Diurnal variation in prednisolone kinetics

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Abstract
Plasma concentrations of free and total prednisolone were measured after oral doses at 4 time points to investigate the possibility of a diurnal variation in the drug''s kinetics. There were marked differences in plasma prednisolone concentrations, clearance rates and bioavailability of both free and total fractions at different times of the day. Changes in the protein binding characteristics of prednisolone with clock time resulted in marked differences between the kinetics of free and total prednisolone. For maximum efficacy and minimum toxicity prednisolone therapy should be confined to once/day dosing in the morning.