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41 Cards in this Set

  • Front
  • Back
Autoimmune diseases that show responsiveness to immunosuppression
acute glommerulonephrits
autoimmune hemolytic anemia
billion dollar drugs
b/c dramatic increase in succes of transplantations
cyclosporin and tacrolimus target the same element. That element is?
Calcineurin in T Cell

Inhibt dephosphorylation of NFAT and thus production of cytokines
Tacolimus compared to cyclosporine A
100x more potent
Solubility of Cyclosporin and Tacrolimus
Cyclo needs to be solublized, Tacro already is
Which drugs has a wide distribution and large accumulation in leukocytes
cyclosporing or tacrolimus: which has fewer side effects

it is more potent so smaller doses needed
Drug interactions with cyclosporin and tacrolimus
Drugs that up P450 clear it faster (phenobarbital, phenytoin, trimethoprim, rifampin)

Vice versa (ampotericin B, erthyomycin, ketoconazole)
Main reason for sccesion of cyclosporin therapy
renal toxicity
diurnal fluctuation in adrenocortico steroids
Fluctuates with cortisol, not aldosterone
The main use of ACTH in clinical settings
Identify patients needing supplemental steroid coverage during stress
Immune mediators without corticosteroids
lead to vasodilation and cardiovascular collapse
Muscle weakness in Addison's vs Cushings
Addisons because steroids necessary for normal function. In cushings, muscles weakness from protein breakdown
Cortisol's effect on the cardiovascular system
Potentia beta adrengergic effects...hypertension
Time after single dose of cortison to supprssion of lympocytes, eosinophils, monocytes and basophils
4-6 hours
Cortisol's method of reducing prostaglandin and leukotriene production
inhibition of phospholipase A2
Electrolyte effects in a pateint with hyperaldrosterone
Steriod with higher Na retaining potency
Steroids with isolated anti-inflammatory and immunosuppression (not mineralcorticoid)

6alpha- methylyprednisolone
11-beta hydroxysteroid dehydrogenase
at mineralcorticoid receptors reduces cortisol to cortisone and which has no mineralcorticoid effects
steroid that seperates metabolic and antifinflammatory effects
None, they are mediated through the same receptor
Flourination at 9 postition ring B
vastaly increases mineralcorticoid activity
Flourination at 9 plus 1,2 double bond A ring
increases glucocorticoid but nto mineral corticoid
double bond at 1,2 positioin on A ring
increases glucocorticoid action 4 times over mineral corticoid action
Two concers with toxicity of steroids
Supraphysiological dose effects (associate complications of steroids)
Effects of steroids on bones
inhibt osteoblasts
inhibit Ca absorption in gut
increase PTH secretion
Effectso f steroids on eyes
Four cytotoxic drugs for immune therapy
Mycophenolate Mofetil
Method of action for azothiprine

Method of delivery
inhibts de novo and salavage pathway puring synthesis

Mycophenolate Mofetil
inhbits inosine monophorphate deyhydrogenase

De nove synthesis inhibitor
difference between mycophenolate mofetil and azothioprine
Mycophenolate mofetil is more selective to T and B cells which rely heavily on de novo synthesis
Specific organ transplanation that mycophenolate mefatil is used in
Cyclophosphamide is used for
suppression of humoral immunity

supress lymphoid elements in bone marrow patients

short use only
Methotrexate works by inhibiting?
dihydropfolate reductase

inhibits purines, thymidylate and methionin
Medical use for methotrexate
autoimmune disease like arthritis
Sirolimus binds to the same protein as what other drugs
Though it uses the same protein at Tacrolimus, what is Sirolimus's mechanism of action
Blocks cell from progressing through late G1 to S phase
Alternate use for Sirolimus
For implantation of stents

Inhibits vascular smooth muscle proliferation
Major side effects of Sirolimus
exaceraet hyperlipidemia
Nephrotoxicity of sirolimus
no direct toxicity but increases toxicity of cyclosporine and tacrolimus