Term
|
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
|
|
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
|
|
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
|
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
|
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
|
Definition
-selective uricosuric agents
-inhibits leukocyte migration
-inhibits crystal phagocytosis
-reduces proinflammatory mediator conc.
-USED for relief in ACUTE attacks |
|
|
Term
|
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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