Multiple-dose quazepam kinetics

Publisher Website
Google Scholar
Abstract
Quazepam, a benzodiazepine hypnotic, was studied in normal subjects to evaluate steady-state kinetics of quazepam and of its major active plasma metabolites 2-oxoquazepam and N-dealkyl-2-oxoquazepam after 15 mg once daily by mouth for 14 days. The kinetics of quazepam and 2-oxoquazepam can be best described by a 2-compartment open model with 1st-order absorption/formation kinetics. Quazepam was rapidly absorbed and its 2 major plasma metabolites appeared quickly in systemic circulation. The elimination t1/2 [half-life] of quazepam, 2-oxoquazepam and N-dealkyl-2-oxoquazepam were 41, 43 and 75 h, respectively. Steady-state levels were predictable from the kinetic data and were reached by the 7th dose for quazepam and 2-oxoquazepam and by the 13th dose for N-dealkyl-2-oxoquazepam. These kinetic profiles may explain the clinical hypnotic effect of quazepam, i.e., rapid induction of sleep and long duration of clinical action without appreciable rebound insomnia.

This publication has 1 reference indexed in Scilit: