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Moreover clearance increased by approximately fold (range –) if the dose of prednisone was >25 mg. The typical value for volume of distribution, V, (98 ± 13 l kg−1) was similar to reported values in kidney transplant patients. The oral bioavailability of tacrolimus was poor and ranged from to Abstract · Introduction · Methods · Results. The effects of renal failure on the pharmacokinetics and bioavailability of tacrolimus were investigated in rats. Experimental These results suggested that the bioavailability of tacrolimus, which is mainly metabolized in the liver and intestine after oral administration, is also influenced by renal function. PMID:
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In adult patients, tacrolimus is generally rapidly absorbed following oral administration (the time to reach maximum concentration is 1 to 2 hours), but in some patients absorption is slow or even delayed. Because of presystemic elimination, the oral bioavailability is low (around 20%) but may vary between 4 and 89%. The pharmacokinetic parameter population estimate for tacrolimus clearance and oral bioavailability were l/h and , respectively (Table 2). The final regression model for the prediction of CL using the significant covariates in an individual patient was: CL (l/h) = l/h (population estimate of clearance) ´ applicable.
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