Pharmacy

Transplant patients take medications each day to prevent organ rejection. Because the patient's immune system recognizes the new organ as a foreign tissue, it is normal for the immune system to try to reject the organ. Drugs (called immunosuppressants) help suppress the immune system to prevent or reverse rejection. At the same time, these drugs may have side effects. Both the patient's risk of rejection and susceptibility to side effects are considered when prescribing drugs and their dosage.

For the most recent information about the various immunosuppressants, please read "Transplant Time: providing care in the community setting", published in Pharmacy Practice (February/March 2009).

Although researchers continue to study new drugs, these are the most common drugs used to prevent organ rejection:

 

Cyclosporine

Cyclosporine is one of the most frequently used anti-rejection drugs, and it is usually combined with prednisone. Cyclosporine is a very potent immunosuppressant, which patients usually have to take for the rest of their life.

Cyclosporine is taken every 12 hours as capsules or a liquid. Most of our transplant patients prefer the capsule for convenience; however, the odor often leaves something to be desired! Periodically, blood samples are taken from patients to measure how much cyclosporine is in the patient's blood, and dose changes are made so that enough drug is given to prevent rejection but not too much to prevent unwanted side effects.

Common side effects may include tremors in the hands (which diminish over time), hair growth on the face or upper body, growth of the gums, headaches, blurred vision, high blood pressure, elevated potassium levels, and decreased kidney function. All immunosuppressive drugs can increase the risk of infection because they suppress the immune system.

Cyclosporine interacts with many other medications. Grapefruit and grapefruit juice can cause cyclosporine blood levels to increase, so consuming these is not recommended. Transplant patients need to check with their pharmacist or transplant team before beginning new prescriptions and before purchasing non-prescription medications to ensure that the combination will not interact.

In Canada, cyclosporine is only available from transplant centers so patients must always be sure that they have enough medication on hand without running out. This information as well as a list of drug interactions is available on the patient handout, "Neoral (cyclosporine) Patient Medication Information".

 

Prednisone

Prednisone continues to be an integral part of anti-rejection drug treatment. Prednisone doses are usually high after the transplant, and are slowly tapered to a lower dose. The body produces its own form of prednisone called cortisol. When prednisone is taken, the body produces less cortisol. Cortisol is necessary to help the body deal with stress such as infections or rejection. Prednisone doses are slowly lowered to allow the body to adjust and produce more cortisol.

Patients should not stop taking prednisone suddenly or they may become very ill. Prednisone may cause some stomach irritation, and it is best taken with food. Other side effects may include moodiness, round face ("cushingoid"), fluid retention or ankle swelling, weight gain, acne, thin skin, easy bruising, poor wound healing, cataracts, high blood sugar, and weakening of the bones (osteoporosis). Transplant teams are aware of these side effects and they attempt to reduce prednisone over time to as low a dose as possible while still preventing rejection.

Prednisone may also be given intravenously (methylprednisolone) immediately after transplant or to treat specific rejection episodes. This IV treatment usually lasts between 3-5 days. LHSC's Pharmacy Services also has the " Prednisone Patient Medication Information" available for our patients.

 

Azathioprine

Azathioprine is taken once a day, and is often combined with cyclosporine or tacrolimus and prednisone.

Azathioprine can cause stomach irritation so it should be taken with food. It may also lower some blood cell counts, mainly the white blood cells that help the body fight infection and the platelets that help the blood clot. If patients experience fever or chills, mouth sores, unusual bleeding or bruising, bloody or tarry stools, blood in the urine, skin rash, or jaundice, they should contact their physician immediately.

 

Tacrolimus

Also known as FK506 or Prograf, this is a relatively new drug on the transplant scene. Tacrolimus is as effective at preventing transplant rejection as cyclosporine, and offers an alternative treatment for patients who cannot take cyclosporine. It may also be used to treat acute and chronic rejection episodes. Tacrolimus affects the immune system in a similar way as cyclosporine, so it is used as a replacement for cyclosporine. Studies are underway to see if patients treated with tacrolimus can use lower doses of prednisone without rejecting their organ.

Tacrolimus is taken every 12 hours just like cyclosporine. Tacrolimus levels in the blood are measured, and dose changes are then made. Like cyclosporine, the dosage is carefully monitored to prevent rejection and to minimize unwanted side effects.

Side effects may include headache, tremors, elevated potassium in the blood, high blood pressure, and decreased kidney function. Tacrolimus also makes some patients more sensitive to touch, causes numbness or tingling especially around the mouth, and can elevate blood sugar.

Tacrolimus interacts with many other medications, in a similar way as cyclosporine. Patients need to check with their doctor or pharmacist before taking any new medications to ensure that their anti-rejection drugs will not be affected. LHSC's Pharmacy Services also has the "Prograf (tacrolimus) Patient Medication Information" sheet available for our patients.

 

Mycophenolate mofetil

Mycophenolate mofetil, also known as CellCept, is another new immunosuppressant. It is similar to azathioprine so patients should not take both drugs at the same time. Mycophenolate must be given with other anti-rejection drugs, for example, cyclosporine or tacrolimus and prednisone.

Mycophenolate mofetil is taken every 12 hours, preferably on an empty stomach as food can slow down the rate of absorption.

If patients experience stomach upset, however, then they may take it with food, which usually helps with stomach problems such as heartburn. Stomach upset and diarrhea are the most common side effects. Patients may also experience heartburn, acne, tremors, constipation, or headache. Like azathioprine, this drug may lower some blood cell counts, especially white blood cells. It's important that patients have their blood checked regularly and keep all clinic appointments. Many transplant patients have had healthy babies while taking anti-rejection drugs. CellCept, however, may be harmful to the unborn baby. Pregnancy and breastfeeding are not advised while taking this medication.

Also, patients should not take antacids containing magnesium or aluminum (such as Mylanta, Maalox, Amphogel) at the same time as they take mycophenolate mofetil because antacids may make this drug less effective. Tums are okay to use and have no effect on mycophenolate. LHSC's Pharmacy Services also has the "CellCept (mycophenolate mofetil) Patient Medication Information" available for our patients.

 

Sirolimus


Sirolimus, also known as rapamycin and Rapamune, is another immunosuppressant, which is given in combination with other anti-rejection drugs.

Sirolimus is usually taken once a day, preferably at the same time every day.

Side effects may include nausea, diarrhea, tremors, dizziness, high blood pressure, high cholesterol and triglycerides, unusual heartbeat, certain types of cancers (eg: skin cancer) or mouth sores.

Several medications do not mix well with sirolimus, and they may affect the level of sirolimus. For example, drugs that are used to treat high cholesterol and triglycerides may become more potent when taken with sirolimus. Patients should not use herbal medications while taking anti-rejection medications, and they should also avoid using non-prescription ("over the counter") medications.

Medication should be stored at room temperature, away from excessive heat and humidity. Sirolimus is a very specialized drug and may not be readily available at every pharmacy so it's important for patients to keep enough on hand so they don't run out. The " Rapamune (sirolimus, rapamycin) Patient Medication Information"sheet includes additional information.

 

Thymoglobulin


This drug may be used after transplant to prevent rejection or to treat acute rejection episodes; it is given intravenously, usually for 10-14 days.

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Last Updated February 24, 2009 | © 2007, LHSC, London Ontario Canada