Information about Tacrolimus
Tacrolimus is a calcineurin inhibitor and potent immunosuppressive agent used largely as a means of prophylaxis against cellular rejection after transplantation.
Liver safety of Tacrolimus
Tacrolimus therapy can be associated with mild serum enzyme elevations, and it has been linked to rare instances of clinically apparent cholestatic liver injury.
Mechanism of action of Tacrolimus
Tacrolimus (ta kroe' li mas), also known as FK506, is a macrolide antibiotic which also has profound immunosuppressive properties, particularly affecting T cells and the cellular immune response. Tacrolimus acts as a calcineurin inhibitor which is responsible for activating an important signal transduction molecule in the pathway of T cell activation. The result of the inhibition is a decrease in maturation of T lymphocytes and reduction in lymphokine production, including IL-2.
FDA approval information for Tacrolimus
Tacrolimus was approved for use in the United States in 1994 and rapidly became an important part of the primary regimen of immunosuppression after allogenic transplantation.
Clinical use of Tacrolimus
Current indications are for prevention of organ rejection after transplantation. It is also used off label as therapy of active and recalcitrant forms of autoimmune diseases.
Dosage and administration for Tacrolimus
Tacrolimus is available as capsules of 0.5, 1 and 5 mg in several generic forms and under the brand name of Prograf. It is also available in extended release forms and as a solution for intravenous administration (5 mg/mL). Because of variability in individual pharmacokinetics of tacrolimus, the maintenance dose varies greatly and proper dosing requires monitoring for drug levels, which is also important because of its many dose dependent side effects and drug-drug interactions.
Side effects of Tacrolimus
Common side effects of tacrolimus include headache, dizziness, paresthesias, neuropathy, hypertension, nephropathy, diabetes, acne, hirsuitism and opportunistic infections. The following drugs used to prevent transplant rejection.