Immunosuppressive drugs


Immunosuppressive drugs, also known as immunosuppressive agents, immunosuppressants and antirejection medications are drugs that inhibit or prevent activity of the immune system. Glucocorticoids influence all types of inflammatory events, no matter their cause. They induce the lipocortin-1 synthesis, which then binds to cell membranes preventing the phospholipase A2 from coming into contact with its substrate arachidonic acid.

Cytostatics inhibit cell division. In immunotherapy, they are used in smaller doses than in the treatment of malignant diseases. They affect the proliferation of both T cells and B cells. Due to their highest effectiveness, purine analogs are most frequently administered.

The alkylating agents used in immunotherapy are nitrogen mustards (cyclophosphamide), nitrosoureas, platinum compounds, and others. Cyclophosphamide (Baxter's Cytoxan) is probably the most potent immunosuppressive compound.

Ciclosporin is thought to bind to the cytosolic protein cyclophilin (an immunophilin) of immunocompetent lymphocytes, especially T-lymphocytes. This complex of ciclosporin and cyclophilin inhibits the phosphatase calcineurin, which under normal circumstances induces the transcription of interleukin-2. The drug also inhibits lymphokine production and interleukin release, leading to a reduced function of effector T-cells.

The drug is used primarily in liver and kidney transplantations, although in some clinics it is used in heart, lung, and heart/lung transplantations. It binds to the immunophilin FKBP1A, followed by the binding of the complex to calcineurin and the inhibition of its phosphatase activity. In this way, it prevents the cell from transitioning from the G0 into G1 phase of the cell cycle.

Almost everyone who has a transplant must take these drugs every day as directed. If your new kidney came from an identical twin, however, you may not have to take them. Even missing a single dose may make it more likely for you to have a rejection. The only time you should skip a dose is if your doctor or other health care team member tells you to do so. If you are not sure, call your doctor.

Yes. One of the side effects of these drugs is an increased chance of infections. This is more of a problem in the early period after a transplant or following treatment of a rejection because the dosage of these drugs is higher at these times. The most common side effects of the immunosuppressant drugs are "stomach upset". If this happens, ask your doctor if you can space your medicine at different times to help with this problem. Changes to immunosuppressant medicine should only be made after checking with your transplant center.

Managing Editor
Journal of Pharmacy Practice and Education