Immunosuppressants - Pharm

Question 0

Mechanism: Calcineurin inhibitor; binds cyclophilin. Blocks T-cell activation by preventing IL-2 transcription.
Use: Transplant rejection prophylaxis, psoriasis, rheumatoid arthritis.
Toxicity: Nephrotoxicity, hypertension, hyperlipidemia, hyperglycemia, tremor, hirsutism, gingival hyperplasia.

Answer 0

Cyclosporine

Question 1

Mechanism: Calcineurin inhibitor; binds FK506 binding protein (FKBP). Blocks T cell activation by preventing IL-2 transcription.
Use: Transplant rejection prophylaxis
Toxicity: Anemia, cyclosporine, increased risk of diabetes and neurotoxicity; no gingival hyperplasia.

Answer 1

Tacrolimus

Question 2

Mechanism: mTOR inhibitor; binds FKBP. Blocks T cell activation and B cell differentiation by preventing IL-2 signal transduction.
Use: kidney transplant rejection prophylaxis
Toxicity: Anemia, thrombocytopenia, leukopenia, insulin resistance, hyperlipidemia, non-nephrotoxic.

Answer 2

Sirolimus (Rapamycin)

Question 3

Mechanism: Monoclonal antibody; blocks IL-2R.
Use: Kidney transplant rejection prophylaxis.
Toxicity: Edema, hypertension, tremor.

Answer 3

Basiliximab

Question 4

Mechanism: Antimetabolite precursor of 6-mercaptopurine. Inhibits lymphocyte proliferation by blocking nucleotide synthesis.
Use: transplant rejection prophylaxis, rheumatoid arthritis, Crohn’s disease, glomerulonephritis, other autoimmune conditions.
Toxicity: Leukopenia, anemia, thrombocytopenia.
Notes: 6-MP degraded by xanthine oxidase; toxicity increased by allopurinol.

Answer 4

Azathioprine

Question 5

Mechanism: Inhibit NF-kB. Suppress both B and T cell function by decreasing transcription of many cytokines.
Use: transplant rejection prophylaxis (immune suppression), many autoimmune disorders, inflammation.
Toxicity:Hyperglycemia, osteoporosis, central obesity, muscle breakdown, psychosis, acne, hypertension, cataracts, peptic ulcers.

Answer 5

Glucocorticoids

Question 6

Recombinant Cytokines:
Agent: Epoetin alpha (erythropoietin)
Clinical use:?

Answer 6

Clinical uses: Anemias (especially in renal failure).

Question 7

Recombinant Cytokines:
Agent: Oprelvekin (interleukin-11)
Clinical use:?

Answer 7

Clinical uses: Thrombocytopenia

Question 8

Recombinant Cytokines:
Agent: Filgrastim (granulocyte colony-stimulating factor).
Clinical uses:?

Answer 8

Clinical uses: Recovery of bone marrow

Question 9

Recombinant Cytokines:
Agent: Sargramostim (granulocyte-macrophage colony-stimulating factor).
Clinical uses:?

Answer 9

Clinical uses: Recovery of bone marrow

Question 10

Recombinant Cytokines:
Agent: Aldesleukin (interleukin-2)
Clinical uses:?

Answer 10

Clinical uses: Renal cell carcinoma, metastatic melanoma

Question 11

Recombinant Cytokines:
Agent: IFN-alpha
Clinical uses:?

Answer 11

Clinical uses: chronic hepatitis B and C, Kaposi sarcoma, hairy cell leukemia, condyloma acuminatum, renal cell carcinoma, malignant melanoma.

Question 12

Recombinant Cytokines:
Agent: IFN-beta
Clinical uses:?

Answer 12

Clinical use: multiple sclerosis

Question 13

Recombinant Cytokines:
Agent: IFN-gamma
Clinical uses:?

Answer 13

Clinical uses: chronic granulomatous disease

Question 14

Therapeutic antibodies:
Target: CD52
Clinical use: CLL
Notes: chronic lymphocytic leukemia

Answer 14

Cancer Therapy:

Alemtuzumab

Question 15

Therapeutic antibodies:
Target: VEGF (Vascular endothelial growth factor)
Clinical use: Colorectal Cancer, renal cell carcinoma

Answer 15

Cancer Therapy:

Bevacizumab

Question 16

Therapeutic antibodies:
Target: EGFR (Epidermal growth factor receptor)
Clinical use: Stage IV colorectal cancer, head and neck cancer.

Answer 16

Cancer therapy:

Cetuximab

Question 17

Therapeutic antibodies:
Target: CD20
Clinical use: B-cell non-Hodgkin lymphoma, rheumatoid arthritis (with MTX), ITP
Notes:

Answer 17

Cancer therapy:

Rituximab

Question 18

Therapeutic antibodies:
Target: HER2/neu
Clinical use: Breast cancer, gastric cancer

Answer 18

Cancer therapy:

Transtuzumab

Question 19

Therapeutic antibodies:
Target: TNF-alpha
Clinical use: IBD, rheumatoid arthritis, ankylosing spondylitis, psoriasis
Notes: rheumatoid arthritis

Answer 19

Autoimmune disease therapy:
Infliximab, adalimumab
Certolizumab, golimumab

Question 20

Therapeutic antibodies:
Target: Alpha4-integrin
Clinical use: multiple sclerosis, Crohn disease
Notes: alpha-4-integrin: leukocyte adhesion. Risk of PML in Px with JC Virus.

Answer 20

Autoimmune disease therapy:

Natalizumab

Question 21

Therapeutic antibodies:
Target: Glycoprotein IIb/IIIa
Clinical use: Anti-platelet agent for prevention of ischemic complications in Px undergoing percutaneous coronary intervention.
Notes: IIb times IIIa equals “xxxxx”

Answer 21

Other:

Abciximab

Question 22

Therapeutic antibodies:
Target: RANKL
Clinical use: Osteoporosis; inhibits osteoclast maturation (mimics osteoprotegrin)

Answer 22

Other:

Denosumab

Question 23

Therapeutic antibodies:
Target: Digoxin
Clinical use: Antidote for digoxin toxicity

Answer 23

Other:

Digoxin immune Fab

Question 24

Therapeutic antibodies:
Target: IgE
Clinical use: Allergic asthma; prevents IgE binding to FcERI

Answer 24

Other:

Omalizumab

Question 25

Therapeutic antibodies:
Target: RSV F protein
Clinical use: RSV prophylaxis for high-risk infants.

Answer 25

Other:

Palivizumab

Question 26

What are the SE of Basiliximab??

Answer 26

Edema, hypertension, and tremor