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106 Cards in this Set
- Front
- Back
What is cycloocygenase? |
An enzyme that catalyzes the synthesis of prostaglandins from archidonic acid |
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What is cycloocygenase also referred to as? Definitely on test |
Prostaglandin H synthase |
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How many enzymes is cycloocygenase associated with? |
3 |
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Cycloocygenase is required to produce these two things? |
prostacyclin and thromboxane |
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Where is COX 1 found? |
gastric mucosa, renal parenychma, and platelets |
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What processes does COX 1 mediate? |
physiological and homeostatic processes |
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COX 2 is _______ and can be ______ at many site. |
inducible; expressed |
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What does COX 2 mediate? |
inflammation, pain, fever, and carcinogenesis |
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What processes does COX 2 mediate? |
Pathological |
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COX 3 may be a target for what medication? |
acetaminophen |
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NSAIDS are all inclusive of these 3 properties? |
analgesic, antipyretic, anti-inflammatory (at higher doses) |
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These drugs inhibit both COX 1 and COX 2? |
traditional drugs |
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Is COX 1 or COX 2 specific? |
COX 2 |
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Name some non-specific drugs. |
toradol, aspirin, ibuprofen, naproxen |
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Name some specific drugs for the COX 2 portion of the enzyme? |
vioxx, bextra, celebrex, |
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NSAIDS inhibit which COX enzymes? |
COX 1 and COX 2 |
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How is the MOA of NSAIDs mediated? |
prostaglandin and non-prostaglandin mediated MOA |
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Describe the analgesic MOA of NSAIDs? |
Mediated through prostaglandin and non-prostaglandin mediation.
Prostaglandin MOA-NSAIDs inhibit prostaglandin synthatase peripherally
Non-prostaglandin MOA-NSAIDs also work by peripheral and chemical chemoreceptors |
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All NSAIDs inhibit? |
cyclooxygenase, and prostaglandin and thromboxane synthesis |
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Cyclooxygenase is required for conversion of ______ to ______. |
arachidonic acid (PGG2) to endoperoxide intermediate (PGH2) |
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Prostaglandins and thromboxanes play crucial roles in? |
Pain, inflammation, fever, excessive blood clotting |
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What are the most common side effects of NSAID's in the cardiovascular system? |
increased BP (by either selsective or non-selective NSAIDs)
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What are the most common side effects of NSAID's in the GI system? |
1. stomach upset (dyspepsia) short term use 2. peptic ulcer diease and bleeding from the stomach (long-term and in high doses) |
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What are the most common side effects of NSAIDs in the Liver system? |
liver toxicity in long term use |
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What are the main systemic side effects of NSAIDs? |
cardiac, GI, liver, kidney, tinnitus |
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What are the most common side effects of NSAIDs in the kidney system? |
kidney toxicity (even with short term use of NSAIDs) |
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In people with underlying kidney disease, what should be monitored yearly? |
BP and kidney function |
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Is tinnitus more common in ASA or NSAIDs use? |
High dose aspirin use, but with NSAIDs as well. The ringing usually resolves when the dose is reduced. |
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What causes Steven Johnson syndrome? |
Viral & bacterial infections Drug reactions (NSAIDs) |
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What are some adverse effects of NSAIDs |
1. hepatocellular injury 2. allergic rhinitis 3. inhibition of platelet aggregation (MI or CAD pts) 4. renal dysfunction 5. tinnitus 6. urticaria (hives) 7. gastric ulceration |
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COX 2 inhibitors are more specific for ____ inhibitors? |
COX 2 |
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No |
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What illnesses are COX 2 inhibitors useful in managing? |
osteoarthritis, acute gout, dysmenorrhea |
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Most adverse effects of COX 2 inhibitors are seen in pts taking drugs chronically for this condition? |
arthritis |
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Chronic use of ASA and other NSAIDs increases or decreases the risk of colon cancer? By how much? |
decreases; 40-50% |
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Chronic NSAID use also decreases the risk of this disease? |
Alzehimer's |
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How does ASA produce analgesia? |
Through it's ability to irreversibly acetylate COX enzyme leading to a decrease in the synthesis and release of prostaglandin |
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Is ASA reversible? |
No, not until the life of the platelet is over. |
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What things is ASA most used for? |
1. low intensity pain with muscle and H/A 2. osteoarthritis and RA 3. anti-platelet for preventation of MI (most common) |
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ASA is confined to a very small or large dose range? |
small |
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Does ASA have a celiling effect? |
Yes, you can increase the dose, but it won't help the pain any faster. It will just kill your kidneys. |
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Is the antiplatelet effect of ASA reversible or irreversible? How? |
irreversible, due to acetlyzation of the platelet through the COX 1 enzyme |
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What populations should ASA not be used in? |
children due to rye's syndrome nursing mother'd due to internal bleeding |
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ASA side effects are? |
Chair Gum 1. CNS stimulation 2. hepatic dysfunction 3. allergic reactions 4. inhibition of platelet function 5. renal dysfunction 6. GI dysfunction 7. uterine effects 8. metabolic alterations |
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Is acetaminophen considered a true NSAID? Why? |
No, due to it's lack of anti-inflammatroy properties |
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Is acetaminophen a good choice to treat arthritis or other inflammatory disorders? |
no |
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What single dose of acetaminophen can cause hepatic necrosis and death? |
a single dose of greater than 15 mg/kg |
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What is the max daily dose of acetaminophen? |
4 gms/day |
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What was the first selective COX 2 inhibitor? |
Celecoxib (Celebrex) |
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Celecoxib (Celebrex) is recommended for the pain and inflammation associated with ____ and ____? |
Rheumatoid arthritis and osteoarthritis |
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What medication is similar to celecoxib (celebrex)? |
motrin |
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Why was Vioxx (Rofecoxib) withdrawn from the market? |
Increased risk of heart attack and stroke aht W |
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What conditions was vioxx (rofecoxib) marketed to treat? |
Osteoarthritis, acute pain conditions, and dysmenorrhea |
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Vioxx (Rofecoxib) work on the COX 1 or COX 2 part of the enzyme? |
COX 2, because it's not keeping platelets from aggregating. |
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Bextra (Valdecoxib) was initially approved then discontinued for the treatment of what conditions? |
Osteoarthritis, adult RA, primary dysmenorrhea
It was withdrawn because it was causing dysmenorrhea |
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What other condition was associated with Bextra (Valdecoxib) |
Steven Johnson's syndrome |
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Which COX 2 inhibitor was never approved by the FDA? What makes it different than the others? |
Parecoxib (Dynastat) 1. available in parental form 2. has no effect on platelet functionhtW
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What is one of the most potent inhibitors of the COX enzyme? |
Indomethicin |
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What 3 properties does indomethacin possess? |
1. analgesic 2. antipyretic 3. anti-inflammatory |
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What is the DOC for ankylosing spondylitis and Reiter's syndrome? |
Indomethacin |
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Indomethacin is the DOC for what condition's? |
ankylosing spondylitis and Reiter's syndrome |
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What is ankylosing spondylitis and Reiter's Syndrome? |
ankylosing spondylitis is a long term arthritis in the spine and pelvis
Reiter's syndrome is arthritic, eye swelling (conjunctivitis), women-cervical inflammation, men-urethral inflammation |
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What acute condition is indomethacin used to treat? |
gout |
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Why is indomethacin not used to treat chronic pain? |
chronic gout needs the COX 2 enzyme |
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How is indomethacin used to treat acute gout? What doesn't it correct? |
treats inflammation it does not correct hyperuricemia |
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What infant abnormality can indomethacin correct with a single dose? |
PDA- It closes the PDA |
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What drug is a substitute analogue of indomethacin? |
Sulindac |
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What is the drug of choice for pt's with renal impairment issues? Why? |
Sulindac, because it does not affect the renal synthesis of prostaglandins as much as other drugs |
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What drug is more potent than salicylates, but less potent than indomethacin? |
Tolmetin (not on test) |
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Name 3 examples of Propionic Acid Derivatives? |
Din ibuprofen, naproxen, and diclofenac (Voltaren) |
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What conditions do propionic acid derivatives treat? |
arthritis (gouty, rheumatoid, osteoarthritis) |
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What is unique about naproxen? |
it has a uniquely long elimination half life (can dose it twice a day) |
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If someone is allergic to salisylates, what other type of medication are they allergic to? |
propionic acid derivatives |
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Phenylbutazone is effective in treating what conditions? |
gout and RA |
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This medication is very powerful and has toxic side effects and should be given for no longer than 7 days for acute pain. |
Phenylbutazone |
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What are the side effects of phenylbutazone? |
anemia agranulocytosis n/v epigastric distress gastric upset |
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This medication is different that other NSAIDs, it is more like salicylates and inhibits prostaglandin synthesis, and is used to reduce pain, swelling, and joint stiffness? |
Piroxicam |
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What medication has potent analgesic effects and mild anti-inflammatory activity? |
Toradol |
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Toradol 30 mg IM is the analgesia equivalent to? |
morphine 10 mg Demerol 100 mg |
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Does toradol effect ventilatory or cardiac depression? |
no |
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Does toradol inhibit platelets? |
yes |
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Waht conditions is toradol good to treat? |
menstrual cramps hystecectomies D & C |
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Which drug is associated with Samter's Triad (Aspirin Triad)? |
Toradol |
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What types of pts are susceptible to Samter's triad? |
people with nasal polyps, asthma, and aspirin intolerant patients |
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What will happen if toradol is given to an asthma pt? |
may cause bronchospasm and be life threatening |
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Should toradol be given to asthma pts? |
no, they may bronchospasm and die |
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What is colchicine used to treat? How? |
acute gouty arthritis, it decreases inflammation and pain |
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What is the medication that is unique for the prevention and treatment of gout? |
Colchicine |
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Is colchicine a good analgesic? |
No, it only treats inflammation. |
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What is the MOA of colchicine? |
it pulls out uremic acid to where it can be excreted in urine and stool |
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What are some side effects of colchicine? |
n/v diarrhea abdominal pain |
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What medication may prolong survival in cirrhosis? |
Colchicine |
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What medication is the preferred therapy of primary hyperuricemia in gout? |
Allopurinol |
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What are the most common side effects of allopurinol? |
Maculopapular rash and itching |
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How many COX enzymes have been identified? |
3 |
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Which statement best describes the COX 2 enzyme? |
highly inducible and production is boosted during the inflammatory process. |
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COX 2 inhibitors may produce a prothrombotic effect by their effect on which fatty acid? |
thromboxane |
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Should one NSAID be taken with another NSAID? |
No, it will increase the side effects |
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Should people taking warfarin and coumadin take NSAIDS? |
Not generally, it puts them at increased risk of bleeding when both classes are taken together. |
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Is celebrex (celecoxib) okay to take with NSAIDs? |
Should be taken with caution and under supervision of a clinician |
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What happens when ASA and NSAIDs are taken together? |
May increase the risk of bleeding |
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What happens if phenytoin and NSAIDS are taken together? |
The phenytoin level can increase |
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If ASA and NSAIDs are taken together, how should the ASA be taken to preserve the low dose ASA for the heart? |
ASA should be taken at least two hours before the NSAID. |
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What risk is involved if cyclosporines and NSAIDs are taken to together? |
theoretical risk of kidney damage |
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If people are taking NSAIDs and phenytoin together what lab test needs to be monitored and when? |
phenytoin level should be drawn when starting or increasing the dose of an NSAID. |
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In addition to transplant pts, what other types of pts take cyclosporines? |
Osteoarthritis and RA pts |