Immunosuppressants

Question 1

Cyclosporine

Answer 1

1. Post-transplant immunosuppression; select autoimmune disorders 2. Binds to cyclophilins. Complex blocks differentiation and activation of Tcells by inhibiting calcineurin–> preventing production of IL-2 and its receptor 3. Nephrotoxicity, hypertension, hyperlipidemia, hyperglycemia, tremor, gingival hyperplasia, hirsutism 4. Think old man with diabetes who wants to look good for his date so he put in dentures and got hair plugs: old (renal failure, HTN, cholesterol), diabetes (hyperglycemia), dentures (gum hyperplasia), hair plugs (hirsutism, and he is taking the drug because of his hair transplant)

Question 2

Tacrolimus (FK-506)

Answer 2

1. Post- organ transplant immunosuppression; POTENT 2. Binds to FK protein->inhibiting calcineurin->preventing IL-2 3. Nephrotoxicity, hypertension, hyperlipidemia, hyperglycemia, tremor 4. Think old with diabetes who is nervous because he is super sick: old (renal failure, HTN, cholesterol), diabetes (hyperglycemia), nervous (tremor), super sick (strong immunosuppressant)

Question 3

Sirolimus (rapamycin)

Answer 3

1. Immunosuppression post-KIDNEY transplant (Give with cyclosporine); used with drug-eluting stents 2. Inhibits mTOR. Decreased cell proliferation in response to IL-2 3. Hyperlipidemia, thrombocytopenia, leukopenia 4. SIROlimus= SERIOUS complications: immunosuppression

Question 4

Azathioprine

Answer 4

1. Immunosuppression post-KIDNEY transplant; autoimmune disorders (including glomerulonephritis and hemolytic anemia) 2. Antimetabolite. precursor of 6-MP-> decreased synthesis of nucleic acids. Toxic to proliferating lymphocytes. 3. Bone marrow suppression. 4. Active metabolite (mercaptopurine) is metabolized by XO so more toxic when given with Allopurinol

Question 5

Muromonab-CD3 (OKT3)

Answer 5

1. Immunosuppression post-KIDNEY transplant 2. Monoclonal antibody to CD3 on T-cells. Blocks interaction with CD3 protein responsible for T-cell signal transduction 3. Cytokine release syndrome, hypersensitivity reaction 4. Antibodies= hypersensitivity, hypersensitivity= cytokine release -nab= monocolonal antibody therapy (usually)

Question 6

Recombinant Cytokines

Answer 6

Aldesleukin (interleukin-2)Epoetin alfa (erythropoietin)Filgrastim (CSF-G)Sargramostim (CSF-GM)Alpha-InterferonBeta-InterferonGamma-InterferonOprelvekin (interleukin-11)Thrombopoietin

Question 7

Aldesleukin

Answer 7

1. Renal cell carcinoma Metastatic Melanoma 2. Cytokine: Interleukin-2 MOA: increases helper, cytotoxic, and regulatory T cells

Question 8

Epoetin alfa

Answer 8

1. Anemias (esp in renal failure) 2. Cytokine: Erythropoietin MOA: Stimulates Erythrocyte replication

Question 9

Filgrastim

Answer 9

1. Recovery of bone marrow 2. G-CSF (Granulocyte Colony Stimulating Factor)

Question 10

Sargramostim (CSF-GM)

Answer 10

1. Recovery of bone marrow 2. GM-CSF (Granulocyte-Macrophage Colony Stimulating Factor)

Question 11

Alpha-Interferon

Answer 11

1. Hepatitis B and C, Kaposi’s Sarcoma, Leukemia, Malignant Melanoma 2. Inhibit viral protein synthesis and activates NK cells to kill virally infected cells

Question 12

Beta-Interferon

Answer 12

Multiple Sclerosis

Question 13

Gamma-Interferon

Answer 13

1. Chronic Granulomatous disease 2. Activates macrophages and Th1 cells Suppresses Th2 cells. 4. (G)amma = (G)ranulomatous

Question 14

Oprelvekin

Answer 14

1. Thrombocytopenia 2. IL-11

Question 15

Thrombopoietin

Answer 15

Thrombocytopenia

Question 16

Muromonab-CD3 (OKT3)

Answer 16

1. Immunosuppression post-KIDNEY transplant 2. Monoclonal antibody to CD3 on T-cells. Blocks interaction with CD3 responsible for T-cell signal transduction 3. Cytokine release syndrome, hypersensitivity reaction 4. Antibodies= hypersensitivity, hypersensitivity= cytokine release -nab= monocolonal antibody therapy (usually)

Question 17

Digoxin Immune Fab

Answer 17

Target: DigoxinUse: Antidote for Digoxin toxicity

Question 18

Infliximab

Answer 18

Target: TNF-alphaUse: Crohn’s Disease, Rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis

Question 19

Adalimumab

Answer 19

Target: TNF-alphaUse: Crohn’s Disease, Rheumatoid arthritis, psoriatic arthritis

Question 20

Abciximab

Answer 20

Target: Glycoprotien IIb/IIIa Use: Prevent cardiac ischemia in unstable angina and patients treated with percutaneous coronary intervention MOA: Prevents platelet aggregation by inhibiting the platelet-GIIb/IIIa-fibrinogen bonds

Question 21

Trastuzumab (Herceptin)

Answer 21

Target: HER2Use: HER2 overexpressing breast cancer

Question 22

Rituximab

Answer 22

Target: CD20Use: B-cell non-Hodgkin’s lymphoma

Question 23

Omalizumab

Answer 23

Target: IgE Use: Additional treatment for severe asthma