NSAIDs Flashcards
What parts of the pain pathway do NSAIDs act on?
modulation and transduction
What are the main effects of NSAIDs?
They prevent inflammation by inhibiting cyclooxygenase (COX) enzymes.
Aside fro analgesia, what are other uses for NSAIDs?
anti-pyretic and inhibit tumor growth (anti-angiogenesis)
T/F: NSAIDs and steroids can be used together.
False
What is the function of COX-1 and what 2 hormones does it produce?
Constitutive, physiologic production of prostaglandins that play an important role in normal homeostasis. Thromboxane A2 and Prostaglandin E1 (PGE1)
COX-2 functions in what?
Inducible production of prostaglandins produced during times of inflammation.
T/F: selective COX-2 inhibitors are over the counter.
False. They are RX only.
T/F: NSAIDs are weak acids.
True.
Which is the strongest NSAID?
Aspirin.
T/F: NSAIDs have a greater effect on chronic inflammation than acute inflammation.
False. greater effect on acute inflammation.
Are NSAIDs highly protein bound?
Yes, about 95-99% of them are protein bound.
T/F: NSAIDs can cross the BBB into the CNS
True
Where are NSAIDs metabolized and where are they excreted?
metabolized in the liver (both phase 1 and 2 if hepatic metabolism in the liver), and excreted in the urine.
T/F: biliary excretion and enterohepatic recirculation is never seen with NSAIDs
False. It is seen with some NSAIDs.
After how many half-lives are drugs nearly completely excreted?
5
What are 2 special uses of NSAIDs?
antithrombotic effects and antineoplastic effects.
What are some adverse effects NSAIDs can have?
GI irritation/ulceration, vomiting, anorexia, diarrhea, renal damage and decreased blood flow, as well as post-op analgesia and hypotension.
Does vomiting, diarrhea, and anorexia mean that there is an ulcer present?
No.
Who is at higher risk of renal damage when using NSAIDs?
Cats
When should NSAIDs be used post-op?
After recovery from anesthesia.
Can hepatotoxicity occur as an adverse effect when using NSAIDs?
Yes, especially in cats. Acetaminophen gets metabolized into toxic intermediates by phase 1 metabolism.
What large animal NSAID is used as an analgesic for colic and endotoxemia in horses, for visceral pain in cattle, and is not recommended for use in small animals?
flunixin meglumine (Banamine)
T/F: flunixin meglumine (Banamine) can be administered PO and IV in cattle.
False, only IV in cattle.
Should flunixin meglumine be used IM in horses? Why or why not?
No, because muscle necrosis has been reported to occur with IM administration.
T/F: flunixin meglumine can be administered IM in pigs.
True
What species should not be given flunixin meglumine?
Birds, causes renal toxicity.
This drug is used commonly in horses, banned from being used in dairy cattle, and is indicated for treatment of musculoskeletal pain.
Phenylbutazone (bute)
What are the routes of administration of phenylbutazone?
PO (most common) and IV. NOT IM/SC.
What can happen if phenylbutazone is administered via intracarotid injection?
Seizures and CNS stimulation.
What drugs are COX-2 preferentials?
Carprofen, meloxicam, and deracoxib
Which 2 of the COX-2 preferentials are available as injectables (SQ)?
carprofen and meloxicam.
What COX-2 preferential is approved for single use in cats?
Meloxicam
What drugs fall under the COX-2 selective class?
Firocoxib and robenacoxib.
Which COX-2 selective is approved for multiple doses in cats (ip to 3 days)?
Robenacoxib (Onsior)
How long should the washout period be if switching from an NSAID to a steroid?
1-2 weeks.
If changing from a steroid to an NSAID, what should the washout period be?
minimum 1 week after weaning off of the steroid.
If you are switching from NSAID to another NSAID, should you still have a washout period?
Yes, based on half life or go for 1 week (conservative default).
T/F: Acetaminophen inhibits COX
False.
Should acetaminophen be used in cats?
No.
What is the most important form of toxicity caused by acetaminophen? What other toxic effect can be seen?
methemoglobinemia. Hepatic necrosis can also be seen.
What is grapiprant’s mode of action?
antagonist at prostaglandin E2 EP4 receptor.
This drug is a neural steroid used in dogs, cats, and horses, and is mainly used to control neuropathic pain.
gabapentin.
Can gabapentin be used as an adjunct treatment for laminitis in horses?
Yes.
When should you be careful using gabapentin?
in renal insufficiency cases because it is renally excreted.
Does amantadine inhibit cox?
No. It has NMDA receptor antagonist properties.
This medication is a less common adjunctive analgesic, it is good for neuropathic or “wind up” pain, and is available as an oral medication.
amantadine
What is the mode of action of Omega 3 fatty acids? What pathways produce these mediators?
modulation of inflammation. COX, LOX, and cytochrome P450 pathways.
Aside from modulating inflammation, what other effects do omega 3 fatty acids have?
they affect immune cell response by regulating gene expression, they act as a ligand for nuclear receptors, they inhibit TLR4 by endotoxin, and produce substrates for resolvins and protectins.
