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48 Cards in this Set

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What are NSAIDs used for?
Pain, fever, inflammation
How do NSAIDs work?
inhibing activity of COX enzymes by preventing the binding site of arachionic acid substrate
Where is COX1 found?
Ubiguitous in all tissues
Where are COX2 found?
in brain, kidny, bone, overies, uterus, and sm intestine
Where can COX2 be induced?
in MGs, monogutes, synoviocytes, chondrocytes, fibroblasts, osteoblasts, endothelial cells
What do PGEs do in inflammation?
dilate blood vessels and increase blood flow--heat and redness, induce migration of phagocytes, vascular permeability
What do PGEs do in pain?
lower threshold to painful stimuli, enhacing depolarization of secondary sensory neurons, recruit leukocytes
What do PGEs do in fever?
PGE in hypothalamus act on OVLT and cause fever
What do PGEs do in the stomach?
inhibit production of gastric acid, increase the production of gastric bicarb, increase production of gastric mucous, causes vasodilation and inc gastric blood flow
How do platelets cause vasoconstriction and promote platelet aggregation and activation?
TXA2 is produced by COX1
What do endothelial cells produce?
PGI2 which is a vasodilator and inhibits platelet aggregation
What do PGEs do in the kidney?
vasodilation, prevent renal ischemia, inc GFR, inc water and salt secretion
Why aren't NSAIDs used in pregnant women?
PGEs stimulate uterine contraction, if PGEs were inhibited, it could delay parturition
Why are neonates given NSAIDs to close a ductus arteriosus?
NSAIDs block PGEs which keep the foramen open
Why might NSAIDs be tumor inhibiting?
PGEs promot neovascularization
What is the MOA of ASA?
ASA acetylates COX1 within its binding site and arachidonic substrate can't bind
Why is ASA less effective on COX2?
Because it has a larger binding site and can still accomodate arachidonic acid
What is Salsalate?
a salicylate, which is converted to salicylic acid after absorption
What is salsalate used for?
mild to moderate pain, fever, inflammation
What is Diflunisal? What does it do?
NSAID, a potent anti-inflammatory, doesn't cross BBB
Which NSAID isn't an anti-pyretic?
Diflunisal
What dose of ASA increases uric acid secretion?
high doses
What causes gastric damage?
direct damage from acid, inhibition of COX1 PGEs causing gastric acid and digestive enzymes
Which drug can be given with NSAIDs to lessen the gastric symptoms?
Misoprostol
What are the hypersensitive symptoms associated with NSAID therapy?
ocular and nasal congestion, urticaria, angioneurotic edema, severe airway obstruction, rarely anaphylactic shock
What is Reye's Syndrome?
fata liver degenerative disease, associated iwth administration of ASA given during febrile viral infection in young children
What are the signs of salicylate toxicity?
tinnitus, vertigo, hyperventilation, mental confusion, metabolic acidosis, dehydration, hyperthermia, convulsions, renal failure
What is low dose ibuprofen used for?
analgesic
What is high dose ibuprofen used for?
anti-inflammation
What is indication for Naproxen?
20X more potent than ASA
What are the indications for Indomethacin?
NSAID used for fever reduction, acute gouty arthritis and OA, patent ductus arteriosus
What is oxaproxin?
NSAID
What is sulindac?
NSAID
What is diclofenac?
more potent anti-inflammatory than indomethacin and naproxen
What is keterolac?
IV analgesic for moderate severe post surgical pain
What is tolmetin?
NSAID ineffective of gout
What is prioxicam?
NSAID, inc incidence of peptic ulcer and bleeding
What is Meloxicam (mobic)?
Preferentially inhibits COX2
What is nabumetone?
Expensive NSAID
What are the GI disturbances of NSAIDs?
reduction in production of cytoprotective PGE
What do NSAIDs do to the kidney?
dec renal blood flow, inc hypertension, risk of renal failure with pts on ACE inhib and diuretics
What can NSAIDs do to CNS?
headaches, tinnitus, anziety, drowsiness, confusion
What can cause photosensitivity?
ibuprofen, ketoprofen, naproxen, ketorolac, piroxicam, diclofenac
What are the rare side effects of NSAIDs?
heart failure, hemolytic anemia, and aplastic anemia
Which NSAIDs raise liver enzymes?
sulindac and diclofenac
What were the three selective COX2 inhibitors?
celecoxib, rofecoxib, valdecoxib
What are COX2 inhibitor used for?
RA and OA
Why is ASA contraindication in gout?
it inhibits the elimination of uric acid by the kidney