Immunosuppressant Drugs Flashcards
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2 main applications of immunosuppressants
1) prevent organ rejection
2) tretment of autoimmune disorders
2 big toxicities of immunosuppressants
Increased risk of infection, increased risk of neoplasm development
Cyclosporine/tacrolimus/pimecrolimus mech of action
Inhibit calcineurin, blocking IL2 for T cell proliferation
Cyclosporine ADRs (3)
- nephrotoxicity
- Increased risk of infection, hypertension, hirsutism, tremor
- Increased risk of lymphoma
DOC for preventing organ rejection after allogenic transplant
Cyclosporine
Cyclosporine differs from other immunosuppressants in that…
Prevent rejection of allogenic organ without suppressing bone marrow
3 most effective immunosuppressants and their class
cyclosporine
tacrolimus
pimecrolimus
Calcineurin inhibitors
mTOR inhibitors mech of action
Inhibit enzyme known as target of rampamycin, a protein kinase in cell proliferation and survival, acts on B and T cells by acting on IL2 but not thru calcineurin
Cytotoxic drugs mech of action
Suppress immune cells by killing B and T cell lymphocytes undergoing proliferation, are toxic to all proliferating cells
Cytotoxic drugs ADRS (4)
- less safe agent than cyclosporine and glucocorticoids
- bone marrow suppression
- GI disturbances
- alopecia
Cyclophosphamide (cytoxan) mech of action and what drug class is it?
Prodrug converted into active form in liver, decreases number of B and T lymphocytes by cross linking DNA, toxic to all cells
Cytotoxic drugs
Cyclophosphamide (cytoxan) ADRs (3)
- neutropenia
- hemorrhagic cystitis
- sterility
Mycophenolate mofentil mech of action, what class of drugs does it belong to?
Prophylaxis of organ rejection, converted to active form after absorption and acts on B and T lymphocytes to inhibit an enzyme needed for synthesis of purines
Cytotoxic drugs
Basiliximab (simulect) mech of action and what drug class does it belong to?
blocks activity of T lymphocytes blocking proliferation of T cells by IL 2 binding
Antibodies
Cyclosporine indications
Prevention of rejection of allogenic organ transplants, as well as RA and psoriasis