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At least 19 recordsLinked to original sources
PubMed1983

Depression-inducing and antidepressive effects of neuroleptics. Experiences with flupenthixol and flupenthixol decanoate.

The antidepressive and anxiolytic efficacy of flupenthixol has been investigated in numerous controlled and open trials involving patients with endogenous, reactive as well as senile depressions. When administered at a mean daily single or multiple dose of 1-2 mg, flupenthixol proved to be a very effective and well-tolerated antidepressant. As opposed to some of the currently available antidepressants, flupenthixol has a rapid onset of action which is often displayed within the first 2-3 days following its application. Flupenthixol decanoate has also a pronounced antidepressive and anxiolytic effect which appears to be adequate enough for treating mild to moderately severe syndromes of depression. This depot neuroleptic has been given at a fortnightly dosage ranging between 2.5 and 30 mg. However, if the aspect of efficacy in relation to tolerance has to be taken in to consideration, then 5 mg are apt to be an appropriate dose. Patients with an agitated depression and/or suicide ideation should, however, be excluded from therapy with this drug. Extrapyramidal movement disorders which may appear during treatment are a disadvantage of this medication. Apparently such disorders are rarely encountered if the dose is kept below 10 mg. Other untoward effects are very seldom indeed. A final and conclusive judgement on the possible application of flupenthixol decanoate in the prophylaxis of phases in patients with bipolar and periodical depressions is as yet not feasible. Further clinical trials are necessary before flupenthixol decanoate can be classified as a possible 'depot antidepressant'.

Anxiety Disorders↗
PubMed1980

Clopenthixol and flupenthixol depot preparations in outpatient schizophrenics. I. A one year double-blind study of clopenthixol decanoate and flupenthixol palmitate.

Clopenthixol decanoate and flupenthixol palmitate, both depot neuroleptics belonging to the thioxanthene group, were studied during double-blind conditions for 12 months using four week intervals between injections. The 60 patients included in the study were chronic schizophrenics and treated as outpatients after earlier admission to hospital and rehabilitation training periods. They had all been treated with depot neuroleptics in the last three years and they had been free from relapse for at least 15 months. The main aim with this trial was to study the two depot drugs during maintenance treatment conditions in an outpatient setting. Ten patients dropped out, 7 because of unsatisfactory effect, mainly because only limited dose levels were accepted according to the design. In spite of the earlier long lasting neuroleptic treatment and the good social adaptation in this schizophrenic subgroup there was observed a symptom decrease in all the rating scales even in these symptom poor patients. This improvement in psychopathology with optimal results after half a year seems to be a combined result of the efficient neuroleptics tested and careful monitoring of the drug.

Adult↗
PubMed1983

Alterations in cerebral dopamine function caused by administration of cis- or trans-flupenthixol for up to 18 months.

Rats received either cis-flupenthixol (0.8-1.2 mg/kg per day) or trans-flupenthixol (0.9-1.2 mg/kg per day) continuously in drinking water for periods up to 18 months. cis-Flupenthixol, but not trans-flupenthixol, initially inhibited apomorphine-induced stereotyped behaviour but by 6 months and thereafter the stereotyped response was enhanced compared to age-matched control animals. Striatal and mesolimbic homovanillic acid and 3,4-dihydroxyphenylacetic acid concentrations were elevated for up to 3 months after starting cis-, but not trans-flupenthixol intake, but thereafter levels generally fell below those for age-matched control animals. Dopamine concentrations were not altered by cis- or trans-flupenthixol administration. The number of striatal [3H]spiperone binding sites (Bmax) was decreased by 40% after 1 months' administration of cis-flupenthixol but this gradually reversed, such that by 18 months a 40% increase in Bmax was apparent. Administration of trans-flupenthixol decreased Bmax up to 3 months but thereafter values were not different from those found in age-matched control animals. The dissociation constant (KD) for [3H]spiperone binding in striatum was not altered by 6 months cis-flupenthixol intake, but then increased as drug administration continued. trans-Flupenthixol administration did not alter striatal KD values. Bmax for [3H]spiperone binding to mesolimbic preparations was not altered by up to 12 months cis-flupenthixol intake, but was decreased after 18 months drug administration. cis-Flupenthixol administration had no effect on mesolimbic KD values. Administration of trans-flupenthixol for up to 18 months did not alter mesolimbic Bmax or KD values for [3H]spiperone binding.(ABSTRACT TRUNCATED AT 250 WORDS)

3,4-Dihydroxyphenylacetic Acid↗
PubMed1982

Increased striatal acetylcholine after 14 months cis-flupenthixol treatment in rats suggests functional supersensitivity of dopamine receptors.

Rats received continuous administration of cis-flupenthixol (0.8-1.2 mg/kg/day) or trans-flupenthixol (0.9-1.2 mg/kg/day) in drinking water for 14 months. The administration of cis-flupenthixol, but not trans-flupenthixol, caused apparent cerebral dopamine receptor supersensitivity. Thus, animals receiving cis-flupenthixol, but not trans-flupenthixol, showed enhanced apo-morphine-induced stereotyped behaviour. Dopamine concentration in striatum was not altered by drug treatment but striatal HVA and DOPAC concentrations were reduced in animals receiving cis-flupenthixol, but not trans-flupenthixol. No consistent change in Bmax of KD for specific striatal 3H-spiperone binding was observed after 14 months drug intake. However, in cis-flupenthixol treated animals a 40% increase in Bmax was observed following 2 weeks drug withdrawal. Continuous cis-flupenthixol intake increased striatal acetylcholine concentrations; trans-flupenthixol was without effect. This suggests the apparent increase in cerebral dopamine receptor supersensitivity caused by continuous long-term cis-flupenthixol administration is of functional importance in the intact animal.

Acetylcholine↗
PubMed1984

Alterations in different populations of striatal dopamine receptors produced by 18 months continuous administration of cis- or trans-flupenthixol to rats.

Administration of cis-flupenthixol (0.8-1.2 mg/kg per day) for 18 months enhanced stereotyped behaviour induced by apomorphine, bromocriptine and lergotrile, but not that induced by amphetamine or lisuride. Catalepsy induced by acute administration of haloperidol, trifluoperazine or cis-flupenthixol was reduced by continuous chronic intake of cis-flupenthixol. The number (Bmax) and dissociation constant (KD) of specific [3H]spiperone binding sites on striatal membranes was increased by chronic administration of cis-flupenthixol, but not trans-flupenthixol. In contrast, the Bmax and KD for specific binding of [3H]N,n-propylnorapomorphine were decreased by administration of cis-flupenthixol compared to the effect of the trans-isomer. Specific binding of [3H]piflutixol was unaffected by chronic administration of cis- or trans-flupenthixol, but chronic administration of cis-flupenthixol enhanced stimulation by dopamine of the activity of striatal adenylate cyclase. As a result of chronic continuous administration of cis-flupenthixol dopamine receptors in the striatum appeared to be supersensitive to most dopamine agonists but sub-sensitive to dopamine antagonists. This was reflected by increased numbers of D-2 antagonist receptor sites of decreased affinity, but by a decreased number of agonist sites of higher affinity. The D-1 recognition sites appeared to be unaltered, but activity of adenylate cyclase stimulated by dopamine was enhanced, suggesting post-junctional changes. The D-2 receptors appear to be primarily concerned with altered function of dopamine receptors.

Adenylyl Cyclases↗
PubMed1986

Neurotic depression accompanied by somatic symptoms: a double-blind comparison of flupenthixol and diazepam in general practice.

A total of 192 patients suffering from mild to moderate depression, with or without anxiety, accompanied by one or more specific somatic symptoms, was entered into a double-blind, multi-centre trial to compare flupenthixol and diazepam as treatments for psychosomatic syndromes in general practice. Each patient was treated for 4 weeks and assessed after 1, 2 and 4 weeks on the Hamilton Depression Scale, with visual analogue scales of depression and somatic symptoms, by global assessments (psychological and somatic symptoms) and on a side-effects scale. The principal somatic symptoms were tension headache (69 patients), epigastric discomfort (59 patients), chest pain (39 patients) and backache (25 patients). There were 9 drop-outs (2 on flupenthixol and 7 on diazepam), of whom 5 (2 on flupenthixol and 3 on diazepam) who were treated for at least 2 weeks were included in the analysis of results. All patients received 1 tablet a day (0.5 mg flupenthixol or 2.5 mg diazepam) for the first week. Thereafter, all except 5 patients (3 on flupenthixol and 2 on diazepam) had their dose doubled for the remaining 3 weeks of study. Both drugs were effective in producing consistent improvement in all four somatic symptom groups in terms of both depression and somatic symptoms over the 4 weeks of study. There was a trend throughout in favour of flupenthixol as the more therapeutically effective. Flupenthixol was significantly more effective in relieving depressive symptoms and somatic symptoms in all four somatic symptom groups considered together. It was also superior to diazepam as measured by its effect on the depression sub-scales, anxiety, agitated depression, retarded depression and melancholia. Both drugs were well tolerated, although diazepam-treated patients showed a moderate increase in side-effects scores initially, while the scores in patients treated with flupenthixol decreased consistently over all 4 weeks of the trial. It is concluded from this study that flupenthixol has an important place in the management of patients with psychosomatic illness.

Adult↗
PubMed1994

Continuous or intermittent cocaine administration: effects of flupenthixol treatment during withdrawal.

Research indicates that chronic daily cocaine injections produce sensitization to, while the chronic continuous infusion of cocaine produces tolerance to, its behavioral and neurochemical effects. The present experiments examined whether flupenthixol administration during withdrawal would attenuate/eliminate the behavioral effects produced by these administration regimens. The rats were pretreated for 14 days with either continuous or intermittent daily injections of cocaine, and were then withdrawn from the pretreatment regimen for 7 days. On days 1-5 of the withdrawal period, subjects received a daily 0.125-2.0 mg/kg IP injection of flupenthixol. Then on day 7 of withdrawal from the cocaine pretreatment, all rats were given a 15.0 mg/kg IP injection of cocaine. Their behavior was rated according to a modified version of the Ellinwood and Balster (6) scale for 60 min. The results indicated that flupenthixol treatment during withdrawal eliminated the tolerance normally associated with the continuous infusion of cocaine. However, this effect of flupenthixol was not dose dependent: the lowest dose had the same effect as the highest dose of flupenthixol. In the cocaine-injection subjects, flupenthixol had a slight but statistically significant reduction in the behavioral effects of cocaine. The same was true in the saline-control rats, except for the highest dose of flupenthixol, which had a significant enhancing effect on the behavioral response to cocaine. The present results suggest that the current procedures may represent an effective screening methodology for potential cocaine pharmacotherapies.

Animals↗
PubMed1981

Flupenthixol decanoate in recurrent manic-depressive illness. A comparison with lithium.

The hypothesis that flupenthixol decanoate may serve as an alternative to prophylactically administered lithium in recurrent manic-depressive illness, bipolar and unipolar type, was tested in two groups of patients. In Group I the patients were allocated randomly to maintenance treatment with either lithium or flupenthixol decanoate. The patients in Group II had previously been given lithium and were switched to flupenthixol decanoate because of unsatisfactory prophylactic effect of lithium, doubtful tablet compliance, troublesome side effects, or fear of later harmful effects. The flupenthixol decanoate dosage was 20 mg every 2-3 weeks. The study was not blind. In Group I neither lithium treatment (14 patients) nor treatment with flupenthixol decanoate (19 patients) led to a significant fall of mean episode frequency or mean per cent time ill. The reasons for this lack of response are not clear, but prognostically negative selection of the patients presumably took place before and possibly also during the hospitalization. Since absent effects cannot be compared, this part of the trial remains inconclusive. In Group II (93 patients) treatment with flupenthixol decanoate was associated with significant falls of the frequency of manic episodes and per cent time ill in mania and with significant rises of the frequency of depressive episodes and per cent time ill in depression. Increase of depressive morbidity was seen only in patients who had been given lithium during the pre-trial period and was presumably a result of the discontinuation of lithium. It is not known whether flupenthixol decanoate is of value in the prophylactic treatment of recurrent manic-depressive illness, but the drug may be worth trying in patients whose disease is dominated more by manic than by depressive recurrences and who do not respond to lithium or do not tolerate it or do not take it.

Bipolar Disorder↗
PubMed1977

Radioimmunoassay for flupenthixol in plasma.

We describe a radioimmunoassay for the neuroleptic drug flupenthixol, suitable for routine monitoring of its concentration in blood. Antibodies for the assay were raised in a sheep against a 7-carboxyflupenthixol/ovalbumin conjugate. The resulting assay, with [3H] flupenthixol as the label, is capable of detecting 2.0 microgram of flupenthixol per liter, in a 100-microliter plasma sample. The antiserum shows no cross reactivity with tricyclic drugs and low interference from the major metabolites of flupenthixol. Concentrations in plasma after a single oral dose of flupenthixol have been followed in one volunteer. Peak values were reached after 3 h. Determinations of flupenthixol after fortnightly intramuscular depot injections of the sustained-release preparation, flupenthixol decanoate, showed the extent of fluctuations during this period.

Cross Reactions↗
PubMed1982

Induction of microsomal enzyme activity by flupenthixol in chronic schizophrenics.

The effect of long-term treatment with flupenthixol on hepatic microsomal enzyme activity was studied in 12 chronic schizophrenic outpatients who had been receiving two weekly maintenance doses for at least 6 months. Antipyrine half-life was measured in the 12 patients while they continued to receive the drug. Flupenthixol was then discontinued for 6 weeks and antipyrine half-life was repeated in 7 of the 12 patients. In the 12 patients the plasma antipyrine elimination half-life was 4-24 h (mean 9.73 +/- 1.61 h) when receiving flupenthixol and there was a significant negative correlation between antipyrine half-life and the dose of flupenthixol (r = 0.582, P less than 0.05). In the seven patients to whom antipyrine was given on two occasions, antipyrine half-life was 7.33 +/- 1.07 h and 12.04 +/- 1.87 h on and off flupenthixol treatment respectively. The clearance significantly decreased when flupenthixol was discontinued, but there was no change in the apparent volume of distribution.

Adult↗
PubMed1994

Effects of the neuroleptic alpha-flupenthixol on latent inhibition in aversively- and appetitively-motivated paradigms: evidence for dopamine-reinforcer interactions.

Three experiments examined the influence of the dopamine (DA) D1/D2 receptor antagonist alpha-flupenthixol on the latent inhibition (LI) effect. LI is a phenomenon which is manifest when non-reinforced pre-exposure to a stimulus retards subsequent conditioning to that stimulus, and has been proposed as an animal model of the selective attentional processes that are disrupted in acute schizophrenia. Experiment 1 extended previous findings that neuroleptics enhance the LI effect in conditioned suppression paradigms in rats to alpha-flupenthixol (0.23 mg/kg). Experiment 2 demonstrated that this enhancement of the LI effect was also seen in a parallel appetitively-motivated conditioning paradigm at the same dose. In both Experiment 1 and Experiment 2, the enhancement of the LI effect by alpha-flupenthixol appeared to be accompanied by a decrease in the impact of the reinforcer (be it appetitive or aversive). Experiment 3 investigated the possible role of the reinforcer in the effect of alpha-flupenthixol on the LI effect in the aversive, conditioned suppression paradigm by increasing the intensity of footshock in rats treated with alpha-flupenthixol. Increasing the intensity of the footshock completely abolished the enhancement of LI found following injection of alpha-flupenthixol, a result which could not be attributed to a floor effect. The results provide no support for interpretations of the influence of DA manipulations on the LI effect that draw parallels with deficits in selective attention observed in acute schizophrenia.

Acoustic Stimulation↗
PubMed1983

Comparative double-blind study of flupenthixol decanoate and fluphenazine decanoate in the treatment of patients relapsing in a schizophrenic symptomatology.

Thirty-two chronic schizophrenics who had relapsed entered a double-blind randomised study and were followed-up for 2 years with the intention of measuring any difference in therapeutic effect and side effects between flupenthixol decanoate and fluphenazine decanoate. No differences could be seen as regards the global effect or the effect on the schizophrenic symptomatology during the first 6 months. After 1 year of treatment flupenthixol decanoate showed a trend towards a better effect on schizophrenic symptomatology. A corresponding result was seen for the depressive symptoms. There were no differences in the appearance of side effects. The need for additional neuroleptics in the initial phase seemed to be identical for both drugs. A possible slow antipsychotic effect with flupenthixol decanoate is probably due to the administered dose being somewhat low (in the present study approximately 31 mg flupenthixol corresponding to 27 mg fluphenazine). This suggests that flupenthixol should have been given in a somewhat higher dose (25 mg fluphenazine decanoate corresponding to 40 mg flupenthixol decanoate).

Adult↗
PubMed1989

An open clinical trial with the long-acting neuroleptics flupenthixol decanoate and fluphenazine decanoate in the maintenance treatment of schizophrenia.

An open clinical trial was carried out in 21 chronic schizophrenics to assess the effectiveness and side-effects of treatment with depot neuroleptics. All patients had been stabilized on fluphenazine decanoate for at least 6 months and on entry to the study were given the choice of continuing with this treatment or changing over to flupenthixol decanoate. Sixteen patients chose to receive flupenthixol decanoate (40 mg) and the other 5 fluphenazine decanoate (25 mg). Doses were given every 4 weeks during the 12-week study period. Clinical assessments were carried out every 4 weeks (Weeks 0, 4, 8 and 12) using the Brief Psychiatric Rating Scale and a side-effects checklist, and the Hamilton Rating Scale for Depression, the Schedule for Affected Disorders and Schizophrenia--Change Version, and the Global Assessment Scale were completed on entry (Week 0) and at the end of the study (Week 12). The results indicated that symptoms of depression, withdrawal, worrying, and psychomotor retardation were improved significantly (p less than 0.05) more with flupenthixol than with fluphenazine. The frequency of side-effects decreased during treatment with flupenthixol and there was a tendency towards fewer side-effects in the flupenthixol group than in the fluphenazine group after 8 weeks of treatment. It is concluded that a group of schizophrenic patients characterized by depressive symptoms or side-effects attributable to a prescribed neuroleptic might benefit from a switch to flupenthixol treatment.

Clinical Trials as Topic↗
PubMed1985

Psychosomatic disorders in general practice: comparisons of treatment with flupenthixol, diazepam and sulpiride.

One hundred and thirteen patients diagnosed as suffering from one of four common psychosomatic syndromes (psychogenic headache, cardiac neurosis, functional disturbance of the colon, or pruritus) were treated by two groups of general practitioners with flupenthixol or diazepam or sulpiride. Flupenthixol was compared with diazepam in 58 patients in one group of Belgian practices, and with sulpiride in 55 patients in another group of practices and assessed over a 4-week period for therapeutic response and adverse effects. Flupenthixol was given in a dosage of 0.5 to 2 mg a day, diazepam in a dosage of 2.5 to 10 mg a day and sulpiride 100 to 200 mg a day, in identical capsules. In the flupenthixol/diazepam comparison, there were 7 drop-outs (3 flupenthixol, 4 diazepam). Marked or moderate reduction in global assessment of illness occurred in both treatment groups, but there was no significant difference in the therapeutic effect of the two drugs. The incidence of side-effects was low and similar in the two groups. In the flupenthixol/sulpiride comparison, there were 10 drop-outs (7 flupenthixol, 3 sulpiride). A significant reduction in symptoms occurred in both treatment groups, but this was more rapid in the flupenthixol group. Side-effects were infrequent and mild in both groups.

Adult↗