Term
| Mediators of inflammation |
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Definition
lipids (prostaglandins)
amines (hisatamines, 5-hydroxytrypramine)
small peptides (bradykinins)
large peptides (IL-1) |
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Term
Local mediators, related lipids
synthesized from the same precursors using interrelated pathways |
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Definition
prostaglandins
thromboxanes
leukotrienes
HEPETEs
HETEs |
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Term
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Definition
20 carbon atoms (eiconanoids)
produced in minute quantities by all tissues
act locally, rapidly metabolized to inactive
do not circulate in significant quantities |
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Term
| what does HPETE stand for |
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Definition
| hydroperoxy elcosa tetra enoic |
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Term
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Definition
| hydroxy eicosa tetra enoic acids |
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Term
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Definition
| Arachidonic acid (AA) released by phospholipase A2 and other acyl hydrolases in a process controlled by hormones and other stimuli |
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Term
What are the two major pathways in forming eicosanoids from AA
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Definition
cyclooxygenase
lipoxygenae |
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Term
| What is made using the cyclooxygenase pathway? |
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Definition
prostaglandins
thromboxanes
COX-1 & COX-2 |
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Term
| what is made using the lipoxygenase pathway |
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Definition
HPETE-HETE
leukotrienes
lipoxins |
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Term
| Remember that arachidonic acid is very... |
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Definition
lipophilic so easily passes through membrane
lots of carbon |
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Term
| A variety of membrane receptors that operate via G proteins which subsequently activate or inhibit adenylyl cyclase or stimulate phospholipase C |
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Definition
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Term
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Definition
local signals that fine tune response of specific cell type
thromboxane(TXA2)platelet aggregation & vasoconstriction
released in allergic or inflammatory
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Term
| many NSAIDS work by inhibting synthesis of... |
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Definition
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Term
| NSAIDS inhibit..... but not...... |
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Definition
| cyclooxygenase but NOT lipoxygenase |
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Term
| COX-1 or COX-2 is constituitive? |
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Definition
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Term
| COX 1 or 2 is inducible and associated with inflammation? |
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Definition
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Term
| Side effect of COX 1 inhibition is... |
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Definition
| inability for form stomach protecting prostaglandins (acid goes up, mucus down) |
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Term
| Which NSAID irreversibly inactivates cyclooxygenase? |
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Definition
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Term
| Do NSAIDS (other than aspirin) and salicylates reversibly or irreversibly inhibit COX? |
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Definition
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Term
| Aspirin acetylates which COX isoenzyme? |
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Definition
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Term
| Deacetylated acetylsalicyclic acid is salicylate which is... |
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Definition
| an NSAID in its own right (reversible) |
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Term
| Aspirin and other salicylates actions |
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Definition
anti-inflammatory action
analgesic action
anti-pyretic action |
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Term
| Aspirin and other salicylates anti-inflammatory actions |
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Definition
decreased formation of prostaglandins which mediate inflammation
does not induce remission in arthritic
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Term
| which salicylate has NO anti-inflammatory effect |
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Definition
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Term
| aspirin and other salicylates analgesic action |
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Definition
decrease PGE2 synthesis = decrease pain
used for low to moderate intensity pain
better than opioids in pain with inflammation
Acetaminophin = effective analgesic
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Term
| ______ may sensitive nerve endings to bradykinin, histamine, and other chemical mediators released locally by inflammatory process (Pain) |
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Definition
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Term
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Definition
| set point of anterior hypothalmic thermoregulatory center is increase |
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Term
| Fever may be caused by PGE2 synthesis stimulated by endogenous pyrogen such as cytokine released by white cells in.... |
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Definition
| infection, hypersensitivity, malignancy, or inflammation |
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Term
| Aspirin and other salicylates antipyretic actions |
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Definition
impede PGE2 synthesis
peripheral vasodilation and sweating caused by aspirin help dissipate heat in febrile patints
no effect on normal body temp
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Term
Aspirin and other salicylates respiratory action
therapeutic dose |
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Definition
increase alveolar ventilation
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Term
Aspirin and other salicylates respiratory action
higher doses |
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Definition
| work on respiratory center in medulla causing hyperventilation and respiratory alkalosis usually compensated for by kidneys |
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Term
Aspirin and other salicylates respiratory action
toxic levels |
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Definition
| central respiratory paralysis and resultant respiratory acidosis from CO2 accumulation |
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Term
Aspirin and other salicylates
GI effects
COX 1 |
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Definition
PGI2 (prostacyclin) inhibits gastric secretion
PGE2 ad PGF2alpha -stimulate mucus (protect)
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Term
| Aspirin decreases PGE2 and PGF2-alpha which results in... |
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Definition
| increased gastric acid and decreased protective mucus |
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Term
| Because aspirin increases acid and decreases mucus it can cause... |
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Definition
dyspepsia
ulceration
hemorrhage |
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Term
| Regular thrombotic actions |
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Definition
TXA2 (COX1) increase platelet aggregation
PGI2 (COX2) decrease platement aggregation (endothelial)
endothelial cells usually winning so keeping platelets pretty cool |
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Term
| Aspirin in low doses can irreversily inhibit what? |
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Definition
| thromboxane (TXA2) production in platelets w/e affecting PGI2 production in the endothelial cells |
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Term
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Definition
| reduced platelet aggregation resultingin an antithrombotic effect with a prolonged bleeding time |
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Term
| Platelets do not have the ability to resynthesize cyclo-oxygenase to make more... |
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Definition
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Term
Aspirin and other salicylates actions
on the kidneys |
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Definition
prevent synthesis of PGE2 and PGI2 which maintain renal blood flow especially w/ circulating vasoconstrictors
decrease prostaglandins = may cause retention of sodium and water and cause edema and hyperkalemia |
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Term
| Interstitial nephritis may occur with all NSAIDS except.... |
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Definition
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Term
| External applications of NSAIDS |
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Definition
salicylic acid applications
methyl salicylate (oil of wintergreen) |
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Term
Aspirin and other salicylates
CV applications |
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Definition
inhibit platelet aggregation (COX1)
decrease TIAs, unstable angina, coronary artery thrombosis, closure of PDA
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Term
| Aspirin may decrease the incidence of... |
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Definition
| colon cancer (inhibiting COX 2) |
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Term
Aspirin and other salicylates
Admin and Distribution |
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Definition
absorbed through intact skin
passively absorbed from stomach-->small intestine
rectal absorption unreliable
cross BBB and placenta |
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Term
| When given in low doses (<300 mg/day) aspirin is used for? |
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Definition
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Term
| Low dose anti-thrombic effect of aspirin uses |
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Definition
reduce recurrent MI
reduce mortality post MI analgesia
prophylactic aspirin w/ clin. manifestations of coronary dis. |
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Term
| Moderate doses of aspirin (300-2400 mg/day) used for... |
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Definition
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Term
| High dose aspirin (2400-4000 mg/day) used for |
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Definition
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Term
| Aspirin is hydrolyzed to salicylate and acetic acid by.. |
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Definition
| esterases in tissues and blood |
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Term
| Salicylate is converted by liver to.... |
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Definition
| water-soluble conjugates, cleared by the kidney |
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Term
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Definition
| aspirin-->salicylate-->water-soluble conjugate |
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Term
| Analgesic dose half life of aspirin and other salicylates |
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Definition
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Term
| Anti-inflammatory dose half life of aspirin and other salicylates |
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Definition
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Term
| Alkalinization of the urine promotes excretion....why? |
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Definition
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Term
Aspirin and other salicylates adverse effects
GI |
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Definition
epigastric distress
NV
microscopic GI bleeding |
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Term
Aspirin and other salicylates adverse effects
Blood |
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Definition
inhibition of platelet aggregation
prolonged bleeding time
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Term
| How long should a patient be off of aspirin prior to surgery? |
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Definition
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Term
Aspirin and other salicylates adverse effects
Respiration toxic doses cause... |
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Definition
respiratory depression
combo of uncompensated respiratory and metabolic acidosis |
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Term
Aspirin and other salicylates adverse effects
Metabolic processes |
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Definition
salicylates in toxic quantities may cause hyperthermia
inhibit oxidase phosphorylation |
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Term
Aspirin and other salicylates adverse effects
Hypersensitivity |
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Definition
| about 15% of patients taking aspirin allergy |
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Term
Aspirin and other salicylates adverse effects
Reyes syndrome |
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Definition
ASA w/ viral infections, a fulminating hep. w/ cerebral edema
seen in children- give acetaminophen instead |
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Term
Aspirin and other salicylates adverse effects
Salicylism
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Definition
NV
hyperventilation
headache
mental confusion
dizziness
tinnitus |
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