Immunosuppressants Flashcards
1
Q
Immunosuppressants
A
Cyclosporine Tacrolimus (FK-506) Sirolimus (rapamycin) Azathioprine Muromonab-CD3 (OKT3)
2
Q
Cyclosporine
A
- Post-transplant immunosuppression; select autoimmune disorders
- Binds to cyclophilins. Complex blocks differentiation and activation of Tcells–> inhibiting calcineurin–> preventing production of IL-2 and its receptor
- Nephrotoxicity, hypertension, hyperlipidemia, hyperglycemia, tremor, gingival hyperplasia, hirsutism
- 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
Q
Tacrolimus (FK-506)
A
- Post- organ transplant immunosuppression; POTENT
- Binds to FK protein->inhibiting calcineurin->preventing IL-2
- Nephrotoxicity, hypertension, hyperlipidemia, hyperglycemia, tremor
- 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
Q
Sirolimus (rapamycin)
A
- Immunosuppression post-KIDNEY transplant (Give with cyclosporine); used with drug-eluting stents
- Inhibits mTOR. Decreased cell proliferation in response to IL-2
- Hyperlipidemia, thrombocytopenia, leukopenia
- SIROlimus= SERIOUS complications: immunosuppression
5
Q
Azathioprine
A
- Immunosuppression post-KIDNEY transplant; autoimmune disorders (including glomerulonephritis and hemolytic anemia)
- Antimetabolite. Blocks 6-mercaptopurine synth-> decreased synthesis of nucleic acids. Toxic to proliferating lymphocytes.
- Bone marrow suppression.
- Active metabolite (mercaptopurine) is metabolized by xanthine oxidase so more toxic when given with allopurinol
6
Q
Muromonab-CD3 (OKT3)
A
- Immunosuppression post-KIDNEY transplant
- Monoclonal antibody to CD3 on T-cells. Blocks interaction with CD3 responsible for T-cell signal transduction
- Cytokine release syndrome, hypersensitivity reaction
- Antibodies= hypersensitivity, hypersensitivity= cytokine release
- nab= monocolonal antibody therapy (usually)
8
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
9
Q
Aldesleukin
A
- Renal cell carcinoma
Metastatic Melanoma - Cytokine: Interleukin-2
MOA: increases helper, cytotoxic, and regulatory T cells
10
Q
Epoetin alfa
A
- Anemias (esp in renal failure)
- Cytokine: Erythropoietin
MOA: Stimulates Erythrocyte replication
11
Q
Filgrastim
A
- Recovery of bone marrow
2. GM-CSF (Granulocyte Colony Stimulating Factor)
12
Q
Sargramostim (CSF-GM)
A
- Recovery of bone marrow
2. GM-CSF (Granulocyte-Macrophage Colony Stimulating Factor)
13
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
14
Q
Beta-Interferon
A
Multiple Sclerosis
15
Q
Gamma-Interferon
A
- Chronic Granulomatous disease
- Activates macrophages and Th1 cells
Suppresses Th2 cells. - (G)amma = (G)ranulomatous
16
Q
Oprelvekin
A
- Thrombocytopenia
2. IL-11
17
Q
Thrombopoietin
A
Thrombocytopenia
19
Q
Theraputic Antibodies
A
Muromonab-CD3 (OKT3 Digoxin Immune Fab Infliximab Adalimumab Abciximab Trastuzumab (Herceptin) Rituximab Omalizumab
20
Q
Muromonab-CD3 (OKT3)
A
- Immunosuppression post-KIDNEY transplant
- Monoclonal antibody to CD3 on T-cells. Blocks interaction with CD3 responsible for T-cell signal transduction
- Cytokine release syndrome, hypersensitivity reaction
- Antibodies= hypersensitivity, hypersensitivity= cytokine release
- nab= monocolonal antibody therapy (usually)
21
Q
Digoxin Immune Fab
A
Target: Digoxin
Use: Antidote for Digoxin toxicity
