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42 Cards in this Set
- Front
- Back
advantages and disadvantages of celecoxib, rofecoxib, valdecoxib?
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(COX 2 selective)
Less GI effects Increased risk of MI and stroke |
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difference between aspirin and other NSAIDs?
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aspirin is irreversible, longer duration of antiplatelet effect
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MOA of NSAIDs?
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inhibit cyclooxygenase which converts arachidonic acid into prostaglandins (inflammation)
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What cells express cox 1 and cox 2?
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cox 1: noninflammatory cells
cox 2: activated lymphocytes, pmns, other inflammatory cells |
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antipyretic effect of NSAIDs?
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inhibits prostaglandin synthesis in CNS that is stimulated by pyrogens
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MOA of typical NSAIDs
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inhibit COX1/2 which suppresses PG synthesis (antipyretic and inhibition of peripheral pain sensors)
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effects of dose ranges of aspirin?
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<300mg/d: antiplt
300-2400mg/d: antipyretic and analgesic 2400-4000mg/d: anti-inflammatory |
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indications for non-aspirin NSAIDs?
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moderate pain, esp MS inflammation from arthritis, gout
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long term use of NSAIDs is associated with what?
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reduced risk of colon cancer
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toxic effects of aspirin
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GI upset
upper GI bleeding acute renal flr, interstitial nephritis inc PT/PTT asthma (in hypersensitive pts) Reye's syndrome (children) high dose: tinnitus, vertigo, hyperventilation, resp alkalosis. very high dose: met acidosis, dehydration, hyperthermia, collapse, coma, death |
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what is Reye's syndrome?
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rare syndrome of rapid liver degeneration and encephalopathy in children with viral infxn who are tx with aspirin
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toxic effects of nonselective NSAIDs
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GI upset
renal damage |
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which NSAID is associated with serious hematologic reactions?
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indomethacin
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MOA of acetaminophen
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unclear -- but weak COX1&2 inhibitor in peripheral tissues, may inhibit COX3 in CNS
no anti-inflammatory effect |
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indications for acetaminophen?
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fever, pain
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DOC for children with viral infection?
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Acetaminophen (to avoid Reye's)
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toxic effects of acetaminophen?
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in OD and alcoholics, hepatotoxicity
(oxidation by phase I P450 enzymes when phase II enzymes are lacking leads to buildup of toxic metabolite) |
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DOC for acetaminophen OD?
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acetylcysteine
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MOA of methotrexate
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reduces number of immune cells available to maintain inflammatory response in RA
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DMARDs that interfere with T-cell activity?
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sulfasalazine, hydroxychloroquine, cyclosporine, leflunomide, mycophenolate mofetil, abatacept
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DMARDs that interfere with B cell activity?
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rituximab
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DMARDs that inhibit TNF-alpha?
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infliximab, adalimumab, etanercept
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MOA of colchicine?
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selective inhib of microtubule assembly, reduces leukocyte migration and phagocytosis
inhib leukotriene B4 synthesis decr free radical formation |
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anti-inflammatory drugs used for gout?
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potent NSAIDs (indomethacin)
Colchicine |
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DOC for acute gouty arthritis?
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indomethacin or glucocorticoid
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toxicity of indomethacin?
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bone marrow suppression, renal damage
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drugs used in gout?
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anti-inflammatory drugs
uricosuric drugs xanthine oxidase inhibitors |
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uricosuric agents?
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probenecid, sulfinpyrazone
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MOA of probenecid?
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increase uric acid excretion by competing with uric acid for reabs by transporters in PCT
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uses of uricosuric agents?
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chronic gout
used to inhibit secretion of penicillins, methotrexate |
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main side effect of uricosuric drugs?
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can precipitate acute gout attack during early phase of action (avoid by also giving colchicine or indomethacin)
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MOA of allopurinol?
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irreversible suicide inhibitor of xanthine oxidase
(converts hypoxanthine to xanthine to uric acid) |
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MOA of febuxostat?
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non-purine inhibitor of xanthine oxidase, more selective than allopurinol/alloxanthine
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use of xanthine oxidase inhibitors?
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given orally in tx of chronic gout, also used as adjunct to cancer chemotherapy (uric acid released in death of neoplastic cells)
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toxic effects of xanthine oxidase inhibitors?
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can precipitate acute gout attack (dose with colchicine or NSAID to avoid), GI upset
Allopurinol: rash, periph neuritis/vasculitis/BM dysfxn (rare), inhibits metab of mercaptopurine and azathioprine Febuxostat: abnml liver fxn, HA |
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NSAID that is relatively safe, inexpensive, moderate effectiveness, 2 h half life?
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ibuprofen
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NSAID with moderate effectiveness, but long half-life?
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naproxen
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strong NSAID with greater anti-inflammatory effectiveness and greater toxic effects
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indomethacin
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parenteral NSAID with greater analgesic effectiveness
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ketorolac
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pts with nasal polyps are predisposed what effect of NSAIDs?
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aspirin hypersensitivity asthma
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DMARDs also used in IBD?
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sulfasalazine, anti TNF drugs (infliximab, etanercept, adalimumab)
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DMARDs also used as antimalarial?
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hydroxychloroquine
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