Term
explain how the two main categories of prostaglandins are made |
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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) |
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Term
what type of receptors do prostaglandins use |
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Definition
G protein receptors that activate or inhibit adenylyl cyclase and phospholipase C |
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Term
explain the 5-lipooxygenase pathway and the 3 effects |
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Definition
5, 12, 15 - HPETE > 5-HETES > leukotriene >>
phagocyte mobilization, change in vascular permeability, inflammation |
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Term
what are the 3 products of the COX pathway |
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Definition
prostacyclin (PGI) prostaglandin (PGE) thromboxane A2 (TXA2) |
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Term
3 effects of prostacyclin |
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Definition
gastric acid secretion decreased platelet aggregation maintain renal flow despite vasoconstrictors |
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Term
6 effects of prostaglandins |
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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 |
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Term
1 effect of thromboxane A2 |
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Definition
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Term
where do corticosteroids dysrupt the prostaglandin pathway |
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Definition
stop phospholipase A2 from breaking phosphitadil inositol from phospholipid membrane into arachidonic acid |
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Term
where do salycylates dysrupt the prostaglanding pathway |
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Definition
stop COX2 from inducing PGI, PGE, TXA2 |
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Term
what are the 4 salicylates |
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Definition
acetylsalicylate (aspirin) choline Mg trisalicylate sulfasalazine diflundail |
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Term
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Definition
acetylsalicylate - irreversible COX2 blocker choline Mg trisalicylate - reversible COX2 blocker sulfasalazine - reversible COX2 blocker diflundail - reversible COX2 blocker |
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Term
which salicylate is differet, why |
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Definition
diflundail: does NOT cross BBB (NO antipyretic), does NOT affect uric acid secretion, 3-4x more potent |
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Term
10 non-respiratory effects of salicylates |
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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 |
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Term
respiratory effects of normal, high, and toxic doses of salicylates |
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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) |
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Term
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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 |
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Term
how does the dose of salicylates effect the function |
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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 |
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Term
side effects of salicylates 7 |
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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 |
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Term
interactions with salicylates 4 |
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Definition
antacids: decrease absorption heparin: hemorrhage probenecid: decrease excretion (contraindicatedin grot)
prolonged t1/2, effects, toxicity of many drugs |
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Term
5 signs of mild salicycate toxicity |
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Definition
N/V hyperventilation headache confusion tinnitus |
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Term
9 signs of severe salicylate toxicity |
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Definition
restlessness delirium hallucinations convulsions dizziness coma death respiratory acidosis metabolic acidosis |
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Term
TX or salicylate toxicity 3 |
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Definition
increase urine pH to help elimination IV dialysis fluids |
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Term
proprionic acid derivatives MOA |
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Definition
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Term
story of proprionic acid derivatives |
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Definition
I bought a flurb producing napping oxen for ketoz profound ox fender |
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Term
6 proprionic acid derivatives and their half lives |
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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 |
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Term
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Definition
GI irritation (bleed is rare) renal failure nephritis nephrotic syndrome less anti-coagulation effects means less interactions |
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Term
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Definition
same as ibprofen plys CV effects |
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Term
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Definition
some lipooxygenase inhibition (no greater antiinflammatory effect) |
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Term
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Definition
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Term
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Definition
val selectively rolfed on his cox |
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Term
3 COX2 inhibitors and their SE |
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Definition
celecoxib - sulfa hypersensitivity, don't anticoagulate (COX2 only), GI bleeds rofecoxib - DC due to CV events valdecoxib - DC due to SJS |
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Term
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Definition
RA osteoarthritis COX2 depressed in colon cancer and alzheimers disease |
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Term
story of COX1/2 inhibitors |
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Definition
so in the back the key tore Dic's fence so now theres a total lack in da mesh |
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Term
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Definition
sulindac ketorolac diclofenac etodolac indomethacin |
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Term
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Definition
related to indomethican less SE converted to sulfide |
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Term
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Definition
potent analgesic moderate anti inflammatory chronic/post-op pain, seasonal allergic conjunctivits |
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Term
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Definition
formula with misoprostol (PGE-E1) to decrease GI SE, accumulates in synovium |
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Term
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Definition
large difference between anti-inflamm dose and GI issue dose |
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Term
indomethacin MOA and uses 7 |
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Definition
potent anti inflammatory used in gout, arthritis, anylosing spondylitis, acute shoulder
tocolytic: supresses contraction in preterm labor
closes PDA |
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Term
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Definition
GI upset hepatic disease (increases amniotransferases) |
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Term
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Definition
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Term
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Definition
GI upset, frontal headaches, neutropenia, thrombocytopenia, aplastic anemia |
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Term
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Definition
analgsic, antipyretic, NO anti inflammatory effect inhibit PGE synthesis in CNS |
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Term
pharmacokinetics of acetaminophen: normal and OD |
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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 |
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Term
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Definition
n-acetyl cysteine sulfhydryl binds NAPQI as antidote |
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Term
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Definition
well tolerated at normal doses, no effect on platelets or uric acid |
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Term
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Definition
analgesic antipyretic DOC reye syndrome prevention (fever in kids with viruses, VZV) DOC gout pt (not reaction with probenicid) |
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