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Eicosanoids
Eicosanoids and NSAIDS
38
Pharmacology
Undergraduate 4
12/02/2010

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Cards

Term
What are autocoids?
Definition
-rapidly synthesized in response to specific stimuli

-act quickly at local site

-fast degredation
Term
What are some examples of Eicosanoids?
Definition
-Prostaglandins (PGs)
-Thromboxane (TXA2)
-Prostacyclin (PGIs)
-Leukotrienes (LTs)
Term
What are the pharmacological interventions for eicosanoids?
Definition
-NSAIDS
-Cyclooxygenase (COX-2)
-Leukotriene inhibitors
Term
What is the key mechanism for the arachidonic acid pathway?
Definition
-conversion of phopholipds to arachadonic acid by phospholipase A2
Term
After arachadonic acid is formed, where the possible bi-products of certain mechanisms?
Definition
-Lipoxins and Leukotrienes via lipooxygenase pathway

-protsglandins, prostacyclin, thromboxane vix COX pathway
Term
What is the COX pathway for AA?
Definition
-First to prost. G
-second to prost. H **key step**
-Then 5 possible products:
*Thromboxane A2
*Prost. I
*Prost. E
*Prost. D
*Prost. F
Term
What are two effects that Prost. I, Prost. E, and Prost. D have in common?
Definition
-increase in RBF

-inhibit gastric acid secretion
Term
What are the unique characteristics of Prost. F2alpha?
Definition
-decrease progesterone
-increase uterine contraction
-vaso and broncho constriction
-glaucoma**
Term
What are the major differences between Cox1 and Cox2 inhibitors?
Definition
-see notes on slide
Term
What chemical structure do all prostaglandins share?
Definition
-20 carbon carboxylic acid cyclopentane ring with a hydroxyl at position 15
Term
What are the cardiovascular effects of PGE2?
Definition
-Vasodilation

-drop in bp in most vascular beds
Term
What are the cardiovascular effects of PGD2?
Definition
-Flushing
-nasal stuffiness
-hypotension
Term
What are the cardiovascular effects of PGI2?
Definition
-relaxes vascular smooth muscle

-Hypotension and reflex tachycardia
Term
What prostaglandins cause broncho constriction?
Definition
-PGF2alpha, and PGD2, and LT's
Term
What two prostaglandine cause broncho relaxation?
Definition
PGE2 and PGI2
Term
What is aspirin induced asthma?
Definition
-inhibits COX 1

-causes shift in AA to LT

-formation leads to bronchoconstriction
Term
What are the general effects of PGE and PGF on GI smooth muscle?
Definition
-cramps (stimulated contraction)

-Diarrhea (h20 movement into intestinal lumen)
Term
What are the general effects of PGE and PGI on GI acid secretion?
Definition
-inhibit acid and decrease pepcin

-increase mucus secretion

**COX-1 dominant source of cytoprot. PGs
Term
What are common application for PGs in the GI tract?
Definition
-PGE analogs can be used for ulcer prevention

-Ex. misoprostol. commonly combined with a NSAID when on chronic therapy to prevent ulcer formation
Term
What are the general effect of PGE2 and PGF2alpha on uterine smooth muscle?
Definition
-stimulation of contractions

-enhances oxytocin action

-"ripening" of cervix
Term
What is dinoprostone and what is it used for?
Definition
-PGE analog

-Cervical ripening, induction of labor, therapeutic abortion.
Term
What is misoprostol? What is it combined with?
Definition
-PGE1 analong

-combo with mifepristone (effective abortifacient)

-AE: hypotension, flush, dizz, fever, cramps, pelvic pain
Term
What is the application of PGE2 and PGI2 in infants?
Definition
-alprostadil (natural PGE1)

-maintain shunt in infants with cogenital heart defects

-indomethacin used to close these shunts
Term
What are possible applications of PGI2?
Definition
-pulmonary hypertension

-epoprotenol iv infusion lowers pulmonary resistance

-brings relieve and prolongs survival
Term
What are the ocular effects of PGs and what PG
Definition
-PGFalpha2

-increase outflow of aqueous humor
-collagen decreases in cilliary muscle
-decrease in outflow resistance
Term
What are some examples of PGF2alpha analogs?
Definition
-Latanaprost (xalantan), travoprost (travatan)
Term
What is the effectiveness of PGF2alpha and what are side effects?
Definition
-equal or more effective than timolol for glaucoma

-red eye, iris darkening, dizziness, and asthma (rare)
Term
Hos is APAP differ from NSAIDS?
Definition
-analgesic properties,
-antypyretic properties

**POOR anti inflammatory action
**weak inhibitor of COX in peripheral tissues
Term
How is aspirin differ from NSAIDs?
Definition
-aspirin is an irreversible inhibitor of platelet and endothelium COX

-NSAIDs are reversible inhibitors
Term
What NSAIDs were pulled off the market and why?
Definition
-Rofecoxib (Vioxx) and valdecoxib (bextra)

-selectivity for COX2 is so great that risk of stroke/MI extremely elevated

-selective COX2 inhibitors have excellent anti inflammatory effects, but COX2 is necessary for prevention of platelets adhering to endothelial walls
Term
What are the different classes of NSAIDs?
Definition
-Salicylates
-propionic acid derivatives
-Acetic acid derivatives
-oxicam derivatives
Term
Salicylate examples

Propionic acid examples

acetic acid examples
Definition
Aspirin

ibuprofen, naproxen, fenoprofen, ketoprofen

indomethacin, sulindac, etodolac
Term
What is gout?
Definition
-inflammatory reaction to deposits (tophi) of sodium urate in joints

-associated with hyperuricemia
Term
What are the pharmacological goals for gout?
Definition
-suppress immune response to crystal formation
-limit extent of inflammation
-reduce uric acid synthesis
-increase renal excretion of uric acid
Term
What is allopurinol?
Definition
-inhibits xanthine oxidase

-lowers uric acid, favors urinary excreation of oxypurines

-**NOT for use during an acute attack,
can precipitate/worsen attack**

-often used in combo with colchicine
Term
What are uricosuric agents?
Definition
-probenacid, sulfinpyrazone

-filtered, secreted and reabsorbed at renal tubules

-inhibits reabsorption of urates (also penicillins/cephalosporins)
Term
What is colchicine?
Definition
-selective uricosuric agents

-inhibits leukocyte migration
-inhibits crystal phagocytosis
-reduces proinflammatory mediator conc.

-USED for relief in ACUTE attacks
Term
What is uloric?
Definition
-febuoxstat, non-purine slective inhibitor of xanthine oxidase

-initial increase in gout flares
-higher rate of CV events than allopurinol
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