Interaction by Cholestyramine on the Uptake of Hydrocortisone in the Gastrointestinal Tract

Abstract

An absolute reduction of the plasma cortisol levels and a delay of the peak concentrations were recorded in 10 healthy human subjects, when a bile-sequestering anionic exchange resin, cholestyramine, was given prior to a single oral hydrocortisone dose, indicating that the resin interferes with the uptake of a neutral sterol in the human gastrointestinal tract. The possibility of a direct binding of drug to resin is supported by the affinity of hydrocortisone to cholestyramine in vitro, which was uninfluenced by the presence of sodium taurocholate. Cholestyramine significantly delayed the gastric emptying of a glucose solution, indicating that the resin not only decreases but also delays hydrocortisone absorption. Careful supervision is recommended when treatment with cholestyramine is given concomitant to neutral sterol drugs.