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Pharmacology Test 3 > NSAIDS (Dr. Boston) > Flashcards

NSAIDS (Dr. Boston) Flashcards

1
Q

NSAIDS general

A

Decrease pain, fever, inflammation

  • Chronic Pain: Osteoarthritis
  • Post operative pain
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2
Q

NSAIDS inhibit production of

A

Protaglandins (PG) from arachidonic acid cascade

  • COX (cyclooxygenase) enzymes
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3
Q

Corticosteroids inhibit:

NSAIDs inhibit:

A

Corticosteroids inhibit: Phospholipase A

NSAIDS inhibit: Cyclooxygenase (COX)

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4
Q

Prostaglandin cascade from Membrane phospholipids

A

Membrane Phospholipids

=> broken down by Phospholipase A to…

Arachidonic Acid (AA)

=> broken down by COX to

Different prostaglandins

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5
Q
A
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6
Q

Traditional (nonselective) NSAIDS

A
  1. Aspirin
  2. Piroxicam
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7
Q

Cox-1 enzymes

(Constitutive Prostaglandins)

A
  1. Housekeeping
  2. Protective effect on gastric mucosa
  3. Platelet function
  4. Renal blood flow

*not related to cell damage, pain, etc

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8
Q

COX-2 enzymes

(Inducible Prostaglandins)

A
  1. Pain
  2. Inflammation
  3. Fever
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9
Q

COX-1, COX-2 ratios

Selective

Non-selective

A

Selective: Ratio > 1 = preference for COX-2

  • Carprofen (Rimadyl)
  • Meloxicam
  • Deramaxx
    • not injectible
  • Onsior
    • FDA approved for cats, good for post-op pain
  • Previcox (Firocoxib)
    • horses

Nonselective: Ratio

  • Ketoprofen
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10
Q

When NOT to prescribe an NSAID

A

1. Renal dz

2. Liver dz

3. GI dz

4. Risk of bleeding or low BP in sx

5. On corticosteroids

6. Cushingoid

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11
Q

Renal blood flow

A
  1. PGs maintain renal blood flow in hypotension (COX-1 > COX-2)
  2. Pre-operative use of NSAIDS
  • Selective NSAIDs
  • IV fluid support
  • Blood pressure monitoring and support
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12
Q

Platelets

Thromboxane

A
  1. Thromboxane
  • involved in clotting
  • product of arachidonica acid metabolilsm
  1. COX-1 inhibition => platelets can’t produce thromboxane for 2-3 days
  • Ketoprofen
  • Piroxicam
  1. Selective NSAIDs probs ok
  • metacam
  • rimadyl
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13
Q

Aspirin

A
  1. Acetylates the COX enzyme irreversibly
  2. Platelets unable to synthesize more COX for the lifetime of the platelet
    * NO SURGERY FOR 7-10 days
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14
Q

Perioperative use of NSAIDS

A
  1. Non-selective NSAIDs NOT RECOMMENDED
  2. COX-2 selective NSAIDS
  • Rimadyl and Meloxicam - injectible
  • No documented effects
    • renal function
    • platelet function
  • Pre-operatively for preemptive analgesia
  • Admin 30-60 minutes prior to recovery
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15
Q

Prostacyclin

A

Cox-2 dependant prostaglandin

prevents clots from forming intravascularly

Selective NSAIDs knock this out and predispose to clots

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16
Q

GI dz and NSAIDs

A

If vomiting diarrhea => stop NSAIDs

  • Can cause perforating ulcer => peritonitis => death
17
Q

Gastric Mucosal Protection

of constiuative house keeping prostaglandins

A

Inc mucus secretion

Inc Bicarbonate secretion

Inc Epithelial cell renewal

Inc Mucosal blood flow

Dec Acid secretion

18
Q

Prostaglandins

In Gastric Mucosal Protection

A

Mostly COX-1

Nitric Oxide

Autonomic nervous system

PGE

19
Q

Mast cell tumor and NSAIDs

A

Mast cells make Histamine

  • Histamine (2 types)
    • anaphylaxis type that induces swelling
    • stomach protectant (decreases acidity)

Don’t know what’s going on in their stomach, if they have a lot of histamine and gastric ulcers

Also treat mast cells with corticosteroids and they don’t mix with NSAIDs

20
Q

NSAID elimination

A

Metabolized in liver

Excreted in bile

Some productes excreted in kidneys

21
Q
  1. Corticosteroids do not prevent production of ……
  2. Corticosteroids do inhibit….

3. Corticosteroids are not…

4. Corticosteroids do not inhibit…

5. Corticosteroids do cause….but…

A
  1. Prostaglandins

(another fatty acid besides Arachadonic Acid can be a precursor)

  1. Arachadonic Acid production

3. Analgesics

4. Platelet function

5. Gastrointestinal dysfunction but by a different mechanism than NSAIDs

-Can cause gastric ulceration

22
Q

Leukotrienes

A

Produced from Lipoxygenase (LOX)

Inflammatory mediators

Gastrotoxic

-decrease circulation to the stomach

23
Q

Corticosteroids overview

A

Glucocorticoids

  • cortisol

Mineralocorticoids

  • aldosterone
24
Q

Cats and drug metabolism

A

Cats don’t metabolize drugs well

(b/c of their dec glucoronidation)

25
Q

Cats and NSAIDs

A
  1. Prolonged elimination half-lives
  2. Many NSAIDs Except: Meloxicam
    * cleared by oxidative enzymes in cats
  3. No NSAIDs prescribed for long-term use in cats
  4. More sensitive to renal effects (dogs more sensitive to GI side effects)
    * Monitor these cats’ chemistries
26
Q

Acetaminophen contraindicated in cats

A
  1. Decreased glucuronidation => metabolism by alternate pathways
  2. Toxic Metabolite
  • N-acetyl-p-benzoquinone
  • Methemoglobinemia
  • Heinz body anemia
  1. Detoxified by glutathione
  • Antidote: Acetylcystein
  • Glutathione precursor

Pharmacology Test 3 (12 decks)

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