Antiinflammatory drugs

Question 1

Division of antiinflammatory drugs:

Answer 1

Non-steroidal antiinflammatory drugs (NSAID)
Steroidal antiinflammatory drugs - glucocorticoids

Question 2

Characterize inflammation:

Answer 2

Complex pathophysiologic response of vascularized tissue to injury.
Injury may result from various stimuli - thermal, chemical, physical, ischemia, infectious etc.

Question 3

Name and characterize the three subphases of initial inflammation:

Answer 3

1. Acute phase: 1-3 days
   - heat, redness, swelling, pain and loss of
   function
2. Subacute phase: 3-4 days to 1 month
   - cleaning phase required before repair
3. Chronic inflammation if subacute phase is not resolved within 1 month
   - several months

Question 4

Characterize NSAIDs:

Answer 4

• analgesic and antipyretic (fever-reducing) effects
• relieve pain and inflammation
  Inhibit activity of cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) that catalyze mediators of inflammation

Question 5

How does cyclooxygenase-1 and -2 function?

Answer 5

COX-1 is in all tissues, and catalyze formation of constitutive prostaglandins.

COX-2 is activated in damaged and inflamed tissues, and catalyze the formation of inducible prostaglandin associated with intensifying the inflammatory response. It is also involved in thermoregulation and pain response to injury.

Question 6

Name some normal physiological effects mediated by COX-1:

Answer 6

Hemostasis
GI mucosal protection
Protection of kidney from hypotensive insult

Question 7

Name the two broad groups of NSAIDs:

Answer 7

carboxylic acid and enolic acid derivaties

Question 8

Which subgroups are included in carboxylic acids?

Answer 8

salicylates
propionic acids
fenamates
phenylacetic acids
aminonicotinic acids

Question 9

Which subgroups are included in enolic acids?

Answer 9

pyrazolones
oxicams

Question 10

Carboxylic acid: Salicylates:

Answer 10

acetylsalicylic acid (aspirin) - pain, fever and inflammation
- mild to moderate pain in
musculoskeletal inflammation or
osteoarthritis
Dosage forms: bolus, oral paste, oral solution, tablets

Question 11

Carboxylic acid: Propionic acid derivatives:

Answer 11

ibuprofen, naproxen, fenoprofen, flubiprofen,
ketoprofen - acute pain up to 5 days, carprofen - pain and inflammation, osteoarthritis, acute pain in soft-tissue+orthopedic surgery in dogs, and vedaprofen - musculoskeletal in dogs&horses, pain + inflammation, colic in horses.

Question 12

Carboxylic acid: fenamates:

Answer 12

mefenamic acid
flufenamic acid
meclofenamic acid - chronic laminitis, horses
tolfenamic acid - fever, post-op pain, acute and chronic inflammatory conditions in cats, dogs, cattle and pigs

Question 13

Carboxylic acid: Phenylacetic acids

Answer 13

Acetaminophen (paracetamol)
- analgesic and antipyretic effect
- weaker antiinflammatory effect
Use in cats can cause methemoglobinemia and centrilobular hepatic necrosis due to their deficiency of glucuronyl transferase

Question 14

Carboxylic acid: Aminonicotinic acids

Answer 14

Flunixin
- visceral pain in colic (horses)
- reduce inflammatory-mediated hemodynamic response to endotoxin
- pain and inflammation associated with arthritis and other musculoskeletal disorders in dogs and cats

Question 15

Enolic acids: Pyrazolones

Answer 15

Phenylbutazone
- tablet, paste, gel and parenteral formula
- acute laminitis in horse
- analgesic/antiinflammatory, antipyretic in dogs, cattle and swine

Question 16

Enolic acids: oxicams

Answer 16

Meolxicam
- injectable
- inhibitor of prostaglandin synthesis
- acute and chronic inflammation in musculoskeletal disease
- post-op pain

Piroxicam - ankylosing spondylitis, and osteoarthritis in dogs, cats and horses

Question 17

New class: the coxib, name examples:

Answer 17

Deracoxib
Firocoxib
Robenacoxib
Mavacoxib

• pain and inflammation

Question 18

What is tepoxalin?

Answer 18

NSAID that works as a dual inhibitor of both COX-1 and COX-2
- dogs as oral tablet

Question 19

Glucocorticoids are:

Answer 19

Steroid antiinflammatory drugs
- the most efficacious antiinflammatory drugs

Question 20

Glucocorticoids are used as:

Answer 20

antiinflammatory drugs
antiallergic agents and immunosuppressants
endocrine drugs
anabolic and catabolic

Question 21

How does glucocorticoids function?

Answer 21

Suppress every component of the inflammatory process
- inhibit phospholipase A2
- decrease synthesis of interleukins & proinflammatory cytokines
- suppress cell-mediated immunity
- reduce complement synthesis
- decrease production and activity of leukocytes

Question 22

Glucocorticoids are used to treat, and manage:

Answer 22

Treat: allergy, inflammation, allergic lung and GI diseases

Manage: chronic allergic bronchitis and feline asthma, alleviation of priritus in acute cases of atopic or flea allergy dermatitis