NSAID 2 Flashcards
1
Q
What drugs are in the classical/traditional group
A
Acetaminophen, aspirin, flunixin meglumine, phenylbutazone
2
Q
Drugs in the preferential group
A
Carprofen and meloxicam
3
Q
Drugs in the COX II selective category
A
Firocoxib, robenacoxib, deracoxib
4
Q
A type of EP4 antagonist
A
Grapiprant
5
Q
NSAIDs absorption
A
- good oral absorption
- weak acids
6
Q
NSAID Distribution
A
- at least 90% bound to albumin
- small Vd
- accumulation @ site of distribution
7
Q
NSAID Hepatic metabolism
A
- hepatic metabolism= primary mode of clearance
- phase 1&2
- enterohepatic circulation
8
Q
Acetaminophen
A
- peroxidase inhibition
- centrally acting analgesic and anti-pyretic
9
Q
Feline acetaminophen toxicity
A
- contraindication for cats
- issue w/ phase 2 metabolism (deficiency in glucuronyl transferase)
- glutathione overwhelmed (hepatic toxicity and methemoglobinemia)
- single adult dose can be lethal
10
Q
Treatment for acetaminophen toxicity
A
Promote glutathione formation, microsomal enzyme inhibitors, antioxidants
11
Q
What promotes glutathione formation
A
N-acetylcysteine and S-adeosyl methionine
12
Q
Cimetidine is a type of
A
Microsomal enzyme inhibitor
13
Q
Disposition of aspirin
A
- variable bioavailability
- 50-70% protein bound
- rapid distribution into ECF (synovial, peritoneal, saliva, and milk)
- elimination via hepatic conjugation with glucuronide
- renal excretion
14
Q
Adverse events of aspirin
A
- antithrombotic (inhibits platelet activity)
- wide safety margin in most species
15
Q
Aspirin adverse events in cats
A
- requires glucuronidation for elimination
16
Q
Clinical signs of aspirin toxicosis
A
Depression, vomiting, electrolyte imbalances, hyperthermia, convulsions, death
17
Q
Chronic signs of aspirin toxicosis
A
Bone marrow depression, toxic hepatitis, GI bleeding, cartilage damage, and renal failure
18
Q
Treatment for aspirin adverse events
A
Supportive care
19
Q
Flunixin meglumine
A
- a nicotinic acid
- used for visceral pain (colic in horses)
- 80% bioavailability
- short 1/2 life
- long duration of effect due to irreversible COX inhibition
20
Q
Flunixin meglumine is approved for use in
A
Cows for pyrexia
21
Q
Flunixin meglumine is prohibited in
A
Veal calves and lactating dairy cattle
22
Q
Adverse effects of flunixin meglumine
A
- mask surgical pain in equine patients
- gastric ulceration
- clostridial myositis from IM injection
23
Q
Structure activity relationship of phenylbutazone
A
- pyrazolone (enolic acid)
- dosing forms (IV, granular, bolus, paste, tablet)
24
Q
Uses of phenylbutazone in horses/cattle and dogs
A
- horses/cattle: musculoskeletal pain
- documented use in K9
25
In which species is phenylbutazone toxic
Cats
(Causes aplastic anemia & bone marrow depression)
26
Disposition of phenylbutazone
- metabolized by liver
- highly protein bound
- excreted in urine (more alkaline urine increases excretion)
27
Adverse effects of phenylbutazone
- narrow therapeutic index
(Use high end dose for short pd. Duration)
- GI ulceration
- low serum protein conc.
- extravasation of IV product (cervical tissue necrosis)
- renal papillary necrosis (if given wrong)
28
What do you treat gastric ulcers w/?
- proton pump inhib. (Omeprazole)
- PGE replacement (misoprostol)
- supportive care (IV fluids, correct acid/base disturb. & electrolyte abnorm.)
29
What happens if Cox1:Cox2 <1?
- less drug to inhibit COX1
(More COX 1. Activity)
30
What happens if COX1:COX2>1
- More drug to inhibit COX1
OR
- More potent for COX2
31
COX1 selective ratio drugs (ratio<1)
Aspirin, ketoprofen, phenylbutazole, flunixin, piroxicam, ibuprofen, naproxen
32
COX2 preferential (ratio>1-100:1)
Carprofen, etodolac, meloxicam
33
COX2 Selective (ratio>100-1000:1)
Firocoxib, robenacoxib, deracoxib
34
Carprofen forms
- injection, tablets, chews
35
Carprofen is a
Proprionic acid
36
Why should you be cautious w/ giving K9s carprofen chews?
Dogs think they’re treats, so if they gain access to the container, its easy for them to OD
37
Uses of carprofen
- 1st COX2 preferential drug approved for use in animals
- in animals: >6 wks, K9s being treated form OA, post-op pain mgmt
38
Why would carprofen be used in K9 puppies >6 wks old
- parvo
- trauma (pediatric spays & neuters)
39
Adverse effects of carprofen
- one of the safer NSAIDS
- gastric ulceration
- hepatotoxicity
- renal tubular disease
40
Hepatotoxicity caused by carprofen
- common in old patients
- seen w/ concurrent use of phenobarb.
- need to monitor carefully (liver enzymes & funct)
41
Forms of meloxicam
Tablet, oral susp., inj.
42
Therapeutic use of meloxicam
- OA in K9
- Cats post-op pain
43
Adverse events in cats using meloxicam
- single dose only
- renal failure
- death
- black box warning
44
Adverse effects of dogs using meloxicam
GI perforation
45
List COX 2 Selective drugs
Drugs that end in “-coxib”
46
EP4 agonist of interest
Grapiprant
47
Dose form of firocoxib
- K9 Chew
- equine inject. & paste
48
Disposition of firocoxib
- variable elim. 1/2 life
- K9: 9 hours
- equine: 48 hrs (loading dose needed)
49
Dose form of deracoxib
- chewable tabs
50
What was the first coxib approved for animal use?
Deracoxib
51
Deracoxib is used for
Post op pain and OA >4 mos
52
Dosage form of robenacoxib
Tabs & inj
53
Use of robenacoxib
- SID
- OA & post op pain
54
Disposition of robenacoxib
- short 1/2 life
- persists longer at site of inflamm
- long DOA
55
Indication of grapiprant
Control pain & inflamm assc. W/ OA in K9
56
EP4 Receptor
- PGE2 ligand
- @ sensory nerve end
- EP4 receptor antagonist
- K9 approved use
57
Nerve growth factor
- prod. By inflamm. Cells
- binds to sensory nerve ending, incr. pain signal rate
- releases more inflamm. Cytokines
58
NGF (nerve growth factor) inhibitor
- reduce pain signals
- reduce inflamm. Response prod.
- monoclonal antibody (bedinvetmab in K9; frunvetmab in cats)
59
Bedinvetmab
- K9 only
- monoclonal antibody that blocks NGF
- QM SQ inj. for osteoarthritis
- onset: 7-28 days; peak: 56 days
- no response after 2 Tx, then choose another Tx
- contraind.: hypersens., <12 mos age, breeding, pregnant, lactating, NGF inhibition messes w/ normal nervous system dev.
- t1/2: 12 days
60
Frunevetmab (Solensia)
- same MOA as bedinvetmab
- OA in cats
- QM SQ inj.
- t1/2: 10 days
- contraind.: <12 mos old, under 2.5 kg, breeding, lactating, pregnant
- AE: Scabbing on head and neck, dermatitis, pruritus
61
Common K9 NSAIDs
- carprofen (>6 wks)
- deracoxib (>4 m)
- meloxicam (>6 m)
- firocoxib (>6m)
62
Common cat NSAIDs
- robenacoxib (>4.5m; >5 lb)
- meloxicam (>6m; black box warning)
