Kinetics and Dynamics of Prednisolone*

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Abstract
I. Introduction THE PHARMACOLOGICAL response (dynamics) to corticosteroids is determined by the affinity of these steroids to specific receptors at the target organ and by the availability and duration of time spent at receptor sites (1). The latter is determined by kinetic factors such as systemic availability, protein binding, distribution, metabolism, and excretion. Two comprehensive reviews of the pharmacokinetics of prednisolone have been published by Pickup in 1979 (2) and Jusko and Rose in 1980 (3). This review examines factors which modulate the kinetics and dynamics of prednisone/prednisolone, the most commonly prescribed synthetic glucocorticosteroids in clinical practice. II. Analytical Techniques In the past, investigations of prednisone and prednisolone metabolism were performed by analyzing the plasma disappearance of [3H]prednisolone (4,5). In those studies chromatography was mandatory before radioactive counting in order to distinguish between prednisolone or prednisone and labeled metabolites (5–7). GLC and spectrophotometric techniques which do not require the administration of radioactive steroid enable one to estimate prednisone and/or prednisolone concentrations in plasma, but these methods lack the sensitivity required for measuring plasma concentrations after usual therapeutic doses (8–11).

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