Pharmacokinetics of a novel hypnotic, 450191-S, in elderly patients.

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A new hypnotic, 450191-S, was administered to five elderly patients [cerebral thrombosis: two patients (81 yr and 78 yr), gastric cancer: one patient (61 yr); chronic hepatitis: twopatients (78 yr and 70 yr)]. Pharmacokinetic behaviors of this drug in these patients werecompared with those in healthy volunteers reported in a previous study. Plasma protein binding ratio of each metabolite and urinary excretion ratio of M-4 inelderly patients were similar to those in healthy volunteers. However, some differencesin plasma concentration time course of metabolites were found between elderly patientsand healthy volunteers. In healthy volunteers, Cmax of M-1 was lower than that of M-2and M-A whereas in elderly patients Cmax of M-1 was higher than M-2 and M-A. Fromthe results of various investigations of the phenomenon, it seems that the higher plasmaconcentration of M-1 in elderly patients may be ascribed to a decrease of first-pass effect.
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