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Pharmacology Exam 3 > Ch.26: NSAIDs (Vickroy) > Flashcards

Ch.26: NSAIDs (Vickroy) Flashcards

1
Q

What are NSAIDs?

A

anti-inflammatory drugs that are clinically and biologically distinct from glucocorticoid steroids (“non-steroidal”)

  • produce analgesic and anti-pyretic (lower fever) actions at low dose, and anti-inflamm. action at high dose
  • VERY widely used
  • originally isolated from white willow tree
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2
Q

NSAIDs all act via which mech.?

A

inhibition of intracellular cyclooxygenase enzymes COX-1 and/or COX-2 –> disrupted metabolism of arachidonic acid –> inhibited synthesis of intracellular autacoids (prostaglandins, thromboxanes, etc.)

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3
Q

Major clinical uses of NSAIDs

A

-acute pain (i.e. post-sx, colic, lesions, pancreatitis, etc.)
-chronic pain
-inflammation
-mastitis, metritis, endotoxemia (along with abx)
-fever
-atherosclerosis (plaque build-up in arteries; humans)
-neurodegenerative disorders (humans)
+/- cancer
*chronic use is usually to alleviate pain, not inflammation.

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4
Q

first COX-2 selective inhibitor

A

celebrex

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5
Q

first NSAID

A

aspirin

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6
Q

phospholipase

A

enzyme released when cell lipid bi-layer damaged by physical/chemical insults, toxin, temp. change, oxides, etc.
*catalyzes the breakdown of membrane phospholipids and releases numerous by-products, including arachidonic acid (AA), which is the precursor for eicosanoids

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7
Q

arachidonic acid is the precursor for:*

A

eicosanoids (signalling molecules that exert complex control over many bodily systems, mainly in inflammation or immunity, and as messengers in the central nervous system)

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8
Q

“dual inhibitors” inhibit which 2 pathways?

A

lipoxygenase and COX pathways

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9
Q

are there single or multiple receptors for eicanosoids? What kind of receptor(s) are they?

A

multiple. G protein-coupled receptors located on various target tissue cells

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10
Q

in general, is it better to selectively inhibit COX-1 or 2?

A

COX-2. COX-1 is important for “housekeeper roles” in homeostasis and is gastro/renal protective, whereas COX-2 is mostly a product of inflammation.

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11
Q

products of COX-1*

A

thromboxane-A2
PGE2
PGI2

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12
Q

Is COX-1 always present on cells? COX-2?

A

COX-1 always present (“constitutive”)
COX-2 is present mostly during inflammation only, besides some constitutive expression on monos, macs, endothelial cells.

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13
Q

advantage of COX-2 selective inhibitors*

A

lower incidence of GI, renal problems

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14
Q

NSAIDs interfere with which chemical mediators?

A 
Eicosanoids
Kinins
Cytokines
Chemokines
Fibrinopeptides (?)
*Key point: they are NOT just COX-inhibitors; they have many other actions
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15
Q

Glucocorticoids interfere with which chemical mediators?

A 
lysosomal release
eicosanoids
platelet-activating factors
complement
cytokines
chemokines
*they are NOT just COX-inhibitors; they have many other actions (probably DNM list)
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16
Q

Most common side effects of NSAIDs**

A

*gastropathy
nephrotoxicity (acute renal failure)
idiosyncratic reactions (bone marrow depression, skin rxns, etc.)

lesser extent: blood dyscrasias, hepatotoxicity, delayed healing (soft tissue and bone)
*most NSAIDs fairly safe to use

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17
Q

How to prevent nephrotoxicity with NSAIDs?

A

good hydration

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18
Q

2 main determinants of how bad NSAID adverse effect will be***

A

DOSE and TIME

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19
Q

2 main populations of dogs administered NSAIDs

A

dogs with osteoarthritis

post-op dogs

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20
Q

adverse drug experience

A

any adverse event assoc. with the use of a new animal drug, whether or not considered to be drug related, and whether or not the new animal drug was used in accordance with the approved labeling

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21
Q

chem. properties of NSAIDs

A
  • synthetic organic acids
  • good lipid solubility
  • stable in GI tract*
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22
Q

risk factors of giving osteoarthritis dog NSAID

A

geriatrics, concomitant hepatic/renal/etc. dz

23
Q

risk factors of giving post-op dog NSAID

A

poor hydration, may have compromised renal fx

24
Q

pharmacokinetic props. of NSAIDs

A
  • highly protein bound*
  • lvl in milk enhanced during mastitis (due to pH effect, protein binding)
  • good oral absorption*
  • distr. limited for MOST NSAIDs due to extremely high plasma protein binding (exception = flunixin)
25
Q

therapeutic advantage of high NSAID protein binding*

A

likely to accumulate in inflammatory exudate, which has high protein content
-actions persist longer than expected relative to plasma levels*

26
Q

penetration of NSAIDs into milk is LOW/HIGH for norm. mammary tissue? Why?

A

LOW (lack of ion trapping, high protein binding)

27
Q

metabolism of NSAIDs

A

mostly hepatic metabolism

protein binding limits renal excretion

28
Q

Name 1 NSAID with a higher volume of distribution?

A

flunixin (cattle)

29
Q

Required NSAIDs

A 
carprofen
deracoxib
flunixin meglumine
ketoprofen
phenylbutazone
tepoxalin
(all in hospital formulary)
30
Q

Is carprofen a selective/non-selective COX-inhibitor?*

A

non-selective

31
Q

Carprofen approved in which animals?

A

dogs only

32
Q

Carprofen side effects and their management

A

GI, renal, hepatic. Higher incidence in Labs

Manage via periodic bloodwork, using wash-out period before switching to another NSAID

33
Q

ketoprofen selective/non-selective COX inhibitor?*

A

non-selective

34
Q

Ketoprofen approved in which animals?*

A

horses**
dogs
cats in Canada only

35
Q

Most common use of ketoprofen in dogs

A

peri or post-operativey

36
Q

Ketoprofen side effects

A

Dogs: GI
Horse: GI/renal complications

37
Q

“coxib” at end of drug name indicates:

A

it is a SELECTIVE COX inhibitor

38
Q

Deracoxib approved in which animals?

A

dogs only

39
Q

Deracoxib selective/non-selective?

A

selective for COX-2

40
Q

Deracoxib side effects

A

generally well tolerated; watch for sulfonamide hypersensitivity

41
Q

Most common uses of Deracoxib

A

post-op pain from orthopedic or dental sx and osteoarthritis in dogs

42
Q

most broadly used NSAID in large animal*

A

flunixin meglumine

43
Q

Flunixin used in which species

A 
horses, swine, cattle
NO dogs (they are sensitive to GI damage)
44
Q

flunixin selective/non-selective COX inhib?*

A

non-selective

45
Q

Major uses of flunixin

A
  • MS pain, inflamm.
  • pyrexia (fever), mastitis, endotoxemia
  • colic
  • post-op pain from de-horning
46
Q

withdrawal times are very important for flunixin**

A

:)

47
Q

phenylbutazone approved in which species

A

horses, dogs

48
Q

phenylbutazone select/non-select. COX-inhib?*

A

non-select.

49
Q

can you give phenylbutazone to animals intended for human consumption?**

A

NO!

50
Q

advantages of pheylbutazone

A

has good analgesic and antipyretic actions

51
Q

Tepoxalin approved in which species

A

dogs

52
Q

Tepoxalin acts on which enzymes?**

A

non-selective COX-1/COX-2 inhibitor + lipoxygenase (LOX) inhibitor. “DUAL-ACTING”
-inhibits formation of prostaglandins, Thromboxanes, and leukotrienes

53
Q

Tepoxalin advantages/disadvantages still widely unknown

A

:)

Pharmacology Exam 3 (11 decks)

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