Immunosuppressants

Question 1

Cyclosporine - MOA

Answer 1

Calcineurin inhibitor - binds cyclophilin and blocks T cell activation by preventing IL-2 transcription

Question 2

Cyclosporine - Use

Answer 2

Transplant rejection prophylaxis, psoriasis, RA, autoimmune disorders

Question 3

Cyclosporine - Toxicity

Answer 3

Nephrotoxicity - bc vasoconstriction of AFF and EFF in kidney; also predisposes patient to viral infections and Lymphomas; hypertension, hyperlipidemia, hyperglycemia, hirsutism, gingival hyperplasia

Question 4

Tacrolimus - MOA

Answer 4

Calcineurin inhibitor - binds FK506 binding protein - prevents IL 2 transcription

Question 5

Tacrolimus - Use

Answer 5

Trasplant rejection prophylaxis

Question 6

Tacrolimus - Toxicity

Answer 6

Nephro AND neuro! causes HTN. NO gingival hyperplasia or hirsutism

Question 7

Sirolimus (Rapamycin) - MOA

Answer 7

Binds to FKBP and inhibits mTOR and prevents IL-2 signal transduction

Question 8

Sirolimus - Use

Answer 8

Kidney transplant, rejection

Question 9

Sirolimus - toxicity

Answer 9

not too important but it is NOT nephrotoxic!!!!!

Question 10

Azathioprine - MOA

Answer 10

Antimetabolite precursor of 6-mercaptopurine - inhibits lymphocytes proliferation by blocking nucleotide synthesis

Question 11

Azathioprine - Use

Answer 11

Tranplant rejection, glomerulonephritis

Question 12

Azathioprine - Toxicity

Answer 12

Bone Marrow suppression - ALSO is degraded by xanthine oxidase therefore increased toxicity by allopurinol