PubMed · 6569711
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J F Peutillot, A Peutillot. 1984. [Moxadil].. https://pubmed.ncbi.nlm.nih.gov/6569711/
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Antidepressant drugs, such as the tricyclics and the serotonin reuptake inhibitors, are well known to decrease paradoxical sleep and occasionally increase slow wave sleep in human and in animals. In order to examine whether amoxapine (a mixed NA reuptake blocker and 5-HT2/5-HT3 antagonist) and cericlamine (a selective 5-HT reuptake inhibitor) exert the same effect in rats, and to investigate the possible relationships between sleep, the action of antidepressants and the serotoninergic system, the effects of these two different drugs were examined under acute and chronic conditions. Acutely, amoxapine (1, 5 and 10 mg/kg; i.p.) and cericlamine (1, 8, 16 and 32 mg/kg; i.p.) decreased paradoxical sleep and increased deep slow wave sleep especially when they were given at a low dose. When administered for 14 days, amoxapine induced a sustained decrease of paradoxical sleep during the whole treatment, while some tolerance was observed with regard to the inhibitory effect of cericlamine on this state of sleep. In addition, a rebound of paradoxical sleep occurred on the first day of cericlamine withdrawal. Thus, amoxapine and cericlamine exerted the same effects on the states of vigilance in the rat as do other antidepressants. The effects of cericlamine on sleep probably reflect its blocking action on 5-HT uptake, whereas the more complex effects of amoxapine might involve its 5-HT2/5-HT3 antagonist properties.
Analysis of National Health Service prescription data for the antidepressants from 1980 to 1989 shows a consistent secular trend towards the increased use of generic names on prescriptions for this group of drugs. This apparently reflects national trends for all drugs, and was similar for most antidepressants. However, generic prescribing had by 1989 increased significantly more rapidly with fluvoxamine, which was introduced in 1987. The two drugs introduced in 1989, fluoxetine and amoxapine, also had a high generic prescribing rate in their year of introduction. Increased generic prescribing may become a feature with further new drugs. However, the use of the generic name on the prescription has relatively little influence on what is dispensed to the patient. Pharmacists may dispense a brand name when given a generic prescription. Moreover, pressures on doctors to write generic names on prescriptions may have limited relevance for some drugs; generic alternatives were available for only four out of 22 antidepressants.
The piperazine N-alkylcarboxylic acids of 2-chlorodibenz[b,f][1,4] oxazepine (3a), 2-chlorodibenzo[b,f] [1,4] thiazepine (3b), and dipenz[b,e] azepine (3c) from the corresponding piperazines (1a-c, R1 = H) were synthesized via the piperazine N-alkylcarboxylates (2a-c). The pharmacological activities of the piperazine N-alkylcarboxylic acids (3a-c) were evaluated. Compared with the parent compounds (1a-c), 3a-c (n = 1-5) showed weak inhibitory activities on the uptake of noradrenaline and 5-hydroxytryptamine (5-HT) into hypothalamus vesicles and moderate antagonistic actions to 5-HT2 and H1 in several tissues.