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Pharm NSAIDS
KYCOM Block 15
46
Pharmacology
Graduate
03/30/2014

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Cards

Term
explain how the two main categories of prostaglandins are made
Definition
phospholipid membrane (phosphitadil inositol) is broken by phospholipase A2 into arachidonic acid

arachidonic acid is converted to either 5-lipooxygenase, COX1, or COX2

to be converted to COX2 it needs to be induced by inflammation (unless in brain and kidney where it is constitutive)
Term
what type of receptors do prostaglandins use
Definition
G protein receptors that activate or inhibit adenylyl cyclase and phospholipase C
Term
explain the 5-lipooxygenase pathway and the 3 effects
Definition
5, 12, 15 - HPETE > 5-HETES > leukotriene >>

phagocyte mobilization, change in vascular permeability, inflammation
Term
what are the 3 products of the COX pathway
Definition
prostacyclin (PGI)
prostaglandin (PGE)
thromboxane A2 (TXA2)
Term
3 effects of prostacyclin
Definition
gastric acid secretion
decreased platelet aggregation
maintain renal flow despite vasoconstrictors
Term
6 effects of prostaglandins
Definition
maintain renal flow despite vasoconstrictors
sensitize nerve endings to bradykinin and histamine causing pain
increase thermoregulatory center in hypothalamus
stimulate stomach mucous
keep PDA open
Term
1 effect of thromboxane A2
Definition
platelet aggregation
Term
where do corticosteroids dysrupt the prostaglandin pathway
Definition
stop phospholipase A2 from breaking phosphitadil inositol from phospholipid membrane into arachidonic acid
Term
where do salycylates dysrupt the prostaglanding pathway
Definition
stop COX2 from inducing PGI, PGE, TXA2
Term
what are the 4 salicylates
Definition
acetylsalicylate (aspirin)
choline Mg trisalicylate
sulfasalazine
diflundail
Term
MOA of the 4 salicylates
Definition
acetylsalicylate - irreversible COX2 blocker
choline Mg trisalicylate - reversible COX2 blocker
sulfasalazine - reversible COX2 blocker
diflundail - reversible COX2 blocker
Term
which salicylate is differet, why
Definition
diflundail: does NOT cross BBB (NO antipyretic), does NOT affect uric acid secretion, 3-4x more potent
Term
10 non-respiratory effects of salicylates
Definition
anti-inflammation (PGE)
decrease pain (PGE)
anti-pyretic (no effect on normal body temp, PGE)
decrease gastric acid (PGI)
decrease stmach mucous (PGE) causes ulcers and hemorrhage
blood thinning (TXA2, PGI) (irreversible lasts life of platelet in aspirin)
closes PDA
vasoconstriction, Na/water retention, and kyperkalemia in renal vessels
Term
respiratory effects of normal, high, and toxic doses of salicylates
Definition
normal: stimulates resporatory medulla, uncouples ETC increasing CO2 stimulating respiratory medilla too, leads to hyperventilation and respiratory alkalosis

toxic: supresses respiratory center causing respiratory acidosis and metabolic acidosis (drug is acid)
Term
uses of salicylates 17
Definition
gout
RA
rheumatic fever
headache
arthralgia
myalgia
corns, callus, wart (topical)
blood thinner
angina
close PDA (dec PGE)
decrease colon cancer
ulcerative collitis
anti pyretic
analgesic
antiinflammatory
Term
how does the dose of salicylates effect the function
Definition
low dose t1/2 3-5h: blood thinner

med dose t1/2 3-5h: anti inflamm

high dose t1/2 15h: zero order kinetics
Term
side effects of salicylates 7
Definition
epigastric distress
N/V
bleeding
metabolic depression
15% have intolerance/hypersensitivity
rye syndrome: aspirin in viral infection in kids causes hepatitis and cerebral edema
Term
interactions with salicylates 4
Definition
antacids: decrease absorption
heparin: hemorrhage
probenecid: decrease excretion (contraindicatedin grot)

prolonged t1/2, effects, toxicity of many drugs
Term
5 signs of mild salicycate toxicity
Definition
N/V
hyperventilation
headache
confusion
tinnitus
Term
9 signs of severe salicylate toxicity
Definition
restlessness
delirium
hallucinations
convulsions
dizziness
coma
death
respiratory acidosis
metabolic acidosis
Term
TX or salicylate toxicity 3
Definition
increase urine pH to help elimination
IV dialysis
fluids
Term
proprionic acid derivatives MOA
Definition
COX 1 and 2 inhibitors
Term
story of proprionic acid derivatives
Definition
I bought a flurb producing napping oxen for ketoz profound ox fender
Term
6 proprionic acid derivatives and their half lives
Definition
ibprofen 2-4h (dose q4-6h)
flubiprofen 2-4h
naproxen 12-24h (dose q12h)
ketoprofen 2-4h
oxaprozin 58h (dose 1x/d)
fenoprofen 2-4h
Term
5 SE ibprofen
Definition
GI irritation (bleed is rare)
renal failure
nephritis
nephrotic syndrome
less anti-coagulation effects means less interactions
Term
SE naproxen
Definition
same as ibprofen plys CV effects
Term
SE ketoprofen
Definition
some lipooxygenase inhibition (no greater antiinflammatory effect)
Term
SE fenoprofen
Definition
interstitial nephritis
Term
story of COX2 inhibitors
Definition
val selectively rolfed on his cox
Term
3 COX2 inhibitors and their SE
Definition
celecoxib - sulfa hypersensitivity, don't anticoagulate (COX2 only), GI bleeds
rofecoxib - DC due to CV events
valdecoxib - DC due to SJS
Term
use of COX2 inhibitors 2
Definition
RA
osteoarthritis
COX2 depressed in colon cancer and alzheimers disease
Term
story of COX1/2 inhibitors
Definition
so in the back the key tore Dic's fence so now theres a total lack in da mesh
Term
5 COX1/2 inhibitors
Definition
sulindac
ketorolac
diclofenac
etodolac
indomethacin
Term
MOA sulindac
Definition
related to indomethican
less SE
converted to sulfide
Term
MOA and use ketorolac
Definition
potent analgesic
moderate anti inflammatory
chronic/post-op pain, seasonal allergic conjunctivits
Term
diclofenac MOA
Definition
formula with misoprostol (PGE-E1) to decrease GI SE, accumulates in synovium
Term
MOA etodolac
Definition
large difference between anti-inflamm dose and GI issue dose
Term
indomethacin MOA and uses 7
Definition
potent anti inflammatory used in gout, arthritis, anylosing spondylitis, acute shoulder

tocolytic: supresses contraction in preterm labor

closes PDA
Term
SE diclofenac 2
Definition
GI upset
hepatic disease (increases amniotransferases)
Term
etodolac SE
Definition
only 5% get GI issues
Term
indomethacin SE 5
Definition
GI upset, frontal headaches, neutropenia, thrombocytopenia, aplastic anemia
Term
MOA acetaminophen
Definition
analgsic, antipyretic, NO anti inflammatory effect
inhibit PGE synthesis in CNS
Term
pharmacokinetics of acetaminophen: normal and OD
Definition
significant first pass: conjugated via glucorindation/sulfination

hydroxylated to NAPQI which at normal dose reacts with glutathione but at toxic dose builds up and depletes glutathione and reacts to hepatic sulhydryl and causes necrosis
Term
acetaminophen antidote
Definition
n-acetyl cysteine sulfhydryl binds NAPQI as antidote
Term
SE acetaminophen
Definition
well tolerated at normal doses, no effect on platelets or uric acid
Term
use of acetaminophen 4
Definition
analgesic
antipyretic
DOC reye syndrome prevention (fever in kids with viruses, VZV)
DOC gout pt (not reaction with probenicid)
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