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Flashcards in Immunosuppressants Deck (48)
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1

Immunosuppressants

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

2

Cyclosporine

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)

3

Tacrolimus (FK-506)

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)

4

Sirolimus (rapamycin)

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

5

Azathioprine

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

6

Muromonab-CD3 (OKT3)

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)

8

Recombinant Cytokines

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

9

Aldesleukin

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

10

Epoetin alfa

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

11

Filgrastim

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

12

Sargramostim (CSF-GM)

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

13

Alpha-Interferon

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

14

Beta-Interferon

Multiple Sclerosis

15

Gamma-Interferon

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

16

Oprelvekin

1. Thrombocytopenia
2. IL-11

17

Thrombopoietin

Thrombocytopenia

19

Theraputic Antibodies

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

20

Muromonab-CD3 (OKT3)

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)

21

Digoxin Immune Fab

Target: Digoxin
Use: Antidote for Digoxin toxicity

22

Infliximab

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

23

Adalimumab

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

24

Abciximab

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

25

Trastuzumab (Herceptin)

Target: HER2
Use: HER2 overexpressing breast cancer

26

Rituximab

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

27

Omalizumab

Target: IgE
Use: Additional treatment for severe asthma

30

-azole

Antifungal
Ex: Ketoconazole

31

-cillin

Penicillin
Ex: Methicillin

32

-cycline

Antibiotic, protein synthesis inhibitor
Ex: Tetracycline

33

-navir

Antibiotic, protease inhibitor
Ex: Saqyubavir

35

-triptan

5-HT 1B/1D agonists (for migranes)
Ex: Sumatriptan