Tacrolimus (prograf)

Tacrolimus (prograf)

Clinical use

A substance produced by the fungus Streptomyces tsukabaenzi, which has immunomodulatory (mainly immunosuppressive) and anti-inflammatory effects. It belongs to the calcineurin inhibitor group, as does cyclosporine. A potent immunosuppressant, it is used generallyólly in the prevention of graft rejection or in the treatment of acute graft rejection and topically in atopic dermatitis. Tacrolimus inhibits the formation of cytotoxic lymphocytesów responsible for graft rejection, inhibits the proliferation of B cells dependent on helper T cells, as well as the formation of lymphokines and the expression of the interleukin-2 receptor. Tacrolimus also has an inhibitory effect on the release of inflammatory mediatorsów from skinóre mast cells, basophils and eosinophils. In the circulatory system, tacrolimus binds strongly to erythrocytes, as a result, the ratio of whole blood to plasma concentration is 20:1. The drug binds more than 98.8% to proteins, mainly albumin and acidic α-1 glycoprotein. T1/2 is 43 h in whole blood. The drug is metabolized in the liver, mainly by CYP3A4, and in the intestinal wall. The therapeutic range has not been clearly defined, but whole blood concentrations of 5 to 20 ng/ml are sought 12 hours after administration of the drug in the early post-transplant period. Achieving higher concentrations is associated with an increased incidence of side effects: kidney damage, nervous system disorders, drops in blood pressure, insomnia and nausea.

Patient preparation

no special requirements

Material: EDTA blood

Interventions

noóre drugs, uric acid - above 20 mg/dl;bilirubin - above 40 mg/dl;lipemia - triglycerideów concentration above 800 mg/dl;protein - above 12 g/dl;hematocrit <25%, >55%