Inflammation Flashcards
What is the mechanism of action of acetylsalicylic acid?
irreversibly acetylares COX-1 and 2
What salicylate drug reversible inhibits COX 1 and 2 and is a metabolite of acetylsalicylic acid?
Salicylic acid
What is acetylsalicylic acid used for?
Antiplatelet
analgesic
antipyretic
What are side effects of acetylsalicylic acid?
GI irritation
Bleeding and anemia
hepatotoxicity
salicylate toxicity
What is the mechanism of action of the salicylate, diflunisal?
Reversibly inhibits COX1 and 2
What is diflunisal used for?
osteoarthritis
MSK strains/sprains
Pain after dental extraction
Postepisiotomy pain
What are the side effects of diflunisal?
Fewer GI side effects and less effect on platelets than aspirin
What class is acetaminophen in?
para-amino phenol
What is the mechanism of action of acetaminophen?
Reversibly inhibits COX-1 and 2
Used as an analgesic and antipyretic similar to aspirin, but has a weak anti-inflammatory effect?
Acetaminophen
What are the side effects of acetaminophen?
Renal tubular necrosis if chronically abused with other NSAIDs
Hepatic necrosis with overdose
What is the toxic intermediate of acetaminophen?
N-acetyl-benzoquinoneimine
What are the 2 indole drugs that reversibly inhibit COX 1 and 2 and are used to treat RA, ankylosing spondylitis, OA and acute gout?
Indomethacin
Sulindac
What are the side effects seen with the 2 indoles (indomethacin and sulindac)?
Thrombocytopenia
aplastic anemia
severe frontal HA
Nephrotoxicity in elderly or hypovolemic pts
What are the 4 propionic acid derivatives that reversibly inhibit COX 1 and 2 and are used to treat rheumatic disorders, OA, ankylosing spondylitis, postpartum pain, dysmenorrhea pain, and many types of surgeries?
Ibuprofen
Flurbiprofen
Naproxen
Oxaprozin
What are the side effects of the propionic acid derivatives? Ibuprofen Flurbiprofen Naproxen Oxaprozin
GI irritation
Hepatotoxicity
What has a longer t 1/2 than most propionic acid derivatives?
Naproxen (13 hrs)
What has a much longer t 1/2 than most propionic acid derivatives?
Oxaprozin (50hrs)
What class is piroxicam in?
Enolic acid
What is the mechanism of action of piroxicam?
Reversibly inhibits COX-1 and 2
What is piroxicam used for?
long-term treatment of RA or OA
Also ankylosing spondylitis, acute MSK disorders, acute gout
What are the two heteroaryl acetic acids that reversibly inhibit COX 1 and 2?
Ketorolac
Diclofenac
What are the uses of ketorolac?
Post-op pain
Inflammatory eye conditions
What are the uses of diclofenac?
Long-term treatment of RA or OA
Also ankylosing spondylitis and migraines
What are the 2 COX-2 inhibitors that have the same anti-inflammatory, antipyretic, and analgesic effects as NSAIDs, but have less GI toxicity?
Celocoxib
Etoricoxib
The 2 COX-2 inhibitors are contraindicated in patients with________.
Heart problems
Pregnancy
