What are the calcineurin inhibitors?

Calcineurin inhibitors are immunosuppressants used in the management of autoimmune conditions such as lupus nephritis, idiopathic inflammatory myositis, interstitial lung disease, atopic dermatitis, and many more. In addition, they are used as mainstays for immunosuppression in solid organ transplants.

How does a calcineurin inhibitor work?

Calcineurin inhibitors are “immunosuppressants” as they work by inhibiting calcineurin, an enzyme that activates T-cells of the immune system. T-cell, also called T lymphocyte, is a type of leukocyte (white blood cell) essential for cell-mediated immunity.

What are antiproliferative agents?

Antiproliferative agents, also known as antimetabolites, inhibit cell-cycle pathways to limit T- and B-cell proliferation and thereby reducing the cytotoxic response directed toward the cardiac allograft.

Is tacrolimus a calcineurin inhibitor?

Cyclosporine and tacrolimus selectively inhibit calcineurin, thereby impairing the transcription of interleukin (IL)-2 and several other cytokines in T lymphocytes. Calcineurin inhibitors have been mainstays of immunosuppression in solid organ transplantation for over three decades.

Is sirolimus a calcineurin inhibitor?

Sirolimus (SRL) is an antiproliferative agent inhibiting the mammalian target of rapamycin (mTOR) proposed as a non-nephrotoxic alternative to calcineurin inhibitors for the prevention of acute rejection in renal transplantation.

How do calcineurin inhibitors cause hypertension?

In this study, stimulation of the β2-adrenergic receptor led to decreased transcription of the gene encoding WNK4 by increasing histone acetylation. In turn, suppression of WNK4 activated NCC, thereby causing salt-sensitive hypertension.

How do antiproliferative drugs work?

Drug-eluting stents elute antiproliferative drugs inhibiting vascular smooth muscle cell proliferation, which occurs in response to injury and thus prevents restenosis.

What are antiproliferative effects?

Medical Definition of antiproliferative : used or tending to inhibit cell growth antiproliferative effects on tumor cells.

What is the function of tacrolimus?

Tacrolimus is used with other medications to prevent rejection of a kidney, heart, liver, or lung transplant. This medication belongs to a class of drugs known as immunosuppressants. It works by weakening your body’s defense system (immune system) to help your body accept the new organ as if it were your own.

What type of immunosuppressant is tacrolimus?

What Is Tacrolimus? Tacrolimus (Prograf ®) is an immunosuppressant drug used to prevent and treat organ rejection in children who have had liver transplants. It is used for long-term immunosuppression.