There are medications capable of affecting bone metabolism and the rate of tooth movement. Among these medications are the immunosuppressants, which act by repressing the action of T lymphocytes, however they can cause bone loss and consequently lead to osteoporosis. Osteoporosis is a common complication following kidney, heart, liver or lung transplantation. The immunosuppressant treatment for preventing organ rejection after transplantation, in general, includes glucocorticoids, cyclosporine, tacrolimus, and sirolimus. All these drugs can have jeopardizing effects on bone mineral homeostasis and consequently influence tooth movement. In recent years, however, the increasing use of immunosuppressants has raised questions about their effects on bone metabolism in patients undergoing orthodontic treatment.