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23 spring: pharm > Test 2: lecture 27 NSAIDs > Flashcards

Test 2: lecture 27 NSAIDs Flashcards

1
Q

what is a common side effect of COX inhibitors

A

GI intolerance- ulcers

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2
Q

what are some negative side effects of COX2 inhibition in humans

A

COX2 blocks prostacyclin, but not thromboxane

causes strokes from increased clot formation and vasoconstriction in humans

Does not happen in dogs

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3
Q

COX inhibition in the GI will cause

A

COX1

peptid ulcers
GI bleed

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4
Q

NSAIDs will do what to the kidneys

A

COX 1 and 2 make PGE2 and PGI1: vasodilation and increased NA and water excretion

Blocking
will cause Na/water retention
hypertension
hemodynamic AKI

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5
Q

NSAIDs and aspirin will do what to the cardiovascular system

A

can cause stroke and MI in humans by inhibiting PGI2 which causes inhibits platelet aggregation → form clots

and not inhibiting thromboxane in platelets

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6
Q

—is an irreversible covalent COX inhibitor

A

aspirin

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7
Q

aspirin is absorbed in the — and binds to — in the serum

A

stomach
albumin

will irreversibly inhibit COX1>COX2

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8
Q

therapeutic effect of aspirin

A

antiinflammatory cause it irreversibly inhibits COX 1+2 → inhibits PG synthesis (reduces pain and fever)

irrevesible COX1 inhibition in the platelets will also block thromboxane synthesis → inhibits platelet aggregation (thins the blood)

body needs to make new platelets to clot

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9
Q

why cant glucocorticoids inhibit platelet thromboxane synthesis?

A

platetes dont have nuclei

steroids need to get into nucleus and cause gene expression

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10
Q

salicylates — inhibit COX

A

competitively
reversible COX inhibitor

Some aspirin is converted to salicylic acid by esterases in tissues and blood

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11
Q

how is aspirin and salicylate metabolized

A

glucuronidation

Salicylate conjugates cleared via kidney

cats do not have UDP-glucuronosyltransferase (UGT) enzymes- therefore half life of aspirin is much higher 37 hr

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12
Q

why is half life of aspirin in cats so high

A

Cats do not have UDP-glucuronosyltransferase (UGT) enzymes

can not metabolize aspirin and salicylate acid

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13
Q

adverse effects of aspirin and salicylates

A

GI issues= ulcers

aspirin is a COX-1 inhibitor → decrease bicarb and mucous secretion in the stomach

can try to counteract this effect by giving buffered aspirin with pH 3.5 or greater

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14
Q

ibuprofen is a — inhibitor and is toxic to —

A

COX- slightly more selective for COX 2 in humans

Dogs (ulcers, kidney failure)

NSAID: Phenylproprionic acid- competitive reversible inhibitor of COX, compete with aspirin for plasma protein binding sites

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15
Q

naproxen is an inhibitor of —

A

COX 1 = COX2

can cause enhanced ulcerogenic potential in dogs

-prolonged enterohepatic recycling: dog half life 74 hrs, horse half life 5 hrs

NSAID: Phenylproprionic acid- competitive reversible inhibitor of COX, compete with aspirin for plasma protein binding sites

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16
Q

what are some NSAID: Phenylproprionic acids

A

naproxen
iburprofen
carprofen (rimadyl)
Etodalac

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17
Q

adverse reactions of NSAID: Phenylproprionic acids

A
  • gastrointestinal toxicities (esp. dogs)
  • possible nephrotoxicity
  • nausea
  • peripheral edema

Ibuprofen, naproxen, carprofen- competitive, reversible inhibitors of COX

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18
Q

how does carprofen (rimadyl) work

A

NSAID: Phenylproprionic acid

selective for COX-2 in dogs
inhibits COX-1 slightly

metabolized in the liver

used for Pain relief, joint pain, post- surgical inflammation

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19
Q

adverse effects of carprofen (rimadyl)

A

GI intolerance / ulceration
Nausea, appetite loss, vomiting, diarrhea (0.1% dogs)
Hepatopathy (1 in 5000 dogs)- in first 3 weeks

should not be given to patients with pre-existing liver, kidney disease or GI
ulcerations

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20
Q

— is similar to carprofen(rimadyl) and is used for managment of chronic OA

A

etodolac (etogesic)

Metabolized in liver
Side effects: GI ulceration

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21
Q

cox2 selective inhibitors in human medicine can cause

A

stroke and heart attack- from clot formation

NO COX2 receptors in platelets: Can not block Thromboxane in platelets → vasoconstiction and platelate formation

blocking COX2→ blocks PGI2 which prevents clot formation

both actions increase clot formations in different ways

Valdecoxib (Bextra)

Rofecoxib (Vioxx)

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22
Q

— are slightly COX2 selective inhibitors in vet medicine

A

Carprofen (Rimadyl)
Etodolac (Etogesic)

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23
Q

— are strongly COX 2 selective inhibitors in vet medicine

A

– Deracoxib (Deramaxx) -dog
– Firocoxib (Previcox) -horse
– Robenacoxib (Onsior) –cats

24
Q

Coxibs are larger than non-selective COX inhibitors and bind to —

A

COX2

Slightly COX2-selective
– Carprofen (Rimadyl)
– Etodolac (Etogesic)
Strongly COX2 selective (coxibs)
– Deracoxib (Deramaxx) -dog
– Firocoxib (Previcox) -horse
– Robenacoxib (Onsior) –cats

25
Q

which coxibs is used in dogs

A

Deracoxib (Deramaxx)

coxibs= cox 2 selective inhibitor

26
Q

which coxibs is approved for horses

A

Firocoxib (Previcox)

coxibs= cox 2 selective inhibitor

27
Q

how does COX selectivity assays work

A

if ratio greater than 1= cox 2 selective

if less than 1 = cox 1 selective

28
Q

two NSAIDs for cats

A

Robenacoxib (Onsior)- cox 2 selective inhibitor
Meloxicam (Metacam)

Cats lack the major UDP-glucuronosyltransferase (UGT) enzymes so they can’t metabolize most NSAIDs

29
Q

repeated usage of — NSAID in cats can cause renal failure and death

A

meloxicam (metacam)

two NSAIDS approved for cats:
Robenacoxib (Onsior)- cox 2 selective inhibitor
Meloxicam (Metacam)

30
Q

meloxicam is moderately — selective

A

COX 2 at low doses

Repeated usage is associated with renal failure and death

approved as NSAID for cat

31
Q

why can meloxicam be given to cats

A

metabolized in the liver (not glucuronidated)

moderately COX-2 selective at low doses

Repeated usage is associated with renal failure and death

32
Q

Flunixin meglumine (Banamine) is a — inhibitor

A

Irreversible, non-covalent COX

NSAID for large animal
Powerful analgesic (on par w/ opiods in horses)

33
Q

advantages of Flunixin meglumine (Banamine)

A

Powerful analgesic (on par w/ opiods in horses)

rapid action (2 hrs) and long duration (24-36hrs)

Useful for relieving pain associated w/ muscoskeletal disorders, surgery, GI spasm (colic) and endotoxic shock.

large animal NSAID

34
Q

adverse effect of Flunixin meglumine (Banamine)

A

Ulceration of tongue, lips, gums, palate, stomach
Anorexia
CNS depression
May cause acute renal failure in dogs via unknown mechanism
– ensure adequate hydration; avoid reductions in blood pressure/volume

large animal NSAID with high pain relief (rapid action and long duration)

35
Q

— is a large animal NSAID that is toxic to humans and can not be used in food animals

A

Phenylbutazone

Irreversibly binds COX (non-covalent)

36
Q

adverse reactions of Phenylbutazone

A

Oral and GI tract erosions, diarrhea, depression

Death - if enteropathy leads to decreased blood volume, hypovolemic shock, circulatory collapse

Do not use if patient has hematocytologic disorders or cardiac, renal or hepatic dysfunction (idiosyncratic bone marrow toxicity in humans)

Can cause permanent kidney damage if animal is dehydrated

large animal NSAID that is toxic to humans= Irreversibly binds COX (non-covalent)

37
Q

grapiprant (galliprant) works as

A

EP4 receptor antagonist (inhibits PGE2 receptor)
– does not inhibit production of homeostatic

Analgesic for canine osteoarthritis

MOA: blocks PGE2-elicited pain via EP4

38
Q

side effects of galliprant

A

Vomiting, diarrhea, decreased appetite

EP4 receptor antagonist
inhibitors prostaglandin receptor → decreases pain

39
Q

— is the primary mediator of the PGE2-elicited sensitization of sensory neurons (inflammation-associated pain)

A

EP4

prostaglandin receptors that sit on nociceptors and trigger pain

galliprant blocks this receptor

40
Q

— are non-cyclooxygenase inhibitors

A

Dimethyl Sulfoxide (DMSO)
Galliprant

41
Q

what does DMSO do

A

anti-inflammatory
analgesic
anti-microbial, anti-fungal, anti-diuretic
anti-cholinesterase

Non-cyclooxygenase inhibitor

42
Q

DMSO is metabolized by

A

expelled through breath - garlic/oyster smell

some is excreted via kidney

43
Q

adverse effects of DMSO

A

dissolves through skin can introduce external toxins into body (wear appropriate gloves)

44
Q

Irreversible, covalent COX inhibitor (“gold standard” NSAID)

A

aspirin

45
Q

Poor anti-inflammatory; analgesic, fever; contraindicated for cats, dogs

A

acetaminophen (tylenol)

46
Q

Enhanced ulcerogenic potential in dogs; contraindicated for dogs

A

ibuprofen

47
Q

Enhanced ulcerogenic potential in dogs; approved for horses

A

naproxen

48
Q

Moderately COX-2 selective; approved for dogs

A

carprofen

49
Q

Weakly COX-2 selective; approved for dogs

A

etodolac(similar to carprofen)

50
Q

Strongly COX-2-selective; approved for dogs

A

Deracoxib

51
Q

Strongly COX-2-selective; approved for dogs and horses

A

Firocoxib

52
Q

Strongly COX-2-selective; only coxib approved for cats

A

Robenacoxib

53
Q

1 of 2 NSAIDs approved for cats- not glucuronidated; single injection to relieve post-operative pain; ok for horses, cattle etc

A

Meloxicam

54
Q

Most common NSAID for horses; non-food animals only; idiosyncratic bone marrow toxicity

A

Phenylbutazone

55
Q

Potent analgesic for horses, cattle (on par w/ opiods)

A

Flunixin

56
Q

EP4 receptor antagonist; Analgesic for dogs

A

galliprant

57
Q

Solvent; penetrates skin; MOA not well understood –prob ROS scavenger

A

DMSO

Non-cyclooxygenase inhibitor

23 spring: pharm (46 decks)

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