Rinsho yakuri/Japanese Journal of Clinical Pharmacology and Therapeutics

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In a controlled double-blind study the hypnotic effect of S-1530 (5 mg q.d. for 7 consecutive nights) was investigated in comparison with that of nitrazepam (5mg) and a matching placebo in a series of 156 insomniac patients divided into three groups. Twenty-one eventually dropped out, then data were analyzed for evidence of hypnotic efficacy.
By the Kruskal-Wallis H-test, there was no evidence of significant difference in effectiveness of drugs among the three groups according to global judgement by the physicians.
The data were further assessed among the three groups by Discrimination Analysis (one of Multi-variate Analysis). No statistically significant difference was demonstrated among the three regimens in hypnotic efficacy of the initial dose, nor in promptness of effect, whereas both S-1530 and nitrazepam were significantly more effective than placebo on day 7 of medication with respect to induction and depth of sleep, number of awakenings before rising, dreaming, and feeling or mood on the following morning. It is suggested from the findings that the moode-levating and tranquilizing effects of S-1530, as well as nitrazepam, were beneficial at least partly in inducing and deepening sleep. The stochastical test, however, failed to reveal any significant difference in efficacy between S-1530 and nitrazepam. Nor was there significant difference among the three regimens with regard to incidence of side effects.

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Clinicopharmacological effects and pharmacokinetics of a new triazolobenzo-diazepine derivative, D-40 TA, were studied in five healthy male volunteers (total cases amounting to six).
A single dose of 4 mg of D-40 TA was given orally between 9 and 10 o'clock in the morning. On the average, all subjects fell asleep within 28±12 min and slept for 4.8±1.7 hr after taking the drug.
Changes of physiological function were observed, such as hypotension, decrease of bowel tone, equilibrium disturbances and lowering of tractive force, but these changes were slight and recovered within twelve hours. There were no significant changes in respiratory rate, pulse rate, cutaneous blood flow, GSR and EKG.
The results of psychomotor performance tests indicated that D-40 TA caused moderate to marked impairment of psychomotor function in three out of five subjects.
The quantitative determination of unchanged D-40 TA in blood, urine and feces was carried out concurrently, but close relationship was not shown between blood level of D-40 TA and clinical symptoms.
It was concluded that D-40 TA had a potent hypnotic activity with good tolerability in man.

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