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Pharmacology > Exam 4- NSAIDS > Flashcards

Exam 4- NSAIDS Flashcards

1
Q

Acid base status of NSAIDS

A

generally they are weak acids, making them good oral drugs

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2
Q

Where in the body are NSAIDS metabolized?

A

most are metabolized by the liver

This does mean they are subjected to the first pass effect.

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3
Q

Flunixin selectivity

A

COX2- selective in horses,

COX1 selective in dogs.

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4
Q

What general effects do we have with Flunixin

A
  • analgesic, anti=inflammatory, anti-pyretic

Only NSAID effective versus visceral pain

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5
Q

Can you use Flunixin for lameness in a food animal?

A

no. This is considered extralable, and is not approved.
This drug is approved for toxic mastitis and Bovine respiratory disease. Only for use as IV or TD only
Swine- FDA approved
- Effective vs. endotoxins (preferred NSAID)- functions by blocking the PG-related events activated by LPS

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6
Q

What drug is used in combination with Flunixin for treatment of endotoxicosis?

A

Ketamine at subanesthetic doses. This seems to prevent the PMN-LPS interaction

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7
Q

Selectivity for Acetaminophen

A

non selective inhibitor, but it is confusing

  • Binds to COX2, COX 3 but not COX1
  • it does not bind to peripheral COX2 (peroxides at the site of inflammation inactivate acetaminophen)
  • Does inhibit central COX2
  • Does inhibit COX3, which is only central
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8
Q

What does the selectivity for Acetominophen do for the theraputic effect?

A
  • lack of pCOX2 inhibition- weak anti-inflammatory
  • anti-cCOX2 activity provides the analgesic effect of acetaminophen
  • The anti Cox3 activity provides antipyretic effect
  • the lack of anti COX1 activity spares the stomach and platelets.
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9
Q

Clinical uses for Acetaminophen

A

antipyretic

analgesic - will reduce the pain associated with inflammation but does not eliminate the cause

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10
Q

side effects for Acetaminophen

A

mnimal GI and coagulation side effects.

- hepatotoxic with long term high dose use.

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11
Q

What are features of Propionic acid derivatives?

A

most nephrotoxic NSAID group

non-selective: except for carprofen

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12
Q

What are examples of Propionic acid derivatives?

A

Ibuprofin
Ketoprofen
Carprofen
Naproxen

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13
Q

What profen is not safe for vetarinary patients?

A

Ibuprofen

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14
Q

Ketoprofen selectivity and use

A

COX inhibitor and partial LOX inhibitor. Only for short term use
- ONLY APPROVED in HORSES

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15
Q

Carprofen selectivity

A

Selective COX2 inhibitor for use in dogs

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16
Q

Carprofen contraindications

A

contraindicated in pregnant animals (tends to prolong pregnancy)
- reversible hepatotoxic incidenses in Laborador retrievers

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17
Q

Contraindications for Ketoprofen

A

Pregnant animals should not receive this

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18
Q

What are the uses for Naproxen?

A

Approvedin horses for myositis

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19
Q

Aspirin Selectivity

A

Selective COX1 inhibitor

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20
Q

Aspirin side effects

A

Prolonged Bleeding time
- platelets cannot make more COX1
GI ulcers
- Likely due to inhibition of platelet activity

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21
Q

Salicylate

A

Reversible COX inhibitor

- has the moiety that falls off the NSAID after leaving the acetyl group on COX1

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22
Q

Clinical considerations for Aspirin

A
  • Cats- low dose every 72 hours provides some relief while minimizing side effects
  • Dogs- Do not use for logn term therapy vs. osteoarthritis. Canine chondrocytes are selective to the complete avsence of COX1 activity and exacerbates the arthritis
  • Sheep: aspirin causes pulmonary edema
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23
Q

How long prior to Sx do you have to remove Aspirin from a patients regimin?

A

7 days

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24
Q

Phenylbutazone selectivity

A

COX2 selectivity NSAID

- most commonly used NSAID in the horse

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25
Q

When would you most likely use Phenylbutazone in a horse?

A

mostly used as a musculoskeletal analgesic vs. lameness

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26
Q

What are the guidelines for use of phenylbutazone in food-producing animals

A

BANNED in food-producing animals especially lactating dairy cattle.
- excreted for extended periods of time in milk, meat and milk residues

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27
Q

What will happen if you use Phenylbutazone long term in equine?

A

horses will develop tolerance. the dose will have to be increased over time

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28
Q

What are examples of Oxicams?

A

Meloxicam

Piroxicam

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29
Q

What is the mode of action for Piroxicam?

A

Used in dogs.

- COX 2 selective agents

30
Q

Meloxicam mechanism of action

A

COX-2 selective agents for cats and dogs

Interferes with ACE inhibitors

31
Q

Reasons for using Meloxicam in Canine patients

A
  • Reasons for using this drug
    1) Cost: coxibs>meloxicam>carprofen>etodolac
    2) Route of administration- meloxicam is an oral suspension that can be dropped into food or transmucosally. Coxibs and carprofen are chewables that some dogs dislike
    3) Post- surgical pain: Can give a post-op injection then dispense the suspension for at-home use
32
Q

Meloxicam in Cats

A

Approved for a single injection
- Extra-label short-term use orally for 3 days
Long term use results in renal failure

33
Q

Piroxicam in dogs

A

Used as an adjunct vs. bladder cancer, specifically transitional cell carcinoma. These neoplastic cells overexpress COX2.

34
Q

What treatments can Piroxicam be combined with?

A

Misoprostol, the gastroprotectant PGE1 analog
A chemotherapy agent
Surgery and/or radiation

35
Q

Examples of Coxibs

A

Rofecoxib
Deracoxib
Firocoxib
Robenocoxib

36
Q

Rofecoxib

A

Withdrawn from the market due to Cardiovascular issues in humans
Higher COX2 selectivity results in a higher risk for CV disease in predisposed patients
- COX2 helps to maintain vascular endothelial integrity
- Dogs do not have any significant chance of devloping CV disease.

37
Q

Deracoxib and FIrocoxib advantages over other NSAIDS

A
  • Best long-term drug versus the pain and inflammation of osteoarthritis
  • Can be sued in dogs with renal insufficiency since these drugs are mostly eliminated via the bile/feces (be aware of coprophagia as this causes re-dosing of the drug)
  • High Vd for firocoxib (good distribution throughout the body)
38
Q

Robenacoxib in dogs

A

Very recently approved, but appears to be tissue-specific and targets joints.
Available as an injectable

39
Q

Disadvantages of Coxibs

A

Cost

Some dogs do not like the chewables

40
Q

Robenacoxib in cats

A

REcently approved for daily oral use for 3 days

one of only 3 NSAIDs that can be used in cats.

41
Q

Tepoxaline targets

A

COX1
COX 2
LOX

42
Q

Tepoxaline and LOX

A

LOX inhibition may diminish GI side effects. Great potential vs. endotoxicosis and anterior uveitis.

43
Q

Etodolac

A

Cheapest sensitive COX2 inhibitor

Can cause keratoconjunctivitis sicca

44
Q

Waht are side effects of Etodolac?

A

Can cause keratoconjunctivitis sicca almost 100% of the time.

45
Q

DMSO mode of action

A

inhibits PGs and scavenges free radicals

Can be used topically, orally, IV

46
Q

What drugs can you use DMSO with?

A

Corticosteroids. DMSO is the only NSAID that can be used in conjunction with a Corticosteroid

47
Q

Can you use DMSO in cattle?

A

no- it is banned in dairy cattle as the stench goes through to the flavor of the milk

48
Q

Grapiprant

A

new PGE4 Receptor antagonist approved in dogs

49
Q

What 3 NSAIDS can be used in cats?

A

Robenicoxib (daily orally for 3 days)
Aspirin (orally once every 3 days)
Meloxicam (one time use via injection)

50
Q

What NSAID has approved use in swine

A

Flunixin

51
Q

What NSAIDS are recommended for cattle/

A

Flunixin (in approved cases)

Aspirin

52
Q

List NSAIDS approved for use in horses

A 
Phenylbutazone
Flunixin
DMSO
Naproxen
Firocoxib
53
Q

List NSAIDS approved for use in dogs

A

etodolac: cheapest
carprofen: cheap, chewable, hepatotoxic
meloxicam: cheaper than coxibs, ease of administration
coxibs: expensive, chewable, best long-term, use even if dog has a renopathy

54
Q

Tramadol

A

Opioid that is a specific agonist of the mu-receptor
Used for moderate pain relief (not inflammation) in dogs
Questionable efficacy because mu-receptor activation does not consistently provide analgesia in dogs

55
Q

what are the functions of COX1

A

gastroprotectant (promotes mucus production)
Platelet aggregation
Regulation fo renal blood flow
- this is constitutively produced

56
Q

What are the functions of COX2

A 
minor function in homeostasis: low basal activity 
- kidney and renin system
- reproduction: especially implantation
Constitutively and inducibly produced 
inducible COX2 activity leads to
1) pain
2) inflammation
3) fever
57
Q

Cox 3 function

A

appears to be a major regulator of pyresis

58
Q

Indications and theraputic uses for NSAIDS

A 
Alleviation of mild to moderate pain
Anti-pyrexia
Anti-inflammatory 
          including anti-endotoxicosis
Anti-coagulation
59
Q

Anti-pyrexia and NSAIDS

A

PGE2 will reset the thermostatic neurons in the hypothalamus

Inhibiton of COX (COX3) therefore restores the status quo of thermoregulation

60
Q

Anti-inflammatory and NSAIDS

A

NSAIDS block PGE2-mediated vasodilation including vasodilation caused by LPS
NSAIDS also block PGE2 mediated synthesis of numerous pro-inflammatory mediators

61
Q

NSAIDS and Anti-coagulation

A

NSAIDS block the synthesis of thromboxanes

not the first choice as an anti-coagulant

62
Q

NSAIDS with anti-lipoxygenase activity

A

LOX acitivity is essentially all inducible as part of severe inflammatory
Leukotrienes are also part of allergic responses
Inhibition of LOX has no effect upon pain
LOX inhibition is gastroprotective; leukotrienes are gastrotoxic
- One NSAID is anti COX and anti-LOX thus minimizing gastric problems

63
Q

GI ulceration and NSAIDS

A

PG’s induce production of gastric mucus
NSAIDS therefore minimize the mucus layer
Gastric Acid can then erode and ulcerate the gastric epithelium

64
Q

How do you prevent GI ulceration when using NSAIDS

A

Prevention involves co-therapy with misoprostol and PGE1 analog
- PGE1 is not really involved in inflammation but is involved in mucogenesis
NSAIDS block the production of PGE2 and PGE1; misoprostol restores PGE1

65
Q

Hepatotoxicity and NSAIDS

A

reversible and mild
hepatitis and cholestasis
mechanism is unclear

66
Q

Nephrotoxicity and NSAIDS

A

PGs have vasodilatory effects via local COX2
PGs modulate renal effects upon fluid elimination and renin secretion
NSAIDs can lead to fluid retention and hyperkalemia

67
Q

Cardiovascular issues with NSAIDs

A
  • COX2 in vascular endothelial cells is responsible for maintaining balance between PGI2 and TXA2
    -PGI2 is vasoprotective by maintaining shape and integrity of vascular endothelium. also inhibits platelet aggregation
    NSAIDS cause PGI2
68
Q

What NSAID drug interactions are contraindicated

A
  • corticosteroids: indifferent to each others activity
  • anticoagulants: potentiate each other
  • antihypertensive: antagonize each other
  • aminoglycoside antibiotics- these drugs are also nephrotoxic
69
Q

NSAIDS and rhumatoid arthritis

A

RA is an autoimmune erosive arthritis
recently, platelets were implicated as a mediator of RA
in RA, activated platelets release microparticles that erode the joint surface.
This release is COX independent

70
Q

Adverse effects and COX selectivity of NSAIDS

A
  • COX 2 plays a larger role in inflammation
    hemostatic functions: kidney hemodynamics and solute regulation, cardiovascular integrity
  • COX1 does not play a major role in pyresis

Pharmacology (7 decks)

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