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21 Cards in this Set

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Describe the Intracellular signaling via steroid hormones (lipid permeable so passes thru plasma membrane).
Steroid Hormone binds LBD element on steroid receptor causing HSP 90 release. This also causes translocation to the nucleus. Here, the dbd element binds the HRE on DNA leading to Pol II activation and regulation of chromatin structure.
Describe the Physiologic action of Corticosteroids on Metabolism.
Metabolism: protein breakdown & lipolysis in periphery,
gluconeogenesis in liver.
Describe the Physiologic action of Corticosteroids on Na/H2O balance
Salt & water balance: induce NaK ATPase, increased Na retention.
Describe the negative effects of Lack or Excess of Corticosteroids.
Bone: excess causes osteoprosis; CNS: complex effects; Cushingoid Syndrome from Excess
TRUE/FALSE - Corticosteroids block migration of PMNs,reduce IL1, and inhibit IL2.
Name 4 conditions that indicate systemic therapeutic usage of corticosteroids.
RhA, SLE, IBD, Asthma
Name 3 conditions that use Topical corticosteroid usage.
Dermatitis, Urticaria, Asthma
Why is Beclomethasone an important corticosteroid?
Effective inhaled for asthma since it is resistant to the 1st pass effect.
TRUE/FALSE - Cyclosporine, prototype selective immunosuppressant, has prominent primary and secondary immmune effects.
False - only primary via blocking IL2 positive feedback.
Cyclosporine/Cyclophilin Complex works to block IL2 gene expression via what mechanism?
The complex binds calceneurin which is necessary to drive IL 2 expression.
Describe the method of absorption, metabolism and excretion of Cyclosporine .
Oral uptake (can be given by IV) with hepatic metabolism via Cytochrome P450, and biliary excretion.
Describe the role of Tacrolimus and its method of action.
Tacrolimus, an immunosuppressant, binds a different cyclophilin and blocks calcineurin.
Describe the mechanism of Sirolimus.
Blocks TOR which inhibits the T cell response to cytokines.
Often used in drug eluting stents to prevent restenosis.
What is the immunosuppressant drug that inhibits IMP dehydrogenase, necssary in purine synthesis?
Mycophenolate mofetil
What monoclonal antibody drugs block IL2R?
daclizumab, basiliximab
What phase of T cell development does IL2 positive feedback cause?
clonal expansion
TRUE/FALSE - Cytotoxic Agents (e.g. MTX, Cyclophosphamide, Azathioprine)inhibit multiplication of immune stem cells.
TRUE/FALSE - With newer steroids, it is possible to separate out the desired salt/water balance effect, immunesuppressive effect, and the metabolic effect.
False - it has not been posible to separate out the metabolic effect from modern steroids.
TRUE/FALSE - Given the powerful immunosuppressive effect of steroids, the infection risk of chronic users is comparable to immune deficient individuals.
Name some common Corticosteroids.
triamcinolone/Aristocort and Kenalog; dexamethasone/Decadron; hydrocortisone/Hydrocortone and Cortef; methyprednisone/ Methapred and Depo-Medrol.
What is the primary use of cyclosporine? The primary adverse effect of cyclosporine?
Use = sustain renal, hepatic and cardiac transplants; Adverse effect = nephrotoxicity