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Action of antidepressant neuroleptics, chlorprothixene and levomepromazine, on the central noradrenergic system: comparison with other antidepressants.

In contrast to imipramine, chlorprothixene (CPX) and levomepromazine (LMZ) given chronically did not affect clonidine-induced hypothermia and depression of noradrenaline synthesis rate, while similarly to imipramine and citalopram depressed the density of cortical 3H-clonidine binding sites and increased their affinity. Two week treatment with the antidepressants did not affect the parameters of 3H-dihydroalprenolol binding sites, while spiroperidol administration increased their density, without changing KD values. The data suggest that changes in alpha 2 adrenoceptor population parameters may be a general characteristics of antidepressant treatment, but not necessarily followed by changes in clonidine effects.

Animals↗

[Relations between the levels of neuroleptics and the doses, the therapeutic effects and the side effects].

The mass fragmentography and the gas-liquid chromatography are available actually for quantitation of very low levels of neuroleptics. The Radio-immunological assay is full of promise. Their plasma levels are not correlated with their dosage in a man to another, but, for some of them, there is lineary relation for one person. A correlation between their levels and their clinical efficacy is not certainly demonstrated for thioridazine and non transformed chlorpromazine; it could be possible for his sulphoxide metabolite and for butaperazine. The sides-effects are relatively correlated with their levels in the begining of the therepautic. The antiparkinsonian drugs, the antidepressants and the lithium could influenced them.

Antipsychotic Agents↗

[Priapism in neuroleptic therapy].

The case of a 47-year old schizophrenic patient, who developed priapism on the fourth day of treatment with 40 mg Haloperidol and 50 mg Levomepromazin daily, is presented. Clinical aspects and possible mechanisms of pathogenesis are discussed.

Drug Therapy, Combination↗

The influence of chronic treatment with antidepressant neuroleptics on the central serotonin system.

Chronic administration of antidepressant neuroleptics chlorprothixene (CPX) and levomepromazine (LMZ) increases the sensitivity of one kind of serotonergic receptors in CNS-5-HT2 receptors (which are involved in such behavioral responses as head-twitches and hyperthermia in heat adapted rats), but do not change 5-HT1 receptor population (responsible for the rate of serotonin synthesis). These results confirm once more the hypothesis about the existence of at least two types of serotonin receptors in the CNS. They also indicate that antidepressant neuroleptics, which are potent serotonin 5-HT2 and alpha 1-adrenergic blocking agents, after chronic administration affect the serotonin system in a manner similar to that produced by chronic treatment with classical antidepressant drugs.

Amitriptyline↗

[Nozinan].

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Humans↗

[An anesthetic technic in dogs for studying the arrhythmogenic effects of acute coronary occlusion].

Intramuscular injection of levomepromazine (0.5 mg/kg) 30 min before intravenous injection of 10 mg/kg pentobarbital sodium induces a good surgical anaesthesia in dogs artificially ventilated with 50% N2O and 50% O2 and given 0.01 mg/kg atropine and 0.1 mg/kg pancuronium intravenously before left thoracotomy. This protocol is suitable for the study of the arrhythmogenic effects of acute one-stage coronary artery ligation in anaesthetized dogs. In fact, minor interference with the autonomic nervous system appears to be involved since heart rate is maintained slow and mean aortic pressure is kept within normal limits, as pH, PaO2, anc PaCO2 during subsequent periods. Acute circumflex coronary arterio-venous pedicle ligation close to the left main trunk division resulted in this model in a high incidence of ventricular fibrillation (10 out of 15 dogs) early (7 +/- 4 min) after occlusion. Specific interventions aimed at reducing the incidence of early post-ischemic life-threatening ventricular arrhythmias might be tested in this model.

Anesthesia, General↗