Immunotherapy Flashcards
Corticosteroids MOA
Inhibits T cell proliferations, cytokine response, decreases response to antibodies, decreases spleen size/content. Broad spectrum.
Corticosteroid use
organ transplants, chronic immunosuppressant, prevent adverse reactions to drugs, topically.
Corticosteroid toxicity
cushings syndrome, suppressed pituitary-hypothalamic axis, osteoporosis, ulcers, menstrual and reproductive issues.
Cyclosporine MOA
Binds to cyclophilin to inhibit calcineurin/T-cell activation to decrease the formation of IL-2. Selective for T-lymphocytes.
Cyclosporine characteristics
No bone marrow suppression, metabolized by CYP3A4 (drug interactions!)
CYP3A4 Inducers
Phenobarbitol, phenytoin, Rifampin.
CYP3A4 Inhibitors
Grape fruit juice, erythromycin, ketoconazole and verapamil.
Cyclosporine uses
Prevents organ rejection (with corticosteroids or azathioprine), organ transplant maintenance, autoimmune diseases.
Cyclosporine toxicity
nephrotoxic, gingival hyperplasia (need good oral hygeine, HTN, tremors, hirsutism, hyperlipidemia, hyperglycemia.
Tacrolimus (FK506) MOA
Similar to cyclosporine but less toxic. Inhibits T cell activation and decreases IL2 and IL4. Narrow therapeutic range. Metabolized by CYP3A4.
Tacrolimus (FK506) uses
Prevent rejection especially in liver and heart transplants.
Tacrolimus (FK506) toxicity
nephrotoxic, HTN, hyperglycemia, HA, tremors, insomnia.
Sirolimus MOA
Inhibits proliferation of T and B cells.
Sirolimus uses
No renal toxicity so used in kidney transplants.
Sirolimus toxicity
increased cholesterol and triglycerides.
Pimecrolimus uses
Cream for atopic dermatitis that doesn’t cause skin atrophy.
Mycophenolate-Mofetil MOA
Decreases DNA synthesis by inhibiting monophosphate dehydrogenase that only T and B cells need for purine synthesis.
Mycophenolate-Mofetil Uses
Does NOT suppress bone marrow. Often combined with Tacrolimus to prevent transplant rejection.
Mycophenolate-Mofetil toxicity
Rash, GI, very high risk of infections.
Thalidomide MOA
blocks TNF alpha.
Thalidomide uses
prevents graft versus host reaction
Thalidomide toxicity
TERATOGENIC. Drowsiness and neutropenia.
Azathioprine MOA
Prodrug that is converted into 6-mercaptopurine which inhibits purine synthesis.
Azathioprine uses
Cancer (high doses), prevents rejection, glomerulonephritis in lupus, severe RA, dentists use in place of steroids.