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DWT > Pharmacology 2: NSAIDs > Flashcards

Pharmacology 2: NSAIDs Flashcards

1
Q

What is the significance of adverse effects?

A

-Severe and potentially fatal

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2
Q

What is the arachidonic Acid pathway?

A

-Membrane phospholipids broken down into arachidonic acids by phospholipase A2
- Cycclooxygenase 1 and 2 break phospholipase in prostaglandin H2
- Lipoxygenase breaks arachindonic acid in leukotrienes
-Prostaglandins further break down into prostanoids

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3
Q

How does an NSAID interact with the Arachidonic pathway?

A

Block Cyclooxgenase-1 and 2
- Only block the prostaglandin H2 arm of the pathway
- Does not block the leukotriene production

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4
Q

Does blocking the prostaglandins increase the leukotrienes?

A

Yes
Leukotrienes common in lung - can activate asthma

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5
Q

What are the prostanoids?

A

PGI2
TXA2
PGE2
PGF2a

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6
Q

PGI2 function?

A

Anti-platelet
Vasodilatory

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7
Q

TXA2 Function?

A

Pro-platelet
Vaconstriction

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8
Q

PGE2 function

A

-Major prostaglandin for blocking inflammation
Pro-inflammatory
Pain
Vasodilation
GI motility

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9
Q

PGF2A

A

Vasoconstriction
SmM constriction (uterus, GIT)
luteolysis
(No common concern for inflammation response)

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10
Q

COX-1 effects?

A
  • Constitutively expressed
  • Cytoprotective to the GI Tract (decrease acid and increase mucus)

GOOD GUY

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11
Q

COX-2 effects?

A
  • Induced by inflammation
  • Pro-inflammatory effect (Heat, pain, swelling, fever)

BAD GUY

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12
Q

Theory behind COX-2 specific inhibitors

A
  • COX-1 sparing
    Block the bad
    leave the good
    no adverse affects
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13
Q

Why doesn’t the COX-1 sparing theory work?

A
  • A lot of overlap
  • COX-2 is needed regularly in the kidney
  • COX-2 is NEEDED for muscosal healing
  • Specificity of most drugs is overcome at high doses (overdose)
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14
Q

COX selectivity characteristics? Example?

A
  • Varies by drug and varies by species
  • Carprofen is not selective in people
  • But is selected in dogs
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15
Q

When do we use NSAIDs?

A
  • Fevers by infections that is so high it will cause destruction to tissue (NSAIDs are not immunosuppressive)

-Pain associated with inflammation

  • Pain independent of inflammation
  • Endotoxinemia/Sepsis
  • Anticoagulant (platelet) activity
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16
Q

Clinical uses of NSAIDs

A

Antipyresis
Analgesia

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17
Q

Antipyresis NSAID action

A

Decrease of fever

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18
Q

Analgesia NSAID action

A

Pain associated with inflammation (Effective)
Pain independent of inflammation (ineffective)

19
Q

Inappropriate clinical use of NSAIDs

A
  • Immune-mediated disease (IMHA)
  • Autoimmune disease (lupus)
  • Allergy disease (atopy)
  • Inflammatory respiratory disease (asthma, Chronic bronchitis)

** Use glucocorticoids instead for all!!

20
Q

PK of NSAIDs

A
  • high bioavailability
  • Small volume of distribution (0.15-0.3 L/Kg)
    -High protein binding (70-99%)
21
Q

Hepatic metabolism effects on PK of an NSAID?

A

Hepatic metabolism predominates:
- lIver can become overwhelmed in overdose and create REALLY long half life
–Capacity-limited (non-linear PK: toxic)
–Species differences: Dosing in one species is UNLIKELY correct for another species
–Neonates

22
Q

Choosing an NSAID Steps

A
  • Many different NSAIDS
  • Check species (BIG DIFFERENCES) and always dose if possible a drug that is labeled for that species
  • Choices made related to pattern of use, experience and tradition
23
Q

In what cases is telling a client “Your pet will die a horrible death if you give it your NSAID” true?

A

Tylenol: cats
Ibuprofen: Dogs, cats

24
Q

Overall idea of adverse effects of NSAIDs

A

Numerous and DANGEROUS

25
Q

What are the adverse effects?

A
  • GI ulcers
  • Nephrotoxicity
  • Hemorrhage
  • Hepatotoxicity
  • IMHA
  • Blood dycrasias
  • Injection site rxn
  • Tissue necrosis
  • Clostridial myositis
26
Q

Characteristics of adverse effect: GI ulcers?

A
  • Not just from oral admin, can happen with injectable too
  • PGE2 effects but PGE2 is needed for healing. Toxic loop.
27
Q

Characteristics of adverse effect: where are GI ulcers dog and cats?

A

Stomach and SI

28
Q

Characteristics of adverse effect: where are gi ulcers in horses?

A

Stomach and colon

29
Q

Characteristics of adverse effect: where are go ulcers in ruminants?

A

Abomasum

30
Q

Why do NSAIDS lead to GI ulcers?

A

Weak acids get trapped in the basic environment of the gastric epithelium resulting in cells death

31
Q

Characteristics of adverse effect: Nephrotoxicity

A
  • Inhibition of PGE2 and PGI2
    – Vasoconstriction, decreased renal BF, possible toxicity
    – Effects exacerbated in dehydrated patients (already compromised renal flow)
    – COX-2 inhibitor not safer- PGE2 constitutively expressed in kidney and needs for healing.
32
Q

Characteristics of adverse effect: where are neurotoxicity lesions?

A

Medullary crest or papillary necrosis
** Less BF
** Is not fatal but animal can no longer concentrate urine

33
Q

Characteristics of adverse effect: Hemorrhage

A
  • Effects platelets
  • Irreversibly binds to COX-1
    -No longer activates thromboxane A2 activity.
  • Platelets do not clot appropriately
  • Lasts for life of platelet (7-10days)
34
Q

Characteristics of adverse effect: of selective COX-2 inhibitors

A
  • Reduces PGI2
  • little or no inhibition of prothrombotic thromboxane (COX-1)
35
Q

Characteristics of adverse effect: hepatotoxicity

A
  • Form all NSAIDs in fairly low incidence
  • Idiosyncratic effect = unpredictable and no reproducible
  • Anorexia, Vomiting, icterus
  • hepatomegaly
  • increased bilirubin, ALT, ALP, AST
36
Q

Characteristics of adverse effect: IHMA

A

Up to 12% of human IHMA drug-induced causes are from NSAIDS
- RARE in animals

37
Q

Characteristics of adverse effect: blood dyscrasias

A
  • Pancytopenia marrow failure
  • Non-regenerative anemia and thrombocytopenia
38
Q

Characteristics of adverse effect: injection site reactions

A
  • Heat, pain, swelling
  • abscess formation
  • tissue necrosis
  • clostridial myositis
39
Q

What drug can lead to clostridial myostitis?

A

Im Flunixin Meglumine in horse

40
Q

How to minimize adverse effects?

A
  • injection site reactions
  • Dose appropriately (lowest effective dose at longest DI)
  • Right drug and formulation
  • GI Protection
  • Avoid co-administering other nephrotoxic drugs
  • Avoid co-administering other NSAID or GCS
  • Use extreme caution in those with preexisting conditions
  • Client education
  • Monitoring
41
Q

How to minimize adverse effects injection site reactions

A

Some can be given orally instead of IM
- Mix with corn syrup to make less irritating and better tasting
- Similar bioavailability

42
Q

How to minimize adverse effects with dosing appropriately?

A
  • lowest effective dose at longest DI
43
Q

How to minimize adverse effects with GI protection

A
  • PGE analog
  • Proton pump inhibitors
44
Q

How to minimize adverse effects in those with preexisting disease?

A

Watch for:
- Renal disease
- GI disease
- Liver disease
- Anorexia
- Dehydration

DWT (28 decks)

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