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39 Cards in this Set
- Front
- Back
what is the mechanism of opiod analgesics?
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act as agonists at opiod receptors to modulate synaptic transmission
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what opiod works at the mu receptor?
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morphine
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what opiod works at the delta receptor?
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enkaphalin
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what opoid workds at the kappa receptor?
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dynorphin
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how do you treat opiod toxicity?
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naloxone or naltrexone (opiod receptor antagonists)
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what is contraindicated in morphine overdose?
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O2 - might contribute to respiratory failure
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toxicity of opiods?
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respiratory depression, miosis (pinpoint pupils), additive CNS depression with other drugs, constipation, addiction
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how do NSAIDs work?
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reversibly inhibit COX-1 and COX-2; block prostaglandin synthesis
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what is used to close a PDA?
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indomethacin
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toxicity of NSAIDs?
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renal damage, aplastic anemia, GI distress, ulcers
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how do celecoxib, valdecoxib work?
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selectively inhibit COX-2, which is found in inflammatory cells and mediates inflammation and pain
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why should COX 2 inhibitors not have the corrosive effects of other NSAIDs on the GI lining?
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spares COX-1, which helps maintain the gastric mucosa
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what are COX 2 inhibitors used for?
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rheumatoid and osteoarthritis
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what is the mechanism of acetominaphen?
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reversibly inhibits cyclooxygenase, mostly in CNS; inactivated peripherally
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what is the antidote for acetominaphen toxicity?
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N-acetylcysteine
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what drug is used for acute gout?
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colchicine
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this gout drug depolymerizes microtubules, impairing leukocyte chemotaxis and degranulation
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colchicine
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what acute gout drug is less toxic than colchicine and therefore is used more frequently?
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indomethacin
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this drug is used for chronic gout - it inhibits resorption of uric acid
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probenecid
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what gout drug inhibits secretion of penicillin?
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probenecid
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what is the mechanism of allopurinol? what is it used for?
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inhibits xanthine oxidase, decreasing conversion of xanthine to uric acid; used for chronic gout (when under control)
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what gout drug is also used in lymphoma and leukemia to revent tumor lysis-associated nephropathy?
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allopurinol
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what is etanercept?
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recombinant form of human TNF receptor that binds TNF-alpha
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what is etanercept used for?
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RA, psoriasis, ankylosing spondylitis
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what is infliximab?
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TNF-alpha antibody
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what is infliximab used for?
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Crohn's disease, RA, ankylosing spondylitis
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this drug binds to cyclophilins, and the complex blocks the differentiation and activation of T cells by inhibiting calcineurin, thus preventing production of IL-2 and its receptor
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cyclosporine
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when is cyclosporine used?
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suppresses organ rejection after transplantation; selected AI disorders
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the nephrotoxicity associated with cyclosporine is preventable with what?
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mannitol diuresis
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what toxicity is associated with cyclosporine?
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predisposes to viral infections and lymphoma
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what is the mechanism of action of tacrolimus (FK-506)? what drug is it similar to?
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binds to FK-binding protein, inhibiting secretion of IL-2 and other cytokines; similar in action to cyclosporine
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what is tacrolimus used for?
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potent immunosuppressive used in organ transplant recipients
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what toxicities are associated with tacrolimus?
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significant nephrotoxicity, peripheral neuropathy, hypertension, pleural effusion, hyperglycemia
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this drug is an antimetabolite derivative of 6-mercaptopurine that interferes with the metabolism and synthesis of nucleic acids; it is toxic to proliferating lymphocytes
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azathioprine
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when is azathioprine used?
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kidney transplants; AI disorders including glomerulonephritis and hemolytic anemia
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toxic effects of this drug may be increased by allopurinol
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azathioprine - active metabolite mercaptopurine is metabolized by xanthine oxidase
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what is the major toxicity associated with azathioprine?
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bone marrow suppression
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acetomeniphen metabolite depletes what in the liver?
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glutahione and forms toxic tissue adducts
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low doses of uricosuric agents and salicylates do what to the serum uric acid concentration?
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increase it
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