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45 Cards in this Set

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NSAIDS
what does cyclooxygenase produce, and from what?
arachadonic acid --> PGH2 (which can be converted to other prostaglandins)
what does arachadonic acid come from?
clel membrane phospholipids
what do prostaglandins made by COX do in the stomach (2)?
1) decrease cAMP and decrease K/H ATPase in parietal cells; 2) stimulate secretion of mucous HCO3- from epithelial cells
what therapy relates to thromboxane A2 and how does it work?
aspirin blocks thromboxane A2 and prevents platelet aggregation
will nonspecific COX inhibitors be effective in treating asthma, and why?
no, because PGF and PGD constrict / PGEs relax bronchial/tracheal muscles
what do PGs do to the CV system?
increase cardiac output, vasodilate (hypotensive)), PGD2 vasoconstricts
what type of pain are salicylates (aspirin, salicylic acid, methyl salicylate) good for?
integument, not visceral
what are salicylates contraindicated in (4)?
1) hemophilia; 2) vit K deficiency; 3) hepatic damage; 4) hypoprothrombinemia (congenital or acquired disorder where factor II (prothrombin) is deficient - this can result from vitamin K deficiency
what are the metabolic effects of salicylate?
hyperglycemia, glycosuria, increase O2 consumption, CO2 production, and metabolic rate, reduce serum triglycerides, increase fat burning, decrease lipogenesis
what are endocrine effects of salicylates (2)?
increae glucocorticoid secretion, decrease thyroid function
what are the effects of salicylates on pregnancy?
decrease birth weight, increase perinatal mortality, anema, and postpartum hemorrhage
what cancer is aspirin helpful with?
colorectal
what are additional contraindications of aspirin?
1) viral infections like flu, chickenpox (Reye's syndrome); 2) peptic ulcers
what effects do very low (1mg/kg), low (10mg/kg); and high (100mg/kg) doses of aspirin have?
very low - antiplatelet; low - analgesic/antipyretic; high - anti-inflammatory
what are three AEs of aspirin?
tinnitus, vertigo, deafness
what happens in aspirin overdose (2) and what results from each?
1) hyperventilation --> respiratory alkalosis; 2) salicylate --> fever, dehydration, and metabolic acidosis
how does aspirin overdose culminate?
shock, coma, organ system failure, death
what is the treatment for aspirin overdose?
1) induce vomiting/lavage; 2) give fluids and electrolytes to support renal function; 3) administer sodium bicarbonate to counter metabolic acidosis and increase urinary clearance
why is acetaminophen not an NSAID?
no antiinflammatory activity
what does it do, and when is it used?
functions only centrally - antipyretic / analgesic (no alteration on bleeding time, uric acid, acid/base)
what can acetaminophen OD cause?
fatal hepatic necrosis
what NSAID is useful for gout, and what class is it a part of?
indomethacin - an acetic acid
what is another acetic acid with limited toxicity and selectivity for COX2?
etodolac
what are fenamates and why are they not used much?
no advantage in anti-inflammatory activity, but cause diarrhea - mefanamic acid, meclofenamic acid
what NSAID was said to have little difference in therapeutic efficacy compared to aspirin, but is better tolerated?
tolmetin
what drug is an effective analgesic, but a poor anti-inflammatory, that can be administered many ways (IM, IV, oral, and also topically for conjunctivitis) and is limited to short term use?
ketorolac
what NSAID is approved for long term treatment of RA, osteoarthritis, and ankylosing spondylitis?
diclofenac
what class of drugs are all anti-inflammatory, analgesic, and antipyretic, and are better tolerated than aspirin and indomethacin?
propionic acids (ibuprofen, naproxen, fenoprofen, ketoprofin, flurbiprofen)
in what case is ibuprofen used, and what is it effective for?
in patients with history of GI intolerance to other NSAIDs - effective analgesic and anti-inflammatory
what what type of toxicity does naproxen have, similar frequency to indomethacin?
GI, CNS (but naproxen better tolerated, generally)
what drug is an effective antiinflammatory agent, but poorly inhibits COX in seminal vesicles, where COX1 is the only type?
nimesulide
what problem occurs with vioxx?
HA, stroke
what additional program (besides HA, stroke, DVT) occurs with bextra?
severe skin reactions
what NSAID suppresed breast tumors in human breast cancer cells, and why?
piroxicam, since human cancer cells expres high levels of COX-2
what drugs reduce the size/number of colorectal polyps in animal models?
aspirin, COX-2 inhibitors
what is the MOA of aspirin?
suicide inhibitor of COX-1 (thromboxane A2)
what drug closes the ductus arteriosus in premature neonates?
indomethacin
what drug is a first generation selective COX 2 inhibitor that is used for RA and osteoarthritis?
celecoxib (celebrex)
what things was it said ibuprofen is useful for (3)?
1) RA; 2) dysmenorrhea; 3) gout; 4) ankylosing spnodylitis
what toxicity does it have, and how well tolerated is it?
gastrix toxicity, but is tolerated as well as any nonselective COX inhibitor
what is achieved at lower doses with ibuprofen - inflammatory or analgesic effects?
analgesic effects achieved at lower doses
what is an early COX inhibitor used for rheumatoid and osteoarthritis?
indomethacin
what is a second generation COX inhibitor that is used for osteo and rheumatoid arthritis, migraine, and fever, with gastric complications and pediatric use?
naproxen