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42 Cards in this Set

  • Front
  • Back
advantages and disadvantages of celecoxib, rofecoxib, valdecoxib?
(COX 2 selective)
Less GI effects
Increased risk of MI and stroke
difference between aspirin and other NSAIDs?
aspirin is irreversible, longer duration of antiplatelet effect
MOA of NSAIDs?
inhibit cyclooxygenase which converts arachidonic acid into prostaglandins (inflammation)
What cells express cox 1 and cox 2?
cox 1: noninflammatory cells

cox 2: activated lymphocytes, pmns, other inflammatory cells
antipyretic effect of NSAIDs?
inhibits prostaglandin synthesis in CNS that is stimulated by pyrogens
MOA of typical NSAIDs
inhibit COX1/2 which suppresses PG synthesis (antipyretic and inhibition of peripheral pain sensors)
effects of dose ranges of aspirin?
<300mg/d: antiplt

300-2400mg/d: antipyretic and analgesic

2400-4000mg/d: anti-inflammatory
indications for non-aspirin NSAIDs?
moderate pain, esp MS inflammation from arthritis, gout
long term use of NSAIDs is associated with what?
reduced risk of colon cancer
toxic effects of aspirin
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
what is Reye's syndrome?
rare syndrome of rapid liver degeneration and encephalopathy in children with viral infxn who are tx with aspirin
toxic effects of nonselective NSAIDs
GI upset
renal damage
which NSAID is associated with serious hematologic reactions?
indomethacin
MOA of acetaminophen
unclear -- but weak COX1&2 inhibitor in peripheral tissues, may inhibit COX3 in CNS

no anti-inflammatory effect
indications for acetaminophen?
fever, pain
DOC for children with viral infection?
Acetaminophen (to avoid Reye's)
toxic effects of acetaminophen?
in OD and alcoholics, hepatotoxicity

(oxidation by phase I P450 enzymes when phase II enzymes are lacking leads to buildup of toxic metabolite)
DOC for acetaminophen OD?
acetylcysteine
MOA of methotrexate
reduces number of immune cells available to maintain inflammatory response in RA
DMARDs that interfere with T-cell activity?
sulfasalazine, hydroxychloroquine, cyclosporine, leflunomide, mycophenolate mofetil, abatacept
DMARDs that interfere with B cell activity?
rituximab
DMARDs that inhibit TNF-alpha?
infliximab, adalimumab, etanercept
MOA of colchicine?
selective inhib of microtubule assembly, reduces leukocyte migration and phagocytosis

inhib leukotriene B4 synthesis

decr free radical formation
anti-inflammatory drugs used for gout?
potent NSAIDs (indomethacin)
Colchicine
DOC for acute gouty arthritis?
indomethacin or glucocorticoid
toxicity of indomethacin?
bone marrow suppression, renal damage
drugs used in gout?
anti-inflammatory drugs
uricosuric drugs
xanthine oxidase inhibitors
uricosuric agents?
probenecid, sulfinpyrazone
MOA of probenecid?
increase uric acid excretion by competing with uric acid for reabs by transporters in PCT
uses of uricosuric agents?
chronic gout

used to inhibit secretion of penicillins, methotrexate
main side effect of uricosuric drugs?
can precipitate acute gout attack during early phase of action (avoid by also giving colchicine or indomethacin)
MOA of allopurinol?
irreversible suicide inhibitor of xanthine oxidase
(converts hypoxanthine to xanthine to uric acid)
MOA of febuxostat?
non-purine inhibitor of xanthine oxidase, more selective than allopurinol/alloxanthine
use of xanthine oxidase inhibitors?
given orally in tx of chronic gout, also used as adjunct to cancer chemotherapy (uric acid released in death of neoplastic cells)
toxic effects of xanthine oxidase inhibitors?
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
NSAID that is relatively safe, inexpensive, moderate effectiveness, 2 h half life?
ibuprofen
NSAID with moderate effectiveness, but long half-life?
naproxen
strong NSAID with greater anti-inflammatory effectiveness and greater toxic effects
indomethacin
parenteral NSAID with greater analgesic effectiveness
ketorolac
pts with nasal polyps are predisposed what effect of NSAIDs?
aspirin hypersensitivity asthma
DMARDs also used in IBD?
sulfasalazine, anti TNF drugs (infliximab, etanercept, adalimumab)
DMARDs also used as antimalarial?
hydroxychloroquine