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29 Cards in this Set
- Front
- Back
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PG do not cause formation of pain signals but sensitize nociceptors (allow pain receptors to generate pain at low chemical signals)
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FYI
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are the prototypic sensitizing agents in the acute inflammatory process
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PGs
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mainly effective against those types of pain in which PGs amplify the basic pain mechanism, i.e., where PGs induce inflammatory pain by causing sensitization, vascular permeability, and vasodilation
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NSAIDS
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NSAIDs inhibit ___ and, therefore, attenuate inflammatory pain.
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PG production
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Where do PGs come from?
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They come from arachidonic
acid (AA), which is a “piece” of a phospholipid |
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Arachidonic Acid (AA) Pathway
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1. prostaglandins (PGs)
2. thromboxanes (TXs) 3. leukotrienes (LTs) |
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COX-1 is a constitutive enzyme
COX-2 is induced in ____ |
inflammatory cells by inflammatory stimuli
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__ and ___ need COX-1 and 2 while ____ uses 5-lipoxygenase
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PGs and TXs
LTs use lipoxygenase |
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acetaminophen (not an NSAID)
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fyi
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list some NSAIDs
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profens, aspirin
indomethacin, sulindac, phenylbutazone |
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Most potent NSAIDs agents; used only when common agents prove unsatisfactory
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indomethacin
sulindac phenylbutazone |
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GCs (via induction of lipocortin) block formations of __ & ___
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LTs and PGs
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Most NSAIDs block formations of PGs and provide 3 effects:
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anti-inflammatory
analgesic antipyretic |
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has no acetylating capacity and does not inhibit PG synthesis
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Salicylate
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a toxicity characterized by dizziness, ringing in ears (tinnitus), dimness of vision, confusion, nausea, vomiting, sweating, thirst, and hyperventilation
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Salicylism
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Aspirin is contraindicated in children b/c of Reyes syndrome
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Reyes syndrome
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warfarin, methotrexate (drug displacement reactions), and aspirin augments warfarin’s inhibition of platelet aggregation
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fyi
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Fatal dose: 10-30 g
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aspirin
Death is usually due to respiratory failure |
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2-Arylpropionic acids (2APA, “profens”)
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This class of NSAIDs is widely used in treatment of:
post-surgical dental pain rheumatoid arthritis osteoarthritis acute gouty arthritis bursitis tendonitis primary dysmenorrhea |
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All 2APAs are non-selective COX inhibitors, but inhibitions are reversible
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fyi
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Potency of ibuprofen = potency of aspirin
Potency of naproxen is ___ greater than that of aspirin or ibuprofen |
20X
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indomethacin
sulindac phenylbutazone |
Potent Traditional NSAIDs (tNSAIDs)
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Unwanted Effects of Traditional NSAIDs
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related to NSAID-interferences with COX-1 prostaglandin (PG) production
inhibit platelet aggregation induce closure of the ductus arteriosus in the fetus |
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NSAIDs/Diuretics: NSAIDs interfere with actions of ___
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diuretics
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COX-2-selective inhibitors have been associated with a higher incidence of
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cardiovascular thrombotic events
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Celecoxib
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highly
selective COX-2 inhibitor |
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weak inhibitor of COX enzymes
no effects on platelets and bleeding time, and does not cause unwanted CV, respiratory, or gastric effects |
Acetaminophen
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has only weak, if any, anti-inflammatory action
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Acetaminophen
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Acute overdosage may cause a dose-dependent
potentially fatal hepatic necrosis and/or renal tubular necrosis. Hepato- and/or renal toxicity are due to production of a toxic metabolite |
Acetaminophen Toxicity
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