Calcineurin Inhibitor
“ALERT: US Boxed Warning
Malignancies and serious infection:
Increased risk for developing serious infections and malignancies with tacrolimus or other immunosuppressants that may lead to hospitalization or death.
Mortality in liver transplantation (Astagraf XL):
Increased mortality in female transplant patients with Astagraf XL. Astagraf XL is not approved for use in liver transplantation.”
CSA NA – FDA Approved – REMS (N) – Can Ship
How Does It Work
Tacrolimus suppresses cellular immunity (inhibits T-lymphocyte activation), by binding to an intracellular protein, FKBP-12, and complexes with calcineurin dependent proteins to inhibit calcineurin phosphatase activity. Inhibition of calcineurin also is important in maintaining neuronal and synaptic integrity and homeostasis for peripheral nerve regeneration.
Indications For Use
Officially indicated for organ rejection prophylaxis. It is also prescribed off-label for use in Crohn disease (perianal/fistulizing disease), graft-versus host disease (prevention/treatment), immunosuppression (maintenance) after lung transplant, intestinal transplant, myasthenia gravis, rheumatoid arthritis (refractory), and peripheral nerve regeneration.
Precautions
Do not use in patients with a known hypersensitivity to tacrolimus.
Do not use in patients with congenital long QT syndrome
Use with caution in patients with heart failure, brady arrhythmia, taking antiarrhythmic mediations or other drugs that can lead to QT prolongation
Immunosuppressant agents including tacrolimus can increase the risk of infection leading to hospitalization or death
Immunosuppressive agents including tacrolimus may be associated with the development of malignancies that can lead to hospitalization or death
Usual Dosing
Immunosuppressants such as tacrolimus have a wide range of dosing options. For a comprehensive listing, please check an official drug monograph.
Side Effects
Immunosuppressants such as tacrolimus have an extensive side effect profile. For a comprehensive listing, please check an official drug monograph.