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45 Cards in this Set
- Front
- Back
cox 1
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is general enzyme
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cox 2
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inducible
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2 types of nsaid
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non selective and selcetive
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non selective
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aspirin
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2 paths for arach
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lipoxygenase and cox
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other name for cox
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pg sythetase
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nsaid side effect
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blockade of platelet aggregation (inhibits thromboxane synth), gi ulceration, uterine dysmotility, hypersensitivity, can use misoprostol which is a pge analogue to prevent gi tox
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non selective v 2
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gast ulcer: NS
inhib of platelet: NS inhib of labor induction: NS and 2 |
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aspirin:
what does this mean? |
irreversible acetylation of cyclooxygenase
Effect on platelet will last life of platelet 8-10 days |
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aspirin adverse
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tinnitus, deafness
renal function gi hepatotox |
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salicylate intox
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acid base balance:
respiratory alk follow by metab acidosis |
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other uses
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juvenile rheum
decrease risk of mi by 40% by taking 81 mg aspirin per day dec inci of colon cancer |
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diflunisal
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difluorophenyl derivative of sal acid
more effectie and longer dur less |
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mesalamine
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salicylate used for local effect
in inflam bowel disease |
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acetaminophen
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analges, antipyr, but weak antiinflam
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side effects
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lacks side effects of aspirin,
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acetamin metab
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glucuronide
but problem is that it can form toxic intermediate by being effected by p450 mixed function oxidases to form n acetyl b benzoquinone imine....this intermediate can continue and produce cell death |
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acetylcysteine
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antidote for tylenol poisoning
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Indomethacin
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probenecid inhibits renal excretion of indo
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adverse
other use |
severe frontal headache
can close patent ductus |
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sulindac
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pro drug,
less ulcerogenic |
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tolmetin
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adverse: gi n/v,
cns, less common than indomethacin |
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diclofenac
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reduce synth of both pg and leukotrienes....so both cox and lox inhib
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adverse
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gi, hepatotox
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ketorolac
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first injectable nsaid
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mech
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pg synth inhib
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use:
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short term management of moderately severe acute pain
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Ibuprofen
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mild inflam and analgesic
otc, however |
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naproxen
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20x more potent than aspirin, long half life 14 hour, approved for acute gout, ank spon, this is aleve
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ketoprofen
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lox and cox
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oxaprozin
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newer propionic acid
around 40-60 hour halflife |
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piroxicam
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long half life around 50 hours
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which nsaid is irreversible
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aspirin
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meloxicam
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inhib cox 2 over cox 1
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nabumetone
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cox 2 prodrug
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celecoxib
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first cox2 selective nsaid, approved for arthritis
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celecoxib advrse
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cardiovascular
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vioxx
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withdrawn in september 2004
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cox 2 adverse
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black box warning
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disease modifiying anti rheum drug
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abatacept, rituximab, etc
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abatacept
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inhib t cell activation
single use for IV injection |
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rituximab
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monoclonal ab against cd20 on b lymphocytes
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etanercept
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binds to tnf and blocks interaction
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adalimumab
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binds tnf alpha specificall and blocks p55 and p75
10 to 20 day half life |
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infliximab
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inhib interaction of tnf a with receptor, long half life
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