Zopiclone in insomniac shiftworkers. Evaluation of its hypnotic properties and its effects on mood and work performance.

Fifty adult insomniac shiftworkers (47 males and 3 females) between the ages of 22 and 55 participated in this two-week, double-blind comparative study of the hypnotic properties and effects on mood and work performance of zopiclone 7.5 mg and placebo. All subjects took inactive medication on the first night of the study and then received either zopiclone or placebo for the following 13 nights according to randomization. Pre-study variables included a demographic profile, medical history, physical examination, laboratory data, profile of insomnia and work shift pattern description. A sleep questionnaire along with mood and work performance questionnaires were filled out on Days 1, 2, 4, 9 and 12 of the study; on Days 7 and 14, adverse events were recorded. After the first placebo night, subjects assigned to receive zopiclone showed significantly improved sleep induction; from the second night on, a distinct pharmacological effect over placebo was observed and maintained since statistically significant increases in quantitative sleep induction and sleep soundness (qualitative and quantitative) were noted during the course of zopiclone treatment. Active hypnotic treatment did not interfere with morning awakening and functioning, nor did it affect mood or work performance. Zopiclone treatment produced significantly more taste disturbance and drowsiness. In summary, zopiclone was shown to be an effective, fast-acting hypnotic which maintained its efficacy over a two-week period in our sample of insomniac shiftworkers and did not produce mood changes or influence work performance.

Zopiclone: a new nonbenzodiazepine hypnotic used in general practice.

Ninety-one insomniacs completed a four-week study of the efficacy and safety of zopiclone (Z), 7.5 mg. Patients were randomly allocated to one of two groups, each of which received placebo (P) during one week of the study. Forty-six subjects received medication in the sequence of ZPZZ, and 45 received it in the sequence of ZZPZ. Twice each week, patients filled out presleep and postsleep questionnaires and reported their morning complaints. Compared with placebo, zopiclone produced statistically significant improvements (P less than 0.05) in sleep induction time, duration of sleep, number of awakenings per night, quality and soundness of sleep, morning state of rest, and daytime sleepiness. Headache, dizziness, nausea, and bitter taste were the predominant complaints. Zopiclone can be considered an efficient and safe hypnotic for chronic insomnia.

In vitro labeling of beta-apolipoprotein with 3H or 14C and preliminary application to turnover studies.

3-H- or 14-C-labeled methyl groups were introduced into apolipoproteins of human and pig low density lipoproteins (LDL). 98% of the label was recovered in the apoprotein of radiomethylated LDL. Such methylated lipoprotein was compared with the corresponding unlabeled LDL with respect to its electrophoretic and immunochemical properties, and its behavior in the analytical ultracentrifuge. The data demonstrated that neither the human nor pig LDL underwent gross changes as a result of methylation. The applicability of radiomethylated pig LDL as a tracer for studying the turnover of LDL in pigs was examined. The results showed that the behavior of unscreened and screened 3-H-labeled LDL was similar. The LDL disappeared with an initial t1/2 of 1.1 hr and a later t1/2 of 30 hr. These values agreed well with those reported for radioiodinated LDL. The technique of radiomethylation of lipoprotein may afford an advantage over radioiodination as it may label peptides that do not have tyrosine.