Pharmacokinetics and metabolism of brotizolam in humans

Pharmacokinetic studies were performed in healthy young volunteers and in elderly patients after oral administration of single doses (0.5 mg), increasing doses (0.5-1.5 mg), and multiple doses (1.0 mg) of brotizolam. Brotizolam was absorbed quickly from the gastro-intestinal tract. Elimination half-lives were in the range of 3.6-7.9 h. In healthy young volunteers as well as in elderly patients, there was neither a tendency for brotizolam to accumulate nor was there any indication of enzyme induction. Brotizolam was metabolized almost completely into hydroxylated compounds which were conjugated prior to renal excretion. After oral administration of [14C]-brotizolam, two-thirds of excretion of radioactivity was renal and was completed within 4 days.