Immunosuppr Rx Flashcards
Immunosuppressants
Cyclosporine Tacrolimus (FK-506) Sirolimus (rapamycin) Azathioprine Muromonab-CD3 (OKT3)
Cyclosporine
- 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)
Tacrolimus (FK-506)
- 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)
Sirolimus (rapamycin)
- 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
Azathioprine
- 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
Muromonab-CD3 (OKT3)
- 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)
Recombinant Cytokines
Aldesleukin (interleukin-2) Epoetin alfa (erythropoietin) Filgrastim (CSF-G) Sargramostim (CSF-GM) Alpha-Interferon Beta-Interferon Gamma-Interferon Oprelvekin (interleukin-11) Thrombopoietin
Aldesleukin
- Renal cell carcinoma Metastatic Melanoma 2. Cytokine: Interleukin-2 MOA: increases helper, cytotoxic, and regulatory T cells
Epoetin alfa
- Anemias (esp in renal failure) 2. Cytokine: Erythropoietin MOA: Stimulates Erythrocyte replication
Filgrastim
- Recovery of bone marrow 2. GM-CSF (Granulocyte Colony Stimulating Factor)
Sargramostim (CSF-GM)
- Recovery of bone marrow 2. GM-CSF (Granulocyte-Macrophage Colony Stimulating Factor)
Alpha-Interferon
- Hepatitis B and C Kaposi’s Sarcoma Leukemia Malignant Melanoma 2. Inhibit viral protein synthesis and activates NK cells to kill virally infected cells
Beta-Interferon
Multiple Sclerosis
Gamma-Interferon
- Chronic Granulomatous disease 2. Activates macrophages and Th1 cells Suppresses Th2 cells. 4. (G)amma = (G)ranulomatous
Oprelvekin
- Thrombocytopenia 2. IL-11
Thrombopoietin
Thrombocytopenia
Theraputic Antibodies
Muromonab-CD3 (OKT3 Digoxin Immune Fab Infliximab Adalimumab Abciximab Trastuzumab (Herceptin) Rituximab Omalizumab
Muromonab-CD3 (OKT3)
- 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)
Digoxin Immune Fab
Target: Digoxin Use: Antidote for Digoxin toxicity