56-Immunosuppressants

Question 1

Use of immunosuppressants?

Answer 1

transplantation, autoimmune diseases, inflammatory diseases

Question 2

prednisone equivalent doses?

Answer 2

less than 7.5 low
7.5-30 medium
30-100 high
100-250 very high
over 250 pulse therapy

Question 3

Glucocorticoids

MOA, use, adverse

Answer 3

change gene expression to decrease inflammatory cytokines as well as influencing cell signaling pathways to produce rapid immunosuppression
Transplant rejection, GVHD, autoimmune disorders
growth retardation, infection, slow healing, hyperension, necrosis of bone, cataracts, hyperglycemia, adrenal crisis if rapid stop

Question 4

Cyclosporine

MOA, use, adverse

Answer 4

calcineurin inhibitor that suppresses T cells immunity by blocking IL-2 (T cell growth factor)
prophylaxis for transplant or GVHD
NEPHROTOXICITY, hirsutism, grapefruit juice increases blood concentrations

Question 5

Tacrolimus

MOA, use, adverse

Answer 5

calcineurin inhibitor suppressed T cell immunity(easier to monitor than cyclosporine)
transplant rejection
nephrotoxic, grapefruit juice increases blood concentrations

Question 6

azathioprine

MOA, use, adverse

Answer 6

purine antimetabolite that inhibits lymphocyte proliferation. It is incorporated into DNA inhibiting proliferation. also blocks de novo purine synthesis
bone marrow suppression, VZV and HSV susceptability, lymphoma risk

Question 7

Mycophenolate mofetil

MOA, use, adverse

Answer 7

selective inhibitor of inosine monophosphate dehydrogenase required for de novo synthesis of guanine nucleotides
transplant, lupus
congenital abnormalities

Question 8

sirolimus

MOA, use, adverse

Answer 8

mTOR inhibitor that blocks t-lymphocyte proliferation. blocks G1-Sphase transition
use in combination with cyclosporine and tacrolimus lowers responsive dose
hypokalemia

Question 9

Antithymocyte globulin

MOA, use, adverse

Answer 9

rabbit polyclonal antiserum blocks complement cytotoxicity and inhibits lymphocytes by binding to cell surface
transplants stuff
mimics septic shock

Question 10

Muromonab-cd3

MOA, use, adverse

Answer 10

mouse antibody directed against CD3
transplant
no repeat use because resistance develops; cytokine storm after infusion

Question 11

Anti-TNF-alpha

names, MOA, use, adverse

Answer 11

infliximab (human/mouse), adalimumab (recombinant human IgG), etanercept (human TNF-alpha receptor fused to IgG1)
prevents TNF-alpha from binding to receptors
Crohn’s disease
risk of infections