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NSAIDs II
cmbm exam IV
51
Chemistry
Graduate
01/31/2010

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Term
what are the two propionic acid derivative NSAIDs?
Definition
ibuprofen and naproxen
Term
what are the 4 As of ibuprofen? how is it different than asa?
Definition
analgesic, antiinflammatory, antipyretic, antiplatelet (reversible - different than ASA, effect is lost within 1-2 days therefore not normally used for this effect)
Term
what are the indications for ibuprofen?
Definition
same as asa: pain, inflammation, fever, (pyrogen-induced and CNS response)
Term
what is the M/A of ibuprofen?
Definition
competetive inhibition of COX
Term
does it have high blood plasma binding? does it interact with oral hypoglycemics/anticoagulants?
Definition
yes, 99%. it does not interact with oral hypoglycemics/anticoagulants <- WITH RESPECT TO BINDING
Term
what are side effects of ibupofen?
Definition
GI, nausea/heartburn, some intestinal erosions, not as much occult blood loss, but some ocular disturbances/skin rashes/headache
Term
what are the effects of naproxen? how is it used?
Definition
same as ibuprofen: analgesic, antiinflammatory, antipyretic, antiplatelet (reversible - different than ASA, effect is lost within 1-2 days therefore not normally used for this effect). it is indicated for the same symptoms as well: analgesic, antiinflammatory, antipyretic, antiplatelet (reversible - different than ASA, effect is lost within 1-2 days therefore not normally used for this effect)
Term
what is the mechanism of naproxen?
Definition
competetive COX inhibitor, inhibits hydrolytic enzymes of lysosomal system, and inhibits migration of PMN leukocytes.
Term
how much does naproxen bind to blood plasma protein? interactions with
Definition
high plasma protein binding: 99% it does not interact with oral hypoglycemics/anticoagulants <- WITH RESPECT TO BINDING
Term
what are some side effect with naproxen?
Definition
less occult blood loss than asa, drowsiness, vertigo, headache, fatigue, ototoxicity, GI disturbance (emesis, dyspepsia, bleeding), pruritis
Term
what are the heteroaryl acetic acids?
Definition
ketorolac (toradol), tolectin (tolectin), diclofenac (voltaren)
Term
what does ketorolac (toradol) do?
Definition
it is an analgesic, antiinflammatory, antipyretic, which also prolongs bleeding time (antiplatelet) reversible 24-48 hr)
Term
what is ketorolac used for/how is it adminstered?
Definition
short term pain relief via IM injection most commonly
Term
what is the M/A for ketorolac? how well does it bind plasma protein? any interaction with other drugs?
Definition
highly potent COX inhibitor. it binds 99% of plasma protein and has little if any interaction with other drugs
Term
what are some side effects of ketorolac?
Definition
nausea, dyspepsia, GI pain (can become gastric-erosive w/long term), drowsiness
Term
what are some contraindications for ketorolac?
Definition
it has additive side effects with other NSAIDs (synergistic - more GI complaints). ketorolac is contraindicated w/partial or complete syndromw of nasal polyps, angioedema and bronchospasm. also contraindicated with previously hypersensitivity to ketorolac.
Term
what are the effects of tolmetin (tolectin)?
Definition
same 4 As: analgesic, antiinflammatory, antipyretic, prolongs bleeding time, and less occult blood than asa (less GI disturbance and less platelet interaction)
Term
what is tolmetin used for?
Definition
RA and osteoarthritis ONLY
Term
what is the M/A for tolmetin? what is its plasma protein binding? does it compete with other drugs for binding?
Definition
competitive COX inhibitor. 99% plasma protein binding and it does not interact with oral hypoglycemics/anticoagulants <- WITH RESPECT TO BINDING
Term
what are side effects for tolmetin? do many people experience them?
Definition
25-40% of people experience epigastric pain, nausea/vomiting, gastric/duodenal ulceration, CNS effects (tinnitus, nervouseness, anxiety, drowsiness). 5-10% discontinue.
Term
what does diclofenac (voltaren) do?
Definition
it is an analgesis, antiinflammatory and antipyretic
Term
what is diclofenac prescribed for?
Definition
*long term management of RA, osteoarthritis and ankylosing spondylitis. also has been used for post op pain, bursitis, and acute musculoskeletal injury
Term
what is the M/A for diclofenac?
Definition
it is a competetive COX inhibitor. it also reduces intracellular concentrations of free arachindonate in leukocytes
Term
what is diclofenac's protein binding? does it compete with any other drugs? is it subject to first pass effect?
Definition
it is 99% plasma protein bound, with minimal competetion with warfarin (if someone is on this and anticoagulant, they need to initially have their levels measured more than once per month). it has a 50% first pass effect
Term
what are side-effects associated with diclofenac?
Definition
20% of pts experience epigastric pain/nausea/emesis/gastric ulceration, CNS effects: tinnitus, nervousness, anxiety, drowsiness, and skin rashes/allergies.
Term
what are the 2 enolic acids?
Definition
piroxicam (feldene) and phenylbutazone (butazolidin)
Term
what does piroxicam (feldene) do?
Definition
4 As (equivalent to asa, indomethacin or naproxen, but much better tolerated)
Term
what is piroxicam used for?
Definition
osteoarthritis, RA, acute gout
Term
what is the M/A of piroxicam?
Definition
it is a potent COX inhibitor that also inhibits activation of neutrophils and hemostasis
Term
how does piroxicam bind to plasma protein? does it compete with other drugs?
Definition
piroxicam binds 99 to plasma protein that may compete with warfarin and has enterohepatic recycling
Term
do pts on piroxicam experience side effects?
Definition
11-46% experience GI symptoms, along with a 1% incidence of peptide ulcers. 4-12% discontinue
Term
what does phenylbutazone do?
Definition
analgesic (though inferior to asa for non-rheumatic pain), antiinflammatory (most prominent) antipyretic, very toxic and uricosuric similar to asa (helps with excretion of uric acid)
Term
what is phenylbutazone used for?
Definition
acute gout and RA (infrequently these days due to toxicities)
Term
what is the mechanism of phenylbutazone? how well does it bind plasma protein? does it compete with other drugs for plasma protein binding?
Definition
it is a COX inhibitor. it binds plasma protein 98% and competes with other NSAIDs, warfarin, oral hypoglycemic, and sulfonamides
Term
what are the side effects of phenylbutazone?
Definition
10-45% of pts commonly experience epigastric pain, nausea, emesis and skin rashes. gastric ulceration, CNS effects (vertigo, insomnia, euphoria, nervousness), nephritis, hepatitis, aplastic anemia, agranulocytosis can also occur. 10-15% discontinue
Term
what are contraindications for phenylbutazone?
Definition
phenylbutazone is contraindicated for pts w/ cardiac, hepatic or renal dysfunction, blood dyscrasias. it can promote retention of Na+ and Cl- w/water leading to cardiac decompensation and pulmonary edema in some pts
Term
what are the indole and indene acetic acids? what do they do?
Definition
the indole and indene acetic acids are indomethacin (INDOCIN) and sulindac (CLINORIL). they are analgesic, antiinflammatory, antipyretic and antiplatelet (leading to significant occult blood loss)
Term
what are indomethacin or sulindac used for?
Definition
RA, ankylosing spondylitis, acute gout. it can be used to close patent ductus arteriosus (all NSAIDs can do this, which is why they are used with caution in pregnancy)
Term
what is the M/A of indomethacin? how is it administered?
Definition
MOST potent inhibitor of COX, also inhibits mobility of PMN lymphocytes. it can be taken PO or IV. it is used only in short term (8 days), or low doses for gout
Term
well does indomethacin bind plasma protein?
Definition
indomethacin/sulindac bind 90% plasma protein (can also bind extensively to tissues).
Term
what are the side effects of indomethacin?
Definition
35-50% experience abdominal pain, nausea, anorexia, gastric ulceration, significant occult blood loss, CNS effects: severe frontal headache, vertigo, mental clouding, depression, psychosis, skin rashes, allergic rxns, nephritis, aplastic anemia, thrombocytopenia. 20% discontinue.
Term
what is indomethacin contraindicated for?
Definition
concurrent administration with warfarin/asa b/c of increased risk of GI bleeding
Term
does indomethacin interact with any drugs?
Definition
antihypertensives of thiazide diuretic class, beta-blockers and ACE inhibitors
Term
what is sulindac? how does it compare to indomethacin?
Definition
a congener of indomethacin, a prodrug where a sulfide metabolite is the active agent. it is less irritating to the gastric mucosa than indomethacin, (but still more irritating to the gastric mucosa than other NSAIDs). its toxic effect is also similar to indomethacin
Term
what are the selective COX2 inhibitors? what do they inhibit?
Definition
celecoxib (celebrex) and rofecoxib (vioox, pulled off market) are both selective inhibitors of COX2 (inflammatory tissue) and do not inhibit COX1 (stomach), at therapeutic conditions
Term
what does celecoxib do?
Definition
anti-inflammatory, analgesic, analgesic, (not antiplatelet b/c platelets do not get inflamed)
Term
how is celecoxib administered? when does it reach peak plasma levels, steady state? how much plasma protein does it bind? what is it metabolized by? how is it excreted?
Definition
celecoxib is absorbed following PO. it reaches peak plasma levels at 3 hours and steady state at day 5. it binds plasma protein 97% and is metabolized by P450 (unlike any other NSAID but acetaminophen). celecoxib is excreted in feces and urine
Term
what are side effects of celecoxib?
Definition
can cause GI ulceration, bleeding, and perforation (but with a lower incidence than other NSAIDs). may cause a premature closure of the ductus arteriosus
Term
what generically available NSAID was close to celecoxib in terms of low GI ulcer incidence?
Definition
diclofenac
Term
what is a contraindication for celebrex?
Definition
sulfa allergies
Term
what is misoprostol (cytotec)? what is a major contraindication for it?
Definition
PGE1 analog, used to suppress gastric ulceration for pts with chronic NSAID treatment. it has a abortifacient property and therefore should not be used in pregnancy.
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