Antiinflammatory drugs Flashcards
Division of antiinflammatory drugs:
Non-steroidal antiinflammatory drugs (NSAID)
Steroidal antiinflammatory drugs - glucocorticoids
Characterize inflammation:
Complex pathophysiologic response of vascularized tissue to injury.
Injury may result from various stimuli - thermal, chemical, physical, ischemia, infectious etc.
Name and characterize the three subphases of initial inflammation:
- Acute phase: 1-3 days
- heat, redness, swelling, pain and loss of
function - Subacute phase: 3-4 days to 1 month
- cleaning phase required before repair - Chronic inflammation if subacute phase is not resolved within 1 month
- several months
Characterize NSAIDs:
- 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
How does cyclooxygenase-1 and -2 function?
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.
Name some normal physiological effects mediated by COX-1:
Hemostasis
GI mucosal protection
Protection of kidney from hypotensive insult
Name the two broad groups of NSAIDs:
carboxylic acid and enolic acid derivaties
Which subgroups are included in carboxylic acids?
salicylates
propionic acids
fenamates
phenylacetic acids
aminonicotinic acids
Which subgroups are included in enolic acids?
pyrazolones
oxicams
Carboxylic acid: Salicylates:
acetylsalicylic acid (aspirin) - pain, fever and inflammation
- mild to moderate pain in
musculoskeletal inflammation or
osteoarthritis
Dosage forms: bolus, oral paste, oral solution, tablets
Carboxylic acid: Propionic acid derivatives:
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.
Carboxylic acid: fenamates:
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
Carboxylic acid: Phenylacetic acids
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
Carboxylic acid: Aminonicotinic acids
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
Enolic acids: Pyrazolones
Phenylbutazone
- tablet, paste, gel and parenteral formula
- acute laminitis in horse
- analgesic/antiinflammatory, antipyretic in dogs, cattle and swine
Enolic acids: oxicams
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
New class: the coxib, name examples:
Deracoxib
Firocoxib
Robenacoxib
Mavacoxib
- pain and inflammation
What is tepoxalin?
NSAID that works as a dual inhibitor of both COX-1 and COX-2
- dogs as oral tablet
Glucocorticoids are:
Steroid antiinflammatory drugs
- the most efficacious antiinflammatory drugs
Glucocorticoids are used as:
antiinflammatory drugs
antiallergic agents and immunosuppressants
endocrine drugs
anabolic and catabolic
How does glucocorticoids function?
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
Glucocorticoids are used to treat, and manage:
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
