Immunosuppressants Flashcards
Sirolimus is synergistic with ___ and is also used in ___.
Cyclosporine
Drug-eluting stents
Mechanism: Epoetin alfa
Recombinant EPO
Other uses: Corticosteroids
Many autoimmune and inflammatory disorders
Adrenal insufficiency
Asthma
CLL
Non-hodgkin lymphoma
Toxicity: Mycophenolate mofetil
GI upset
Pancytopenia
Hypertension
Hyperglycemia
Less nephrotoxic and neurotoxic
Clinical use: IFN-beta
Multiple sclerosis
6-MP (azathioprine) degraded by ___; increased toxicity by ___
Xanthine oxidase
Allopurinol and febuxostat
Mechanism: Mycophenolate mofetil
Reversibly inhibits IMP dehydrogenase → inhibiting purine synthesis of B and T cells
Other use: Cyclosporine
Psoriasis
RA
Clinical use: Oprelvekin
Thrombocytopenia
Clinical use: IFN-gamma
Chronic granulomatous disease
Clinical use: Aldesleukin
Renal cell carcinoma
Metastatic melanoma
Mechanism: Sirolimus (rapamycin)
Binds FKBP → inhibits mTOR
Blocks T-cell activation and B-cell differentiation by preventing response to IL-2 (blocks G1→S)
Toxicity: Azathioprine
Myelosuppression → pancytopenia
Hepatotoxicity
GI distress
Other uses: Basiliximab
Kidney transplant rejection prophylaxis specifically
Mechanism: Azathioprine
Purine (thiol) analog → decreases de novo purine synthesis
Activated by HGPRT
Metabolized into 6-MP
Mechanism: Eltrombopag
Thrombopoetin receptor agonist