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34 Cards in this Set
- Front
- Back
General mechanism of NSAIDs
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--inhibition of PG biosynthesis
--inhibits PG synthetase (cyclooxygenase) |
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Major differences between NSAID analgesics and narcotic analgesics
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(1) NSAIDs have much lower maximal effects than do opiods
(2) no addiction associated w/ NSAIDs (3) free of unwanted CNS effects of the opiods (4) treat low - moderate intensity pain |
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List general side effects of analgesic-antipyretic and anti-inflammatory agents.
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--GI ulceration, intolerance = most common!
--block platelet aggregation --inhibit uterine motility --analgesic abuse nephropathy --hypersensitivity |
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Which two side effects of nonselective COX inhibitors are NOT shared by selective COX-2 inhibitors?
a) inhibition of platelet function b) alteration in renal funciton c) inhibition of labor induction d) GI ulceration and intolerance |
These 2 COX-1 inhibitor side effects are NOT shared by COX-2 inhibitors..
(a) inhibition of platelet function (d) GI ulceration and intolerance The other side effects (renal function inhibition and labor induction inhibition) are common to both COX-1 and COX-2 inhibitors. |
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Aspirin
--mechanism --uses --contraindications |
Aspirin
Mechanism: irreversible acetylation of COX Uses: analgesic, antipyretic, anti-inflammatory (also juvenile RA, dec incidence of colon cancer & MI) Contraindications: ulcer, gout, asthma, flu |
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Aspirin
--side effects --signs of intoxication |
Aspirin
SE's: tinnitus, dec renal function, GI intolerance, hypersensitivity, hepatotoxicity Intoxication: respiratory alkalosis followed by metabolic acidosis, headache, mental confusion, ringing in ears |
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Diflunisal does not have which of the following effects:
(a) anti-pyretic (b) anti-inflammatory |
(a) anti-pyretic
Diflunisal has no anti-pyretic effect but has a greater anti-inflammatory potency compared to aspirin. |
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This NSAID is used to treat IBD.
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Mesalamine
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Of the following aspirin effects, which one is NOT shared by acetaminophen?
(a) anti-pyretic (b) anti-inflammatory (c) analgesic |
(b) anti-inflammatory
Acetaminophen is a weak anti-inflammatory drug. |
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Give this antidote within 10 hours of acetaminophen OD..
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N-acetylcysteine
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Acetaminophen can be metabolized to these 3 non-toxic metabolites
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(1) sulfate
(2) glucoronide (3) glutathione compound which is eventually converted to mercapturic acid |
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This severe adverse effect can result from acetaminophen OD.
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fatal hepatic necrosis
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TRUE or FALSE
Chronic alcoholism can increase the risk of acetaminophen toxicity. |
TRUE
Chronic alcoholism induces P-450 enzymes, which is the key player in forming a toxic metabolite that can cause hepatic necrosis. |
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Indomethacin
--uses --adverse effects --what drug inhibits indomethacin renal secretion? |
Indomethacin
--tx: acute gout, ankylosiing spondylitis, management of patent ductus arteriosus --adverse effects: GI, CNS severe frontal headache --probenecid inhibits renal secretion of indomethacin |
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Sulindac
--uses --rare complication |
Sulindac
--tx: RA, osteoarthritis, ankylosing spondylitis, acute gout suppress polyp formation in colon cancer Rare complication: renal stone |
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These 2 drugs can reduce the synthesis of both prostaglandins and leukotrienes.
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(1) diclofenac
(2) ketoprofen These drugs inhibit both lipooxygenase and cyclooxygenase enzymes. |
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This NSAID inhibits lipoxygenase and cycloxygenase and is not recommended for children, pregnant or nursing women.
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Diclofenac
(as a comparison, ketoprofen aslo inhibits lipoxygenase and cycloxygenase) |
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This NSAID can be used short-term for moderate - severe pain.
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Ketorolac
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TRUE or FALSE
Ibuprofen has a more potent analgesic effect compared to its anti-inflammatory effect. |
TRUE
Larger ibuprofen doses are needed to produce anti-inflammatory effects. |
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This NSAID is 20x more potent than aspirin and can cross the placenta.
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Naproxen
It is used to treat spondylitis, juvenile RA and acute gout. |
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Naproxen
--uses --potency --main route of elimination |
Naproxen
--tx: juvenile RA, acute gout, akylosing spondylitis --20x more potent than aspirin --handled mainly by kidneys |
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Name the 5 NSAIDs with (relatively) long half-lives.
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(1) naproxen -- 14hr
(2) meloxicam -- 20hr (3) nabumetone -- 24hr (4) oxaprozin -- 50hr (5) piroxicam -- 55hr |
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This NSAID is structurally distinct from other NSAIDs and has a long half life.
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Piroxicam
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This NSAID inhibits COX-2 over COX-1 and treats osteoarthritis.
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Meloxicam
(as a comparison, nabumetone also preferentially inhibits COX-2; nabumetone however is a non-acid NSAID and it is also a prodrug) |
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This is the only nonacid NSAID. It preferentially inhibits COX-2 at low dose, but it is not purely selective.
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Nabumetone
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This drug is a COX-2 selective inhibitor that is approved for osteoarthritis and RA.
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Celecoxib
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List the 3 TNF-alpha blocking agents.
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(1) etanercept
(2) adalimumab (3) infliximab |
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Inhibition of lipoxygenase prevents the formation of this molecule.
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leukotrienes
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The inducible COX-2 enzyme is involved in the formation of this molecule.
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prostaglandins
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The housekeeping COX-1 enzyme is involved in the formation of these 2 molecules.
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COX-1 involved in formation of:
(1) prostaglandins (2) thromboxane |
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Name the specific NSAID that would treat each of the following..
(1) short term moderate - severe pain (2) IBD (3) management of patent ductus arteriosus (4) suppression of polyp formation in colon cancer (5) RA without effect on prothrombin time |
(1) moderate-severe pain: ketorolac
(2) IBD: mesalamine (3) patent DA: indomethacin (4) suppress polyp formation: sulindac (5) no effect on prothrombin time: celecoxib |
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Why is adminstering N-acetylcysteine appropriate in the case of acetaminophen overdose?
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In the case of acetaminophen OD, metabolism by conjugation becomes saturated, and the drug is oxidatively metabolized by the CYP enzymes into a toxic metabolite.
N-acetylcysteine is a precursor of glutathione and as such, increases glutathione conjugation of the toxic intermediate. Thus, the toxic intermediate is converted to a glutathione-containing compound rather than a toxic adduct that causes hepatocyte apoptosis and/or liver necrosis. |
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Which 2 NSAIDs and which anti-rheumatic drug would be appropriate for treatment of juvenile RA?
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Used to treat juvenile RA:
--aspirin --naproxen --abatacept |
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Which NSAIDs would be appropriate for treatment of ankylosing spondylitis?
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Used to treat ankylosing spondylitis..
--indomethacin --sulindac --naproxen |