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Equine Clinical Immunology > Chapter 23 NSAIDs > Flashcards

Chapter 23 NSAIDs Flashcards

1
Q

What is the basic mechanism of action for NSAIDs?

A

Inhibition of the active binding site of cyclooxygenase (COX), involved in the formation of eicosanoids by oxidation of arachidonic acid.

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2
Q

What are the two isoforms of cyclooxygenase (COX)?

A

COX1 and COX2.

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3
Q

What is the role of COX1?

A

Referred to as the housekeeping isoform, it is continuously expressed in tissues like platelets, gastrointestinal mucosa, and kidneys.

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4
Q

What is the role of COX2?

A

Constitutively expressed in some tissues and inducible by pro-inflammatory signals, it is involved in inflammatory responses.

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5
Q

What is the significance of COX isoforms?

A

Differential binding of NSAIDs to COX1 versus COX2 explains the common gastrointestinal and renal side effects of non-specific COX inhibitors.

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6
Q

What are prostanoids?

A

Products of COX activity, including prostaglandins, thromboxane, and prostacyclin, involved in inflammation and regulation of physiological functions.

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7
Q

What is prostaglandin E2 (PGE2)?

A

A prostanoid involved in various functions like reducing gastric acid secretion, stimulating gastric mucus secretion, vasodilation, and increasing body temperature.

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8
Q

What is thromboxane A2 (TXA2)?

A

A product of COX activity primarily found in platelets, it is a potent vasoconstrictor and enables platelet aggregation.

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9
Q

What is prostacyclin (PGI2)?

A

A product of COX activity found in endothelial cells, functioning as a physiological antagonist to TXA2.

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10
Q

What are non-selective NSAIDs?

A

Drugs that inhibit both COX1 and COX2 enzymes.

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11
Q

What is phenylbutazone (bute)?

A

An enolic acid derivative and non-selective COX inhibitor, widely used for its analgesic and anti-inflammatory properties in horses.

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12
Q

What are the recommended doses for phenylbutazone?

A

4.4 mg/kg PO or IV BID as a loading dose and 2.2 mg/kg PO or IV BID to SID as a maintenance dose.

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13
Q

What are the common adverse effects of phenylbutazone?

A

Anorexia, depression, gastric and urinary bladder ulceration, renal papillary necrosis, neutropenia, anemia, protein losing enteropathy, colitis, and death.

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14
Q

What is flunixin meglumine?

A

A nicotinic acid derivative NSAID known for its potent analgesic effect in controlling acute visceral pain.

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15
Q

What is the recommended dose for flunixin meglumine?

A

1.1 mg/kg PO or IV BID as an anti-inflammatory dose.

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16
Q

What are the common side effects of flunixin meglumine?

A

Gastric ulceration and renal papillary necrosis.

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17
Q

What is aspirin (acetylsalicylic acid)?

A

A non-selective COX inhibitor used primarily as an antithrombotic agent due to its ability to irreversibly bind COX in platelets.

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18
Q

What is ketoprofen?

A

A propionic acid derivative and non-selective COX inhibitor with a long duration of action, often used once daily in horses.

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19
Q

What is the recommended dose for ketoprofen?

A

2.2 mg/kg IV SID for up to five days.

20
Q

What are the common adverse effects of ketoprofen?

A

Gastric ulceration and renal toxicity.

21
Q

What is naproxen?

A

A member of the propionic acid subclass of NSAIDs, characterized as a non-selective COX inhibitor.

22
Q

What is carprofen?

A

A propionic acid derivative NSAID, with better analgesic than anti-inflammatory properties in horses.

23
Q

What is meclofenamic acid?

A

An anthranilic acid derivative and non-selective COX inhibitor, available only in oral formulation for horses.

24
Q

What is eltenac?

A

An acetic acid derivative NSAID, shown to be a non-selective COX inhibitor in horses.

25
Q

What is the recommended dose for eltenac?

A

0.5 mg/kg IV SID.

26
Q

What is vedaprofen?

A

An arylpropionate derivative NSAID, highly COX1-selective, used in horses.

27
Q

What is firocoxib?

A

A second generation COX2 inhibitor, the first COX2-selective inhibitor approved for both oral and intravenous use in horses.

28
Q

What is the recommended dose for firocoxib?

A

0.1 mg/kg PO or 0.09 mg/kg IV SID for up to 14 days.

29
Q

What are the common adverse effects of firocoxib?

A

Gastric ulceration and nephropathy are significantly less likely compared to non-selective COX inhibitors.

30
Q

What is meloxicam?

A

An enolic acid NSAID of the oxicam group, structurally similar to piroxicam, and a COX2 selective inhibitor.

31
Q

What is the recommended dose for meloxicam?

A

0.6 mg/kg PO or IV SID.

32
Q

What is deracoxib?

A

A diaryl-substituted pyrazole, structurally related to celecoxib, and a COX2 selective inhibitor approved for dogs.

33
Q

What is etodolac?

A

An indole acetic acid derivative and COX2 selective inhibitor approved for use in dogs.

34
Q

What is diclofenac sodium?

A

A phenylacetic acid derivative available in oral, intravenous, and topical formulations, used as an NSAID.

35
Q

What is the effect of diclofenac when given orally to ponies?

A

Significant leukopenia and prolongation of prothrombin and activated partial thromboplastin times.

36
Q

What are antihistamines used for in horses?

A

Most commonly used for allergic mediated skin disease.

37
Q

What is hydroxyzine?

A

A first generation H1 receptor antagonist antihistamine, commonly used for chronic urticaria in horses.

38
Q

What is chlorpheniramine?

A

A first generation H1 receptor antagonist antihistamine, with low bioavailability and reduced efficacy in horses.

39
Q

What is diphenhydramine?

A

An ethanolamine derivative first generation antihistamine, used for immune-mediated dermatopathies and reversing extrapyramidal excitation induced by fluphenazine.

40
Q

What is pyrilamine?

A

An ethylenediamine first generation antihistamine, the only antihistamine with label approval for use in horses in the United States.

41
Q

What is doxepin?

A

A dibenzoxazepine derivative tricyclic antidepressant with antihistamine, anticholinergic, and alpha-adrenergic blocking effects.

42
Q

What is cetirizine?

A

A second generation H1 receptor antagonist, a metabolite of hydroxyzine, used for insect bite hypersensitivity and eosinophilic keratitis in horses.

43
Q

What is dimethyl sulfoxide (DMSO)?

A

A by-product of the wood and paper industry, used for its solvent properties and anti-inflammatory effects.

44
Q

What are the unique properties of DMSO?

A

Rapid penetration of skin, mucous, and cell membranes, facilitation of other substances’ penetration, and inhibition or stimulation of enzymes.

45
Q

What is the significance of flunixin meglumine in gastrointestinal disorders?

A

It is popularized for treatment of acute gastrointestinal disorders associated with endotoxemia.

46
Q

What is the role of PGE2 in inflammation?

A

Up-regulation of inducible PGE2 biosynthesis explains the cardinal signs of inflammation: rubor, heat, pain, and swelling.

47
Q

What is the impact of COX2 selective inhibitors on intestinal barrier function?

A

They do not delay mucosal recovery following ischemic injury, unlike non-selective COX inhibitors.

Equine Clinical Immunology (32 decks)

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