Immunopharmacology Flashcards
Prednisone
Corticosteroid —> General immunosuppression
Rapid anti-inflammatory effect, but takes time for immune suppression to develop
Can be used for organ transplant, long term immunosuppression, general things
Adverse effects of corticosteroids
Short term: Hyperglycemia Long term: Weight gain Cushing like syndrome Pituitary-hypothalamic axis suppression Osteoporosis
T-cell suppressants
Relatively selective for T-lymphocytes, leaving rest of immune response intact (no bone marrow suppression)
Used to prevent organ rejection
Examples:
Calcineurin Inhibitors (Cyclosporine, Tacrolimus)
Proliferation Signal Inhibitors
Cyclosporine
Calcineurin Inhibitor —> selective inhibition of T lymphocytes (IL-2)
NO bone marrow suppression - good for BM transplants
Drug interactions are common, and therapeutic range is narrow
• No grapefruit juice
• No rifampin
• No erythromycin, ketoconazole
Cyclosporine toxicities
RENAL Gingival hyperplasia hypertension CNS issues Hyperglycemia
Tacrolimus
Also a calcineurin inhibitor but a lot less toxic than cyclosporine
No bone marrow suppression
Widely used drug of choice for preventing organ rejection
Toxicities - nephro, HTN, hyperglycemia
Sirolimus
Inhibits T-cell proliferation by binding to mTOR
NO renal toxicity —> great for kidney transplant anti rejection therapy
Mycophenolate-Mofetil
Prevents de novo purine synthesis in T/B lymphocytes
Used for preventing rejection, in combo with tacrolimus and corticosteroids
Azathioprine
Converted in Vito to 6-mercaptopurine (anticancer drug) —> inhibits purine synthesis
Do NOT combine with allopurinol
Used to prevent rejection in transplant patients
BM suppression and TERATOGENIC
Methotrexate
Inhibitors purine biosynthesis
Significant side fx:
BM suppression
Stomatitis
Can produce fetal death — dont use in pregnancy
Cyclophosphamide
Direct T and B cell effect
Prevents DNA crosslinks
Blocks response to new antigens and can inhibit established immune response
Used for BM transplants
GIVE WITH MESNA to prevent hemorrhagic cystitis
Basiliximab
Binds to IL-2 receptor (CD25) on activated T cells
Used at time of transplant for induction of immunosuppression
Reduces renal rejection by 50%
Examples of biological used to treat psoriasis and rheumatoid arthritis
Abatacept (Orencia)
Adalimumab (Humira)
Eat receipt (Enbrel)
Hematopoietic stimulating drugs
G-CSF (Neupogen)
Erythropoietin (Epogen)
Essential to be able to maintain therapy that cause causes polycytopenias
Neupogen
Human recombinant granulocytes colony stimulating factor
Used to treat severe neutropenia