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Pharm > Immunosuppressants > Flashcards

Immunosuppressants Flashcards

1
Q

Immunosuppressants

A 
Cyclosporine
Tacrolimus (FK-506)
Sirolimus (rapamycin)
Azathioprine
Muromonab-CD3 (OKT3)
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2
Q

Cyclosporine

A
  1. Post-transplant immunosuppression; select autoimmune disorders
  2. Binds to cyclophilins. Complex blocks differentiation and activation of Tcells–> 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)
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3
Q

Tacrolimus (FK-506)

A
  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)
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4
Q

Sirolimus (rapamycin)

A
  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
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5
Q

Azathioprine

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

Muromonab-CD3 (OKT3)

A
  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)
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7
Q

Recombinant Cytokines

A 
Aldesleukin (interleukin-2)
Epoetin alfa (erythropoietin)
Filgrastim (CSF-G)
Sargramostim (CSF-GM)
Alpha-Interferon
Beta-Interferon
Gamma-Interferon
Oprelvekin (interleukin-11)
Thrombopoietin
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8
Q

Aldesleukin

A
  1. Renal cell carcinoma
    Metastatic Melanoma
  2. Cytokine: Interleukin-2
    MOA: increases helper, cytotoxic, and regulatory T cells
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9
Q

Epoetin alfa

A
  1. Anemias (esp in renal failure)
  2. Cytokine: Erythropoietin
    MOA: Stimulates Erythrocyte replication
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10
Q

Filgrastim

A
  1. Recovery of bone marrow

2. GM-CSF (Granulocyte Colony Stimulating Factor)

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11
Q

Sargramostim (CSF-GM)

A
  1. Recovery of bone marrow

2. GM-CSF (Granulocyte-Macrophage Colony Stimulating Factor)

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12
Q

Alpha-Interferon

A 
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
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13
Q

Beta-Interferon

A

Multiple Sclerosis

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14
Q

Gamma-Interferon

A
  1. Chronic Granulomatous disease
  2. Activates macrophages and Th1 cells
    Suppresses Th2 cells.
  3. (G)amma = (G)ranulomatous
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15
Q

Oprelvekin

A
  1. Thrombocytopenia

2. IL-11

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16
Q

Thrombopoietin

A

Thrombocytopenia

17
Q

Theraputic Antibodies

A 
Muromonab-CD3 (OKT3
Digoxin Immune Fab
Infliximab
Adalimumab
Abciximab
Trastuzumab (Herceptin)
Rituximab
Omalizumab
18
Q

Muromonab-CD3 (OKT3)

A
  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)
19
Q

Digoxin Immune Fab

A

Target: Digoxin
Use: Antidote for Digoxin toxicity

20
Q

Infliximab

A

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

21
Q

Adalimumab

A

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

22
Q

Abciximab

A

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

23
Q

Trastuzumab (Herceptin)

A

Target: HER2
Use: HER2 overexpressing breast cancer

24
Q

Rituximab

A

Target: CD20
Use: B-cell non-Hodgkin’s lymphoma

25
Q

Omalizumab

A

Target: IgE
Use: Additional treatment for severe asthma

Pharm (18 decks)

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