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152 Cards in this Set
- Front
- Back
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Estimated hospitalizations per yr from NSAIDS?
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a. 120,000
b. 107,000 c. 95,000 d. 48, 000 |
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Estimated NSAID deaths per yr?
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a. 15,000
b. 22,000 c. 16,500 d. 24,500 |
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Only cox2 selective inhibitor on the market?
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Celecoxib
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Ibprofen, Naproxen, Fluriprofen, Ketoprofen, Fenoprofen, Oxaprozin-type of NSAIDS?
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Arylpropionic Acids
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Name 2 Salicylic acid derivites?
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ASA, Sulfasalazine
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Paraminophenol derivites?
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Acetaminophen
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Heteroaryl Acetic Acids?
name 3 |
Tolmetin
Diclofenac Ketorolac |
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3 Indole & Indene Acetic Acids?
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Indomethacin
Sulindac Etodolac |
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Anthranili Acids (Fenamates)?
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Mefenamic Acid
Meclofenamic Acid |
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Enolic Acids?
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Oxicams (piroxicam, tenoxicam)
Pyrazolidinediones (phenylbutazone, oxyphenthatrazone |
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Alkanones?
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Nabumetone
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AA precursor?
a. cyclo-oxygenase b. 12-HETE c. phospholipase A2 d. 5-lipoxygenase |
c. phospholipase A2
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Phospholipid location?
a.mitochondria b.gogli body c. cytoplasm d.cell membrane |
d.cell membrane
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PG are produced in most cells in response to what?
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stimuli (inflamation, pain)
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Eicosanoids aka?
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PG
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Eicosanoids derived from what?
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20-carbon unsaturated fatty acids
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3 precursors for eicosanoids?
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arachidonic acid (AAA), eicosapentaenoic acid (EPA),
dihomo-y-linolenic acid (DHA) |
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AA come from primarily what in our diet?
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meat
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EPA aka?
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fish oil
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EPA & AAA forms which PG series?
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PG2 series
(2 double bonds) |
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DHA forms which PG series?
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PG1 series
(1 double bond) |
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Eicosapentaenoic acid forms which PG series?
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PG3
(3 double bonds) |
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First eicosanoid found where?
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semen
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Capital letter following PG refers to what?
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chemical structure of 5-membered ring
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Subscript following PG refers to what?
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number of double bonds in two side chains
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PGs are preformed.
T/F |
False
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AA precursor from the diet is?
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linoleic acid
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What enzyme liberates AA from phospholipids in the cell membrane?
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phospholipase A2
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Name 2 izosymes of cyclooxygenases?
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cyclooxygenase I & II
aka Cox-1, Cox-2 |
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Lipoxygenases act on AA to form what?
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LT
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Cox-1 & Cox-2 act on AA to produce what?
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PG
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What types of PG & LT are produced from EPA (vs AAA)?
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Series 3 PG, Thromboxanes
Series 5 LT |
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Cox-1 activation leads to homeostasis via...
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PLT aggregation/disaggregation; cytoprotection; vascular responses; renal protection
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Cox-1 associated with thromboxain production?
T/F |
True
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Cox-2 associated with PGI2 (prostacycline) production?
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true
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Cox-2 activation leads to?
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inflammation; pain; fever
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Cox-2 activation is physiological.
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false, pathological
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Cox-1 activation is physiological?
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true; "housekeeping"
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Upon activation Cox-1 increases by...
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2-4 fold increase
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Upon activation Cox-2 increases by....
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10-20 fold increase
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Cox-2 are involved in normal renal activity & vascular PGI2 production.
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True
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Type of stimulus to activate Cox-2?
a.endotoxin b.tumor promotor c.growth factors d.cytokines e.all of above |
e. all of above
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Cox-1 has a wider channel and extra binding site?
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false, cox-2 does
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PLTs form what PG using TXA2 synthase?
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thromboxane (TXA2)
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Endothelieal cells in blood vessels form what PG using what synthase?
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PGI2 synthase forms prostacyclin (PGI2)
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Some PG are preferentially formed in certain tissues based on what?
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the synthase that is present in the tissue
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Cyclic endoperoxides PGG2 & PGH2 are intermediates to PGs from AA?
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true
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5-lipoxygenase (5-LO) forms what?
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LT
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5-LO-activating protein (FLAP) does what?
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translocates 5-lipoxygenase (5-LO) to cell membrane where its activated
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Lipoxygenases are found in what cells?
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eosinophils, mast cells, polymorphonuclear leukocytes, monocytes
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SRS-A?
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slow reacting substance of anaphylaxis
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LTC4 + LTD4 + LTE4 LEADS TO?
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SRS-A
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2 types of signal transduction that PG use?
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1. coupled with G-proteins to adenylyl cyclase to make cAMP
2.phosphotidylinositol system to make IP3 & DAG |
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Most complex PG receptor?
a.EP b.FP c.DP d.TP |
a. EP
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PGI2 activates adenylyl cyclase to increase cAMP and decrease.....
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intracellular calcium
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Top 3 PGI2 effects?
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vasodilation
inhibits PLT aggregation diuresis |
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Top 3 TXA2 effects?
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vasoconstriction
stimulates PLT aggregation bronchoconstriction |
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PGF2a increases ....
a.gastric mucus secretion b.aqueous humor outflow c.gastric acid secretion d.bronchoconstriction |
b.aqueous humor outflow to decrease IOP
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PGF2a relaxes uterine tone.
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false, it increases uterine tone
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PGF2a effects include? Name 3
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increase uterine tone
bronchoconstriction increase aqueous humor outflow |
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PGE2 acting on receptor EP2 ....
a.relaxes gi tone/bronchodilates b.constrict gi tone/bronchocontrict |
a. relaxes & dilates
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PGE2 acting on EP3 receptors produce cytoprotective effects?
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true; inhibits gastric acid secretion, increases gastric mucus secretion,
(also stimulates uterine contractions) |
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Physiological effects of PG:
a.cytoprotective b.vasodilatory c.PLT aggregation/disaggregation d.increase uterine tone/contractions e.all of above |
e. all of above
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3 pathological effects of PG?
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inflammation
fever pain |
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Does PG effects of pain work peripherally, centrally or both?
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both
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PG cause increased peripheral nociceptor sensitivy.
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true
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PG slow transmission of pain signals in spinal cord?
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false, they enhance transmission
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Which COX relates to the pathological effects of PG?
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COX-2
inflammation pain fever |
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What 3 PG effect inflammation?
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PGE2
PGI2 PGD2 |
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Cell-derived mediators in inflammatory response?
Accronym: HELPP C |
Histamine
Enzymes LT PG PLT activating factor Cytokines |
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What 2 PG effect pain?
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PGE2
PGI2 |
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PGE2, PGI2 & PGD2 potentiate effect of histamine & bradykinin in the inflammation response.
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true
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PGE2 & PGI2 are both involved with what pathological effects?
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inflammation
pain |
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What PG is involved in all 3 pathological effects?
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PGE2
inflammation pain fever |
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What stimulates the synthesis & release of PGE2 & what is the effect?
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pyrogens
fever also thought to sensitize nerve endings to inflammatory mediators (bradykinin, histamine, ect) |
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Where is PGE2 synthesized & relased from when causing fever?
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hypothalmus
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Cox-2 PGs:
increase pain increase inflammation increase fever |
true
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PGI2 has what effect on PLTs via increased cAMP levels?
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disaggregation
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Normal PLT activity is a balance between what 2 PG?
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PGI2
TXA2 |
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TXA2 has what effect on PLTs via increased IP3 levels & mobilized intracellular calcium?
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aggregation
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The only NSAID used for PLT effects?
a.Indomethacin b.Ibprofen c.Acetaminophen d.ASA |
d.ASA
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PLT can synthesize proteins.
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False, they can NOT synthesize proteins which is why ASA works by irreversibly inhibits Cox-1 which is needed for TXAs
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Cox 1 located in:
a.gi tract b.PLTs c.WBC d.vascular lining e. all of above |
b. PLTs
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Cox-2 located:
a.gi tract b.PLTs c.WBC d.vascular lining e.all of above |
d. vascular lining
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Prostacyclin aka
a.Cox-2 b.TXA2 c.PGI2 d.PGH2 |
c.PGI2
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Thromboxane A2 aka
a.Cox-1 b.Cox-2 c.TXA2 d.PGH2 |
c.TXA2
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PGI2 causes PLT
a.aggregation b.disaggregation |
b.DISaggregation
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TXA2 causes PLT
a.aggregation b.disaggregation |
a.aggregation
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Prostacyclin synthase is located in the ...
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vascular lining
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Thromboxane synthase is located in the....
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PLTs
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PGI2 has 3 effects....
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vasodilates
PLT disaggregates diuresis |
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TXA2 has 3 effects...
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vasocontriction
PLT aggregation bronchoconstriction |
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PGE2 is a profound bronchoconstrictor
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false, profound bronchodilator
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TXA2 & PGI2
which is major constrictor? Which is major dilator? |
TXA2-constrictor
PGI2-dilator |
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Limits to using PG as drugs...
a.wide range of activities b.short duration of action c.all of above |
c.all of above
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Epoprostenol (PGI2 analog) used for hemodialysis & pulm HTN why?
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inhibits PLT aggregation
vasodilator |
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Epoprostenol & Trepostinil both are what type of drug?
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PGI2 analogs-both used in pulm HTN
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Alprostadil (PGE1) given as continuous IV infusion for...
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ductus arteriosus in neonates; maintains patency until surgery
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Indomethacin can be used to treat delayed closure of ductus arteriosus.
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True
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Alprostadil (PGE1) is a smooth muscle relaxant.
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true
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Caverject, Muse, Edex used for
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impotence
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When PG used to stimulate intestinal motility what is a common side effect?
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colicky cramps
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PGE2 & PGF2a have potent oxytoxic actions.
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True. Stimulates uterine contractions
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How do PG affect pregnancy?
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Can terminate pregnancy at any stage
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PGEs & PGFs are decreased in labor.
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false. they are increased
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PGE & PGF do what to the uterus?
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increase tone and contractions
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Dinoprostone (PGE2 analog) is
a.cytoprotective b.toxic c.oxytocix d.protective |
c.oxytocix
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PGF2a analog used for 2nd trimester abortion & postpartum hemorrhage..
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Carboprost tromethamine
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Method of delivery of Carboprost tromethamine
a.IM b.IV c.SC d.PR |
IM
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PGE2 & PGI2 do NOT have cytoprotective effects.
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false
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Dose of Misoprostol
a.300mcg QID b.200mcg QID c.200mcg BID d.300mcg TID |
b. 200mcg QID
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Misoprostol (PGE1 derivative) FDA approved for what?
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prevention of NSAID-induced peptic ulcers
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Misoprostol can also be used for
a.constipation b.abortion c.gi bleed d.menstral cramping |
b.abortion
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PGE2 & PGI2 do what to kidney?
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vasodilation & increased GFR
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Name the 5 PG that come from cyclo-oxygenase pathway for arachidonate.
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PGI2-vasodilator, hyperalgesic, platelet disaggregation
PGF2a-bronchoconstrictor, myometrial contraction PGD2-platelet disaggregation, vasodilator PGE2-vasodilator, hyperalgesic TXA2-thrombotic, vasoconstricotr |
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If you inhibit phospholipase A2 you..
a.increase production of AA b.inhibit production of LT & PG c.inhibit production of COX2 d.increase cell membrane permeability |
b. inhibits production of LT & PG b/c phospholipase A2 is what liberates AA from the cell membrane. AA is precurser for LT & PG
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What is the precursor for the double bond PG series?
a.EPA b.AA c.ATP d.DHA |
b. AA is precursor for double bond PG series
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What is the precursor for the triple bond PG series?
a.EPA b.AA c.ATP d.DHA |
a.EPA is precursor for triple bond PG series
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If you block the COX 1 & COX 2 pathway what will happen to AA?
a. decrease b. move to 5-LOX pathway c.move to PG synthase pathway d.none of the above |
b. move to 5-LOX pathway-there are 2 paths AA can take the COX 1&2 paths or 5-LOX, so if you block one it will just go to the other
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The end products of the 5-LOX pathway of AA is?
a.PGE2 b.LT c.PG synthase d.cox 1 |
b. LT come from the 5-LOX pathway, and PG come from the COX pathway
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COX 1 & COX 2 are both ______ protective.
a.cardiovascular b.renal c.pulmonary d.nuerological |
b.renal; so if u inhibit them remember you may be putting kidney in danger
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Cyclic endoperoxides (PGG2 & PGH2) are intermediates to PGs from AA.
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true
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All PGs are metabolized...
a.slowly b.rapidly c.in conjuction with synthase d.in the nucleus |
b.rapidly to ketone
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COX inhibitors primarily do what
a.act like PGs b.inhibit formation of AA c.inhibit synthesis of PGs d.block TXA2 receptors |
c.inhibit synthesis of PGs by blocking AA from the cox pathway
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PLA2 inhibitors primarily do what?
a.act like PGs b.inhibit formation of AA c.inhibit synthesis of PGs d.block TXA2 receptors |
b.inhibit formation of AA by blocking the PLA2 enzyme from liberating AA from membrane
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PG analogs primarily do what?
a.act like PGs b.inhibit formation of AA c.inhibit synthesis of PGs d.block TXA2 receptors |
a. act like PGs
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LT synthesized by what?
a.13-LO b.LTE4 c.5-lipoxygenase d.phospholipase |
c.5-lipoxygenase in eosinophils, mast cells, polymorphonuclear leukocytes or monocytes
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What type of signal transduction do PG utilize?
a.ion channels b.Na exchange channels c.g coupled proteins d.enzyme linked channels |
c. G coupled proteins to either adenylyl cyclase (to form cAMP) or phosphotidylinositol system (productin IP3 & DAG)
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Match:
TXA2 inhibits cytoprotection PGF2a vasodilation PGI2 lower IOP PGD2 bronchoconstrictor PGE2 diuresis |
TXA2 bronchoconstrictor
PGF2a lower IOP PGI2 diuresis PGD2 vasodilation PGE2 inhibits cytoprotection |
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PGE2, PGI2 & PGD2 are linked to inflammation.
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true, they cause increased blood flow, vasodilation, edema, erythema, leukocyte infiltration, tissue damaging free radicals, potentiate effects of histamind and bradykinin
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PGE2 & PGI2 are linked to pain.
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true, they increase nociceptor sensitivity peripherally, enhance transmission of pain signals in spinal cord
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PGE2 is linked to fever.
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true, pyrogens release IL-1 to increase PGE2 synthesis & release in hypothalmus, resets temp set point in hypothalmus
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PLT activity is mainly the opposing effects of PGI2 & TXA2.
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true
PGI2-disaggregation via cAMP TXA2-aggregation via increased IP3 & intracellular Ca mobilization |
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PGE2 is a potent bronchodilator but persistently causes what side effect?
a.rebound constriction b.coughing c.metalic taste d.vertigo |
b.coughing, all analogs cause this
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Epoprostenol (Flolan)
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PGI2 analog
-PLT aggregation inhibitor -vasodilator -in dialysis instead of heparin -primary pulm HTN |
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Trepostinil
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PGI2 analog
-longer t1/2 -vasodilator for pulm HTN |
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Alprostadil (Prostin VR Pediatric)
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PGE1, smooth muscle relaxant
-temp maintain patency of ductus arteriosus until surgery -continuous IV infusion -ADR: apnea, bradycardia,hypotension, pyrexia |
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Alprostadil (Caverject, Muse, Edex)
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PGE1, smooth muscle relaxant
-impotence -erection lasts 1-3 hours -urethral pellet or intravavernosal injection |
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Dinoprostone
(Prostin E2, Prepidil) |
PGE2 analog- oxytoxic
-vaginal supp, gel or controlled release prep -induces 2nd trimester abortion -mean time = 17 hours -softens cervix, shortens delivery time -SE: n/v, diarrhea |
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Carboprost tromethamine
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PGF2a analog
-induces 2nd trimester abortion -controls postpartum bleeding -can induce labor -IM -SE: gi problems -high likely hood of gi toxicity with oral route |
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PGE2 & PGI2 are linked to cytoprotection.
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true, inhibit gastric acid secretions,stimulate mucus prod, increase bicarb secretion, increase mucosal blood flow
-accelerates ulcer healing |
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GI motility is linked to PGE2 & PGF2a.
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true, both contract longitudinal muscles
-PGF2a-contracts circular muscle -PGE2-relaxes circular muscle |
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PGEs & PGFs are linked to uterine tone.
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true, both are increased during labor
-increase uterine tone -increase uterine contractions |
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PG can be taken during pregnancy & breast feeding b/c they do not cross membranes.
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false, PG can terminate pregnancy at any stage
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Misoprostol (Cytotec)
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PGE1 derivative
-cytoprotective -prevent NSAID-induced ulcer -200mcg QID -duration: 3 hours -more effective healing with gastric than duodenal ulcers -SE: abd cramping, diarrhea -oxytoxic-used for abortion |
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PGE2 & PGI2 are linked to renal effects.
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true.
-vasodilation, increased GFR -increased medullary blood flow -natriuretic effect -blocks ADH effect on adenylyl cyclase to increase H2O clearance -B1 receptor controlled -increases renin release (minor) |
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What problems may you encounter with COX-1 inhibition r/t PLT aggregation?
a.bleeding b.decreased PLT count c.increased PLT count d.clotting |
a.bleeding; gi bleeding, ulcer bleeding
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What problems may you encounter with COX-2 inhibition r/t PLT aggregation?
a.bleeding b.decreased PLT count c.increased PLT count d.clotting |
d.clotting, stroke, MI
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PGF2a is linked to the eye
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true. increases aqueous humor outflow, decreased IOP
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Latanoprost (Xalatan)
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PGF2a derivative
-eye drop -for open angle glaucoma -for ocular HTN -no major systemic SE -SE: darkens iris color at 6mo or 12mo; some stinging, burning, tearing |
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Name the 3 main biological properties of LTs
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1.increased vascular permeability
2.bronchoconstriction 3.chemotactic |
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LTB4 does what in the inflammation response?
a.apoptosis b.phagocytosis c.stimulate cytoprotection d.chemoattraction of leukocytes |
d.chemoattraction of leukocytes
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