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PubMed1997

[The effect of Imovane on sleep structure and respiratory indices during sleep in insomnia patients].

Night sleep was examined in 120 patients with different forms of insomnia. The positive effect of Imovane was shown both on presomnic and intrasomnic disorders. Transitory side effects (dryness, bitter taste in the mouth) were in some cases that didn't need cessation of therapy. Polysomnographic studies confirmed effectivity of Imovane: there were observed either lengthening of the duration of sleep, its 2 stage, delta-sleep, or decrease of the duration of falling asleep. There were no respiratory changes after course of Imovane, meanwhile some indices positive dynamics was revealed in this case.

Adolescent↗
PubMed1997

[Zopiclone dependence. Report of one case].

We report a 55 years old married woman without history of drug dependence. Due to a severe marital conflict she developed a chronic adjustment disorder with depressed mood. Zopiclone, 7.5 mg at night was prescribed for her insomnia and she rapidly became tolerant and dependent to the hypnotic. She was admitted to a psychiatric clinic, slowly detoxified and treated with pharmacotherapy and psychotherapy. Six months later, she has resumed her housekeeping and professional activities and is maintained with a benzodiazepine at night for insomnia.

Azabicyclo Compounds↗
PubMed1998

[Adverse effects of zopiclone].

In 1994 zopiclone (Imovane), a cyclopyrrolon, was introduced in Norway as a new kind of hypnotic. In 1996 zopiclone had a 26% share of the hypnotic market. This review of relevant literature has revealed a lack of documentation on the adverse effects of zopiclone. The similarities between zopiclone and benzodiazepine hypnotics are more striking than the differences. The bulk of comparative research has been carried out with triazolam, a drug taken off the Norwegian market in 1991. With zopiclone there is less inhibition of psychomotor function the day after intake than with flunitrazepam. Zopiclone causes less subjective "hangover" than nitrazepam, but there is a similar inhibition of psychomotor function the day after intake, and in some cases greater addictive potential.

Azabicyclo Compounds↗
PubMed1998

Zopiclone in the treatment of insomnia: an open clinical trial.

The purpose of this study was to examine the efficacy and adverse effects of zopiclone in Thai psychiatric patients. Thirty-two insomniac outpatients with a variety of diagnoses participated in this study. Zopiclone at the dose of 7.5-15 mg was administered 15 minutes before bedtime. The sleep-questionnaire items included: 1) sleep induction; 2) duration of sleep; 3) number of awakenings, 4) sleep quality; 5) dream incidence; and 6) condition in the morning. The mean scores of each item were compared by using pair t-test. One week after treatment, significant improvement was found in all items, except item 5. In comparison between sleep at 1 week and 3 weeks after treatment, further improvement was still found in the first three items. The adverse effects found were bitter taste, drowsiness, and headache. In conclusion, zopiclone is an effective hypnotic with few adverse effects.

Adult↗
PubMed1998

[An autopsy case of poisoning by neuropsychopharmaceuticals including zopiclone].

We report here a suicide case involving neuropsychopharmaceuticals. The deceased was a 30-year-old housewife, 151 cm in height and 46.0 kg in weight. Macroscopically, slight lung congestion and edema and slight brain edema were noted. The stomach contained approximately 200 ml of a greenish-brown material with many solid granules. Toxicological analysis demonstrated 44.9 micrograms/ml of zopiclone (ZP), 12.8 micrograms/ml of phenobarbital (PB), 10.9 micrograms/ml of chlorpromazine (CPZ), and 4.8 micrograms/ml of promethazine (PM) in the gastric contents; 0.5 microgram/ml of ZP, 8.6 micrograms/ml of PB, 0.2 microgram/ml of CPZ, and 0.3 microgram/ml of PM in the serum; and 43.0 micrograms/ml of ZP, 8.1 micrograms/ml of PB, 1.3 micrograms/ml of CPZ, and 1.3 micrograms/ml of PM in the urine. On the basis of these findings, the cause of death was considered to be neuropsychopharmaceutical poisoning; ZP was most probably responsible for her death.

Adult↗
PubMed2000

Synthesis and analgesic activity of some side-chain modified anpirtoline derivatives.

New derivatives of anpirtoline and deazaanpirtoline modified in the side chain have been synthesized. The series includes compounds 3 with side-chains containing piperidine or pyrrolidine rings, compounds 4 containing 8-azabicyclo[3.2.1]octane moiety, and compounds 5 having piperazine ring in their side-chains. Their receptor binding profiles (5-HT1A, 5-HT1B) and analgesic activity (hot plate, acetic acid induced writhing) have been studied. Optimized structures (PM3-MOPAC, Alchemy 2000, Tripos Inc.) of the synthesized compounds 3-5 were compared with that of anpirtoline.

Analgesics↗
PubMed2000

Chemical synthesis and cytotoxicity of some azinomycin analogues devoid of the 1-azabicyclo[3.1.0]hexane subunit.

A series of compounds related to the left-hand domain of the azinomycins have been made and evaluated for cytotoxic activity against a small panel of human tumour cell lines. The epoxide ring is shown to be essential for biological activity. Cytotoxicity is also shown to be sensitive to changes in the substitution pattern on the aromatic ring and the amide group.

Anti-Bacterial Agents↗
PubMed1983

2-Acetylpyridine thiosemicarbazones. 5. 1-[1-(2-Pyridyl)ethyl]-3-thiosemicarbazides as potential antimalarial agents.

Reduction of the azomethine bond of 2-acetylpyridine thio- and selenosemicarbazones with sodium borohydride readily afforded the corresponding thio- or selenosemicarbazides when they were N4,N4-disubstituted. This conversion failed, however, when the thio- or selenosemicarbazones were N4-substituted or unsubstituted. A more general route to the desired thio- or selenosemicarbazides consisted of reduction with sodium borohydride of methyl 3-[1-(2-pyridyl)ethylidene]hydrazinecarbodithioate to give the 2-pyridylethyl derivative. Displacement of methyl mercaptan from the thio ester moiety of the latter by amines produced 1-[1-(2-pyridyl)ethyl]-3-thiosemicarbazides. These compounds were somewhat more active as antimalarial agents in Plasmodium berghei infected mice than the corresponding thiosemicarbazones; however, the enhancement of activity was accompanied by an increase in toxicity. Compound 7, 3-azabicyclo[3.2.2]nonane-3-carbothioic acid 2-[1-(2-pyridyl)ethyl]hydrazide, is the most potent derivative of 2-acetylpyridine we have evaluated to date.

Animals↗