Immunosuppressants

Question 1

Calcineurin

Answer 1

converts NFAT-P to NFAT –> transcribes inflammatory cytokine genes (IL-2)

Question 2

NF-KB

Answer 2

stimulates production of inflammatory cytokine genes

Question 3

IL-2R

Answer 3

Activates mTOR –> proliferation of genes

Question 4

IMP dehydrogenase

Answer 4

Used to make purine nucleotides –> De novo purine synthesis –> DNA replication

Question 5

PRPP amidotransferase

Answer 5

Used to make purine nucleotides –> De novo purine synthesis –> DNA replication

Question 6

Cyclosporine (cyclophilin)

Answer 6

Inhibits calcineurin; bind cyclophilin

Blocks T-cell activation by inhibiting IL-2 transcription

Question 7

Tacrolimus (FK506)

Answer 7

Inhibits calcineurin; binds FK506/FKBP

Blocks T cell activation by also preventing transcription of IL-2 (like cyclosporin)

Question 8

Sirolimus

Answer 8

mTOR inhibitor

Prevents response to IL-2 (cell growth/ gene proliferation)

Question 9

Daclizumab, basiliximab

Answer 9

monoclonal antibody that blocks IL-2 receptor

Question 10

Azathioprine

Answer 10

Antimetabolite precursor of 6-MP

Inhibits PRPP amidotransferase; thereby blocking purine synthesis

Question 11

Mycophenolate mofetil

Answer 11

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

Question 12

Corticosteroids

Answer 12

Inhibit NF-KB; suppresses transcription of many cytokines (suppresses both B and T cells)

Induces apoptosis in T lymphocytes

Question 13

All of these immunosuppressant drugs are used for:

Answer 13

Transplant rejection prophylaxis

Question 14

Cyclosporine- unique uses

Answer 14

prophylaxis, psoriasis, (RA- normally use etanercept –> mab against TNF-alpha)

Question 15

KIDNEY transplant rejection prophylaxis drugs (3)

Answer 15

Sirolimus (Rapamycin) and daclizumab, basiliximab

Question 16

Azathioprine

Answer 16

Used for RA, Crohn, glomerulonephritis, and other autoimmune conditions

Question 17

Mycophenolate mofetil

Answer 17

Used for lupus nephritis

Question 18

Corticosteroids

Answer 18

Autoimmune and inflammatory disorders

Question 19

Cyclosporine vs. Tacrolimus- toxicity

Answer 19

Both are NEPHROTOXIC, neurotoxic

Only cyclosporine causes gingival hyperplasia and hirsuitism

Question 20

Sirolimus- toxicity

Answer 20

Pan”SIR”topenia (pancytopenia)

Not nephrotoxic