What are the immunosuppressive drugs?

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Immunosuppressive drugs decrease the function of your immune system so that your immune system does not react to (that is, reject) the new organ. Without immunosuppressive drugs the immune system would recognize the new organ as foreign and attack it.

The following includes the commonly prescribed immunosuppressive agents and their side effects. After transplantation you will be prescribed several, but not all, of these medications.

Tacrolimus

Tacrolimus (also called Prograf, FK-506) is a primary immunosuppressive agent and, like cyclosporine, a calcineurin inhibitor. It is newer than cyclosporine and was approved for use in the United States in 1995. Tacrolimus is never used in conjunction with cyclosporine.

Notes About Tacrolimus

• You should not stop taking tacrolimus or change the dose or the time at which you take it unless your transplant team instructs you to do so.

• Tacrolimus should be taken in the morning and at night, about 12 hours apart.

• The amount of tacrolimus in your blood is monitored by blood tests. Do not take tacrolimus on the day you are having blood tests done until after the blood is drawn.

• Always take the correct dose of tacrolimus after your blood has been drawn.

• Tacrolimus may interact with some commonly used medications, such as antibiotics and high blood pressure medications. It is important that you check with the transplant team before starting any new medications.

Possible Side Effects

Headaches; nausea; diarrhea; stomach cramps; hand tremors or shaking; high blood sugar; high blood potassium; abnormal kidney function; hair loss; sleep disturbances; numbness and tingling in hands, feet, and mouth; decreased ability of the body to fight infection; increased risk of certain types of cancer, such as skin cancer, cervical cancer, and rarely lymphoma (lymph node cancer).

Cyclosporine

Cyclosporine (also called Neoral, Sandimmune, SangCya, Gengraf, Eon) is a primary immunosuppressive agent that is classified as a calcineurin inhibitor. This drug has been in use to prevent rejection in transplant recipients for more than 30 years.

Notes About Cyclosporine

• You should not stop taking cyclosporine or change the dose or the time at which you take it unless your transplant team instructs you to do so.

• Cyclosporine should be taken in the morning and at night, about 12 hours apart. Some patients need only one dose daily.

• The amount of cyclosporine in your blood is monitored by blood tests. Do not take cyclosporine on the day you are having blood tests until after the blood is drawn.

• Always take the correct dose of cyclosporine after your blood has been drawn.

• Cyclosporine may interact with some commonly used medications, such as antibiotics and high blood pressure medications. It is very important that you check with the transplant team before starting any new medications, especially antibiotics.

Possible Side Effects

Hand tremors or shaking; numbness or tingling in the hands, feet, mouth, or lips; decreased ability of the body to fight infection; abnormal kidney function tests; high blood pressure; swollen gums; hair growth; runny nose; high cholesterol; upset stomach; headache; increased risk of certain types of cancer, such as skin cancer, cervical cancer, and rarely lymphoma (lymph node cancer).

Sirolimus

Sirolimus (Rapamune, rapamycin) is another immunosuppressant that is similar in chemical structure to tacrolimus.

It does not cause kidney dysfunction but cannot be used immediately after transplantation because it delays healing of the surgical wound and rarely causes blood clots in the artery leading to the liver. Sirolimus is sometimes used several months or years after transplantation in patients who are at risk of kidney failure. It can be used in combination with low doses of cyclosporine or tacrolimus.

Notes About Sirolimus

• Take sirolimus 4 hours after cyclosporine or tacrolimus.

• Sirolimus comes in liquid and pill form. The liquid can be mixed only with water or orange juice and must be placed in a glass or plastic container.

• Sirolimus comes in a multidose bottle or single-dose foil pouches.

• Sirolimus liquid should be kept refrigerated.

Possible Side Effects

Elevated cholesterol and triglycerides, high blood pressure, rash, acne, anemia, joint pain, low potassium, low white blood cells, low platelets, anemia, diarrhea.

Prednisone

Prednisone (Deltasone, Orasone) is an immunosuppressant and anti-inflammatory medication. Although this drug is associated with many side effects, it remains an essential part of most posttransplant immunosuppressive regimens. You will receive your first dose of prednisone intravenously during the transplant operation.

Notes About Prednisone

• Do not stop taking prednisone or change the dose or the time at which you take it unless your transplant team instructs you to do so. A sudden discontinuation of prednisone can result in a severe illness called adrenal insufficiency

• Always take prednisone with food or milk.

• If you have an episode of rejection, you may be instructed to take higher doses of prednisone.

Possible Side Effects

Increased appetite, acne, bruising, muscle weakness (especially in the upper legs and arms), stomach irritation, increased body and facial hair, mood change, decreased ability of the body to fight infections, high blood sugar, visual changes, delayed wound healing, softening of bones (osteoporosis), fluid and salt retention, anxiety, cataracts, glaucoma, night sweats, increased risk of certain cancers, menstrual irregularity.

Mycophenolate

Mycophenolate or mycophenolic acid (CellCept, Myfortic) belongs to a class of medications called antiproliferative drugs. These drugs are typically used in addition to a primary agent such as a calcineurin inhibitor. 

Notes About Mycophenolate

• Do not stop taking mycophenolate mofetil or change the dose or the time at which you take it unless your transplant team instructs you to do so.

• Always swallow the capsules whole. Do not crush them, chew them, or open them.

• If a capsule comes apart, do not inhale the powder and do not let the powder touch your skin. If the powder touches your skin, wash it thoroughly with soap and water. If the powder comes in contact with your eyes, rinse them well with water.

• Do not take mycophenolate mofetil with antacids that contain magnesium or aluminum, such as Mylanta.

• Stomach cramps, nausea, and diarrhea may be controlled by spreading the dosage of mycophenolate mofetil over the course of the day. Ask your transplant team if this is an option for you. Do not make any changes in your medication schedule before talking with them.

• You will have regular blood tests to monitor the effects of mycophenolate mofetil on your white blood cell count.

• Take mycophenolate mofetil 2 hours after cyclosporine or tacrolimus.

• Do not become pregnant or father a child while taking mycophenolate mofetil.

Possible Side Effects

Nausea; vomiting; diarrhea; stomach cramps; gas; decrease in appetite; decreased ability of the body to fight infection; increased risk of certain types of cancers, such as skin cancer, cervical cancer, and lymphoma (lymph node cancer).

Azathioprine

Azathioprine (Imuran) is an antiproliferative agent that is similar to mycophenolate. The two drugs are never used together.

Notes About Azathioprine

• Do not stop taking azathioprine or change the dose or the time at which you take it unless your transplant team instructs you to do so.

• You will have regular blood tests to monitor the effects of azathioprine on your white blood cell count.

• Do not take allopurinol (Zyloprim) for gout while taking azathioprine without discussing this issue with the transplant team.

• Women should avoid pregnancy while taking azathioprine. Contact your transplant team if you do become pregnant.

Possible Side Effects

Decreased ability of the body to fight infection; abnormal liver function tests (very rare); mouth sores; thinning hair; nausea; vomiting; bruising; increased risk of certain cancers, such as skin cancer, cervical cancer, and lymphoma (lymph node cancer).

Basiliximab

Basiliximab (Simulect) is a monoclonal antibody directed against parts of the immune system that cause acute rejection.

Notes About Basiliximab

• Basiliximab is used to prevent (but not to treat) episodes of acute rejection.

• Basiliximab can only be given intravenously.

• The first dose is usually administered in the operating room during the transplant operation.

• A second dose of basiliximab is given intravenously 4 days after the operation. 

Possible Side Effects

Acne, constipation, nausea, diarrhea, headache, heartburn, trouble sleeping, weight gain, excessive hair growth, muscle or joint pain.

Daclizumab

Daclizumab (Zenapax) is a monoclonal antibody directed against parts of the immune system that cause acute rejection.

Notes About Daclizumab

• Daclizumab is used to prevent (but not to treat) episodes of acute rejection.

• Daclizumab can only be given intravenously.

• The first dose is usually administered in the operating room during the transplant operation.

• A second dose of Daclizumab is given intravenously 4 days after the operation. 

Possible Side Effects

Chest pain, coughing, dizziness, fever, nausea, rapid heart rate, shortness of breath, swelling of the feet or lower legs, trembling or shaking of the hands or feet, vomiting, weakness.

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