Term
What is the major side effect of fenamate? |
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Definition
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Term
What are pyrazoles used in the treatment of? |
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Definition
Gout and rheumatoid arthritis |
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Term
What property of pyranozoles limit their usefulness? |
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Definition
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Term
What activity is greatest in phenylbutazone, antipyretic, antiinflammatory, or analgesic? |
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Definition
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Term
What are the most serious adverse effects of pyridazoles? |
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Definition
agranulocytosis and aplastic anemia |
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Term
Name one ocular effect of pyrazoles? |
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Definition
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Term
What are two potential side effects of pyrazoles that result from decreased uptake of iodide by the thyroid gland? |
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Definition
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Term
How long is Tx with pyrazole permitted? |
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Definition
Up to one week with frequent blood tests due to its potential adverse effects |
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Term
What three conditions is diclofenac approved in the treatment of? |
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Definition
arthritis osteoarthritis ankylosing spondylitis
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Term
Where does diclofenac accumulate? |
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Definition
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Term
Which is the most potent, indomethacin, naproxen, or diclofenac? |
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Definition
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Term
Where is diclofenac primarily excreted? |
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Definition
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Term
What other route of administration can ketorolac be given than oral? |
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Definition
intramuscularly for post op pain |
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Term
How is ketorolac administered for topical allergies? |
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Definition
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Term
Where is ketorolac metabolized? Where is the drug and its metabolites excreted? |
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Definition
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Term
What enzyme act on membrane phospholipids to produce arachidonic acid? |
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Definition
phospholipase A2 and other acyl hydrolases |
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Term
What two mediators stimulate the formation of arachidonic acid? |
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Definition
bradykinin and angiotensin |
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Term
What is the pKa range of most NSAIDS? Are they readily absorbed at gastric pH? |
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Definition
pKa-3-5 They're readily absorbed at gastric pH and thus may contribute to GI toxicity.
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Term
What enzyme do corticosteroids inhibit? |
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Definition
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Term
Which enzyme is responsible for physiologic production of prostanoids? |
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Definition
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Term
Which enzyme is responsible for elevated production of prostanoids that occurs in sites of disease and inflammation? |
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Definition
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Term
Which COX enzyme has a larger and more flexible substrate channel and has a larger space at the site where inhibitors bind? |
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Definition
COX-2, hence some drugs can be more selective for COX-2 than COX-1 |
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Term
Do prostaglandins increase or decrease intracellular Calcium? |
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Definition
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Term
What percent of patients show an intolerance to aspirin? |
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Definition
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Term
What is the weakest action of acetaminophen, antipyretic, anti-inflammatory, or analgesic? |
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Definition
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Term
Does aspirin bind reversibly or irreversibly to COX-1 and COX-2? |
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Definition
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Term
What is the least effective action of diflusinal, analgesic, antipyretic, or anti-inflammatory? |
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Definition
antipyretic because it does not distribute into the CNS and thus has no effect on fever |
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Term
How much more potent is diflusinal as an analgesic and anti-inflammatory agent than other NSAIDs? |
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Definition
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Term
Where in the body do NSAIDs block prostaglandin synthesis? |
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Definition
- thermoregulatory center in the hypothalamus
- peripheral target sites
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Term
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Definition
PGE2 sensitizes the nerve endings to bradykinin, histamine, and other mediators released by the inflammatory process. |
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Term
For what type of pain are NSAIDs effective in treating? |
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Definition
Mild to moderat pain arising from the peripheral structures rather than from the visceral structures |
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Term
For what type of pain are NSAIDs combined with opioids effective in treating? |
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Definition
pain in malignancy (terminal cancer) |
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Term
For what type of pain treatment are NSAIDs superior to opiods? |
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Definition
pain due to the inflammatory process |
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Term
Low doses of aspirin cause respiratory _____ while higher doses act on the respiratory center in the medulla causing respiratory______. |
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Definition
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Term
Which prostaglandins incresase secretion of mucus in the stomach and small intestine? Which prostaglandin inhibits gastric acid secretion? |
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Definition
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Term
What drug is used to treat the adverse effects of NSAIDs in the stomach? |
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Definition
misoprostol, a PGE1 derivative |
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Term
What prostaglandin decreases platelet aggregation? |
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Definition
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Term
What prostaglandin promotes platelet aggregation? |
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Definition
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Term
Which prostaglandins are responsible for maintaining renal blood flow especially in the presence of circulating vasoconstrictors? |
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Definition
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Term
What is a potential negative effect of PGE2 and PGI2 inhibition? |
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Definition
Retention of Na+ and H2O and edema and hyperkalemia in some patients |
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Term
All NSAIDs can cause interstitial nephritis except? |
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Definition
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