Elie R, Frenay M, Le Morvan P, Bourgouin J
Department of Psychiatric Research, Louis-H. Lafontaine Hospital, Canada.
Int Clin Psychopharmacol. 1990 Apr;5 Suppl 2:39-46.
Most studies with zopiclone, a cyclopyrrolone derivative with a short elimination half life (5 h) have compared its hypnotic activity with that of long elimination half life molecules. In this double-blind study in geriatric patients, drugs were administered during 3 weeks and the therapeutic effects of zopiclone at optimal dosage (5 or 7.5 mg) were compared to those of triazolam (0.125 or 0.25 mg). After a 3 day single-blind washout period, placebo responders were excluded and 48 patients were thereafter treated with either placebo (Tétreault et al., 1965), zopiclone or triazolam (Pegram et al., 1980). The initial dosage was increased when indicated at the end of the first week and kept constant thereafter. At the end of the third week of double-blind treatment, a 4 day single-blind placebo washout was performed to assess drug withdrawal effects. Results confirmed the safety and efficacy of both drugs over placebo during active administration. Hypnotic activity was maximal at 7.5 mg of zopiclone and 0.25 mg of triazolam. Drug efficacy was found constant over the 3 week administration both for triazolam and zopiclone. During withdrawal, no true rebound effect was demonstrated but the active drugs were significantly worse than placebo during the first day for sleep onset duration, sleep soundness and quality of sleep. With triazolam some effects persisted up to the third day of withdrawal.
大多数关于佐匹克隆(一种消除半衰期较短,为5小时的环吡咯酮衍生物)的研究,都将其催眠活性与消除半衰期较长的分子进行了比较。在这项针对老年患者的双盲研究中,药物给药为期3周,并将佐匹克隆最佳剂量(5或7.5毫克)的治疗效果与三唑仑(0.125或0.25毫克)的治疗效果进行比较。经过3天的单盲洗脱期后,排除了安慰剂反应者,此后48名患者接受安慰剂(泰特罗等人,1965年)、佐匹克隆或三唑仑(佩格拉姆等人,1980年)治疗。如果在第一周结束时需要,初始剂量会增加,此后保持不变。在双盲治疗的第三周结束时,进行了为期4天的单盲安慰剂洗脱,以评估停药效果。结果证实了两种药物在积极给药期间相对于安慰剂的安全性和有效性。佐匹克隆7.5毫克和三唑仑0.25毫克时催眠活性最大。发现三唑仑和佐匹克隆在3周给药期间药物疗效保持不变。在停药期间,未显示出真正的反跳效应,但在停药第一天,活性药物在入睡持续时间、睡眠深度和睡眠质量方面明显比安慰剂差。使用三唑仑时,一些影响持续到停药第三天。