Copy of Immunosuppressants and Drug Endings - Sheet1 Flashcards
Cyclosporine
- Post-transplant immunosuppression; select autoimmune disorders
- Binds to cyclophilins. Complex blocks differentiation and activation of Tcells by 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)
Tacrolimus (FK-506)
- 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)
Sirolimus (rapamycin)
- 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
Azathioprine
- Immunosuppression post-KIDNEY transplant; autoimmune disorders (including glomerulonephritis and hemolytic anemia)
- Antimetabolite. precursor of 6-MP-> decreased synthesis of nucleic acids. Toxic to proliferating lymphocytes.
- Bone marrow suppression.
- Active metabolite (mercaptopurine) is metabolized by XO so more toxic when given with Allopurinol
Muromonab-CD3 (OKT3)
- Immunosuppression post-KIDNEY transplant
- Monoclonal antibody to CD3 on T-cells. Blocks interaction with CD3 protein responsible for T-cell signal transduction
- Cytokine release syndrome, hypersensitivity reaction
- 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
- Cytokine: Interleukin-2 MOA: increases helper, cytotoxic, and regulatory T cells
Epoetin alfa
- Anemias (esp in renal failure)
- Cytokine: Erythropoietin MOA: Stimulates Erythrocyte replication
Filgrastim
- Recovery of bone marrow
- G-CSF (Granulocyte Colony Stimulating Factor)
Sargramostim (CSF-GM)
- Recovery of bone marrow
- GM-CSF (Granulocyte-Macrophage Colony Stimulating Factor)
Alpha-Interferon
- Hepatitis B and C, Kaposi’s Sarcoma, Leukemia, Malignant Melanoma
- Inhibit viral protein synthesis and activates NK cells to kill virally infected cells
Beta-Interferon
Multiple Sclerosis
Gamma-Interferon
- Chronic Granulomatous disease
- Activates macrophages and Th1 cells Suppresses Th2 cells.
- (G)amma = (G)ranulomatous
Oprelvekin
- Thrombocytopenia
- IL-11
Thrombopoietin
Thrombocytopenia
Muromonab-CD3 (OKT3)
- 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)
Digoxin Immune Fab
Target: Digoxin Use: Antidote for Digoxin toxicity
Infliximab
Target: TNF-alpha Use: Crohn’s Disease, Rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis
Adalimumab
Target: TNF-alpha Use: Crohn’s Disease, Rheumatoid arthritis, psoriatic arthritis
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
Trastuzumab (Herceptin)
Target: HER2 Use: HER2 overexpressing breast cancer
Rituximab
Target: CD20 Use: B-cell non-Hodgkin’s lymphoma
Omalizumab
Target: IgE Use: Additional treatment for severe asthma