Immunosuppressants Flashcards
Binds cyclophilins
Inhibits activation, differentiation of T cells
by inhibiting calcineurin (no IL-2 production)
Suppress organ rejection, autoimmune disease
Nephrotoxic, HTN, hyperlipidemia, hyperglycemia, tremor
YES gingival hyperplasia, hirsutism
Cyclosporine
Binds FK-binding protein
inhibits calcineurin (no IL-2 secretion)
Suppresses organ rejection
Nephrotoxic, HTN, hyperlipidemia, hyperglycemia, tremor
NO gingival hyperplasia, hirsutism
Tacrolimus
(FK-506)
Inhibits mTOR
Prevents T-cell differentiation in response to IL-2
Kidney transplants, drug-eluting stents
Hyperlipidemia, thrombocytopenia, leukopenia
Sirolimus
(Rapamycin)
w/ cyclorsporine and corticosteroids to prevent
kidney transplant rejection.
Interferes with nucleic acid synthesis
Precursor of 6-mercaptopurine
Kidney transplant, autoimmune
(glomerulonephritis, hemolytic anemia)
Bone marrow supprssion
(what increases toxicity?)
Azathioprine
Active metabolite: mercaptopurine
metabolized by xanthine oxidase
Toxicity increased by allopurinol
Monoclonal antibody
Binds CD3 on T-cells, prevents signal transduction
Kidney transplant
Cytokine release syndrome, hypersensitivity
Muromonab-CD3
(OKT3)
Renal cell carcinoma, metastatic melanoma
(Cytokine)
Aldesleukin (IL-2)
Anemias
(Cytokine)
Epoetin alfa (EPO)
Recovery of bone marrow
(2 cytokines)
Filgrastim
(granulocyte colony-stimulating factor)
Sargramostim
(granulocyte-macrophage colony-stimulating factor)
- HBV, HCV
- Kaposi’s sarcoma
- Leukemia, malignant melanoma
(Cytokine)
IFN-_alpha_
Multiple sclerosis
(Cytokine)
IFN-_beta_
Chronic granulomatous disease
(Cytokine)
IFN-_gamma_
Thrombocytopenia
(2 cytokines)
Oprelvekin (IL-11)
Thrombopoietin
Acute transplant rejection
Targets CD3
Muromonab-CD3
(OKT3)
Antidote for digoxin intoxication
Target: digoxin
Digoxin immune Fab
Crohn’s disease, rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis
Target: TNF-alpha
Infliximab
