Kinetics of five benzodiazepine hypnotics in healthy subjects

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Abstract
Kinetics of 5 benzodiazepine hypnotics (15 mg flurazepam, 1 mg flunitrazepam, 5 mg nitrazepam, 10 mg temazepam and 0.5 mg triazolam) were compared in the same group of 12 healthy subjects. Plasma concentrations of parent drugs were determined by capillary gas chromatography with electron-capture detection. For flurazepam, the N-desalkyl metabolite (DAF) was measured. Flunitrazepam, nitrazepam, temazepam and triazolam were rapidly absorbed, although there was considerable variability; mean peak times (ranges) were: 1.3 (0.3-3) h; 1.8 (0.7-6) h; 1.2 (0.3-4) h; and 1.1 (0.7-2) h. Plasma concentrations of DAF increased rather slowly and reached their maximum between 3 and 48 h aftter flurazepam. There were considerable differences in elimination t1/2 [half-life], with means of 35 (15-66) h for flunitrazepam, 28 (22-33) h for nitrazepam, 12 (8-22) h for temazepam, 2.4 (1.4-3.9) h for triazolam and 84 (40-114) h for DAF. Sex differences in elimination t1/2 were only observed for DAF i.e., 99 h in women and 69 h in men. There are considerable differences in the kinetics of the diazepines.

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