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
Cyclosporine drug interactions
Aminoglycosides, grapefruit juice, and amphoterecin B
Because of serious adverse effects, cytotoxic drugs are reserved for….
…patients not responding to safer agents (cyclosporine and glucocorticoids)
Methotrexate summary, what class of drugs does it belong to?
Anticancer drug also used for immunosuppression
Cytotoxic
Mycophenolate mofentil unique characteristic among cytotoxic drugs
It only inhibits B and T lymphocytes because of the purine synthesis pathway it targets
