Immunosuppressants

Question 1

Cyclosporine

Answer 1

Calcineurin inhibitor, binds cyclophilin

Blocks T-cell activation by preventing IL-2 transcription

Question 2

Toxicity of cyclosporine:

Answer 2

NEPHROTOXICITY, HTN, hyperlipidemia, neurotoxicity, GINGIVAL HYPERPLASIA, hirsutism

Question 3

Tacrolimus

Answer 3

Calcineurin inhibitor, binds FK506 binding protein (FKBP)

Blocks T-cell action by preventing IL-2 transcription

Question 4

Toxicity of Tacrolimus:

Answer 4

NEPHROTOXICITY, increased risk of DM, neurotoxicity

Question 5

Sirolimus (rapamycin):

Answer 5

mTOR inhibitor, binds FKBP

Blocks T-cell and B-cell activation differentiation by preventing response to IL-2

Also used in drug-eluting stents by blocking the G1 to S phase to prevent smooth muscle proliferation

Question 6

Sirolimus Toxicity:

Answer 6

Pancytopenia, insulin resistance, hyperlipidemia

Question 7

Basiliximab

Answer 7

Monoclonal Ab; blocks Il-2R

Question 8

Basiliximab Toxicity:

Answer 8

Edema, HTN, tremor

Question 9

Azathioprine

Answer 9

Antimetabolite of 6-MP

Inhibit lymphocyte proliferation by blocking nucleotide synthesis

Degraded by xanthine oxidase, so allopurinol increases risk for toxicity

Question 10

Azathiprine Toxicity:

Answer 10

Pancytopenia

Question 11

Mycophenolate Mofetil

Answer 11

Reversibly inhibits IMP dehydrogenase preventing purine synthesis of B and T cells

Question 12

Toxicity of Mycophenolate Mofetil:

Answer 12

GI upset, pancytopenia, HTN, hyperglycemia

Question 13

Glucocorticoids

Answer 13

Inhibits NF-kB

Suppresses both B and T cell function by decreasing the transcription of many cytokines

Induce T-cell apoptosis

Question 14

Toxicity of Glucocorticoids:

Answer 14

Cushing syndrome, osteoporosis, hyperglycemia, DM, amenorrhea, atrophy, peptic ulcers, psychosis, cataracts, avascular necrosis of the femoral head