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37 Cards in this Set
- Front
- Back
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Do you develop a tolerance or dependence with NSAIDs
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no
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What is the mechanism by which NSAIDs work
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inhibition of cyclooxygenase
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What is the function of cyclooxygenase
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a key enzyme in prostaglandin synthesis
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What are the two isoforms of cyclooxygenase
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COX-1 and COX-2
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What is the general function of COX-1 and three specific roles
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cellular housekeeping and homeostasis
-vascualr homeostasis -GI cytoprotection -kidney function |
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Where is COX-1 found (6 locations)
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platelets, endothelial cells, kidney, vascular smooth muscle, stomach
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T/F - COX-1 is constituitive
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-true
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As an inducible enzyme, where is COX-2 located
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endoplasmic reticulum and nuclear membrane
-functions as a early immediate gene |
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When COX-2 is activated how much do levels increase
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10-80 fold
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What induces COX-2 to be transcribed (3 things)
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cytokines
growth factors LPS |
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Where is COX-2 located in the body (4 locations)
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brain, prostate gland, monocytes, synoviocytes
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What is the precursor for prostaglandins (the chemical COX works on)
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arachidonic acid
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What are three homeostatic functions regulated by COX-1
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stomach/GI protection
platelet aggregation renal blood flow |
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What are three pathophysiologic functions regulated by COX-2
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inflammation, pain, fever
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What is affected if you block COX-1 (6 items)
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endothelial integrity
vascular patency (unblocked) gastric mucosal integrity bronchodilation renal function platelet function |
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What is affected if you block COX-2
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inflammation
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What are 7 effects of taking an NSAID (by blocking COX-1 and 2)
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-renal ischemia
-GI irritation -ulcers -delayed labor -antiinflammation -analgesia |
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T/F - all NSAIDs have the same specificity for COX-1
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false, a ratio can be determined for the selectivity of COX-1 (larger = more selective)
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Which has more serious side-effects: drugs that are more/less selective for COX-1
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-more selective for COX-1
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What are 5 therapeutic application for mixed COX-1 and 2 inhibitors?
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-rheumatoid and osteoarthritis (chronic inflammation)
-prophylaxis against platelet aggregation -analgesia -mild to moderate inflammation due to injury -fever |
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What are the pharmacological factors of NSAIDs (absorption, binding, metabolism, excretion)
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-rapid GI absorption
-high protein binding (displaces other drugs) -hepatic metabolism -renal excretion |
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What are 3 serious side effects of mixed COX-1 and 2 inhibitors and how frequent are they?
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-GI irritaion/ulcers (2-4% of users/year)
-decreased renal function (acute renal failure 1%) -reduced platelet function (contributes to M&M of GI bleeds) |
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T/F - the majority of patients with serious GI adverse effects have had symptoms
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false - 80% are asymptomatic before event
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Which NSAID is an irreversible inhibitor of COX
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aspirin - all others are reversible
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Which NSAID protects against cardiovascular disease
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aspirin
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T/F - COX-2 inhibitors (COXIBs) offer protection against heart disease
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false, only those that inhibit COX-1 do
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T/F - COX-2 inhibitors generally don't have the side-effects of traditional NSAIDs
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-true
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Explain what is known about the serious side effects of COXIBs
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-GI PUBs are significantly less in <6 mo use, but mixed for long-term w/serious complications not lowered
-reports of increased (3.4x) risk of CD events after using >18 months |
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T/F - all COXIBs have been removed from the market due to CV effects
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false - only rofecoxib (Vioxx) was removed
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Aspirin, ibuprofen, naproxen, indomethacin classify:
-type of drug -wanted effects -severe side effects |
COX-1 & 2 inhibitors
-antiinflammatory, antipyretic, analgesic -severe GI side effects - mortality from bleeding ulcers |
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Celecoxib, rofecoxib, valdecoxib - classify:
-type of drug -wanted effects -side effects |
Cox-2 inhibitors
-antiinflammatory, antipyretic, analgesic -fewer GI, CV and renal side effects in theory, but recent reports of increased CV events |
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T/F - APAP is an NSAID
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false - it is an NSAID-like drug = interferes with the synthesis of some prostaglandins
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How is APAP different in wanted effects from other NSAIDs?
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-provides analgeesia and antipyretic but is NOT an anti-inflammatory drug
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In what regard is acetaminophen better than other NSAIDs?
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-has few GI side effects
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Which drug is the most common cause of acute liver failure in the US?
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acetaminophen (36% in US)
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T/F - NSAIDs are less potent AND less efficacious than opiods
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true
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Where do opioids differ - efficacy or potentcy
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-potency, all opioids are equally efficacious
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