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39 Cards in this Set

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