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Details

pirotte Pharm
nsaids, arthritis, gout
84
Other
Not Applicable
10/20/2005

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Cards

Term
PM phospholipids to AA
Definition
PLA2
Term
in what cells can cox2 be induced?
Definition
macro, mono, synovio, chondro, fibro, osteoblasts, endothelials
Term
where is cox2 expressed constituitively?
Definition
brain, kid, bone, ovary, uterus, si
Term
where in the cell is cox found?
Definition
ER
Term
what Pgs mediate vasodilation?
Definition
pge2, pgi2
Term
pgi2 aka?
Definition
prostacyclin
Term
3 actions of pgs on pain
Definition
1. lowers act threshold of 1ary neurons, 2. enhance depol of DH 2ary neurons, 3. inc. leuks --> more proinflammatory mediators
Term
which pg is pyrogenic?
Definition
e2
Term
what do pgs do to bone?
Definition
inc. resorption (osteoclasts)
Term
main cox in GI?
Definition
1
Term
what do pge2 and pgi2 do in the gut?
Definition
dec acid, inc bicarb, inc mucous, inc blood flow
Term
what cox do platelets express?
Definition
1
Term
why do endothelial cells not produce txa2?
Definition
they lack the requisite synthase
Term
what cox do endothelials express?
Definition
1 and 2
Term
kidney fxns of pgs?
Definition
vasodilation, inc blood flow, inc GFR, inc Na/H2o excretion
Term
what role do pgs have in angiogenesis?
Definition
neovasc/VEGF
Term
describe a postualted role for the use of NSAIDS in cancer...
Definition
block angiogenesis
Term
effects of pgs on female GU
Definition
stim uterine contract, nsaids may delay labor, pgs maintain a PDA
Term
3 propionic acid NSAIDs
Definition
ibu, naproxen, oxaprozin
Term
acetic acid NSAIDs
Definition
indomethacin (diclofenac, sulindac, ketoralac, tolmentin)
Term
unique MOA for aspirin
Definition
irreversible cox1i, also inhibits cox2, inhibits nf-kb at hi dose
Term
why is salicylate not as potent as aspirin?
Definition
it in a competitive antag rather than an irreversible one
Term
why does low-dose aspirin inhibit txa2 but not pge2?
Definition
txa2 is made by platelets that can't resynth cox1, endothelial cells can resynth cox1
Term
why is anti-platelet activity of aspirin diminished at higher doses?
Definition
inc inhibition of pge2 in endothelium
Term
key points with diflunisal
Definition
not anti-pyretic, fewer gi se
Term
when would you think about another salicylate over aspirin?
Definition
inc GI risk or bleeding tendency
Term
excretion of aspirin?
Definition
liver, kidney
Term
elimination kinetics of low dose aspirin (anti-platelet)?
Definition
1st
Term
elimination kinetics of hi dose aspirin (anti-inf)?
Definition
0
Term
effects of aspirin dose on uric acid excretion?
Definition
low decreases, high increases
Term
therapeutics for salicylate tox?
Definition
alkalinize the urine
Term
SE of aspirin
Definition
GI (distress, n/v, bleed, ulcer), dec renal blood flow/fxn, prolonged bleeding, resp depression (tox), hyperthermia (tox), hypersensitivity, reve's syndrome
Term
gastric damage of aspirin - 2 moa
Definition
direct damage (ion trapping), inhibit pg
Term
2 options to limit gi tox of ASA
Definition
misprotol (pg analog), ppi
Term
talk about the ASA hypersensitivity rxn...
Definition
though to result from lots of leukotrienes due to buidup of AA
Term
what is reve's disease?
Definition
aspirin given during febrile viral infection in kids can result in fatal liver disease with encephalopahty, don't give ASA to kids
Term
key features of traditional NSAIDs...
Definition
reversible inhibitors of cox, anti-inf, anti-pyretic, analgesic
Term
advantages of propionic acids over ASA?
Definition
less gi side effects
Term
rel potency of naproxen?
Definition
asa x 20
Term
novel moa of naproxen?
Definition
directly inhibits leuks
Term
advantages of oxaprozin
Definition
very long hl, mildly uricosuric
Term
indomethacin rx?
Definition
close PDA
Term
most effective anti-pyretic NSAID?
Definition
indomethacin
Term
what limits use of indomethacin?
Definition
CNS tox
Term
NSAID SEs
Definition
GI, HTN, Allergy, CNS, photosens, liver
Term
why do cox2s show inc cardiac risk?
Definition
inhibition of Cox2 decreases endothelial pgi2 and is pro-thrombotic
Term
contraindications for NSAIDs?
Definition
ulcer, bleeding disorder, renal disease, ASA hypersensitivity, pregnancy, elderly
Term
which NSAID does not work on gout?
Definition
tolmentin
Term
drugs interacting w/ NSAIDs?
Definition
oral anti-coags, anti-HTN, diuretics, uricosurics, oral hypoglycemics, Li, methotrexate, aminoglycosides
Term
when might you give Cox2i?
Definition
hx of gi ulcer/bleed
Term
drug of choice for OA pain?
Definition
acetaminophen
Term
topical analgesic for OA pain?
Definition
capsaicin (depletes SubsP)
Term
NSAIDs for OA pain?
Definition
ASA, ibu, naprox
Term
moa Acetaminophen
Definition
weak inhibition of cox1/2, inhibit cox3 (cns)
Term
effects of acetaminophen
Definition
anti-pyretic, analgesic (not anti-inf, not anti-plate)
Term
serious interaction for Acetaminophen?
Definition
booze
Term
does acetaminophen contribute to gout?
Definition
nyet
Term
rx for acetaminophen tox?
Definition
n-acetyl cysteine (replace glutathione)
Term
inflamm mediators in RA?
Definition
tnf-a, il-1, pg
Term
gen classes of meds for RA?
Definition
NSAIDs, analgesics, corticosteroids, DMARDS, BRM
Term
why is use of low-dose corticosteroids for RA controversial?
Definition
can lead to osteoporosis, weight gain, fluid retention, hypergly, HTN, infection
Term
when does one use DMARDs?
Definition
when NSAIDs/corticosteroids have not prevented sx
Term
4 common DMARDs
Definition
methotrexate, hydroxychloroquine, salfasalazine, leflunomide
Term
MOA methotrexate
Definition
inc adenosine
Term
big CI for DMARDs
Definition
pregnancy -- teratogens except for sulfasalazine
Term
MOA hydroxychlorqunione
Definition
inhibit leukocyte fxn?
Term
how long does it take the effects of hydroxychloroquinone to appear?
Definition
3-6m
Term
how long does it take the effects of methotrexate to appear?
Definition
4-6w
Term
info points on sulfasalazine
Definition
safe for pregancy, more toxic than HCQ
Term
bad combo of DMARDs for the liver?
Definition
leflunomide, methotrexate
Term
TNFa comes from?
Definition
macro, mast, CD4
Term
3 TNFais
Definition
etanercept, infliximab, adlimumab
Term
1 IL-1i
Definition
anakinra
Term
big c/i for TNFai?
Definition
infection!!!
Term
another drug that is good to use with TNFai?
Definition
methotrexate (dec antibodies and clearance)
Term
typical DMARD combo for mild RA?
Definition
HCQ, sulfasalazine
Term
age/sex for gout/
Definition
men in 30s/40s
Term
MOA for colchicine?
Definition
prevents tubulin polymerization --> blocks leuk mig/phag
Term
big NSAIDs for gout?
Definition
Naprox, indomethacin
Term
2 uricosurics
Definition
porbenecid, sulfinpyrazone
Term
MOA of uricosurics?
Definition
dec reabsorption of uric acid
Term
SE of uricosuric rx?
Definition
kidney stones due to inc. excretion, don't give to pts that are naturally uricosuric
Term
MOA allopurinol?
Definition
xanthine oxidase inhibitor
Term
c/i of allopurinol?
Definition
acute gouty attack (can worsen)
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