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120 SECTIon II Immunology ` Immunology—ImmunoSuppreSSantS Immunology ` Immunology—ImmunoSuppreSSantS

` Immunology—ImmunoSuppreSSantS

Immunosuppressants Agents that block lymphocyte activation and proliferation. Reduce acute transplant rejection by
suppressing cellular immunity (used as prophylaxis). Frequently combined to achieve greater
efficacy with  toxicity. Chronic suppression  risk of infection and malignancy.
drug mechanISm IndIcatIonS toXIcIty noteS
Cyclosporine Calcineurin inhibitor; Psoriasis, rheumatoid Nephrotoxicity,
binds cyclophilin arthritis hypertension,
Blocks T-cell activation hyperlipidemia, Both calcineurin
by preventing IL-2 neurotoxicity, gingival inhibitors are
transcription hyperplasia, hirsutism highly nephrotoxic,

Tacrolimus (FK506) Calcineurin inhibitor; Similar to cyclosporine, especially in higher
binds FK506 binding  risk of diabetes doses or in patients
protein (FKBP) and neurotoxicity; with decreased renal
Blocks T-cell activation no gingival function
by preventing IL-2 hyperplasia or
transcription hirsutism
Sirolimus (Rapamycin) mTOR inhibitor; binds “PanSirtopenia” Kidney “sir-vives.”
FKBP (pancytopenia), Synergistic with
Blocks T-cell Kidney transplant insulin resistance, cyclosporine
activation and B-cell rejection prophylaxis hyperlipidemia; Also used in drug-
differentiation by specifically not nephrotoxic eluting stents
preventing response Sir Basil’s kidney
to IL-2 transplant
Basiliximab Monoclonal antibody; Edema, hypertension,
blocks IL-2R tremor
Azathioprine Antimetabolite Rheumatoid arthritis, Pancytopenia 6-MP degraded by
precursor of Crohn disease, xanthine oxidase;
6-mercaptopurine glomerulonephritis, toxicity  by
Inhibits lymphocyte other autoimmune allopurinol
proliferation by conditions Pronounce “azathio-
blocking nucleotide purine”
synthesis
Mycophenolate Reversibly inhibits Lupus nephritis GI upset, Associated with
Mofetil IMP dehydrogenase, pancytopenia, invasive CMV
preventing purine hypertension, infection
synthesis of B and T hyperglycemia
cells Less nephrotoxic and
neurotoxic
Glucocorticoids Inhibit NF-κB Many autoimmune Cushing syndrome, Demargination
Suppress both B- and and inflammatory osteoporosis, of WBCs causes
T-cell function by disorders, adrenal hyperglycemia, artificial leukocytosis
 transcription of insufficiency, asthma, diabetes, amenorrhea, Adrenal insufficiency
many cytokines CLL, non-Hodgkin adrenocortical may develop if drug is
Induce T cell apoptosis lymphoma atrophy, peptic ulcers, stopped abruptly after
psychosis, cataracts, chronic use
avascular necrosis
(femoral head)

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