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Antirejection immunosuppressants: Nursing Pharmacology



cyclosporine (Sandimmune, Gengraf, Neoral), tacrolimus (Astagraf XL)
mycophenolate (Cellcept, Myforic)
sirolimus (Rapamune)
Inhibition of transcription
Inhibition of nucleotide synthesis
Inhibition of growth factor signal transduction
DNA alkylation
Prevention of organ transplant rejection and graft-versus-host disease (GvHD)
  • Increased risk of cancers, new infections, reactivation of previous infections (hepatitis B)
  • Myelosuppression
  • Hepatotoxicity
  • Cardiotoxicity
  • Teratogenic
  • Vomiting, nausea
  • Hyperglycemia
  • Menstrual irregularities
  • Skin rash, alopecia, hypersensitivity reactions
  • Active infections, lymphoma
  • Pregnancy, breastfeeding
  • Concomitant vaccine administration
  • Renal or hepatic impairment
  • Tacrolimus and sirolimus (boxed warning): infants and children, clients undergoing liver transplant
  • Cyclosporine (boxed warning): systemic hypertension and nephrotoxicity
Assessment and monitoring: cyclosporine 
  • Weight 
  • Vital signs; especially blood pressure, temperature
  • Transplant site: redness, swelling, drainage
  • Symptoms of rejection: swelling of hands and legs, decreased urine output, chills, nausea, vomiting 
  • Laboratory test results: CBC, renal and hepatic function, negative pregnancy test for female clients

  • Side effects: vital signs; renal and hepatic function 
  • Evaluate therapeutic response: absence of transplant rejection
  • Purpose of medication: to prevent immune system from attacking their kidney 
  • Take consistently with or without food, at the same time each day 
  • Correct self-administration technique 
  • Avoid grapefruit and grapefruit juice 
  • Side effects
    • Increased risk of infection 
      • Hand hygiene, avoid large crows, people with infections, live virus vaccines, undercooked meats 
      • Contact healthcare provider: fever, rash, diarrhea, chills, sore throat, fatigue
    • Increased risk of skin cancer
      • Avoid excessive exposure to the sun; wear protective clothing, use sunscreen when outdoors
    • Elevated blood pressure
      • Follow up regularly with healthcare provider for monitoring 
    • Hyperglycemia 
      • If diabetic: check blood glucose more often; monitor for symptoms of hyperglycemia
    • Report symptoms
      • Nephrotoxicity: decreased urine output, hematuria, or urinary hesitancy 
      • Hepatotoxicity: abdominal pain, nausea, vomiting, loss of appetite, dark-colored urine, yellowing of the skin or eyes 
      • Transplant rejection: fever, decreased urine output, significant weight changes, pain at the transplant site 
    • Female clients use a reliable form of birth control; let healthcare provider know if they become pregnant

Antirejection immunosuppressants are medications used to prevent organ rejection after a transplant, which can occur when the recipient’s immune system attacks the transplanted organ. These medications are also used to prevent graft-versus-host disease, or GvHD for short, which can occur after a bone marrow transplant. GvHD is similar to transplant rejection but works the other way around, so it’s the donor or graft T cells that reject the recipient or host; and as a result, the recipient can develop life-threatening inflammation involving various organs.

Now, based on their primary mechanism of action, antirejection immunosuppressants can be classified into several groups. The first group covers inhibitors of transcription, and the main representatives here are cyclosporine and tacrolimus; the second group includes inhibitors of nucleotide synthesis, like mycophenolate; while the third group covers inhibitors of growth factor signal transduction, such as sirolimus. Finally, the fourth group includes DNA alkylating agents, like cyclophosphamide. These medications are primarily administered orally or intravenously, and once administered, all immunosuppressants ultimately suppress and disrupt the inflammatory process and prevent the progression of the disease.

Unfortunately, these medications can also increase the risk of side effects like myelosuppression; development of new infections; or reactivation of previous infections, such as hepatitis B. Some immunosuppressants, like tacrolimus and mycophenolate, have a boxed warning for the development of certain cancers, especially lymphoma and skin cancer.

Other important side effects include hepatotoxicity, cardiotoxicity, as well as teratogenic effects. Some clients might experience vomiting, nausea, hyperglycemia, and menstrual irregularities, or may develop a skin rash, alopecia, and hypersensitivity reactions like anaphylaxis. Lastly, cyclosporine has a boxed warning for systemic hypertension and nephrotoxicity.

It’s important to note that immunosuppressants are contraindicated or have boxed warnings in individuals with active infections and lymphomas, as well as during pregnancy and breastfeeding. Another important contraindication is concomitant vaccine administration. Finally, these medications should be used with caution in clients with renal or hepatic impairment. Tacrolimus and sirolimus have a boxed warning against use in infants and children, as well as in clients undergoing liver transplant.

Now, when caring for a client who has had a kidney transplant and is prescribed cyclosporine as part of their antirejection regimen, first, perform a baseline assessment including weight and vital signs, especially blood pressure and temperature. Also assess the transplant site, making note of any redness, swelling, or drainage; as well as other symptoms of rejection, which can include swelling of the hands and legs, decreased urine output, chills, nausea, and vomiting. Lastly, review their most recent laboratory test results including CBC, renal and hepatic function tests; and confirm a negative pregnancy test as needed.

Okay, moving on to client education. Explain to your client that the medication helps prevent their immune system from attacking their kidney. Encourage them to take their medication consistently with or without food, and at the same time each day. Teach your client to dispense the medication into a glass cup using the provided oral dosing syringe, mix the medication with a liquid like orange or apple juice, and to drink all of the liquid immediately. To ensure they get the full dose, instruct them to pour a little more of the drink into the glass, swirl the glass around, and then drink the liquid. Caution your client not to rinse the syringe before or after use, only dry it and replace the protective cover. Lastly, stress the importance of avoiding grapefruit and grapefruit juice while taking their medication.