[Oxypertine, peperazine derivative of tryptophan with neuroleptic and dynamogenic properties].
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Biomedical subjects
Publications and source records attributed to J Bobon.
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Eighteen inpatients suffering from a severe anxiety received in double-blind and crossover conditions iv and im injections of 10 mg diazepam, 5 mg lorazepam or saline t.i.d. during 5 days. The morning injections was made iv in a CCTV studio. Before injection and 20 mn after it, the patient filled out a 100 mm Visual Analogue Scale; his doctor-in-charge proceeded to a standard interview and to physiological measurements (tremor of hand, patellar reflexes, blood pressure, pulse rate). The videotaped interviews were randomly, i.e. time-blind, rated by two independent observers on 3 scales: the VAS, the Hamilton Anxiety Scale and an ad hoc Verbal and Non-Verbal Anxiety Scale (VNVA). The statistical analysis was completed by a logical analysis according to Lewis Carroll. The results demonstrate the superiority of lorazepam over diazepam on psychic anxiety, somatic anxiety, sleep and blood pressure, the only significant side-effect being drowsiness.
The first thioxanthene derivative without the double bind up to now considered mandatory for the antipsychotic effect, teflutixol, was administered in a phase II pilot efficacy trial to acute or subacute psychotic inpatients (mean age 36,1) during at least 5 weeks at a dosage of 3 to 20 mg p.d. once a day. The patients were abruptly switched from a haloperidol baseline therapy, which was administered on an average for 3 weeks at 15 mg p.d. Preliminary results are reported for the first 11 patients on a purely clinical basis. Despite the limitations of a small sample and of a qualitative analysis of data, it is hypothesized that teflutixol is a potent and original neuroleptic drug combining at 6 mg p.d. or less potent antidelusional, hallucinolytic and antiautistic effects. Latency and duration of action approximate 2 days. At 6 mg and above appear side-effects of the desinhibiting type (anxious and/or aggressive mood, withdrawal, flaring up of delusions, insomnia, agitation) and extrapyramidal side-effects of the akathisia type. No adrenolytic, anticholinergic or toxic effects were prominent. The patient followed up for the longest period (6 months on 3 mg p.d.) has not relapsed and has normal liver functions.
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Clopimozide is, in our opinion, a noteworthy neuroleptic drug. Its action is mainly ataraxic but also antidelusional, long-acting and accompanied with minimal side-effects. It is therefore particularly indicated in the maintenance therapy of psychotics, at a weekly dosage of 7.5 to 25 mg. The present conclusions are preliminary because of the limited number of patients (10) but also because of the rigidity of the trial protocol suggested to us.