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Pharmacology > NSAID 2 > Flashcards

NSAID 2 Flashcards

1
Q

What drugs are in the classical/traditional group

A

Acetaminophen, aspirin, flunixin meglumine, phenylbutazone

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2
Q

Drugs in the preferential group

A

Carprofen and meloxicam

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3
Q

Drugs in the COX II selective category

A

Firocoxib, robenacoxib, deracoxib

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4
Q

A type of EP4 antagonist

A

Grapiprant

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5
Q

NSAIDs absorption

A
  • good oral absorption
  • weak acids
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6
Q

NSAID Distribution

A
  • at least 90% bound to albumin
  • small Vd
  • accumulation @ site of distribution
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7
Q

NSAID Hepatic metabolism

A
  • hepatic metabolism= primary mode of clearance
  • phase 1&2
  • enterohepatic circulation
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8
Q

Acetaminophen

A
  • peroxidase inhibition
  • centrally acting analgesic and anti-pyretic
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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
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10
Q

Treatment for acetaminophen toxicity

A

Promote glutathione formation, microsomal enzyme inhibitors, antioxidants

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11
Q

What promotes glutathione formation

A

N-acetylcysteine and S-adeosyl methionine

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12
Q

Cimetidine is a type of

A

Microsomal enzyme inhibitor

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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
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14
Q

Adverse events of aspirin

A
  • antithrombotic (inhibits platelet activity)
  • wide safety margin in most species
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15
Q

Aspirin adverse events in cats

A
  • requires glucuronidation for elimination
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16
Q

Clinical signs of aspirin toxicosis

A

Depression, vomiting, electrolyte imbalances, hyperthermia, convulsions, death

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17
Q

Chronic signs of aspirin toxicosis

A

Bone marrow depression, toxic hepatitis, GI bleeding, cartilage damage, and renal failure

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18
Q

Treatment for aspirin adverse events

A

Supportive care

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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
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20
Q

Flunixin meglumine is approved for use in

A

Cows for pyrexia

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21
Q

Flunixin meglumine is prohibited in

A

Veal calves and lactating dairy cattle

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22
Q

Adverse effects of flunixin meglumine

A
  • mask surgical pain in equine patients
  • gastric ulceration
  • clostridial myositis from IM injection
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23
Q

Structure activity relationship of phenylbutazone

A
  • pyrazolone (enolic acid)
  • dosing forms (IV, granular, bolus, paste, tablet)
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24
Q

Uses of phenylbutazone in horses/cattle and dogs

A
  • horses/cattle: musculoskeletal pain
  • documented use in K9
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25
Q

In which species is phenylbutazone toxic

A

Cats

(Causes aplastic anemia & bone marrow depression)

26
Q

Disposition of phenylbutazone

A
  • metabolized by liver
  • highly protein bound
  • excreted in urine (more alkaline urine increases excretion)
27
Q

Adverse effects of phenylbutazone

A
  • 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
Q

What do you treat gastric ulcers w/?

A
  • proton pump inhib. (Omeprazole)
  • PGE replacement (misoprostol)
  • supportive care (IV fluids, correct acid/base disturb. & electrolyte abnorm.)
29
Q

What happens if Cox1:Cox2 <1?

A
  • less drug to inhibit COX1
    (More COX 1. Activity)
30
Q

What happens if COX1:COX2>1

A
  • More drug to inhibit COX1

OR

  • More potent for COX2
31
Q

COX1 selective ratio drugs (ratio<1)

A

Aspirin, ketoprofen, phenylbutazole, flunixin, piroxicam, ibuprofen, naproxen

32
Q

COX2 preferential (ratio>1-100:1)

A

Carprofen, etodolac, meloxicam

33
Q

COX2 Selective (ratio>100-1000:1)

A

Firocoxib, robenacoxib, deracoxib

34
Q

Carprofen forms

A
  • injection, tablets, chews
35
Q

Carprofen is a

A

Proprionic acid

36
Q

Why should you be cautious w/ giving K9s carprofen chews?

A

Dogs think they’re treats, so if they gain access to the container, its easy for them to OD

37
Q

Uses of carprofen

A
  • 1st COX2 preferential drug approved for use in animals
  • in animals: >6 wks, K9s being treated form OA, post-op pain mgmt
38
Q

Why would carprofen be used in K9 puppies >6 wks old

A
  • parvo
  • trauma (pediatric spays & neuters)
39
Q

Adverse effects of carprofen

A
  • one of the safer NSAIDS
  • gastric ulceration
  • hepatotoxicity
  • renal tubular disease
40
Q

Hepatotoxicity caused by carprofen

A
  • common in old patients
  • seen w/ concurrent use of phenobarb.
  • need to monitor carefully (liver enzymes & funct)
41
Q

Forms of meloxicam

A

Tablet, oral susp., inj.

42
Q

Therapeutic use of meloxicam

A
  • OA in K9
  • Cats post-op pain
43
Q

Adverse events in cats using meloxicam

A
  • single dose only
  • renal failure
  • death
  • black box warning
44
Q

Adverse effects of dogs using meloxicam

A

GI perforation

45
Q

List COX 2 Selective drugs

A

Drugs that end in “-coxib”

46
Q

EP4 agonist of interest

A

Grapiprant

47
Q

Dose form of firocoxib

A
  • K9 Chew
  • equine inject. & paste
48
Q

Disposition of firocoxib

A
  • variable elim. 1/2 life
  • K9: 9 hours
  • equine: 48 hrs (loading dose needed)
49
Q

Dose form of deracoxib

A
  • chewable tabs
50
Q

What was the first coxib approved for animal use?

A

Deracoxib

51
Q

Deracoxib is used for

A

Post op pain and OA >4 mos

52
Q

Dosage form of robenacoxib

A

Tabs & inj

53
Q

Use of robenacoxib

A
  • SID
  • OA & post op pain
54
Q

Disposition of robenacoxib

A
  • short 1/2 life
  • persists longer at site of inflamm
  • long DOA
55
Q

Indication of grapiprant

A

Control pain & inflamm assc. W/ OA in K9

56
Q

EP4 Receptor

A
  • PGE2 ligand
  • @ sensory nerve end
  • EP4 receptor antagonist
  • K9 approved use
57
Q

Nerve growth factor

A
  • prod. By inflamm. Cells
  • binds to sensory nerve ending, incr. pain signal rate
  • releases more inflamm. Cytokines
58
Q

NGF (nerve growth factor) inhibitor

A
  • reduce pain signals
  • reduce inflamm. Response prod.
  • monoclonal antibody (bedinvetmab in K9; frunvetmab in cats)
59
Q

Bedinvetmab

A
  • 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
Q

Frunevetmab (Solensia)

A
  • 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
Q

Common K9 NSAIDs

A
  • carprofen (>6 wks)
  • deracoxib (>4 m)
  • meloxicam (>6 m)
  • firocoxib (>6m)
62
Q

Common cat NSAIDs

A
  • robenacoxib (>4.5m; >5 lb)
  • meloxicam (>6m; black box warning)

Pharmacology (20 decks)

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