MSK 1 (pharm)
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| what is the mechanism of opiod analgesics? | act as agonists at opiod receptors to modulate synaptic transmission
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| what opiod works at the mu receptor? | morphine
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| what opiod works at the delta receptor? | enkephalin
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| what opoid workds at the kappa receptor? | dynorphin
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| how do you treat opiod toxicity? | naloxone or naltrexone (opiod receptor antagonists)
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| what is contraindicated in morphine overdose? | O2 - might contribute to respiratory failure
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| toxicity of opiods? | respiratory depression, miosis (pinpoint pupils), additive CNS depression with other drugs, constipation, addiction
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| how do NSAIDs work? | reversibly inhibit COX-1 and COX-2; block prostaglandin synthesis
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| what is used to close a PDA? | indomethacin
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| toxicity of NSAIDs? | renal damage, aplastic anemia, GI distress, ulcers
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| how do celecoxib, valdecoxib work? | 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? | spares COX-1, which helps maintain the gastric mucosa
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| what are COX 2 inhibitors used for? | rheumatoid and osteoarthritis
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| what is the mechanism of acetominaphen? | reversibly inhibits cyclooxygenase, mostly in CNS; inactivated peripherally
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| what is the antidote for acetominaphen toxicity? | N-acetylcysteine
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| what drug is used for acute gout? | colchicine
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| this gout drug depolymerizes microtubules, impairing leukocyte chemotaxis and degranulation | colchicine
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| what acute gout drug is less toxic than colchicine and therefore is used more frequently? | indomethacin
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| this drug is used for chronic gout - it inhibits resorption of uric acid | probenecid
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| what gout drug inhibits secretion of penicillin? | probenecid
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| 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)
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| what gout drug is also used in lymphoma and leukemia to revent tumor lysis-associated nephropathy? | allopurinol
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| what is etanercept? | recombinant form of human TNF receptor that binds TNF-alpha
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| what is etanercept used for? | RA, psoriasis, ankylosing spondylitis
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| what is infliximab? | TNF-alpha antibody
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| what is infliximab used for? | 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 | cyclosporine
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| when is cyclosporine used? | suppresses organ rejection after transplantation; selected AI disorders
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| the nephrotoxicity associated with cyclosporine is preventable with what? | mannitol diuresis
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| what toxicity is associated with cyclosporine? | 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? | 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? | potent immunosuppressive used in organ transplant recipients
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| what toxicities are associated with tacrolimus? | 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 | azathioprine
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| when is azathioprine used? | kidney transplants; AI disorders including glomerulonephritis and hemolytic anemia
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| toxic effects of this drug may be increased by allopurinol | azathioprine - active metabolite mercaptopurine is metabolized by xanthine oxidase
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| what is the major toxicity associated with azathioprine? | bone marrow suppression
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| acetomeniphen metabolite depletes what in the liver? | 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? | increase it
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| what type of ossification is not affected in achondroplasia? | membranous - skull, facial bones, and axial skeleton are normal
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