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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
When would you most likely use Phenylbutazone in a horse?
mostly used as a musculoskeletal analgesic vs. lameness
26
What are the guidelines for use of phenylbutazone in food-producing animals
BANNED in food-producing animals especially lactating dairy cattle. - excreted for extended periods of time in milk, meat and milk residues
27
What will happen if you use Phenylbutazone long term in equine?
horses will develop tolerance. the dose will have to be increased over time
28
What are examples of Oxicams?
Meloxicam | Piroxicam
29
What is the mode of action for Piroxicam?
Used in dogs. | - COX 2 selective agents
30
Meloxicam mechanism of action
COX-2 selective agents for cats and dogs | Interferes with ACE inhibitors
31
Reasons for using Meloxicam in Canine patients
- 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
Meloxicam in Cats
Approved for a single injection - Extra-label short-term use orally for 3 days Long term use results in renal failure
33
Piroxicam in dogs
Used as an adjunct vs. bladder cancer, specifically transitional cell carcinoma. These neoplastic cells overexpress COX2.
34
What treatments can Piroxicam be combined with?
Misoprostol, the gastroprotectant PGE1 analog A chemotherapy agent Surgery and/or radiation
35
Examples of Coxibs
Rofecoxib Deracoxib Firocoxib Robenocoxib
36
Rofecoxib
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
Deracoxib and FIrocoxib advantages over other NSAIDS
- 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
Robenacoxib in dogs
Very recently approved, but appears to be tissue-specific and targets joints. Available as an injectable
39
Disadvantages of Coxibs
Cost | Some dogs do not like the chewables
40
Robenacoxib in cats
REcently approved for daily oral use for 3 days | one of only 3 NSAIDs that can be used in cats.
41
Tepoxaline targets
COX1 COX 2 LOX
42
Tepoxaline and LOX
LOX inhibition may diminish GI side effects. Great potential vs. endotoxicosis and anterior uveitis.
43
Etodolac
Cheapest sensitive COX2 inhibitor | Can cause keratoconjunctivitis sicca
44
Waht are side effects of Etodolac?
Can cause keratoconjunctivitis sicca almost 100% of the time.
45
DMSO mode of action
inhibits PGs and scavenges free radicals | Can be used topically, orally, IV
46
What drugs can you use DMSO with?
Corticosteroids. DMSO is the only NSAID that can be used in conjunction with a Corticosteroid
47
Can you use DMSO in cattle?
no- it is banned in dairy cattle as the stench goes through to the flavor of the milk
48
Grapiprant
new PGE4 Receptor antagonist approved in dogs
49
What 3 NSAIDS can be used in cats?
Robenicoxib (daily orally for 3 days) Aspirin (orally once every 3 days) Meloxicam (one time use via injection)
50
What NSAID has approved use in swine
Flunixin
51
What NSAIDS are recommended for cattle/
Flunixin (in approved cases) | Aspirin
52
List NSAIDS approved for use in horses
``` Phenylbutazone Flunixin DMSO Naproxen Firocoxib ```
53
List NSAIDS approved for use in dogs
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
Tramadol
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
what are the functions of COX1
gastroprotectant (promotes mucus production) Platelet aggregation Regulation fo renal blood flow - this is constitutively produced
56
What are the functions of COX2
``` 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
Cox 3 function
appears to be a major regulator of pyresis
58
Indications and theraputic uses for NSAIDS
``` Alleviation of mild to moderate pain Anti-pyrexia Anti-inflammatory including anti-endotoxicosis Anti-coagulation ```
59
Anti-pyrexia and NSAIDS
PGE2 will reset the thermostatic neurons in the hypothalamus | Inhibiton of COX (COX3) therefore restores the status quo of thermoregulation
60
Anti-inflammatory and NSAIDS
NSAIDS block PGE2-mediated vasodilation including vasodilation caused by LPS NSAIDS also block PGE2 mediated synthesis of numerous pro-inflammatory mediators
61
NSAIDS and Anti-coagulation
NSAIDS block the synthesis of thromboxanes | not the first choice as an anti-coagulant
62
NSAIDS with anti-lipoxygenase activity
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
GI ulceration and NSAIDS
PG's induce production of gastric mucus NSAIDS therefore minimize the mucus layer Gastric Acid can then erode and ulcerate the gastric epithelium
64
How do you prevent GI ulceration when using NSAIDS
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
Hepatotoxicity and NSAIDS
reversible and mild hepatitis and cholestasis mechanism is unclear
66
Nephrotoxicity and NSAIDS
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
Cardiovascular issues with NSAIDs
- 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
What NSAID drug interactions are contraindicated
- corticosteroids: indifferent to each others activity - anticoagulants: potentiate each other - antihypertensive: antagonize each other - aminoglycoside antibiotics- these drugs are also nephrotoxic
69
NSAIDS and rhumatoid arthritis
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
Adverse effects and COX selectivity of NSAIDS
- 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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