Efficacy of and tolerance to 0.25 mg brotizolam and 0.25 mg triazolam were compared in hospitalised patients (aged 20 to 69 years) with sleep difficulties. Over 6 days there were no differences in efficacy and tolerance. The physicians reported the effectiveness of the drugs as good‐to‐satisfactory in 88.6% with brotizolam and 92.0% with triazolam. The patients reported with both drugs reduced time to fall asleep, less awakenings, increased duration of sleep and improved condition on awakening.

Plasma brotizolam levels were measured in 5 elderly patients given 0.25 mg daily. The half-life of brotizolam elimination was 6.0 h after a single dose and 6.9 h after continuous administration for 3 weeks. The brotizolam concentration in plasma 2 h after the dose was 3.5 and 3.4 ng/ml, respectively, on the first and last days of the study. Brotizolam levels measured several times during the study 10 h after dosing were between 1.2 and 1.8 ng/ml. Thus, administration of brotizolam 0.25 mg/d to elderly patients for 3 weeks led neither to its accumulation nor to faster elimination. The half-life of brotizolam elimination in elderly patients was in the upper range of that found in young volunteers.

1 Efficacy of and tolerance to brotizolam when used as a preoperative hypnotic were studied in two double-blind, randomised parallel group studies. 2 Brotizolam (0.25 and 0.50 mg) was superior to placebo. Efficacy was assessed as good-tosatisfactory in 73.0% of patients with 0.25 mg and in 88.0% with 0.5 mg. A similar assessment was reached in 40.0% of patients with placebo. Brotizolam 0.5 mg was superior to 0.25 mg, and with the higher dose subjective assessments of anxiety were reduced. 3 Efficacy of tolerance to 0.5 mg brotizolam and 2.0 mg flunitrazepam were compared, and both drugs were found to be effective and well tolerated. Brotizolam maintained sleep throughout the night more effectively than flunitrazepam. 4 A dose range of 0.25-0.5 mg brotizolam is recommended as a pre-operative hypnotic.

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A long-term study of brotizolam (minimum 4 weeks: maximum 26 weeks) was carried out in hospitalized patients (29 to 95 years) who complained of sleep disturbance. 3.0% of the patients used 0.125 mg, 86.4% used 0.25 mg, and 10.0% used 0.5 mg daily. During the trial there was no evidence of tolerance. There were no symptoms of overdosage, physical and psychological dependency or withdrawal, and there were no interactions with the concurrently prescribed drugs. There were no changes in vital functions, haematology, or in the biochemical investigations of blood or urine which could be attributed to the drug.