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Effect of Glycosylation on Carbamazepine‐Serum Protein Binding in Humans

Effect of glycosylation on carbamazepine‐serum protein binding was investigated in vitro using the serum from 24 diabetics and 10 healthy subjects, and in vivo using the serum from 49 patients receiving carbamazepine. In both binding studies, nonglycosylated albumin levels were strongly correlated with the carbamazepine free fraction (%). To evaluate the effect of glycosylation in vivo, the patients were divided into two groups according to glycosylated albumin levels (%): a healthy group (10–15) and a high group (15 and over). The high group had decreased nonglycosylated albumin levels and an increased carbamazepine free fraction. Our results suggest that one should not use total concentrations for the monitoring of serum carbamazepine concentrations, but free concentrations, especially in poorly controlled diabetics.