Calcineurin inhibitors are a class of immunosuppressant medications that are commonly used to prevent rejection after organ transplantation. The two major calcineurin immunosuppressants used are cyclosporine and tacrolimus.

Workings

Calcineurin Inhibitor work by inhibiting the action of calcineurin, which is an enzyme that plays a key role in the immune system's response. When an organ transplant is performed, the immune system sees the transplanted organ as foreign and mounts an attack. Calcineurin activates T cells, which are white blood cells that are essential for transplant rejection. By blocking calcineurin, the calcineurin immunosuppressants prevent T cell activation and suppress the immune response, reducing the risk of transplant rejection.

Types of Calcineurin Inhibitors
The two main types of calcineurin immunosuppressants are cyclosporine and tacrolimus:

- Cyclosporine was one of the first immunosuppressant drugs developed for organ transplantation and is still commonly used today. It was approved for medical use in the 1980s.

- Tacrolimus, also known as FK506, was developed in the 1980s as an alternative to cyclosporine. It is considered more potent than cyclosporine. Tacrolimus became the most commonly used calcineurin immunosuppressant after kidney transplantation in the 1990s.

Both cyclosporine and tacrolimus come in various formulations including capsules, injections, and topical ointments. The specific formulation used depends on the type of transplant and individual patient factors.

Uses of Calcineurin Inhibitors
Calcineurin immunosuppressants are routinely used as the backbone of most immunosuppressive regimens following organ transplantation. They help prevent rejection of the transplanted organ and have been shown to significantly improve short and long-term transplant survival rates. Some common uses include:

- Kidney transplantation - calcineurin immunosuppressants are a key part of standard triple immunosuppression therapy along with corticosteroids and an anti-proliferative drug like mycophenolate or azathioprine.

- Liver transplantation - Tacrolimus is generally the preferred first-line calcineurin immunosuppressant due to its lower risk of nephrotoxicity compared to cyclosporine.

- Heart transplantation -Tacrolimus is the predominant calcineurin immunosuppressant used due to its more potent immunosuppressive effects. It helps reduce rejection risks.

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