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.
Azathioprine toxicity
Myelosuppression, hepatotoxicity, teratogenic, metabolized by xanthine oxidase (allopurinol).
Cyclophosphamide MOA
Effects T and B cells. Blocks new antigens and can inhibit an established immune response (treat a rejection attack).
Cyclophosphamide toxicity
hemorrhagic cystitis (treat with MESNA and hydration).
Methotrexate MOA
Human dihydrofolate reductase inhibitor.
Methotrexate uses
psoriasis, antineoplastic, severe RA and asthma.
Methotrexate toxicity
hepatotoxicity and teratogenic.
Daclizumab/Basiliximab MOA
Binds IL2 receptors on activated T cells to inhibit IL2 activation.
Daclizumab/Basiliximab uses
great for kidney transplants. No side effects. No general immunosuppression.
Bevacizumab/ranibizumab and Degaptanib/aflibercept MOA
Bind VEGF-A to inhibit angiogenesis. Used in macular degeneration.
Interleukin 2 MOA
Immunomodulator that increases the proliferation and differentiation of helper T and cytotoxic T cells.
Interleukin 2 Uses
renal cell carcinoma and malignant melanoma.
Interleukin 2 toxicity
pulmonary edema, hypotension, hematological.
Filgrastim (neupogen) MOA
granulocyte colony stimulation factor for severe neutropenia. Given as subcutaneous depot
Filgrastim (neupogen) Toxicity
bone pain (making new marrow).
Epoetin-alfa (procrit; epogen) MOV
EPO for severe anemia caused by zidovudine, interleukin, chemo or kindey disease. subcutaneaous depot.
Epogen toxicity
HTN and thrombosis/stoke.
Interferon alpha and beta
respond to viruses
Interferon gamma
activates T lymphocytes and NK cells. Activates macrophages.
interferon alfa-2b
Used with Hep C and uveitis
Interferon beta-1B
multiple sclerosis.
Glatiramer
Multiple sclerosis. acts as decoy. antibodies bind the drug instead of the nerves.
Fingolimod
Multiple sclerosis. decreases lymphocytes to reduce the autoimmune response.
Dimethyl fumarate
Multiple sclerosis. reduces inflammation.