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86 Cards in this Set

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  • Back
these two NSAIDs have moderate anti-inflammatory effectiveness
Ibuprofen and Naproxen
this NSAID has greater anti-inflammatory effectiveness than ibuprofen and naproxen?
Indomethacin
this NSAID has greater analgesic effectiveness?
Ketorolac
2 NSAIDs that are in the subgroup of selective COX2 inhibitors
Celecoxib and Rofecoxib
COX1 is primarily expressed on this cell type
non-inflammatory
COX2 is expressed on these cells?
activated lymphocytes, polymorphonuclear cells, and other inflammatory cells
what is the action of COX?
cyclooxygenase is the enzyme at the head of the enzymatic pathway for prostaglandin synthesis
define DMARDs and what htey are used for?
Disease-modifying antirheumatic drugs, aka SAARDs (slow-acitng antirheumatic drugs). diverse drugs that modify the inflammatory processes underlying rheumatic disease; slow onset (weeks to months) for clinical effects
what is Reye's syndrome?
a rare syndrome of rapid liver degeneration and encephalitis in children treated with aspirin during viral infection
name drugs in the class of uricosuric agents?
prodenecid and sulfinpyrazone (increases renal excretion of uric acid)
what enzyme metabolizes uric acid and what drug inhibits this enzyme?
Xanthine oxidase (inhibited by Allopurinol)
aspirin and the older non-selective NSAIDs inhibit both COX isoforms, what is the effect of this?
decreases prostaglandin and thromboxane synthesis throughout the body (homestatic prostaglandins AND inflammatory prostaglandins)
name two NSAIDs that have less effect on homeostatic prostaglandins?
Celecoxib and Rofecoxib (selective for COX-2)
what is the major difference between the MOA of aspirin and the other NSAIDs?
Aspirin acetylates and thereby IRREVERSIBLY inhibits COX, other NSAIDS have reversible inhibition
the irreversible action of aspirin results in longer duration of this effect?
antiplatelet
prostaglandin synthesis in the CNS that is stimulated by pyrogens is suppressed by NSAIDs, resulting in this effect?
reduction of fever
aspirin dose of less than 300mg/day is used for this?
reducing platelet aggregation
aspirin doses of 300 to 2400mg/day is used for this?
antipyretic and analgesic effects
aspirin doses of 2400 to 4000mg/day is used for this?
anti-inflammatory effect
salicylate is a _____(reversible or irreversible) nonselective inhibitor of COX
REVERSIBLE
elimination of salicylate is ___order
FIRST
how does salicylate leave the body?
excreted via KIDNEYS
COX-2 inhibitors are primarily used in these types of disorders?
inflammatory
this NSAID is used mainly as a SYSTEMIC ANALGESIC, NOT an ANTI-INFLAMMATORY?
Ketorolac
what is the only NSAID that is available in a PARENTERAL formulation?
Ketorolac
nonselective NSAIDs and COX-2 selective drugs have this effect in pts with primary familial adenomatous polyposis?
reduction in polyp formation
long term use of NSAIDs has this effect on colon cancer risk?
reduces the risk
chronic use of aspirin can have these negative effects?
gastric ulceration, upper GI bleeding, renal effects, including acute failure and interstitial nephritis
aspirin has this effect on bleeding time?
increases it
key clinical finding in aspirin hypersensitivity
nasal polyps (may experience asthma from increased synthesis of leukotrienes as well)
side effects of higher dose aspirin regimens?
tinnitus, vertigo, hyperventilation, and respiratory alkalosis
children with viral infections are at increased risk for developing this syndrome if given aspirin?
Reye's (hepatic fatty degeneration and encephalopathy)
there is risk of damage to this organ with any of the NSAIDs?
kidney (especially in pts with preexisitng renal disease)
this older NSAID should not be used chronically because it causes aplastic anemia & agranulocytosis?
Phenylbutazone
the selective COX-2 inhibitors may have a reduced risk of GI effects?
Celecoxib, Rofecoxib, and Valdecoxib
this type of NSAID does not have antiplatelet effects and are therefore NOT cardioprotective?
Selective COX-2 inhibitors (Celecoxib, Rofecoxib, and Valdecoxib)
this NSAID is a sulfonamide and thus may cause hypersensitivity rxn in pts with sulfa allergy?
Celecoxib
these agents are called diseases modifying drugs because some evidence shows slowing or even reversal of joint damage, an effect NEVER seen with NSAIDs?
DMARDS
how long does it take for the effects of DMARDS to be evident?
6 weeks to 6 months (thus also called SAARDS for slow acting effects)
what anti-inflammatory drugs are intermediate between NSAIDS and DMARDS?
Corticosteroids
this class of drugs probably act by reducing the numbers of immune cells available to maintain the inflammatory response?
cytotoxic drugs (eg Methotrexate)
which component of Sulfasalazine is more important as an antirheumatic?
Sulfapyridine moiety.... (conversely 5-aminosalicylic acid component more imp. for Ulcerative colitis)
this drug may interfere with T lymphocyte activity, decrease leukocyte chemotaxis, stabilize lysosomal membranes, interfere with DNA & RNA synthesis and trap free radicals?
Hydroxychloroquine
what drug has similar anti-inflammatory effect as Hydroxychloroquine?
Penicillamine
this compound alters the activity of macrophages that play a central role in the inflammation of arthritis, and also suppresses the phagocytic activity of PMLs?
Organic Gold Compounds
this prodrug is rapidly metabolized to a compound that inhibits Dihydroorotate dehydrogenase, an enzyme required by activated lymphocytes for synthesis of pyrimidines that are needed for RNA synthesis?
Leflunomide (inhibition of the enzyme results in cell cycle arrest in lymphocytes)
Rheumatoid drug associated with these toxicities: rash, GI distubance, dizziness, headache and leukopenia?
Sulfasalazine
Rheumatoid drug associated with these toxicities: rash, GI disturbance, OTOTOXICITY, MYOPATHY, PERIPHERAL NEUROPATHY?
Hydroxychloroquine
Rheumatoid drug associated with these toxcities: Nausea, MUCOSAL ULCERS, hematotoxicity, TERATOGENICITY
Methotrexate
Rheumatoid drug associated with these toxicities: NEPHROTOXICITY, HYPERTENSION, peripheral neuropathy?
Cyclosporine
Rheumatoid drug associated with these toxicities: upper RESPIRATORY INFECTION, activation of latent TB?
Infliximab
Rheumatoid drug associated with these toxicities: INJECTION SITE REACTIONS?
Etanercept
Rheumatoid drug associated with these toxicities: TERATOGEN, HEPATOTOXICITY, GI disturbance, skin reactions
Leflunomide
Rheumatoid drug associated with these toxicities: diarrhea, dermatitis, HEMATOLOGIC abnormalities (APLASTIC ANEMIA)?
Gold compounds
Rheumatoid drug associated with these toxicities: PROTEINURIA, dermatitis, GI disturbance, APLASTIC ANEMIA (and other hematologic abnormalities)
Penicillamine
drug that is a chelating agent?
Penicillamine
two Anti-rheumatoid drugs that can be used in inflammatory bowel disease?
Sulfasalazine and Infliximab
anti-Rheumatoid drug that is also used as an Antimalarial?
Hydroxychloroquine
anti-Rheumatoid drug that is also an anti-Cancer agent?
Methotrexate
anti-Rheumatoid drug that is also used in tissue transplantation?
Cyclosporine
these drugs bind to and prevent the action of TNF-a, a cytokine key in chronic inflammation?
Infliximab and Adalimumab (Monoclonal antibodies)
drug that is a recominant fusion protein comprising 2 TNF receptors linked to immunoglobulin, thus acting as a "decoy" decreasing cellular actions of TNF-a?
Etanercept
what is the only OTC NON-anti-inflammatory analgesic commonly available in the US?
Acetaminophen
this drug is an analgesic and antipyretic agent LACKING ANTI-INFLAMMATORY or ANTI-PLATELET effects?
Acetaminophen
drug useful as an aspirin replacement in virus infected children?
Acetaminophen
analgesic drug that is metabolized in the liver and thus is unaffected by renal disease?
Acetaminophen
antidote to Acetaminophen overdose?
Acetylcysteine, a sulfhydryl donor
this group of people is at risk for acetaminophen induced hepatotoxicity?
people who consume 3 or more ALCOHOLIC drinks per day
this potent NSAID is effective in inhibiting the inflammation of acute gouty arthritis?
Indomethacin
drug that is a selective inhibitor of microtubule assembly, reduces leukocyte migration and phagocytosis, and may reduce produciton of leukotriene B4 and dec. free radical formation?
Colchicine
in addition to gouty use Colchicine can be used for this condition?
Mediterranean fever (disease of unknown cause characterized by fever, hepatitis, peritonitis, pleuritis, arthritis, and amyloidosis (occassionally))
toxicity of Indomethacin?
renal damage or bone marrow depression
short courses of this drug can cause BEHAVIORAL changes and IMPAIRED GLUCOSE CONTROL?
Glucocorticoids
these agents are weak acids that compete with uric acid for reabsorption by the weak acid transport mechanism in the PCT of the kidney?
Uricosuric agents
Uricosuric drugs inhibit a large # of other weak acids such as___ and ___ in addition to inhibiting reabsorption of uric acid?
Penicillin and Methotrexate
chronic Gout is treated with one of these agents?
Uricosuric OR Allopurinol
can Uricosurics or Allopurinol be used in an acute Gouty attack?
NO! and they are best withheld for 1 to 2 weeks after an acute gouty episode
this class of drugs may actually PRECIPITATE a gouty attack during the early phase of their action?
Uricosuric agents (avoided by simulatneous admin. of Colchicine or Indomethacin)
these gout drugs are sulfonamides, so may share allergenicity of other classes of sulfonamide drugs?
Uricosuric drugs
this drug is converted to Oxypurinol (alloxanthine) by Xanthine oxidase?
Allopurinol
what enzyme converts Hypoxanthine to Xanthine and Xanthine to Uric Acid?
Xanthine Oxidase
this drugs is an irreversible suicide inhibitor of Xanthine oxidase?
Allopurinol (and oxipurinol)
what is the result of inhibition of Xanthine oxidase?
inc. conc. of more soluble Hypoxanthine and Xanthine and dec. conc or less soluble Uric Acid
why is Allopurinol used as an adjunct in chemo?
it slows the formation of Uric Acid from Purines released by the death of large #'s of neoplastic cells
like Uricosuric drugs this drug can precipitate acute attacks of gout in the early phase of treatment?
Allopurinol
Allopurinol inhibits the metabolism of these two drugs that depend on Xanthine oxidase for elimination?
Mercaptopurine and Azathioprine