ketoprofen contraindicated in pregnant animals?
Due to the inhibition of PGF2-alpha, pregnancy can be prolonged.
Carprofen is (more expensive or cheaper) than coxibs?
Cheaper
Which of the “profens” is approved for use in horses against myositis?
Naproxen
What is the disadvantage to Naproxen?
Expensive
When is really the only time Naproxen should be used versus myositis in a horse?
When the myositis is first unresponsive to Phenylbutazone.
Aspirin is a selective COX__ inhibitor.
COX1
What are the 4 therapeutic effects of Aspirin?
- Analgesia
- Anti-inflammatory
- Anti-pyretic
- Anti-coagulant
Aspirin irreversibly acetylates the COX1 enzyme. This irreversibility causes 2 dramatic side effects. What are they?
- Prolonged bleeding time
2. GI ulcers
What is the moiety that “falls off” the NSAID after leaving the acetyl group on COX1?
Salicylate
Salicylate is a reversible ____ inhibitor.
COX
Canine chondrocytes are very sensitive to the complete absence of COX__ activity.
COX1
In sheep, aspirin causes what unwanted side effect?
Pulmonary edema
Is Phenylbutazone a selective or non-selective NSAID?
Selective
Phenylbutazone is a COX__ inhibitor.
COX2
What is the NSAID with the longest t1/2 in the horse?
Flunixin
What is the most commonly used NSAID in horses?
Phenylbutazone
Phenylbutazone is a ____ analgesic versus ____, such as laminitis.
Phenylbutazone is a MUSCULOSKELETAL analgesic versus LAMENESS, such as laminitis.
Which NSAID is banned in food-producing animals, especially lactating dairy cattle?
Phenylbutazone
How does Phenylbutazone cause tolerance to build up in the horse?
Phenylbutazone induces microsomal enzymes that accentuate its metabolism.
Phenylbutazone is banned in food-producing animals because it causes what in humans?
Blood dyscrasias
In which species can Meloxicam be used?
Cats & dogs
In which species can Piroxicam be used?
Dogs
Meloxicam and Piroxicam are selective ____ inhibitors.
COX2
Put the following in order of least to most expensive: Carprofen, Meloxicam, Coxibs, Etodolac
Etodolac
Meloxicam interferes with ____ inhibitors.
ACE
For what is Meloxicam approved in the cat?
As a single injection
What is the adverse effect of long-term Meloxicam use in the cat?
Renal failure
What is Piroxicam most commonly used to treat in the dog?
Bladder cancer (specifically Transitional cell carcinoma)
What is specific about bladder cancer that allows Piroxicam able to treat it?
The neoplastic cells overexpress COX2 and are dependent on that. By blocking the COX2, you decrease their lifespan.
With what 3 things should Piroxicam be combined when treating bladder cancer?
- Misoprostol
- Chemotherapy
- Surgery
Which drug can be used as an alternative to Piroxicam?
Deracoxib
What is the advantage of Deracoxib over Piroxicam?
Deracoxib would not have the nasty effects on the stomach.
Which NSAIDs have the highest affinity/selectivity for COX2?
Coxibs
Which drug was withdrawn from use in humans because of its CV issues?
Rofecoxib
What are the BEST drugs for long-term use against the pain and inflammation of osteoarthritis?
Deracoxib & Firocoxib
True or False: Deracoxib & Firocoxib can be used in dogs with renal insufficiency.
TRUE
Why are you able to use Deracoxib & Firocoxib in dogs with renal insufficiency?
These drugs are eliminated via the bile/feces. (Downside: if you have a dog that likes to eat its own feces, they are taking in double the dose.)
Firocoxib: low or high Vd?
High Vd
NSAIDs: low or high Vd?
Low Vd
Robenacoxib appears to be tissue specific. Which tissue does it target?
Joints
True or False: Robenacoxib is approved for use in cats.
TRUE
Robenacoxib is approved for daily oral use in cats for how long?
3 days
What is the cheapest selective COX2 inhibitor?
Etodolac
What is the adverse side effect associated with Etodolac?
Keratoconjunctivitis sicca
What does Tepoxaline inhibit? (Ex: COX1? COX2? COX3?)
COX1, COX2, LOX
DMSO works by inhibiting what?
Inhibits PGs and scavenges free radicals
How is DMSO administered?
Topically, orally, IV
What is DMSO used against in dogs?
Lick granulomas
In which animal(s) is DMSO banned?
Dairy cattle
True or False: DMSO is not to be used in conjunction with corticosteroids.
FALSE - DMSO can be combined with corticosteroids.
True or False: Dipyrone is approved for use in food animals.
FALSE - Dipyrone is BANNED in food animals.
What are the only 3 NSAIDs that can be used in cats?
- Aspirin
- Meloxicam
- Robenicoxib
Which NSAID can be used in swine?
Flunixin
Which 2 NSAIDs can be used in cattle?
Flunixin & aspirin
Which 5 NSAIDs can be used in horses?
- Flunixin
- Phenylbutazone
- DMSO
- Naproxen
- Fibrocoxib