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14 recordsLinked to original sources
PubMed1976

Anti-dopaminergic and anti-muscarinic effects of dibenzodiazepines: relationship to drug induced Parkinsonism.

1. The anti-dopaminergic effects of several dibenzodiazepines were examined on the dopamine-stimulated adenylate cyclase in rat striatal homogenates. The "cis" isomer of clozapine, HF-2046, was the most potent in this respect and perlapine, which is devoid of neuroleptic activity, was the weakest. 2. The anti-muscarinic effects of the same compounds were measured by using the muscarinic affinity label 3H-propylbenzilylcholine mustard. HF-2046 was the most potent and loxapine the least potent of the drugs used. 3. The anti-dopaminergic effects of the drugs correlate well with neuroleptic but not with extrapyramidal effects. The anti-dopaminergic/anti-muscarinic ratio, however, correlates well with extrapyramidal rather than neuroleptic effects.

Adenylyl Cyclases↗
PubMed1977

Clothiapine in the management of schizophrenia.

Forty Black men diagnosed as schizophrenic and admitted to Ingutsheni Hospital during a period of 3 months, were allocated alternately to treatment with either clothiapine or chlorpromazine. Six patients were excluded from the trial because of an incorrect diagnosis and 34, 17 in each group, completed the trial. The 2 groups were comparable for both severity and symptoms of their illnesses. Degrees of regression of psychotic symptoms as assessed by the Brief Psychiatric Rating Scale, were comparable for the 2 groups. Adverse effects were not troublesome with clothiapine and there was no evidence of disturbed liver function, but haemoglobin values and white cell counts were sometimes decreased. EEG studies showed that clothiapine produced an increase in the slow activity but no paroxysmal acitvity. It was concluded that clothiapine is a valuable drug for the management of actue schizophrenia.

Acute Disease↗
PubMed1977

Effects of clozapine and other dibenzo-epines on central dopaminergic and cholinergic systems. Structure-activity relationships.

Structure-activity relationships of 16 dibenzoepines, including clozapine, loxapine, clothiapine and perlapine, have been investigated with regard to locomotor inhibition, cataleptogenesis, apomorphine antagonism, arousal inhibition, effect on striatal dopamine metabolism, and in vivo and in vitro anticholinergic potency. Thioridazine and the classical neuroleptics haloperidol and chlorpromazine were included in the study for comparison. The classical tests used to detect neuroleptic activity in laboratory animals were found to be poor predictors of possible clinical effectiveness of the dibenzo-epines.

Animals↗
PubMed1975

The drug management of acute behavioural disturbances.

Some aspects of drug management of acute behavioural disorder are discussed. Drug management aims at the amelioration of the patient's ineraction with his environment; it is used as a diagnostic procedure, and to facilitate further definitive diagnosis and investigation, as a form of psychotherapeutic contact, to facilitate further psychotherapy, and to initiate a treatment programme aimed at returning the patient to being a useful and health member of society. Some methods of rapid tranquillisation are described and the drug management of the following specific behavioural disturbances are discussed: schizophrenic distrubance, acute mania, depressive behavioural disturbance, acute anxiety states, acting-out psychopathic behaviour, toxic states, epileptic furore and dyscontrol syndrome, behavioural disturbances of the elderly, and behavioural disturbances in organic conditions.

Acting Out↗
PubMed1979

Antagonism between dopaminergic and neuroleptic drugs. I. Acute administration.

In this paper we report our results concerning the antagonism between dopaminergic (bromocriptine, apomorphine, piribedil) and neuroleptic (haloperidol, chlorpromazine, reserpine, clotiapine) drugs on the eeg and behaviour of rabbits. The Monnier and Gangloff stereotaxic method was used in order to record cortical and deep structures. The use of neurophysiologic methods also enabled us to verify the magnitude and modes of the antagonism between the two types of drugs. Particularly, the dissociation between eeg and behavioural effects of this antagonism is discussed; this fact seems to confirm the hypothesis that dopaminergic drugs have a double point of attack in the CNS.

Animals↗
PubMed1979

Antagonism between dopaminergic and neuroleptic drugs. II. Chronic administration.

In this work the eeg and behavioural effects obtained after the administration of dopaminergic drugs (bromocriptine, apomorphine, piribedil) in rabbits chronically pretreated with haloperidol, chlorpromazine, clotiapine, are shown. The Monnier and Gangloff stereotaxic method was used. The aim of the study was to verify receptor supersensitivity by neurophysiologic methods. The neurophysiologic pattern of receptor supersensitivity induced by long-lasting treatment with neuroleptic drugs and its peculiarity are discussed.

Animals↗