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23 Cards in this Set

  • Front
  • Back
tell me about corticosteroid (eg. prednisone/prednisolone) mechanism
enter cell, bind hormone response element on nucleus, LIPOCORTIN INDUCTION, reduce phospholipase A2, reduce inflammatory molecule synthesis (esp prostaglandins!)
what are the good and bad effects of reducing prostaglandins non-selectively (like you do with corticosteroids)?
good = reduce inflammation, fever and pain (so you relieve sx's)

bad = reduce GI mucosal protection (get GI ulcers)
what are the key glucocorticoid uses?
hormone replacement therapy for Addison's dz (adrenal glands do not produce enough steroid hormones)

rheumatoid arthritis, asthma and collagen-based diseases (ie SLE)
what are the short term vs. long term side effects of glucocorticoid therapy?
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)
what type of administration options can be useful with glucocorticoids for:

- allergies
- asthma
- psoriasis
allergies = intermittent administration

asthma-= inhaled administration

psoriasis = topical administration
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)
triamcinolone is a type of:

a. glucocorticoid
b. immunosuppressive
A.
dexamethasone is a type of:

a. glucocorticoid
b. immunosuppressive
A.
what are the 2 major uses for immunosuppression?
1. autoimmune dz's (myasthenia gravis, rheumatoid arthritis)

2. organ transplantion
in immunosuppression, what’s the important molecule that you’re trying to stop action of?
IL-2
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.
name two calcineurin inhibitors and their mechanism, uses, and major SE
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
sirolimus's NOVEL mechanism?
inhibits a different kinase (mTOR kinase) and blocks cell cycle progression (doens't have any effect on calcineurin activity)
main use and SE's of sirolimus
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
which is more readily inhibited by immunosuppressives?

a. primary immune response
b. secondary immune response
A.
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.
how does mycophenolate mofetil work?
selectively inhibits purine synthesis in lymphocytes, blocking their proliferation
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
today, azathioprine has largely been replaced by which drug for immunosuppresion for kidney graft?
mycophenolate mofetil
what are the uses of methotrexate as an immunosuppressant?
rheumatoid arthritis and psoriasis
how do basiliximab and daclizumab work? (hint: they work the same way)
they both are monoclonal Ab drugs used to prevent renal allograft rejection

mech = blocks CD25, the IL-2 receptor (so IL-2 competitive antagonist)
muromonab-CD3 mechanism and use?
binds to the CD3 glycoprotein and prevents kidney and liver transplant acute phase rejection when used in combination with other immunosuppressive drugs
what is the mechanism and use of rituximab?
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.)