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ANTI INFLAMMATORY DRUGS
Submitted to: Dr Hafiz Manzoor
Submitted by: M. Mutahir
2017-DVMN-029
References
Theresa Welch Fossum ( 151-152)
Complications in small animal surgery ( 92 , 97-105)
Merck veterinary manual (2707-2721)
Clinical vet guide ( 1-8)
Plumb’s veterinary drug handbook
Inflammation
•Inflammation is the complex pathophysiological response of
vascularized tissue to injury
•The injury may result from various stimuli, including thermal,
chemical, or physical damage; ischemia; infectious agents and
antigen-antibody interactions
NSAIDS
•NSAIDs have the potential to relieve pain and inflammation
without the potential metabolic, hemodynamic, and
immunosuppressive adverse effects associated with corticosteroids
•However, all NSAIDs have the potential for other adverse effects
that should be considered
Mode of action
•NSAIDs act primarily to reduce the biosynthesis of prostaglandins
by inhibiting Cyclooxygenase (COX)
•ln general, NSAIDs do not inhibit the formation of 5-lipoxygenase
(5-LOX) and hence leukotriene, or the formation of other
inflammatory mediators
•The novel NSAID tepoxalin is an exception in that it inhibits both
COX and 5-LOX
Pharmacologic effects
•All NSAlDs, except for acetaminophen ( also named paracetamol),
are antipyretic, analgesic, and anti-inflammatory
•They are routinely used for the relief of pain and inflammation
associated with osteoarthritis in dogs and horses and for colic,
navicular disease, and laminitis in horses
•As analgesics, they are generally less effective than opioids
Common NSAIDS
Flunixin
Ketoprofen
Naproxen
Meloxicam
Piroxicam
Phenylbutazone
Aspirin
Ketorolac
Acetaminophen
Flunixin
Uses/Indications:
Alleviation of inflammation and pain associated with
musculoskeletal disorders and alleviation of visceral pain
associated with colic
In cattle for the control of pyrexia associated with BRD and
endotoxemia, and control of inflammation in endotoxemia
In ruminants, flunixin is a better analgesic for visceral pain rather
than musculoskeletal pain
May improve hemodynamics in animals with septic shock
Contraindications
•Flunixin should be used cautiously in animals with renal, hepatic,
or hematologic diseases
•When using to treat colic, flunixin may mask the behavioral and
cardiopulmonary signs associated with endotoxemia or intestinal
devitalization
•In horses with known or suspected EGUS, use should be
avoided; repeated doses can exacerbate gastric ulcers
•Flunixin is usually considered contraindicated in cats
Adverse effects
•In horses following IM injection, reports of localized swelling,
induration, stiffness, and sweating have been reported
•Do not inject intra-arterially as it may cause CNS stimulation
(hysteria), ataxia, hyperventilation, and muscle weakness
•Flunixin appears to be a relatively safe agent for use in the horse, but
the potential exists for GI intolerance, hypoproteinemia, and
hematologic abnormalities to occur
•IM injections may rarely be associated with clostridial myonecrosis
•Hematochezia and hematuria have been reported in cattle treated
for longer than the 3-day recommendation.
•In dogs, GI distress is the most likely adverse reaction
•Clinical signs may include, vomiting, diarrhea, and ulceration
•In birds, flunixin has been shown to cause significant renal ischemia
and nephrotoxicity
Brand names
Ketoprofen
Uses/Indications:
•Ketoprofen is used in horses for the alleviation of inflammation and
pain associated with musculoskeletal disorders
NSAID of choice for short-term analgesia in cats
•Indicated for use in dogs and cats for the alleviation of inflammation,
lameness and pain due to osteoarthritis, hip dysplasia, disc disease,
spondylosis, panosteitis
•For the management of post-surgical pain
Contraindications/Precautions
•Patients with significant renal or hepatic impairment
•ketoprofen is highly protein bounded
Adverse Effects
•Ketoprofen appears to have low toxicity in horses
•Potentially, gastric mucosal damage and GI ulceration, renal crest
necrosis, and mild hepatitis may occur
•Do not administer intra-arterially and avoid SC injections
•In dogs or cats, ketoprofen may cause vomiting, anorexia, and GI
ulcers
Meloxicam
Uses/Indications:
•Meloxicam is principally used for the symptomatic treatment of
osteoarthritis in dogs
•In for cats for the control of postoperative pain and inflammation
associated with orthopedic surgery, ovariohysterectomy and
castration pre-operatively
•In calves to treat painful procedures such as castration or
dehorning
Contraindications/Precautions
•It should be used with caution in patients with impaired hepatic,
cardiac or renal function and hemorrhagic disorders
•Due to its long half-life in dogs, a 5–7 day washout period after
stopping meloxicam has been recommended before starting a new
NSAID
•Use extreme caution in dehydrated, hypovolemic, or hypotensive
animals as there is a potential increased risk of renal toxicity
Adverse Effects
•GI distress is the most commonly reported adverse effect
•Elevation of liver enzymes, pruritis, elevated creatinine, and renal
failure
•Repeated use of meloxicam in cats is associated with renal failure and
death
Piroxicam
Uses/Indications:
•In dogs, piroxicam may be beneficial in reducing the pain and
inflammation associated with degenerative joint disease
•Its primary use is in dogs as adjunctive treatment of bladder
transitional cell carcinoma
•It may also be of benefit in squamous cell carcinomas, mammary
adenocarcinoma, and transmissible venereal tumor (TVT)
Contraindications/Precautions
• Because peripheral edema has been noted in some human
patients, it should be used with caution in patients with severely
compromised cardiac function
•Piroxicam has not been evaluated for use in cats
Adverse Effects
•Doses as low as 1 mg/kg given daily have caused significant GI
ulceration, renal papillary necrosis, and peritonitis
• In dogs include: CNS effects (headache, dizziness), otic effects
(tinnitus), pruritis and rash, and peripheral edema
•In cats, GI effects (vomiting, anorexia, diarrhea) may be seen
•There are reports of piroxicam decreasing hematocrits in cats
when dosed daily for 7- 14 days
Phenylbutazone
Uses/Indications:
•“For the relief of inflammatory conditions associated with the
musculoskeletal system in dogs and horses”
• It has been used primarily for the treatment of lameness in
horses
Contraindications/Precautions
•Cautious use is recommended because of increased incidences of
hypoproteinemia and GI ulceration
•Phenylbutazone may cause decreased renal blood flow and sodium
and water retention, and should be used cautiously in animals with
preexisting renal disease or CHF
•Do not administer injectable preparation IM or SC as it is very irritating
(swelling, to necrosis and sloughing)
Adverse Effects
•Toxic effects in horses include oral and GI erosions and ulcers,
hypoalbuminemia, diarrhea, anorexia, and renal effects
•Phenylbutazone-induced blood dyscrasias and hepatotoxicity have
also been reported in dogs
•Bone marrow effects (aplastic anemia), renal and cardiovascular effects
(fluid retention to acute renal failure), and GI effects (dyspepsia to
perforated ulcers)
•The use of H2 blockers (cimetidine, ranitidine) have been suggested
for use in treating the GI effects
Brand names
1. Fenylbutazone: 200mg/ml : Orient traders
2. Pain go : 200mg/ml : Leads Pharma
3. Butadin :200mg/ml : Star Labs
Acetaminophen
Uses/Indications:
•Acetaminophen is occasionally used as an oral analgesic in dogs
•It may be particularly beneficial in dogs with renal dysfunction for
the treatment of chronic pain conditions
•In situations where moderate pain occurs, it may be used in
combination with tramadol
Contraindications/Precautions
•Acetaminophen is contraindicated in cats at any dosage
•Severe methemoglobinemia, hematuria, and icterus can be seen
•While dogs are not as sensitive to acetaminophen as cats, they may
also be susceptible to methemoglobinemia when given high dosages
•In dogs, it is generally not recommended during the immediate post-
operative phase due to an increased risk of hepatotoxicity
Brand names
Ketorolac
Uses/Indications:
•Ketorolac is used primarily for its analgesic effects for short-
term treatment of mild to moderate pain in dogs and rodents
•The duration of analgesic effect in dogs is about 8–12 hours
Contraindications/Precautions
•Ketorolac is relatively contraindicated in patients with a history of,
or preexisting, hematologic, renal or hepatic disease
•It should be used cautiously in patients with a history of GI ulcers,
or heart failure (may cause fluid retention), and in geriatric patients
•Because Ketorolac has a tendency to cause gastric erosion and
ulcers in dogs, long-term use (>3 days) is not recommended
Adverse Effects
•The primary issue in dogs is its GI toxicity
•GI ulceration can be common if the drug is used chronically
•Like other NSAIDS, platelet inhibition, renal, and hepatic
toxicity are also possible with this drug
Aspirin
Uses/Indications:
•Aspirin is used in all species for its analgesic and antipyretic effects
•Aspirin is used therapeutically for its effects on platelet aggregation in
the treatment of DIC and pulmonary artery disease secondary to
heartworm infestation in dogs
•It is also used in cats with cardiomyopathy
•Aspirin (at low doses) may be of benefit in the adjunctive treatment of
glomerular disease
Contraindications/Precautions
• It is relatively contraindicated in patients with hemorrhagic
disorders, asthma, or renal insufficiency
•Because aspirin is highly protein bound to plasma albumin, patients
with hypoalbuminemia may require lower dosages to prevent clinical
signs of toxicity
•Because of its effects on platelets, aspirin therapy should be halted,
if possible, one week prior to surgical procedures
Adverse Effects
•The most common adverse effect at therapeutic doses is gastric
(nausea, anorexia, vomiting) or intestinal irritation with varying
degrees of occult GI blood loss occurring
•The resultant irritation may result in vomiting and/or anorexia
•Severe blood loss may result in a secondary anemia or
hypoproteinemia
•Cats may develop acidosis from aspirin therapy
CORTICOSTEROIDS
Two classes of steroid hormones, mineralocorticoids and glucocorticoids,
are naturally synthesized in the adrenal cortex from cholesterol
Mineralocorticoids ( aldosterone) are so named because they are important
in maintaining electrolyte homeostasis
Glucocorticoids suppress virtually every component of the inflammatory
process; they inhibit PLA2, decrease synthesis of interleukins and
numerous other inflammatory cytokines, suppress cell-mediated immunity
and decrease production and activity of leukocytes
Dexamethasone
Uses/Indications:
Glucocorticoids have been used in an attempt to treat practically every
malady that afflicts animal, but there are three broad uses:
1) Replacement of glucocorticoid activity in patients with adrenal
insufficiency
2) As an antiinflammatory agent
3) As an immunosuppressive
Contraindications/Precautions
•Because dexamethasone has negligible mineralocorticoid effect, it
should generally not be used alone in the treatment of adrenal
insufficiency
•Do not administer the injectable rapidly intravenously ;
hypotension, collapse, and hemolytic anemia can occur
•There is a high incidence of gastrointestinal bleeding and colonic
perforation in canine neurosurgical patients treated with
dexamethasone
•Systemic use of Glucocorticoids is generally considered
contraindicated in systemic fungal infections
•Animals that have received glucocorticoids systemically should be
tapered off the drugs
•Animals, particularly cats, at risk for diabetes mellitus or with
concurrent cardiovascular disease should receive glucocorticoids
with caution due to these agents’ potent hyperglycemic effect
Adverse Effects
•Glucocorticoids can retard growth in young animals
•In dogs, polydipsia , polyphagia and polyuria , may all be seen
•Very high doses in dogs with spinal cord injuries have caused fatal
colon perforations
•Adverse effects associated with immunosuppressive doses are more
common
•Administration of dexamethasone may play a role in the development
of
laminitis in horses
Prednislone
Uses/Indications:
•There are there are four primary uses and dose ranges:
1) replacement or supplementation
2) as an antiinflammatory
3) as an immunosuppressive
4) as an antineoplastic agent
Anti inflammatory drugs

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Anti inflammatory drugs

  • 1. ANTI INFLAMMATORY DRUGS Submitted to: Dr Hafiz Manzoor Submitted by: M. Mutahir 2017-DVMN-029
  • 2. References Theresa Welch Fossum ( 151-152) Complications in small animal surgery ( 92 , 97-105) Merck veterinary manual (2707-2721) Clinical vet guide ( 1-8) Plumb’s veterinary drug handbook
  • 3. Inflammation •Inflammation is the complex pathophysiological response of vascularized tissue to injury •The injury may result from various stimuli, including thermal, chemical, or physical damage; ischemia; infectious agents and antigen-antibody interactions
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  • 7. NSAIDS •NSAIDs have the potential to relieve pain and inflammation without the potential metabolic, hemodynamic, and immunosuppressive adverse effects associated with corticosteroids •However, all NSAIDs have the potential for other adverse effects that should be considered
  • 8. Mode of action •NSAIDs act primarily to reduce the biosynthesis of prostaglandins by inhibiting Cyclooxygenase (COX) •ln general, NSAIDs do not inhibit the formation of 5-lipoxygenase (5-LOX) and hence leukotriene, or the formation of other inflammatory mediators •The novel NSAID tepoxalin is an exception in that it inhibits both COX and 5-LOX
  • 9. Pharmacologic effects •All NSAlDs, except for acetaminophen ( also named paracetamol), are antipyretic, analgesic, and anti-inflammatory •They are routinely used for the relief of pain and inflammation associated with osteoarthritis in dogs and horses and for colic, navicular disease, and laminitis in horses •As analgesics, they are generally less effective than opioids
  • 11. Flunixin Uses/Indications: Alleviation of inflammation and pain associated with musculoskeletal disorders and alleviation of visceral pain associated with colic In cattle for the control of pyrexia associated with BRD and endotoxemia, and control of inflammation in endotoxemia In ruminants, flunixin is a better analgesic for visceral pain rather than musculoskeletal pain May improve hemodynamics in animals with septic shock
  • 12. Contraindications •Flunixin should be used cautiously in animals with renal, hepatic, or hematologic diseases •When using to treat colic, flunixin may mask the behavioral and cardiopulmonary signs associated with endotoxemia or intestinal devitalization •In horses with known or suspected EGUS, use should be avoided; repeated doses can exacerbate gastric ulcers •Flunixin is usually considered contraindicated in cats
  • 13. Adverse effects •In horses following IM injection, reports of localized swelling, induration, stiffness, and sweating have been reported •Do not inject intra-arterially as it may cause CNS stimulation (hysteria), ataxia, hyperventilation, and muscle weakness •Flunixin appears to be a relatively safe agent for use in the horse, but the potential exists for GI intolerance, hypoproteinemia, and hematologic abnormalities to occur
  • 14. •IM injections may rarely be associated with clostridial myonecrosis •Hematochezia and hematuria have been reported in cattle treated for longer than the 3-day recommendation. •In dogs, GI distress is the most likely adverse reaction •Clinical signs may include, vomiting, diarrhea, and ulceration •In birds, flunixin has been shown to cause significant renal ischemia and nephrotoxicity
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  • 17. Ketoprofen Uses/Indications: •Ketoprofen is used in horses for the alleviation of inflammation and pain associated with musculoskeletal disorders NSAID of choice for short-term analgesia in cats •Indicated for use in dogs and cats for the alleviation of inflammation, lameness and pain due to osteoarthritis, hip dysplasia, disc disease, spondylosis, panosteitis •For the management of post-surgical pain
  • 18. Contraindications/Precautions •Patients with significant renal or hepatic impairment •ketoprofen is highly protein bounded
  • 19. Adverse Effects •Ketoprofen appears to have low toxicity in horses •Potentially, gastric mucosal damage and GI ulceration, renal crest necrosis, and mild hepatitis may occur •Do not administer intra-arterially and avoid SC injections •In dogs or cats, ketoprofen may cause vomiting, anorexia, and GI ulcers
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  • 24. Meloxicam Uses/Indications: •Meloxicam is principally used for the symptomatic treatment of osteoarthritis in dogs •In for cats for the control of postoperative pain and inflammation associated with orthopedic surgery, ovariohysterectomy and castration pre-operatively •In calves to treat painful procedures such as castration or dehorning
  • 25. Contraindications/Precautions •It should be used with caution in patients with impaired hepatic, cardiac or renal function and hemorrhagic disorders •Due to its long half-life in dogs, a 5–7 day washout period after stopping meloxicam has been recommended before starting a new NSAID •Use extreme caution in dehydrated, hypovolemic, or hypotensive animals as there is a potential increased risk of renal toxicity
  • 26. Adverse Effects •GI distress is the most commonly reported adverse effect •Elevation of liver enzymes, pruritis, elevated creatinine, and renal failure •Repeated use of meloxicam in cats is associated with renal failure and death
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  • 32. Piroxicam Uses/Indications: •In dogs, piroxicam may be beneficial in reducing the pain and inflammation associated with degenerative joint disease •Its primary use is in dogs as adjunctive treatment of bladder transitional cell carcinoma •It may also be of benefit in squamous cell carcinomas, mammary adenocarcinoma, and transmissible venereal tumor (TVT)
  • 33. Contraindications/Precautions • Because peripheral edema has been noted in some human patients, it should be used with caution in patients with severely compromised cardiac function •Piroxicam has not been evaluated for use in cats
  • 34. Adverse Effects •Doses as low as 1 mg/kg given daily have caused significant GI ulceration, renal papillary necrosis, and peritonitis • In dogs include: CNS effects (headache, dizziness), otic effects (tinnitus), pruritis and rash, and peripheral edema •In cats, GI effects (vomiting, anorexia, diarrhea) may be seen •There are reports of piroxicam decreasing hematocrits in cats when dosed daily for 7- 14 days
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  • 37. Phenylbutazone Uses/Indications: •“For the relief of inflammatory conditions associated with the musculoskeletal system in dogs and horses” • It has been used primarily for the treatment of lameness in horses
  • 38. Contraindications/Precautions •Cautious use is recommended because of increased incidences of hypoproteinemia and GI ulceration •Phenylbutazone may cause decreased renal blood flow and sodium and water retention, and should be used cautiously in animals with preexisting renal disease or CHF •Do not administer injectable preparation IM or SC as it is very irritating (swelling, to necrosis and sloughing)
  • 39. Adverse Effects •Toxic effects in horses include oral and GI erosions and ulcers, hypoalbuminemia, diarrhea, anorexia, and renal effects •Phenylbutazone-induced blood dyscrasias and hepatotoxicity have also been reported in dogs •Bone marrow effects (aplastic anemia), renal and cardiovascular effects (fluid retention to acute renal failure), and GI effects (dyspepsia to perforated ulcers) •The use of H2 blockers (cimetidine, ranitidine) have been suggested for use in treating the GI effects
  • 40. Brand names 1. Fenylbutazone: 200mg/ml : Orient traders 2. Pain go : 200mg/ml : Leads Pharma 3. Butadin :200mg/ml : Star Labs
  • 41. Acetaminophen Uses/Indications: •Acetaminophen is occasionally used as an oral analgesic in dogs •It may be particularly beneficial in dogs with renal dysfunction for the treatment of chronic pain conditions •In situations where moderate pain occurs, it may be used in combination with tramadol
  • 42. Contraindications/Precautions •Acetaminophen is contraindicated in cats at any dosage •Severe methemoglobinemia, hematuria, and icterus can be seen •While dogs are not as sensitive to acetaminophen as cats, they may also be susceptible to methemoglobinemia when given high dosages •In dogs, it is generally not recommended during the immediate post- operative phase due to an increased risk of hepatotoxicity
  • 44. Ketorolac Uses/Indications: •Ketorolac is used primarily for its analgesic effects for short- term treatment of mild to moderate pain in dogs and rodents •The duration of analgesic effect in dogs is about 8–12 hours
  • 45. Contraindications/Precautions •Ketorolac is relatively contraindicated in patients with a history of, or preexisting, hematologic, renal or hepatic disease •It should be used cautiously in patients with a history of GI ulcers, or heart failure (may cause fluid retention), and in geriatric patients •Because Ketorolac has a tendency to cause gastric erosion and ulcers in dogs, long-term use (>3 days) is not recommended
  • 46. Adverse Effects •The primary issue in dogs is its GI toxicity •GI ulceration can be common if the drug is used chronically •Like other NSAIDS, platelet inhibition, renal, and hepatic toxicity are also possible with this drug
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  • 49. Aspirin Uses/Indications: •Aspirin is used in all species for its analgesic and antipyretic effects •Aspirin is used therapeutically for its effects on platelet aggregation in the treatment of DIC and pulmonary artery disease secondary to heartworm infestation in dogs •It is also used in cats with cardiomyopathy •Aspirin (at low doses) may be of benefit in the adjunctive treatment of glomerular disease
  • 50. Contraindications/Precautions • It is relatively contraindicated in patients with hemorrhagic disorders, asthma, or renal insufficiency •Because aspirin is highly protein bound to plasma albumin, patients with hypoalbuminemia may require lower dosages to prevent clinical signs of toxicity •Because of its effects on platelets, aspirin therapy should be halted, if possible, one week prior to surgical procedures
  • 51. Adverse Effects •The most common adverse effect at therapeutic doses is gastric (nausea, anorexia, vomiting) or intestinal irritation with varying degrees of occult GI blood loss occurring •The resultant irritation may result in vomiting and/or anorexia •Severe blood loss may result in a secondary anemia or hypoproteinemia •Cats may develop acidosis from aspirin therapy
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  • 55. CORTICOSTEROIDS Two classes of steroid hormones, mineralocorticoids and glucocorticoids, are naturally synthesized in the adrenal cortex from cholesterol Mineralocorticoids ( aldosterone) are so named because they are important in maintaining electrolyte homeostasis Glucocorticoids suppress virtually every component of the inflammatory process; they inhibit PLA2, decrease synthesis of interleukins and numerous other inflammatory cytokines, suppress cell-mediated immunity and decrease production and activity of leukocytes
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  • 57. Dexamethasone Uses/Indications: Glucocorticoids have been used in an attempt to treat practically every malady that afflicts animal, but there are three broad uses: 1) Replacement of glucocorticoid activity in patients with adrenal insufficiency 2) As an antiinflammatory agent 3) As an immunosuppressive
  • 58. Contraindications/Precautions •Because dexamethasone has negligible mineralocorticoid effect, it should generally not be used alone in the treatment of adrenal insufficiency •Do not administer the injectable rapidly intravenously ; hypotension, collapse, and hemolytic anemia can occur •There is a high incidence of gastrointestinal bleeding and colonic perforation in canine neurosurgical patients treated with dexamethasone
  • 59. •Systemic use of Glucocorticoids is generally considered contraindicated in systemic fungal infections •Animals that have received glucocorticoids systemically should be tapered off the drugs •Animals, particularly cats, at risk for diabetes mellitus or with concurrent cardiovascular disease should receive glucocorticoids with caution due to these agents’ potent hyperglycemic effect
  • 60. Adverse Effects •Glucocorticoids can retard growth in young animals •In dogs, polydipsia , polyphagia and polyuria , may all be seen •Very high doses in dogs with spinal cord injuries have caused fatal colon perforations •Adverse effects associated with immunosuppressive doses are more common •Administration of dexamethasone may play a role in the development of laminitis in horses
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  • 63. Prednislone Uses/Indications: •There are there are four primary uses and dose ranges: 1) replacement or supplementation 2) as an antiinflammatory 3) as an immunosuppressive 4) as an antineoplastic agent