Immunosuppressants

Question 1

Cyclosporine mech

Answer 1

Calcineurin inhibitor; binds cyclophilin. Blocks T cell activation by preventing IL-2 TRANSCRIPTION.

Question 2

Cyclosporine use:

Answer 2

Transplant rejection, prophylaxis, psoriasis, rheumatoid arthritis

Question 3

Cyclosporine Toxicity:

Answer 3

NEPHROTOXICITY, HTN, hyperlipidemia, hyperglycemia, tremor, hirsutism, gingival hyperplasia

Question 4

Tacrolimus mech:

Answer 4

Calcineurin inhibitor; binds FK506 binding protein (FKBP). Blocks T cell activation by preventing IL-2 transcription.

Question 5

Tacrolimus use:

Answer 5

Transplant rejection prophylaxis

Question 6

Tacrolimus Toxicity:

Answer 6

Similar to cyclosporine, increased risk of diabetes and neurotoxicity; no ginigival hyperplasia or hirsutism.

Question 7

Siroliums (Rapamycin) mech:

Answer 7

mTOR inhibitor; binds FKBP. Blocks T cell activation and B cell differentiation by preventing IL-2 signal transduction.

Question 8

Sirolimus (Rapamycin) use:

Answer 8

Kidney transplant rejection prophylaxis

Question 9

Sirolimus (Rapamycin) toxicity:

Answer 9

Anemia, thrombocytopenia, leukopenia, insulin resistance, hyperlipidemia; NON-NEPHROTOXIC.

Question 10

Sirolimus notes:

Answer 10

Kidney ‘sir-vives’. synergistic with cyclosporine. Also used in drug-eluting stents.

Question 11

Basiliximab mech:

Answer 11

monoclonal antibody; blocks IL-2R

Question 12

Basiliximab use:

Answer 12

kidney transplant rejection prophylaxis.

Question 13

Basiliximab toxicity:

Answer 13

Edema, HTN, tremor

Question 14

Azathiprine mech

Answer 14

Antimetabolite precursor of 6-MP. Inhibits lymphocyte proliferation by blocking nucleotide synthesis.

Question 15

Azathioprine clinical use:

Answer 15

Transplant rejection prophylaxis, rhematoid arthritis, Crohn disease, glomerolonephritis, other autoimmune conditions

Question 16

Azathioprine toxicity:

Answer 16

Leukopenia, anemia, thrombocytopenia

Question 17

Azathioprine additional notes:

Answer 17

6-MP degraded by xanthine oxidase; toxicity increased by allopurinol. pronounced ‘azathioPURINE’

Question 18

Glucocorticoids mech

Answer 18

inhibit NF-kB. Suppress both B and T cell function by decreasing transcription of many cytokines.

Question 19

Glucocorticoids use:

Answer 19

Transplant rejection prophylaxis (immune suppression), many autoimmune disorders, inflammation

Question 20

Glucocorticoids toxicity:

Answer 20

Hyperglycemia, osteoporosis, central obestity, muscle breakdown, psychosis, acne, HTN, cataracts, peptic ulcers

Question 21

Epoetin alfa (erythropoietin) use:

Answer 21

Anemias (especially renal failure

Question 22

Thrombopoietin:

Answer 22

Thrombocytopenia

Question 23

Oprelvekin (IL-11) use:

Answer 23

Thrombocytopenia

Question 24

Filgrastim (granulocyte colony stimulating factor) use:

Answer 24

Recovery of bone marrow

Question 25

Sargramostim (granulocyte-macrophage colony stimulating factor) use:

Answer 25

Recovery of bone marrow

Question 26

Aldesleukin use:

Answer 26

IL-2; RCC, metastatic melanoma

Question 27

IFN alpha:

Answer 27

Chronic Hep B and C, Kaposi Sarcoma, Kaposi Sarcoma, Hairy Cell Leukemia, Condyloma Acuminatum, RCC, malignant melanoma

Question 28

IFN beta:

Answer 28

MS

Question 29

IFN gamma

Answer 29

Chronic granulomatous disease

Question 30

Therapeutic antibodies Are next

Answer 30

.....

Question 31

Alemtuzumab

Answer 31

TARGET: CD52, Use: CLL, Notes: 'ALYMtuzumab' - chronic LYMphocytic leukemia

Question 32

Bevacizumab

Answer 32

TARGET: VEGF. Use: Colorectal cancer, RCC

Question 33

Cetuximab

Answer 33

Target: EGFR. USE: Stage IV colorectal cancer, head and neck cancer

Question 34

Rituximab

Answer 34

Target CD20. USE: B-cell non-hodgkin lymphoma, rheumatoid arthritis (with MTX), ITP

Question 35

Trastuzumab

Answer 35

Target: HER2/neu. USE: Breast cancer, gastric cancer. Notes: Tras2zumab

Question 36

Autoimmune disease therapy:

Answer 36

infliximab, adalimuab, nataliziumab

Question 37

INFLIXimab and aDALIMumab

Answer 37

Target: TNF-alpha. USE: IBD, rheumatoid arthritis, ankylosing spondylitis, psoriasis

Question 38

Natalizumab

Answer 38

Target: alpha4-integrin (leukocyte adhesion). Use: MS, Crohn disease. RISK OF PML IN PATIENTS WITH JC VIRUS

Question 39

Abciximab

Answer 39

Target: Glycoprotein IIb/IIIa. Clinical Use: anti-platelet agent for prevention of ischemic complications in patients undergoing percutaneous coronary intervention. NOTE: IIb times IIIa = abSIXimab

Question 40

Denosumab

Answer 40

Target: RANKL. osteoporosis; inhibits osteoclast maturation (mimics OPG)

Question 41

Digoxin immune Fab

Answer 41

Target: digoxin. Use: Antidote for digoxin toxicity

Question 42

Omalizumab

Answer 42

Use: Allergic asthma; prevents IgE binding to FcERI

Question 43

Palivizumab

Answer 43

Target: RSV F protein. USE: RSV prophylaxis for high risk infants. paliVIzumab for VIrus