Immunology- Immunosuppressants Flashcards
Cyclosporine
- Mechanism
- uses
- Toxicity
Calcineurin inhibitor, preventing IL-2 transcription.
Psoriasis, rheumatoid arthritis.
Nephrotoxicity, hypertension, hyperlipidemia,
neurotoxicity, gingival hyperplasia, hirsutism.
Tacrolimus (FK506)
- Mechanism
- Toxicity
Calcineurin inhibitor, preventing IL-2 transcription.
Similar to cyclosporine, higher risk of diabetes and neurotoxicity; no gingival hyperplasia or hirsutism.
Sirolimus (Rapamycin)
- Mechanism
- uses
- Toxicity
mTOR inhibitor; Blocks T-cell activation and B-cell
differentiation, by preventing IL-2 response.
Kidney transplant rejection prophylaxis specifically.
“PanSirtopenia” (pancytopenia), insulin resistance, hyperlipidemia; not nephrotoxic.
Basiliximab
- Mechanism
- uses
- Toxicity
Monoclonal antibody; blocks IL-2R.
Kidney transplant rejection prophylaxis specifically.
Edema, hypertension, tremor.
Azathioprine
- Mechanism
- uses
- Toxicity
Antimetabolite precursor of 6-mercaptopurine.
Inhibits lymphocyte proliferation
Rheumatoid arthritis, Crohn disease, glomerulonephritis,
other autoimmune conditions.
Pancytopenia
Mycophenolate Mofetil
- Mechanism
- uses
- Toxicity
Reversibly inhibits IMP dehydrogenase, preventing purine synthesis of B and T cells.
Lupus nephritis.
GI upset, pancytopenia, hypertension, hyperglycemia.
Less nephrotoxic and neurotoxic. Associated with
invasive CMV infection.
Glucocorticoids
- Mechanism
- uses
- Toxicity
Inhibit NF-κB. Suppress both B- and T-cell function.
Many autoimmune and inflammatory disorders, adrenal
insufficiency, asthma, CLL, non-Hodgkin lymphoma.
Cushing syndrome
Erythropoietin
- Agent
- Uses
Epoetin alfa (EPO analog)
Anemias (especially in renal failure).
Colony stimulating factors
- Agent
- Uses
Filgrastim (G-CSF), Sargramostim (GM-CSF)
Leukopenia; recovery of granulocyte and monocyte counts.
Thrombopoietin
- Agent
- Uses
Romiplostim (TPO analog), eltrombopag (TPO receptor agonist).
Autoimmune thrombocytopenia
Interleukin-2
- Agent
- Uses
Aldesleukin
Renal cell carcinoma, metastatic melanoma
Interferon
- Agent
- Uses
IFN-α: Chronic hepatitis C (not preferred) and B, renal
cell carcinoma.
IFN-β: Multiple sclerosis
IFN-γ: Chronic granulomatous disease
Alemtuzumab
- Target
- Clinical uses
CD52
CLL, MS
Bevacizumab
- Target
- Clinical uses
VEGF
Colorectal cancer, renal cell carcinoma, non-small cell lung cancer.
Cetuximab
- Target
- Clinical uses
EGFR
Stage IV colorectal cancer, head and neck cancer.
Rituximab
- Target
- Clinical uses
CD20
B-cell non-Hodgkin lymphoma, CLL, rheumatoid arthritis, ITP, multiple sclerosis.
Trastuzumab
- Target
- Clinical uses
HER2
Breast cancer, gastric cancer HER2—“tras2zumab”
Adalimumab, certolizumab, golimumab, infliximab (Etanercept is a decoy TNF-α receptor)
- Target
- Clinical uses
Soluble TNF-α
IBD, rheumatoid arthritis, ankylosing spondylitis, psoriasis.
Daclizumab
- Target
- Clinical uses
CD25 (part of IL-2 receptor)
Relapsing multiple sclerosis
Eculizumab
- Target
- Clinical uses
Complement protein C5
Paroxysmal nocturnal hemoglobinuria, HUS
Natalizumab
- Target
- Clinical uses
α4-integrin
Multiple sclerosis, Crohn disease
Risk of PML in patients with JC virus.
Ustekinumab
- Target
- Clinical uses
IL-12/IL-23
Psoriasis, psoriatic arthritis
Abciximab
- Target
- Clinical uses
Platelet glycoproteins IIb/IIIa
Antiplatelet agent for prevention of ischemic complications in patients undergoing percutaneous
coronary intervention.
Denosumab
- Target
- Clinical uses
RANKL
Osteoporosis; inhibits osteoclast maturation (mimics osteoprotegerin)
Digoxin immune Fab
- Target
- Clinical uses
Digoxin
Antidote for digoxin toxicity
Omalizumab
- Target
- Clinical uses
IgE
Refractory allergic asthma; prevents IgE binding to FcεRI
Palivizumab
- Target
- Clinical uses
RSV (respiratory sincital virus) F protein
RSV prophylaxis for high-risk infants