Knowing Your Immunosuppressive (anti-rejection) Medications

By Pradeep Kadambi, M.D.

Immunosuppressive MedicationsFirst of all, hearty congratulations to you on receiving an organ transplant. You and your loved ones, and your health care professionals have invested a lot of time and effort to make this happen. It is our collective responsibility to make sure that the transplant procedure is a success and that you stay healthy for a long time! To achieve this, you have to make a commitment to take care of yourself, by taking the medications as prescribed and adhering to the advice of your transplant professionals. Remember, you were not born with the transplanted organ and hence your body will try to reject it, and the immunosuppressants will help your body to prevent the rejection.

Most of the immunosuppressants are powerful drugs, and hence have side effects. For some of them, levels in the blood are to be monitored frequently. Too little of the drug will put you at risk for rejection, while too much might mean side effects. So, it takes your caregivers some time to achieve the right balance of immunosuppression.

Broadly, the immunosuppressants can be classified into 2 categories:

  1. Induction agents: Powerful antirejection medications used at the time of transplant
  2. Maintenance agents: Antirejection medications used for the long term.

Think of a real estate mortgage; the down payment serves as the induction agent and the monthly payments serve as maintenance agents. If the down payment is good enough you can reduce the monthly payments substantially, and the concept is similar for immunosuppression.

The maintenance agents are generally 4 classes of drugs

  • Calcineurin Inhibitors: Tacrolimus and Cyclosporine
  • Antiproliferative agents: Mycophenolate Mofetil, Mycophenolate Sodium and Azathioprine
  • mTOR inhibitor: Sirolimus
  • Steroids: Prednisone

Although there are multiple methods of mixing and matching the above drugs, the most common combination employed by the transplant centers is Tacrolimus, Mycophenolate Mofetil and Prednisone.

The blood levels of Tacrolimus, Cyclosporine and Sirolimus have to be monitored closely. There are many other medications and food and supplements that alter the levels (up or down) in the blood, and you need to be aware of it. The list is long but some of the common ones are grapefruit juice, St. John's Wort, erythromycin, anti TB medications, antiseizure medications and common blood pressure medications (cardizem or diltiazem, and Verapamil).

Calcineurin Inhibitors and the antiproliferative agents are taken twice daily, and Sirolimus and prednisone are taken once daily. Try to be consistent about the time of the day when you take your medications, that way you will remember to take them. Also, when you have a clinic appointment, do not take your antirejection medications till the blood is drawn for lab work.

The most common side effects of the immunosuppressants are some sort of "stomach upset". Sometimes spacing the calcineurin inhibitors and the antiproliferative agents by more than an hour might help. Other specific side effects include:

  • Tacrolimus: tremors, hair loss, headaches and increased chance of developing diabetes
  • Cyclosporine: Hair growth (does not grow hair if you are already bald…sorry!), gum enlargement, and tremors
  • Sirolimus: Rash, bone marrow problems (anemia, low white count and low platelets), swelling of ankles, frothy urine (because of protein leakage from urine)
  • Prednisone: This is branded as an "evil drug" because of the many side effects (weight gain, water retention, diabetes, acne etc). However, for the long term use a very small dose is prescribed (5 mg), and the major side effect is bone thinning which can be countered easily.

Again it is important for you to ask what types of immunosuppressant combinations are used by your transplant center.

About 6 months to a year after transplant, the immunosuppression is generally lowered and the risk of side effects should be low. If you still continue to experience side effects, you need to speak to your transplant professional to either adjust the dose or switch to a different medication. Always, the immunosuppression should be handled (or changed) in consultation with your transplant center.

There are many newer medications that are being tested in clinical trials, and the one medication that is tested is an intravenous medication, given once a month and it is used instead of the calcineurin inhibitors. The blood levels of the drug do not need to be monitored. So far it has been successful. It may take a few years for other new medications to be used on a regular basis.

Finally, the success of transplantation depends on many factors. You need be adherent to your medications, exercise and adopt a healthy diet and lifestyle. Other important issues include getting appropriate tests for cancer screening (mammograms, colonoscopy, pap smears, etc), always wear sun block, and get vaccinated every year for flu and every other year for pneumonia.

Dr. Kadambi is Assistant Professor of Medicine Director, Nephrology Physician Directed Practice Section of Nephrology, The University of Chicago, and the recipient of the 2007 NKF of Illinois Community Service award.

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©2012 National Kidney Foundation. All rights reserved. This material does not constitute medical advice. It is intended for informational purposes only. No one associated with the National Kidney Foundation will answer medical questions via e-mail. Please consult a physician for specific treatment recommendations.