Immunosupressants Flashcards
Agents that block lymphocyte activation and proliferatino
Immunosuppressants
Immunosuppresants are useful as profylaxis of ____ transplant rejection
Acute
Calcineurin inhibitors
Cyclosporin
Tacrolimus (FK506)
Cyclosporin binds to
Cyclophilin
Prevent IL-2 transcription thus blocking T cell activation
Cyclosporine
Tacroliums (FK506)
Calcineurin inhibitors most common toxicity
Nephrotoxicity
Increases risk of DM
Tacrolimus
Gingival hiperplasia
Cyclosporine
Tacrolimus binds to
FK506 binding protein (FKBP)
Specifical prophylaxis for kidney transplant rejection
Sirolimus (Rapamycin)
mTOR inhibitor
Sirolimus
Blocks T cell activation and B cell differentiation by preventing response to IL-2
Sirolimus
Sirolimus binds
FKBP
Sirolimus (rapamycin) toxicity
Pancytopenia
Insulin resistance
Hyperlipidemia
NOT NEPHROTOXIC
Sirolimus kidney toxicity
NO kidney toxicity associated to sirolimus
Synergistic with cyclosporine
Sirolimus
Used in drug-eluting stents
Sirolimus: prevents cell proliferation that could block the stent
Monoclonal antibody that blocks IL-2R
Basiliximab (B=2nd letter of alphabet)
Inhibits lumphocyte prolferation by blocking nucleotide synthesis
Azathioprine
Precursor of 6 mercaptopurine
“AzathioPURINE”
Toxicity of azathioprine
Pancytopenia
Increased toxicity with allopurinol
6 mercaptopurine, as it is degraded by xantine oxidase
Reversibly inhibits IMP dehydrogenase, preventing purine synthesis of B and T cells
Mycophenolate mofetil
Inhibit NF-kappaBetta
Corticosteroids
Corticosteroids toxicity
Cushing syndrome Osteoporosis Hyperglycemia: diabetes Amenorrhea Adenocortical atrophy Peptic ulcers Psychosis Cataracts Avascular necrosis: femoral head
IL2R antagonists
Basiliximab
Daclizumab
Cytokine used to recover bone marrow and WBC counts by granulocyte stimulation
FilGRAstim: GRAnulocyte (G-CSF)
Cytokine used to recover bone marrow and WBC counts by granulocyte and monocyte stimulation
SaGRA-MOstim: Granulocytes and monocytes (GM-CSF)
Cytokine used to treat chronic granulomatous disease
IFN gamma
Cytokine used to treat thombocytopenia
Rombiplostim: thrombopoyetin analog
Eltrombopag: thrombopoyetin receptor agonist
Oprelvekin (IL-11)
Cytokine used to treat multiple sclerosis
IFN beta
Cytokine used to treat chronic hepatitis A and B
Kaposi sarcoma
Malignant melanoma
IFN alpha
Cytokine used to anemias, especially in renal failure
Erythropoietin: epoetin alpha
Cytokine used to treat renal cell carcinoma and metastasic melanoma
Aldesleukin (IL-2)
Anti-VEGF
Bevacizumab
Anti CD20
Rituximab
Anti HER2
Trastuzumab: Tras2zumab
ANti TNG alpha
Adalimumab
GOlimumab
Infliximab
Certolizumab
Etanercept
Decoy TNF alpha receptor, not an ANTIBODY!
Use of daclizumab
Relapsing multiple sclerosis
Anti Complement protein C5
Eculizumab
Use of eculizumab
Paroxysmal nocturnal hemoglibinuria
Increases risk of PML in patients with JC virus
Natalizumab
Anti alpha 4 integrin
Natalizumab
Ustekinumab
Anti IL-12/23
Anti RANKL
Denosumab: inhibits osteoclast maturations: mimics osteoprotegerin
Anti IgE
Omalizumab
Used in ARMD (DMAE)
Anti VEGF: bevacizumab
RSV prophylaxis for high risk infants
Palivizumab: RSV F protein
Anti platelet glycopreints IIb/IIIa
Abciximab: antiplatelet agent for prevention of ischemic complications in patients undergoing percutaneous coronary intervention
Used in the treatment of chronic lymphocytic leukemia
Alemtuzumab: anti CD52