Immunosuppressive Drugs

basiliximab (Simulect)

Monoclonal Antibodies. IV. Monoclonal antibody that act as IL-2 receptor antagonist by inhibiting binding of IL-2; inhibits T-cell activation and proliferation. Side effects: generally none, rarely: acute hypersensitivity reaction, including anaphylaxis.

daclizumab (Zenapax)

Monoclonal Antibodies. IV. Monoclonal antibody that acts as IL-2 receptor antagonist by inhibiting the binding of IL-2; inhibits T-cell activation and proliferation. Side effects: generally none, rarely: acute hypersensitivity reaction, including anaphylaxis.

Calcineurin Inhibitors

Route: PO, IV. Acts on T helper cells to prevent production and release of IL-2 and y-interferon, inhibits production of T cytotoxic lymphocytes and B cells. Side effects: nephrotoxicity, increased risk for infection, neurotoxicity (tremors, seizures), hepatotoxicity, lymphoma, HTN, tremors, hirsutism, leukopenia, gingival hyperplasia

Corticosteroids

Route: PO, IV. Suppress inflammatory response, inhibit cytokine production (IL-1, IL-6, TNF) and T-cell activation and proliferation. Side effects: PUD, hypertension, osteoporosis, Na+ and water retention, muscle weakness, easy bruising, delayed healing, hyperglycemia, increased risk for infection

cyclosporine (Sandimmune, Neoral, Gengraf).

Calcineurin inhibitor. Less effective, less toxic than cyclosporine. PO, IV

tacrolimus (Prograf, FK506)

Calcineurin inhibitor. More effective, more toxic that cyclosporine. PO, IV

prednisone, methylprednisolone (Solu-Medrol)

Corticosteroid.

muromonab-CD3 (Orthoclone OKT3)

Monoclonal Antibodies. IV push. Monoclonal antibody that binds to CD3 receptors on T cells, causing cell lysis; inhibits function of cytotoxic T cells. Side effects: fever, chills, dyspnea, chest pain, nausea and vomiting, anaphylactic reactions include pulmonary edema, cardiac or respiratory arrest

azathioprine (Imuran)

Cytotoxic (Antiproliferative) Drug. PO, IV. Blocks purine synthesis, suppresses cell-mediated and humoral immune responses by inhibiting proliferation of T and B cells. Side effects: bone marrow suppression: neutropenia, anemia, thrombocytopenia

mycophenolate mofetil (CellCept, Myfortic)

Cytotoxic (Antiproliferative) Drug. PO, IV. Inhibits purine synthesis; suppresses proliferation of T and B cells. Side effects: Diarrhea, nausea and vomiting, severe neutropenia, thrombocytopenia, increased risk of infection, increased incidence of malignancies

cyclophosphamide (Cytoxan, Neosar)

Cytotoxic (Antiproliferative) Drug. PO. Cross-links DNA, leading to cell injury and death. Results in decrease in number and activity of T and B cells. Side effects: neutropenia, hemorrhagic cystitis

sirolimus (Rapamune)

Cytotoxic (Antiproliferative) Drug. PO. Suppresses T-cell activation and proliferation. Side effects: increased risk for infection, leukopenia, anemia, thrombocytopenia, hyperlipidemia, hypercholesterolemia, arthralgias, diarrhea, increased incidence of malignancies, not used in liver and lung transplants

Lymphocyte immune globulin (Atgam)

Polyclonal Antibody. IV. Prepared by immunizing horse with human T cells. Polyclonal antibodies directed against T cells, thus depleting them. Side effects: serum sickness (fever, chills, muscle and joint pain), tachycardia, back pain, SOB, hypotension, anaphylaxis, leukopenia, thrombocytopenia, rash, increased risk for infection