Immunosuppressants Flashcards
What drug has a MoA: Calcineurin inhibitor; binds cyclophilin. Blocks T-cell activation by preventing IL-2 transcription.
Cyclosporine
What drug has ADR: Nephrotoxicity, hypertension, hyperlipidemia, neurotoxicity, gingival hyperplasia, hirsutism.
Cyclosporine
What drug has a MoA: Calcineurin inhibitor; binds FK506 binding protein (FKBP). Blocks T-cell activation by preventing IL-2 transcription.
Tacrolimus (FK506)
What drug has ADR: increased risk of diabetes and neurotoxicity; no gingival hyperplasia or hirsutism.
Tacrolimus (FK506)
Both calcineurin inhibitors are highly toxic to what organ?
kidneys
How are Cyclosporine and Tacrolimus different from Sirolimus?
Sirolimus blocks T-cell activation AND B-cell differentiation by preventing RESPONSE to IL-2.
Cyclosporine/Tacrolimus block T-Cell Activation only and prevent IL-2 TRANSCRIPTION
ADR of Sirolimus?
“PanSirtopenia” (pancytopenia), insulin resistance, hyperlipidemia; not nephrotoxic.
Another name for Sirolimus?
Rapamycin
What drug is synergistic with cyclosporine and also used in drug-eluting stents.
Sirolimus (Rapamycin)
Daclizumab, basiliximab have what MoA?
Monoclonal antibodies; block IL-2R.
Edema, hypertension, tremor are the side effects of what drug?
Daclizumab, basiliximab
What drug is an antimetabolite precursor of 6-mercaptopurine.
Azathioprine
Mechanism of Azathioprine
Inhibits lymphocyte proliferation by blocking nucleotide synthesis.
Side effects of Azathioprine (3)
Leukopenia, anemia, thrombocytopenia.
Relationship with Azathioprine and Allopurinol?
6-MP degraded by xanthine oxidase; toxicity increased by allopurinol.
What drug has MOA: Reversibly inhibits IMP dehydrogenase, preventing purine synthesis of B and T cells.
Mycophenolate mofetil
What drug can be used to treat lupus nephritis?
Mycophenolate mofetil
What drug has the ADR: pancytopenia, hypertension, hyperglycemia.
Mycophenolate mofetil
What drug is associated with invasive CMV infection?
Mycophenolate mofetil
Corticosteroids inhibit what transcription factor?
Inhibit NF-κB.
What drug has ADR: Hyperglycemia, osteoporosis, central obesity, muscle breakdown, psychosis, acne, hypertension, cataracts, avascular necrosis (femoral head).
Corticosteroids
Cyclosporine MoA?
Calcineurin inhibitor; binds cyclophilin. Blocks T-cell activation by preventing IL-2 transcription.
Tacrolimus MoA?
Calcineurin inhibitor; binds FK506 binding protein (FKBP).
Blocks T-cell activation by preventing IL-2 transcription.
Sirolimus (Rapamycin) MoA?
mTOR inhibitor; binds FKBP.
Blocks T-cell activation and B-cell differentiation by preventing response to IL-2.
Aldesleukin (IL-2) use (2)
Renal cell carcinoma, metastatic melanoma
Epoetin alfa (erythropoietin) use (1)
Anemias (especially in renal failure)
Filgrastim (G-CSF) use (1)
Recovery of bone marrow
Sargramostim (GM-CSF) use (1)
Recovery of bone marrow
IFN-α use (3)
Chronic hepatitis B and C, Kaposi sarcoma, malignant melanoma
IFN-β use (1)
Multiple sclerosis
IFN-γ use (1)
Chronic granulomatous disease
Romiplostim, eltrombopag (thrombopoietin receptor agonists) use (1)
Thrombocytopenia
Oprelvekin (IL-11) use (1)
Thrombocytopenia
