Tacrolimus Research Paper

The major elimination process of Tacrolimus metabolites include biliary route, about 95 % of elimination takes place here (Buijsch, 2007). Urinary excretion accounts for about 2.4 % Tacrolimus elimination. Concentration of Tacrolimus metabolites is reported to increase through the biliary distraction (Buijsch, 2007). Tacrolimus metabolism goes through o-demethylation, hydroxylation and oxidtie metabolic reaction by the enzymes of , CYP3A4 and CYP3A5, in the liver and the intestinal walls. Cytochrome P450 , 13-O-demethyltacrolimus, demethylhydroxy tacrolimus, and hydroxy tacrolimus are some of the few metabolites produced by the the two step reaction (Gonschior, 1996). These metabolites contribute to the 42% blood concentration in the liver and 44.8% in the kidney (Gonschior, 1996). The blood concentration for the therapeutic range is higher in the kidney than in the liver, because the activity of the Cytochrome P450 enzymes is lower in the liver than it is in the kidney (Gonschior, 1996).
“Reduction of the 11-oxo to the 11alpha-hydroxyl group by the enzyme 11beta-hydroxydehydrogenase converts prednisone to prednisolone, its biologically active form” (Data Bank, 2008). Ones in its active form the drug can be used as an anti-inflammatory, immunosuppressant and mineralocorticoid (Medsafe,