Is tacrolimus used for preventing organ rejection and treating autoimmune diseases?

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Last updated: June 20, 2025View editorial policy

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From the Guidelines

Yes, tacrolimus is used for preventing organ rejection and treating certain autoimmune diseases. Tacrolimus (also known by brand names Prograf, Advagraf, or Astagraf XL) is a potent immunosuppressant medication primarily prescribed to prevent rejection in organ transplant recipients, particularly for kidney, liver, and heart transplants. It works by inhibiting the enzyme calcineurin, which reduces T-cell activation and suppresses the immune response that would otherwise attack the transplanted organ. For transplant patients, typical oral dosing ranges from 0.05-0.1 mg/kg/day divided into two doses, with blood levels carefully monitored to maintain therapeutic concentrations (typically 5-15 ng/mL, though target ranges vary by transplant type and time since transplantation) 1. Beyond transplantation, tacrolimus is also used topically (as ointment or cream) for treating autoimmune skin conditions like atopic dermatitis and psoriasis, and systemically for conditions such as ulcerative colitis, lupus nephritis, and rheumatoid arthritis. Common side effects include nephrotoxicity, neurotoxicity, hypertension, diabetes, and increased infection risk, necessitating regular monitoring of kidney function, blood pressure, blood glucose, and drug levels.

Some key points to consider when using tacrolimus include:

  • Monitoring blood work, including CBC count, renal function, glucose level, lipid profile, and potassium and magnesium levels, as well as frequent blood pressure measurements 1.
  • Being aware of potential drug interactions, as tacrolimus is metabolized through the CYP3A4 system and can affect or be affected by other medications 1.
  • Considering the use of renal-sparing regimens, which may include combining tacrolimus with other immunosuppressants, to minimize side effects such as nephrotoxicity 1.
  • Recognizing the importance of therapeutic drug monitoring, especially when switching between different formulations of tacrolimus or other immunosuppressants 1.

Overall, tacrolimus is a valuable medication for preventing organ rejection and treating autoimmune diseases, but its use requires careful monitoring and management to minimize potential side effects.

From the FDA Drug Label

Tacrolimus capsule is a calcineurin-inhibitor immunosuppressant indicated for the prophylaxis of organ rejection in adult patients receiving allogeneic liver, kidney, or heart transplants and pediatric patients receiving allogeneic liver transplants in combination with other immunosuppressants.

Tacrolimus is used for preventing organ rejection in patients receiving allogeneic liver, kidney, or heart transplants. However, the provided drug label does not directly support the use of tacrolimus for treating autoimmune diseases. 2

From the Research

Uses of Tacrolimus

  • Tacrolimus is used for preventing organ rejection in patients with solid organ transplants, including liver, kidney, heart, lung, pancreas, and intestinal transplants 3, 4, 5, 6.
  • It is also used as rescue therapy in patients who experience rejection or poor tolerability to cyclosporin 3, 4, 7.
  • Tacrolimus has been shown to be effective in reducing the incidence of acute rejection and allowing for the reduction of corticosteroid use 3, 4.
  • It has a different tolerability and efficacy profile compared to cyclosporin, making it a useful alternative for patients who experience adverse effects with cyclosporin 3, 4, 7.

Autoimmune Diseases

  • While the provided studies primarily focus on the use of tacrolimus in preventing organ rejection, there is limited information on its use in treating autoimmune diseases.
  • However, tacrolimus has been shown to have immunosuppressive properties, which may be beneficial in treating autoimmune diseases 6.

Adverse Effects

  • Tacrolimus can cause adverse effects such as nephrotoxicity, neurotoxicity, diabetes mellitus, and gastrointestinal intolerance 3, 4, 6, 7.
  • These adverse effects can be managed by converting patients to cyclosporine-microemulsion-based therapy, which has been shown to be an effective treatment option 7.

References

Professional Medical Disclaimer

This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.

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