Immunosuppressants Flashcards
Cyclosporine MOA
Binds to cyclophilins. Complex blocks the differentiation and activation of T cells by inhibiting calcineurin, thus preventing the production of IL-2 and its receptor
Cyclosporine Clinical Use
Suppresses organ rejection after transplantation, selected autoimmune disorders
Cyclosporine Toxicity
Nephrotoxicity HTN Hyperlipidemia Hyperglycemia Tremor Gingival hyperplasia Hirsutism
Tacrolimus MOA
Similar to Cyclosporine
Binds to FK-binding protein, inhibiting calcineurin and secretion of IL-2 and other cytokines
Tacrolimus Clinical Use
Potent immunosuppressive use in organ transplant recipients
Tacrolimus Toxicity
Nephrotoxicity HTN Hyperlipidemia Hyperglycemia Tremor
Sirolimus MOA
Inhibits mTOR
Inhibits T cell proliferation in response to IL2
Sirolimus Clinical Use
Immunosupression after kidney transplantation in combo with cyclosporine and corticosteroids
Drug-eluting stents
Sirolimus Toxicity
Hyperlipidemia
Thrombocytopenia
Leukopenia
Azathioprine MOA
Antimetabolite precursor of 6-mercaptopurine that interferes with the metabolism and synthesis of nucleic acids
Toxic to proliferating lymphocytes
Azathioprine Clinical Use
Kidney transplantation Autoimmune disorders (glomerulonephritis and hemolytic anemia)
Azathioprine Toxicity
Bone marrow suppression
Active metabolite mercaptopurine is metabolized by xanthine oxidase so toxic effects can be increased by allopurinol
Muromonab-CD3 (OKT3) MOA
Monoclonal Ab that binds to CD3 (epsilon chain) on the surface of T cells. Blocks cellular interaction with CD3 protein responsible for T-cell signal transduction
Muromonab-CD3 (OKT3) Clinical Use
Immunosuppression after kidney transplantation
Muromonab-CD3 (OKT3) Toxicity
Cytokine release syndrome
Hypersensitivity reaction
Aldesleukin
IL-2 (anti-tumor)
Renal Cell Carcinoma
Metastatic Melanoma
Epoetin Alfa
Erythropoietin
Anemias (esp in renal failure)
Filgrastim
Granulocyte colony-stimulating factor
Recovery of bone marrow
*-GRA (granulocyte), -STIM (stimulating)
Sargramostim
Granulocyte-macrophage colony stimulating factor
Recovery of bone marrow
*-GRA (granulocyte), -MO (macrophage), -STIM (stimulating)
alpha-interferon
Hepatitis B and C
Kaposi’s sarcoma
Leukemias
Malignant melanoma
beta-interferon
Multiple sclerosis
gamma-interferon
Chronic granulomatous disease
Oprelvekin
IL-11
Thrombocytopenia
Thrombopoietin
Thrombocytopenia
Muromonab-CD3 (OKT3)
Targets CD3
Prevent acute transplant rejection
Digoxin Immune Fab
Targets Digoxin
Antidote for digoxin intoxication
Infliximab
Targets TNF-alpha
Crohn’s dz, RA, psoriatic arthritis, ankylosing spondylitis
Adalimumab
Targets TNF-alpha
Crohn’s dz, RA, psoriatic arthritis
Abciximab
Targets glycoprotein IIb/IIIa
Prevents cardiac ischemia in unstable angina and in patients treated with percutaneous coronary intervention
Trastuzumab (Herceptin)
Targets HER2
HER2 overexpressing breast cancer
Rituximab
Targets CD20
B-cell non-Hodgkin’s lymphoma
Omalizumab
Targets IgE
Additional line of treatment for severe asthma
