NSAIDs 1 Flashcards
Carprofen (Rimadyl)
-oral chews and injectable)
-considered Cox-2 selective
>racemic mixture (S+R, S more selective for cox 2)
-used for osteoarthritis (chronic) and post-op pain
How do analgesic endpoints differ?
-various endpoints (behaviour? movement? cortisol? pressure?)
-differences in how procedure is performed
-drug administration affects dose, route, timing
Carprofen adverse effects
-low incidence of vomiting and diarrhea
-idiosyncratic (not dose dependent) hepatic toxicity in dogs
>occurs up to 1/2000 dogs
>occurs few days/weeks of therapy
>detected with pre-treatment blood sample
Meloxicam
-cox-2 preferential
-oral suspension (1.5mg/ml in dogs; 0.5 mg/ml in cats), tablets (1 or 2.5mg for dogs), injectable (0.5%; 5mg/ml for dogs and cats)
Why is meloxicam oral suspension useful?
Easier to individualize the dose
-can titrate down and use less but still get desired effect
Meloxicam indications
-acute and chronic musculoskeletal disorders in dogs
-acute musculoskeletal disorders in cats
-useful for post-op pain (orthopedic, soft tissue surgery)… better than butorphanol
**EBM study: arthritis high level of comfort
Adverse drug events from Meloxicam
Dogs: low incidence of vomiting and diarrhea
Cats: renal failure (often linked with dehydration)
USA: no musculoskeletal claim in cats (Black box warning- for long use)
Deracoxib (deramaxx)
-cox 2 selective
-chewable tablets
-use in dogs
Deracoxibb (deramaxx) indications
-chronic osteoarthritis in dogs
-orthopedic post-op pain in dogs
Deracoxib (deramaxx) adverse effects
-low incidence of vomiting and diarrhea
-renal tubular degeneration at high doses
-causes of GI tract perforation at high doses or with other NSAIDs/steroids
Firocoxid (previcox, prevequine)
-cox 2 selective
-chewable tablets for dogs and horses
-doses in dogs is 50x higher than horse. Means you are giving exact same amount for both species
Firocoxib (previcox, prevequine) indications
-osteoarthritis in dogs and horses
-post op pain in dogs
Firocoxib adverse events
-low incidence of vomiting and diarrhea (possibly lower than other NSAIDs)
-smaller therapeutic index in young dogs
Robenacoxib (onsior)
-cox 2 selective (very high in cats 502:1)
-oral tables and injectable solution
-a lot of evidence
Robenacoxib indications for cats
- Acute pain and inflammation (scratches/bites without abscesses and musculoskeletal injuries such as sprains and strains)
- Post op pain and inflammation
- Chronic musculoskeletal disorders
**no other NSAIDs have chronic claim in cats (but likely meloxicam will work as well)
Robenacoxib indications for dogs
- Osteoarthritis in dogs
- Post op pain associated with soft tissue
Human NSAIDs in vet med?
Not approved
-Advil, tylenol (watch for methemoglobinemia), aspirin, aleve, voltaren
Toxicity! Mostly ibuprofen (Advil)
**Safety and efficacy is much lower than vet approved drugs. Often a small therapeutic window
Galliprant (grapiprant) mechanism
-PGE2 receptor antagonist (not a cox inhibitor)
>Blocks EP4 receptor by blocking PGE2 and mediating sensitization of sensory neurons
Galliprant use
-used for dogs with arthritis; no claims for use in post-op
-alternative to NSAIDs; can’t use them concurrently
-oral tablet (various sizes)
**Thought to be safer than NSAIDs, but efficacy might be lower.
>may want to use galliprant though in cases where dog may have GI ulcer history or liver/kidney diseases
Galliprant possible adverse events
-vomiting
-diarrhea
-inappetence
-lethargy
-buccal ulcers
-immune mediated hemolytic anemia
Solensia (frunevetmab) mechanism
-Not a drug; considered a biologic
-Monoclonal antibody specific for blocking feline nerve growth factor (NGF)
>NGF upregulated during chronic inflammatory conditions and are needed for pain response
Solensia use
-Used in cats for arthritis
-Long-acting injection(half life=10-12 days, repeated monthly, need two injections to reach steady state)
>elimination=proteolysis
-Cmax= 3-7 days after dose
-minimal accumulation in plasma after 5 doses
Solensia efficacy and safety
Efficacy: it works; but some individuals undergo placebo effect
Safety: high safety levels
Librela (bedinvetmab)
Monoclonal antibody specific for canine nerve growth factor (NGF)
-similar to solensia
-repeated monthly
-Safety and efficacy high
Can you combine NSAIDs with non-NSAIDs for osteoarthritis analgesia?
-Not great evidence. Benefits for multi-modal analgesia with other painful conditions
>synergism may not occur
issues with determining NSAID safety
- cannot compare different products by adverse events because number of sales will affect it
2.Conditions of use vary between NSAIDs (one time vs long term)
- Voluntary reporting is skewed
- Amount of evidence
What are you looking for in terms of safety in NSAIDS?
-vomiting and diarrhea are most common signs
-hepatic adverse effects; may lead to idiosyncratic rxn
-kidney injury and GI effects are dose dependent
NSAID metabolism in cats
Cats are poor glucuronidators and hepatic clearance, therefore increased half life and then possibly increased toxicity risk
Approved products: meloxicam and robenacoxib
Other drugs, but not much data supporting their use: firocoxib
carprofen
Using meloxicam in cats
-can be used in cats long term
>need to ensure they are hydrated
**safety: safely given to cats with renal failure (no decrease in lifespan) and may even slow renal disease in some cats suffering from both CKD and DJD
KEYS to NSAID use in small animals
Effects: Gi lesions, GI signs, hepatic damage, renal damage
No newer NSADI is consistently more effective than others
Use lowest effective dose
Phenylbutazone (Bute)
-NSAID
-oral and injectable products
-very old drug used for musculoskeletal inflammation (lameness) label indications
Flunixin meglumine (Banamine)
-injectable solution (IV or IM)
-indicated for musculoskeletal disorders and visceral pain (ex.colic)
Firocoxib (Prevequine)
-NSAID
-Used for osteroarthritis in horses
-generally safe
-oral tablet
Meloxicam in horses?
-Extra label use in Canada but in UK, used for acute and chronic musculo-skeletal disorders, colic pain
Pregnant mare NSAIDs?
No approved NSAIDs for pregnant mares
Meloxicam injectable in food animals uses
Cattle: diarrhea, used for de-horning pain, mastitis, abdominal surgery
Sheep: pain and inflammation
Swine: non-infectious locomotor disorders to reduce lameness and inflammation
-not labelled for castration, BRD, anti-pyretic
**will have meat and milk withdrawal times
Meloxicam oral suspension in food animals
-Only labelled for castration
*double the dose of injectable
-cheaper than injectable
Flunixin (banamine)
-NSAID for food animals in toxic shock (endotoxemia) and pyrexia (fever); not analgesia
>believed to bind the endotoxin
-injectable
**has severe injection site rxns so can only be used IV
Flunixin used transdermally
-Label use for pyrexia of BRD and mastitis, and analgesia for foot rot
Ketoprofen (anafen)
-food animal NSAID (not other animals!!) for fever, pain, inflammation for a lot of disorders
-injectable
-cost is reasonable because able to earn it back from milking her
***no milk withdrawal period, short meat withdrawal time
Aspirin
-not approved in USA, approved in Canada
-very poor bioavailability from the rumen
-cheap but get what you pay for
Meloxicam use in sheep
-single dose lasts for days (14 days) to alleviated pain and inflammation
*no oral formulations approved for small ruminants; only approved in beef cattle
*Buccal meloxicam used in Australia
NSAIDS used in pigs
-Ketoprofen (IM)- used for fever and inflammation due to respiratory disorders
Flunixin (IM)- pyrexia associated with SRD
Acetaminophen :pyrexia associated with SRD. Medicated water, 3 day WP
Meloxicam for swine
-injectable (more dilute version for pigs)
-used for relief of post op pain associated with minor soft tissue surgery such as castrating and tail docking
Resflor
Combination of flunixin and florfenicol
-used for BRD and fevers in cattle
Zeleris
combination of Meloxicam and florfenicol
-used for BRD and fevers in cattle
Draxxin KP
-combination of tulathromycin and ketoprofen
-used for BRD and fevers in cattle
*small dose volume
