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23 Cards in this Set
- Front
- Back
tell me about corticosteroid (eg. prednisone/prednisolone) mechanism
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enter cell, bind hormone response element on nucleus, LIPOCORTIN INDUCTION, reduce phospholipase A2, reduce inflammatory molecule synthesis (esp prostaglandins!)
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what are the good and bad effects of reducing prostaglandins non-selectively (like you do with corticosteroids)?
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good = reduce inflammation, fever and pain (so you relieve sx's)
bad = reduce GI mucosal protection (get GI ulcers) |
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what are the key glucocorticoid uses?
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hormone replacement therapy for Addison's dz (adrenal glands do not produce enough steroid hormones)
rheumatoid arthritis, asthma and collagen-based diseases (ie SLE) |
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what are the short term vs. long term side effects of glucocorticoid therapy?
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short term = none
long term = 1) cushingoid syndromes - Muscle weakness (dec muscle mass), central obesity, moon face, abd stria, glucose intolerance, neuropsychiatric disorders. 2) immunosuppression (increase risk of infection) 3) peptic ulcers (esp in pts with high dose/long-term steroid therapy, hx of peptic ulcer, concomitant NSAID use) 4) skeletal effects (osteoporosis, osteonecrosis) |
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what type of administration options can be useful with glucocorticoids for:
- allergies - asthma - psoriasis |
allergies = intermittent administration
asthma-= inhaled administration psoriasis = topical administration |
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in terms of withdrawal from glucocorticoid therapy:
a. what is the most FREQUENT problem? b. what is the most SEVERE problem? |
frequent = "flare-up" of the dz
severe = acute adrenal insufficiency, resulting from too rapid withdrawal of glucocorticoids (SO YOU MUST WITHDRAW CAREFULLY OVER TIME) |
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triamcinolone is a type of:
a. glucocorticoid b. immunosuppressive |
A.
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dexamethasone is a type of:
a. glucocorticoid b. immunosuppressive |
A.
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what are the 2 major uses for immunosuppression?
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1. autoimmune dz's (myasthenia gravis, rheumatoid arthritis)
2. organ transplantion |
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in immunosuppression, what’s the important molecule that you’re trying to stop action of?
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IL-2
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prednisone & prednisolone, in addition to being a glucocorticoid, are also useful immunosuppressives.
what is their mechanism, uses, and SEs? |
mech = suppress T cell resp to antigens/mitogens; inhibit IL-2 synthesis
uses = SLE, polymyositis/dermatomyositis SEs = cushingoid syndrome, etc. |
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name two calcineurin inhibitors and their mechanism, uses, and major SE
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cyclosporin, tacrolimus
mech = block calcineurin--> inhibiting IL-2 production by T cells and inhibits further T cell signaling (aka. they block T cell signal transduction via ser/thr phosphatase inhibition) use = kidney, liver, heart, lung tranplants major SE = nephrotoxicity (dose-limiting, meaning that we may not give enough for a good effect) REMEMBER THAT TACROLIMUS IS 100X MORE POTENT THAN CYCLOSPORIN |
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sirolimus's NOVEL mechanism?
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inhibits a different kinase (mTOR kinase) and blocks cell cycle progression (doens't have any effect on calcineurin activity)
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main use and SE's of sirolimus
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main use is kidney transplants
SE = less nephrotoxicity than tacrolimus/cyclosporin (which is good, so use it for kidney transplants) bad for liver and lung transplants |
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which is more readily inhibited by immunosuppressives?
a. primary immune response b. secondary immune response |
A.
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which drugs provide both anti-inflammatory and immunosuppressive activity?
a. calcineurin inhibitors, b. adrenocorticosteroids c. IL-2 receptor blockers d. none of the above |
B.
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how does mycophenolate mofetil work?
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selectively inhibits purine synthesis in lymphocytes, blocking their proliferation
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what is mycophenolate mofetil used for?
SEs? |
used in combo with cyclosporin and corticosteroids for RENAL GRAFTS
-also used for SLE and rheumatoid arthritis SEs: GI (diarrhea/vomiting) and he |
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today, azathioprine has largely been replaced by which drug for immunosuppresion for kidney graft?
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mycophenolate mofetil
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what are the uses of methotrexate as an immunosuppressant?
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rheumatoid arthritis and psoriasis
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how do basiliximab and daclizumab work? (hint: they work the same way)
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they both are monoclonal Ab drugs used to prevent renal allograft rejection
mech = blocks CD25, the IL-2 receptor (so IL-2 competitive antagonist) |
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muromonab-CD3 mechanism and use?
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binds to the CD3 glycoprotein and prevents kidney and liver transplant acute phase rejection when used in combination with other immunosuppressive drugs
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what is the mechanism and use of rituximab?
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use = tx of B cell non-Hodgkin's lymphoma
mech = binds to CD20 antigen on >90% of B-cell non-Hodgkin's lymphomas (remember that CD20 is expressed on the surface of all mature B-cells.) |