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Animal Disease 1 > NSAIDs > Flashcards

NSAIDs Flashcards

1
Q

What are chondroprotective drugs?

A

Used in osteoarthritis and other joint diseases to protect cartilage that has been damaged in these conditions. First used in equine medicine, then canine medicine, and little used in cats. Component building blocks of cartilage and involve the use of substances that act as lubricants to joints. Build up the cartilage matrix building blocks to help prevent further damage to the cartilage and joint.

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2
Q

What are the properties of NSAIDs?

A
  • Inhibit cyclooxygenase, which reduces prostaglandin and thromboxane synthesis
  • Anti-inflammatory
  • Anti-pyretic
  • Analgesic
  • They all have undesirable effects.
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3
Q

Where are NSAIDs most commonly used?

A

Non-infectious or non-allergic inflammation to control inflammation and pain, such as trauma, post-surgery and osteoarthritis.

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4
Q

How is arachidonic acid converted in a 2 step process?

A
  1. Converted to prostaglandin H2, which can then be converted to the end product.
  2. 2 stage process is carried out by cyclooxygenase enzyme.
  3. First step is an endoperoxide synthase step to form prostaglandin G2 and the second in a peroxidase step to give PGH2.
  4. Cyclooxygenase is the enzyme that is blocked or inhibited by NSAIDs. Majority of these drugs block the first step.
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5
Q

Name the 2 isoforms of cyclooxygenase.

A

COX-1
COX-2

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6
Q

Describe the function and properties of COX-1.

A
  • Constitutively expressed
  • Involved in gastric protection, blood clotting and renal blood regulation
  • Inflammation is not the main role
  • Binding pocket is narrow
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7
Q

Describe the function and properties of COX-2.

A
  • Induced by inflammation
  • Produces prostaglandins, which mediates inflammation
  • Binding pocket is wide
  • So there is an idea that COX-2 selective drugs may be beneficial in treating inflammation without side effects, but this is an idea not fully borne out in clinical practice.
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8
Q

What is the significance of the difference in the binding pockets of COX-1 and COX-2?

A

COX-2 has a larger binding pocket with a side pocket. So bigger molecules can easily fit into the COX-2 pocket but less so with COX-1. These are coxib drugs, they are selective inhibitors, of COX-2. A slimmer molecule will be able to inhibit COX 1 and 2.

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9
Q

Which NSAIDs are COX-2 selective?

A
  • Firocoxib and meloxicam are COX-2 selective.
  • Carprofen is slightly COX-2 selective.
  • Phenylbutazone is only very slightly COX-2 selective.
  • The coxibs: cimicoxib, enflicoxib, firocoxib, mavacoxib, robenacoxib

Paracetamol has no anti-inflammatory action and no one knows why, but it is a good anti-pyretic and analgesic.

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10
Q

Name the 4 mostly commonly used NSAIDs.

A

Carprofen
Meloxicam
Firocoxib
Phenylbutazone

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11
Q

How does COX-1 inhibition cause gastric ulceration.

A
  1. Via inhibition of PGE2 and PGI2 synthesis, which usually protect gastric mucosa.
  2. Some drugs cause direct damage, such as aspirin, which can precipitate in cells lining the stomach.
  3. COX-1 inhibitors inhibit platelet aggregation
  4. In particular, aspirin and phenylbutazone irreversibly inhibits platelet CPX-1.
  5. Concurrent glucocorticoid administration increases GI damage, as do dehydration, hypovolaemic shock and disruption to gastric blood flow.
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12
Q

What is the effect of enterohepatic recycling?

A

Enterohepatic recycling increases time the drug spends in the GI tract. Dogs have increased enterohepatic recycling – half life increased. Can increase GI side effects.

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13
Q

What is the effect of COX-2 inhibition?

A
  • Sodium retention in the kidney
  • Hypertension
  • Reduce effectiveness of some diuretics
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14
Q

Summarise the side effects of COX-1 and COX-2.

A

So COX-1 inhibitors cause GI damage and COX-2 selective drugs have less GI side effects but can reduce kidney function.

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15
Q

What are the other possible side effects of NSAIDs?

A
  • Renal toxicity – if renal function already reduced. Seen in humans and horses, not well described in cats and dogs.
  • Hepatotoxicity – rare. Paracetamol use in cats
  • Haematology and haemostasis – increases risk of bleeding but not serious at clinical doses. No increased risk of cardiovascular events in animals (risk factors different than in humans).
  • Injury to articular cartilage – chronic NSAID use leads to worsening of cartilage damage in osteoarthritis due to impaired proteoglycan synthesis.
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16
Q

Describe the metabolism of NSAIDs.

A
  • Primarily via hepatic metabolism by mixed function enzymes
  • Differences between species and so differences in half lives
  • Metabolites usually less active or inactive. Aspirin and phenylbutazone have active metabolites (salicylate and oxyphenbutazone)
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17
Q

What are the species differences in how NSAIDs are metabolised?

A

Cats have low capacity to glucuronidate NSAIDs, a main metabolism pathway). Increased drug half life and toxicity.

Some drugs have zero order kinetics in some species:
- Phenylbutazone in dogs
- Salicylate in cats

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18
Q

Describe paracetamol licensing and its risk.

A
  • Not often used in vet practice – licensed for pigs and dogs
  • May be given by owners
  • Can cause liver toxicity – cats particularly susceptible due to lack of glucuronidation
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19
Q

What is the use of phenylbutazone?

A
  • Commonly used in horses for relief of pain and inflammation
  • Mot allowed for animals entering food chain – reduces white blood cell count in humans
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20
Q

List the regularly used NSAIDs used in small animal practice.

A

Carprofen, cinchophen, firocoxib, ketoprofen, maracoxib, meloxicam, metamizole, nimesulide, paracetamol, tolfenamic acid, vedaprofen.

Aspirin but not licensed

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21
Q

List the NSAIDs used in small animal specialist practice.

A

Phenylbutazone and piroxicam

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22
Q

List the rarely used NSAIDs in small animal practice.

A

Dapsone

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23
Q

List the regularly used NSAIDs in equine practice.

A

Dipyrone (plus hyoscine in buscopan), flunixin meglumine, firocoxib, ketoprofen, meloxicam, phenylbutazone, eltenac.

Diemthylsukphoxide but not licensed

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24
Q

List the NSAIDs used in specialist equine practice.

A

Carprofen, meclofenamic acid, acetylsalicylic acid.

Topical diclofenamic acid but not licensed

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25
Q

List the rarely used NSAIDs in equine practice.

A

Not licensed: isopyrin, naproxen, ramifenazone, vedaprofen

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26
Q

List the regularly used NSAIDs in food production farm animal practice.

A

Carprofen, ketoprofen, meloxicam, tolfenamic acid, flunixin

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27
Q

List the regularly used anti-inflammatories in small animal practice.

A

Betamethasone, dexamethasone, prednisolone, triamcinolone, methylprednisolone.

Not licensed: fluticasone, hydrocortisone

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28
Q

List the anti-inflammatories used in specialist small animal practice.

A

Budesonide

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29
Q

List the rarely used anti-inflammatories in small animal practice.

A

Fluoromethalone

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30
Q

List the regularly used anti-inflammatories in equine practice.

A

Dexamethasone.

Not licensed: betamethasone, fluticasone, hydrocortisone, prednisolone, triamcinolone, beclomethasone

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31
Q

List the rarely used anti-inflammatories used in equine practice.

A

Not licensed: chlorpheniramine, soxylamine succinate, pyrilamine maleate

32
Q

List the regularly used anti-inflammatories in food production farm animal practice.

A

Dexamethasone, methylprednisolone, prednisolone

33
Q

List the regularly used anti-histamines in small animal practice.

A

Loratadine.

Not licensed: chlorphenamine, clemastine, cyproheptadine, diphenhydramine, hydroxyzine

34
Q

List the anti-histamines used in small animal specialist practice.

A

Not licensed: certirizine

35
Q

List the rarely used anti-histamines used in small animal practice.

A

Not licensed: promezathine

36
Q

List the regularly used anti-histamines in equine practice.

A

Not licensed: cyproheptadine, hydroxyzine

37
Q

List the rarely used anti-histamines in equine practice.

A

Not licensed: chlorpheniramine, soxylamine succinate. Pyrilamine maleate

38
Q

Name 4 chondroprotective drugs.

A

Polysulphated glycosaminoglycan
Pentosan polysulphate sodium
Hyaluronan
Orgotein

39
Q

For what species, conditions and administrations can polysulphated glycosaminoglycan be used?

A
  • Dogs and horses
  • Clinical signs associated with non-infectious, degenerative or traumatic arthritis
  • Intramuscular use in dogs. Intramuscular and intraarticular use in horses
40
Q

What is the putative mechanism of action for polysulphated glycosaminoglycan?

A

Incorporated into healthy and damaged cartilage. Inhibits PGE2 and catabolic enzymes. Increases synthesis of hydraulic acid, proteoglycan and collagen.

41
Q

For what species, conditions and administration can pentosan polysulphate sodium be used?

A
  • Humans, dogs and horses
  • Interstitial cystitis in humans. Osteoarthritis in dogs
  • Oral for humans and injection for humans, dogs and horses
42
Q

What is the putative mechanism of action for pentosan polysulphate sodium?

A

Unknown mechanism. But stimulates hydraulic acid and GAG synthesis in damaged joints, inhibits proteolytic enzymes and scavenges free radicals. May also reduce cytokine activity. Decreases overall cartilage damage.

43
Q

For what species, condition and administration can hyaluronan be used?

A

Horses
Osteoarthritis
Intraarticular

44
Q

What is the putative method of action for hyaluronan?

A

Responsible for viscosity of synovial fluid and contributes to lubrication and joints. Inhibits PGE2 synthesis and may inhibit inflammatory enzymes and reduce pain.

45
Q

For what species, conditions and administration can orgotein be used?

A
  • Horses and dogs
  • Soft tissue inflammation in horses and arthritis in dogs
  • Intraarticular but can be intramuscular or subcutaneous
46
Q

What is the putative mechanism of action for orgotein?

A

Onset response may be 2-6 weeks. Has superoxide dismutase activity scavenging free oxygen radicals.

47
Q

What are the gastrointestinal side effects of NSAIDs?

A
  • Tend to occur in the first couple of weeks of administration and then the gut may adapt to NSAID administration.
  • Expect low grade GI ulceration in all patients receiving NSAIDs (endoscopy studies)
  • Of concern in animals with ulcerative GI disease and animals undergoing gut surgery
  • Gastroprotectants, H2 antagonists are not sufficiently protective against ulceration
48
Q

What are the renal side effects of NSAIDs?

A
  • PGI2 (prostacyclin) in the kidney is important to maintain renal blood flow during periods of hypertension. Risk of renal ischaemia following NSAID administration to patients that become hypotensive.
  • Hypotension is a big concern around the time of anaesthesia. Is it safe to give NSAIDs pre-operatively?
49
Q

What are the hepatic side effects of NSAIDs?

A
  • Hepatopathy is a rare idiosyncratic reaction to NSAIDs
  • More commonly reported in dogs
  • NSAID administration may be associated with an elevation in liver enzymes (does not relate to overt hepatic dysfunction)
  • NSAIDs are liver metabolised. Liver dysfunction may lead to drug accumulation and side effects. Check liver function before starting therapy?
50
Q

What are the CNS side effects of NSAIDs?

A
  • Dullness and lethargy is reported in cats after NSAID administration
  • Mechanism not understood
51
Q

What are the platelet function side effects of NSAIDs?

A
  • NSAIDs with COX-1 effects block the production of thromboxane A2 in platelets.
  • May prolong indicators of blood clotting, rarely associated with overt clotting dysfunction.
  • NSAIDs with COX-2 effects may inhibit the production of prostacyclin, which is responsible for vasodilation and limiting the clotting cascade. Risk of increased thrombosis? Reported in people and not reported in animals.
52
Q

What are the non-selective NSAIDs?

A

Non selective NSAIDs – no greater selectivity for COX-2 over COX-1

  • Flunixin
  • Ketoprofen
  • Phenylbutazone and suxibuzone
  • Tolfenamic acid
53
Q

Which is an NSAID that doesn’t use COX inhibition?

A

Grapiprant (Galliprant) PG receptor antagonist specifically blocks the EP4 receptor which is the primary mediator of canine OA pain.

54
Q

What can you do if NSAIDs are contraindicated for acute pain?

A
  • Easy to find alternatives for NSAIDs
  • Other classes of painkillers like opioids
  • Some anaesthetic drugs like local anaesthetics, like ketamine
55
Q

What can you do if NSAIDs are contraindicated for chronic pain?

A
  • Harder to find alternatives
  • Disease modifying agents such as for osteoarthritis
  • Lifestyle changes, such as weight loss
  • Supplements, such as for osteoarthritis
  • Some drugs like gabapentin (but licenced)
56
Q

Describe the NSAIDs that can be used for dogs.

A

A wide array of NSAIDs are licensed for administration to dogs. Acute and chronic use.

  • Ketoprofen; Tolfenamic acid
  • Carprofen; Meloxicam
  • The ‘Coxibs’ = cimicoxib, enflicoxib, firocoxib, mavacoxib, robenacoxib
  • Grapiprant
57
Q

Describe how NSAIDs can be given to older dogs with pre-existing conditions.

A
  • Dogs are well studied and appear to tolerate NSAIDs well, even when older
  • Lowest possible dose
  • May need to try several – use a washout period between each
  • Give with food
  • Monitor health regularly, at least every 6 months
  • Owners should be aware of potential adverse effects
58
Q

Describe NSAID use in cats and the main 2 used.

A

Limited number of NSAIDs are licensed in cats, which does make the choice much easier.

  • Meloxicam – injectable and oral preparation. Long term license in cats for chronic pain.
  • Robenacoxib – injectable and oral preparation. Licensed for 3 days only in cats although looks like chronic admin may be licensed soon.
59
Q

What are 3 other possible NSAIDs to be used in cats?

A
  • Carprofen – licensed as a single injection only (due to unpredictable half-life in cats)
  • Ketoprofen – injectable and oral preparation. Up to 5 days only
  • Tolfenamic Acid – injectable + oral preparation. Up to 3 days only
60
Q

Describe NSAID use for older cats or those with pre-existing conditions.

A
  • Cats are much more likely to develop side effects compared to dogs hence why fewer NSAIDs are licensed in cats.
  • Many older cats have chronic renal failure
  • Lowest possible dose, possibly every other day and not daily
  • May need to try several, use a washout period between each
  • Give with feed
  • Monitor health regularly every 6 months, ideally with blood work
  • Owners should be aware of potential adverse effects
61
Q

Describe NSAID use in horses.

A
  • NSAIDs are widely used for the management of acute and chronic pain
  • NSAIDs are also prescribed for their anti-endotoxaemia effects in horses with colic
  • Renal side effects appear to be less problematic in horses although they can occur
  • Gastrointestinal ulceration does occur, particularly in foals
62
Q

Describe NSAIDs use in rabbits.

A

There are no licensed NSAIDs in rabbits.

  • Prescribe under cascade
  • Meloxicam is most widely used. Studies reported for acute and chronic use but more data needed.
  • Carprofen – also been used but less data. Possibky more prudent to stick to meloxicam as a vet in practice.
63
Q

Describe NSAIDs use in cattle and pigs.

A
  • Injectable rather than oral preparations are available
  • Observe meat and milk withdrawal periods – very dependent on the drug.
  • Side effects like those in animals although renal side effects appear to be less of a concern compared to cats and dogs
  • COX-2 selective – meloxicam and carprofen
  • Non-selective NSAIDs – ketoprofen and flunixin
64
Q

Describe NSAIDs use in sheep and goats.

A

There are no licensed NSAIDs in sheep and goats:

  • Prescribe under the cascade from those available in other food producing animals.
  • Just because none are licensed does not mean to say that sheep and doats do not feel pain
  • Studies have demonstrated beneficial effects with acute pain from castration and tail docking
65
Q

How can NSAID side effects be avoided in all species?

A
  • Do not exceed the licensed dose
  • Do not give more than 1 NSAID at the same time
  • Do not combine NSAID and corticosteroid treatment
  • Ensure animals are adequately hydrated and normotensive at the time of administration (small animals only – can ignore this for adult horses and farm species)
  • In some cases, NSAIDs are relatively or absolutely contraindicated; in which case analgesia should be considered with an alternative class of analgesic or other management methods
66
Q

Distinguish acute and chronic pain in companion animals.

A

Cats, dogs, horses and rabbits

Acute pain management – trauma and peri-operative pain

Chronic pain management – management of pain associated with osteoarthritis and other chronic pain conditions.

67
Q

Why are NSAIDs used so routinely?

A
  • Efficacious – good evidence to support use
  • Not subject to Controlled Drugs regulations
  • Can be continued in the home environment
68
Q

How is an NSAID for peri-operative use chosen?

A
  • Handy to have a drug with an injectable preparation so that do not need to tablet at the time of anaesthesia.
  • May depend on practice relationships with drug companies
  • Is there an injectable to oral indication on the SPC
  • Cost-benefit analysis
69
Q

What are the benefits of pre-operative NSAID administration?

A
  • Some evidence that giving an NSAID pre-operatively as opposed to post-operatively might be beneficial in dogs.
  • Prevented secondary hyperalgesia after OVE (Lascelles and colleagues)
  • But intra-operative analgesia can be provided with other classes of analgesic drug such as opioids, ketamine, alpha2agonists
70
Q

What are the risks of pre-operative administration?

A
  • Does the patient have concurrent disease that may make it more likely to become hypotensive during anaesthesia?
  • Long surgery?
  • Expect blood loss?
  • Underlying CVS disease?
  • Geriatric?
  • Surgery type may predispose to CVS compromise, such as intrathoracic surgery
71
Q

How are NSAIDs given to CVS stable patients pre-operatively?

A

If concerned about management of blood pressure, delay administration until the end of anaesthesia when the animal is recovered and normotensive

72
Q

Why may NSAIDs be administered to farm animals?

A

Used for their anti-pyretic, analgesic and anti-endotoxaemic properties:
- Calf pneumonia
- Calf scour
- Toxic metritis + mastitis
- Peri-operatively after surgery: digit amputation, left displaced abomasum, caesarian section

73
Q

How are NSAIDs used for dystocia in cattle?

A

Dystocia is inevitably painful for cattle. Studies have investigated whether giving NSAIDs to cows with dystocia is beneficial:

  • Poor data sets available (animals not adequately matched between groups)
  • Blanket treatment of all cows after calving with an NSAID is probably not justified
  • Difficult to interpret the data on cows with dystocia
74
Q

How can you discriminate between the different NSAIDs?

A
  • What formulation will the owner find easiest to give? Tablet (chewable or swallowed), palatable tablet, injectable, liquid, powders
  • Cost – will be more important for bigger dogs and horses
  • Relationship with drug companies – may get one NSAID at a discount
  • Compliance and convenience – monthly or daily administration
  • Newer vs older NSAIDs
  • Licensed indications – acute, chronic or both?
  • Duration of action – monthly or daily administration?
75
Q

Why must you be cautious when phenylbutazone is given to horses?

A
  • Plasma concentrations are dependent on whether it is given orally to horses fasted of hay or allowed hay access
  • Prolonged time to peak plasma concentration when given to horses fed hay around the time of dosing (6 hours versus 13 hours)
  • But not to be used in horses intended for human consumption.
  • Treated horses may never be slaughtered for human consumption.

Animal Disease 1 (25 decks)

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