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45 Cards in this Set
- Front
- Back
Arachidonic acid is formed from ____ ____ which caan only be obtained from dietary sources
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Linoleic Acid
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What causes release of AA from cellular phospholipids
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Phospholipase A2
NOTE**** this is the overall rate determining step in the gen. eicosanoids!!! |
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The cyclooxygenase pathway leads to the formation of what 3 things
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Prostaglandins, prostacyclin and thromboxanes
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Lipoxygenase pathways leads to formation of what 2 things
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Leukotrienes and lipoxins
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Consider COX-1 and 2, which one is involved in maintaining homeostasis?
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COX-1
COX-2 is involved in INFLAMMATION n shit |
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The most prevalent prostaglandin is ____ because they are direct derivatives of arachidonic acid
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PG2
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What is the precursor to PGD2 PGE2 PGF2alpha and TxA2 and PGI2????
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PGH2!
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The chief eicosanoid of platelets
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Thromboxane (vasoconstrictor)
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The chief eicosanoid of the endothelium
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PGI2 (vasodilator)
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What catalyzes the first two steps in leukotriene biosynthesis
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LOX-5
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LTA4 is converted to LTB4 in (1)
and converted to LTC4 in (2) |
1. Erythrocytes, neutrophils
2. Mast cells, eosio's, baso's macrophages |
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Binding of LTB4 induces what
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Proinflammatory response
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Cysteinyl leukotrienes (LTC4 LTD4) cause
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vasoconstriction, bronchospasm, increased vascular perm.
***Responsible for asthmatic allergic and hypersensitivity processes |
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Lipoxins are important in resolution of
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inflammation! they regulate leukotrienes
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Zileutin and FLAP inhibitors prevent
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5-LOX - prevents synthesis of 5-HPETE - USED TO TREAT ASTHMA!
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Zafirlukast and montelukast are antagonists at the receptor for all ____ _____ and are used in the chronic management of asthma
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cysteinyl leukotrienes
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Lipoxins act as stimulators/inhibitors of the leukotriene initiated inflammatory response
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inhibitors
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Epoxyeicosatraenoic acid inhibits the expression of what therefore regulating the inflammatory response
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ICAMs intercellular adhesion molecules
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Arachidonic acids that have undergone free radical mediated peroxidation gives rise to the
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Isoprostanes
***high levels may be indicative of oxidative stress and a wide range of pathology |
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To generate large numbers of eicosanoids, many different cell types swap eico. intermediates - this is known as
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Transcellular Biosynthesis
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What prostaglandin inhibits B, T lymphocyte as well as NK cell activity
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PGE2
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What leukotrienes regulate T cell prolif
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LTB4 and the cysteinyl leukotrienes
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What p-glandins are pain sensitizers
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PGE2, PGI2
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LTC4 and LTD4 are more/less potent bronchoconstrictors than histamine
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MORE
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Elevated levels of what leukotriene are found in both Crohns and ulcerative colitis?
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LTB4
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What are elevated in the joints of someone with Rheum. arthrit.
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PGE2 and COX-2
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____ inhibitors administered early on in glomerulonephritis prevents glomerular inflammation and evidence of structural damage
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LOX
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Phospholipase A2 inhibition is mostly caused by the use of
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Glucocorticoids (prednisone)
they act by inducing "lipcortins" which interfere with pA2 activity |
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Name 4 NSAIDS with long elimination half lives
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Naproxen, salicylate, piroxicam, phenylbutazone
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What pathways does aspirin act on in an irreversible manner?
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COX-1 and 2
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A child develops hepatic encephalopathy and liver steatosis after being administered aspirin, what is this syndrome called?
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Reye's syndrome
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Ibuprofen, naproxen, ketoprofen, flurbiprofen are all
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Propionic acid NSAIDS
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Indomethacin, sulindac, etodolac, diclofenac, ketorolac are all
Which is used in the treatment of renal stone pain? Which is used to help close a PDA in newborns? |
acetic acid NSAIDs
Diclofenac Indomethacin |
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Nabumetone has preferential activity against COX1/2
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COX 2
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The difference between acetaminophen and aspirin as far as pain relief and inflammation go is that
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Acetaminophen HARDLY inhibit's COX pathways and therefor has an insignificant anti-inflammatory effect
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Celecoxib, rofecoxib, valdecoxib, and meloxicam are all
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COX-2 selective inhibitors, note the COX in them
Celecoxib is the only approved one |
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Celecoxib inhibits PPAR as well which can lower the risk of cancer in people with
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Familial adenomatous polyposis
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What two cytokines stimulate the COX-2 pathway?
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TNF, and IL-1
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Etanercept, infliximab, and adalimumab are all ____ antagonists and are used in the treatment of rheumatoid arthritis
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TNF
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Dazoxiben, pirmagrel, and ridogrel all antagonize TxA2 but which one(s) are TxA2 receptor antag.'s and which are TxA2 snthase inhibitors
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ridogrel - TxA2 rec. antag.
pirmagrel, dazoxiben - inhib txa2 synthase |
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What drug inhibits 5-LOX by chelating it's nonheme iron and is used in asthma
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Zileuton
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Adenosine inhibits ___ synthesis by regulating AA release
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LTB4
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Montelukast and zafirlukast are used to treat asthma, they are both ____ ____ receptor antagonists
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Cysteinyl Leukotriene
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Myocardial infarction is a serious adverse effect of this COX-2 selective inhibitor
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Celecoxib
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All drugs with PROST in the name are prostanoid mimetics and one is used for the maintenance of PDA and erectile dysfx but has SE of heart failure - which one
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Alprostadil
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