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