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At least 19 recordsLinked to original sources

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↗

PubMed1976

A controlled comparison of flupenthixol and amitriptyline in depressed outpatients.

Sixty depressed outpatients were allocated to treatment with either amitriptyline (75-225 mg/day) or flupenthixol (1-5-4-5 mg/day) in flexible dosage for six weeks under double-blind procedures. Various objective and subjective assessments were carried out before and after one, three, and six weeks of treatment. Twenty-three patients completed the course of amitriptyline and 28 the course of flupenthixol. Almost all variables improved significantly over time, irrespective of drug. On most ratings there were no significant differences between the two drugs, but the trends favoured flupenthixol. In particular, flupenthixol lessened anxiety scores more than amitriptyline. Unwanted effects were few and not troublesome except in two patients receiving amitriptyline. Flupenthixol, in low dosage, is a useful alternative antidepressant for depressed outpatients.

Adult↗

PubMed1977

Long-term behavioural and biochemical effects following prolonged treatment with a neuroleptic drug (flupenthixol) in rats.

The effects of long-term treatment (36 weeks) with a neuroleptic drug (flupenthixol) were investigated behaviourally and biochemically in rats. Sixteen rats were trained on a DRL (differential reinforcement of low rate) 15-s schedule until stable responding was obtained. During the following 36 weeks 9 rats were injected weekly with flupenthixol dissolved in Viscoleo [4 mg/kg(i.m.)] and seven rats received Viscoleo alone. During this period the animals were not run on the DRL schedule. Retesting on DRL 7 weeks after the last drug injection yielded highly significant differences between the flupenthixol-treated animals and the controls. Thorough neurological examinations of the animals just preceeding the retesting period also revealed some deficits in the flupenthixol-treated animals. At sacrifice, 14-18 weeks after the last drug injection, levels of homovanillic acid (HVA) were measured in the corpus striatum and total 3-methoxy-4-hydroxyphenylglycol (MOPEG) in the rest of the forebrain. The results indicate a nonsignificant increase of 25% in the dopamine metabolite HVA, while the noradrenergic metabolite MOPEG was significantly decreased by 14% in experimental animals. The possibility of persistent functional and biochemical effects produced by prolonged treatment with a neuroleptic drug is highlighted in the results presented here.

Animals↗

PubMed1979

Behavioral effects produced by long-term administration of a neuroleptic drug (flupenthixol) upon social interaction in a group of eight rats.

The behavioral effects produced by chronic treatment with alpha-flupenthixol decanoate followed by a 3-month pause upon social interaction in a group of eight rats were studied. alpha-Flupenthixol decanoate induced total disruption of two of the group formations studied, i.e., three or more in a group outside a corner and three or more following (running in a row)--the overall behavioral change shows a general depressive effect of the drug and a change in the pattern of social interaction. The shift in balance between the behavioral categories measured appeared as a significant difference in the time spent in the various group formations. Disintegration of group coherence, as shown in the measures of the degree of isolation, appeared only in the alpha-flupenthixol decanoate-treated group. An apomorphine test, which concluded the experiment 3 months after the last alpha-flupenthixol decanoate injection, revealed a significant difference in relation to licking response between the test group and the control group. The apomorphine test reported in this paper showed effects up to 90 days after the last drug treatment.

Animals↗

PubMed1975

Peroral and parenteral administration of long-acting neuroleptics: a double-blind study of penfluridol compared to flupenthixol decanoate in the treatment of schizophrenia.

Fifty-six out of 60 schizophrenic patients completed a double-blind study of two long-acting neuroleptics, penfluridol (peroral) and flupenthixol decanoate (parenteral). Half of the patients were on maintenance therapy of flupenthixol prior to the study, the other half on penfluridol. The actual double-blind study (12 weeks) was commenced after a preliminary period of 4 weeks, the patients in the two main groups being randomly divided into two further groups, one continuing the medication unchanged, the other changing to the alternative drug. It was found possible to make a sudden switch from penfluridol to flupenthixol decanoate and vice versa without any significant change in the condition of the patient. The same dosage (in 70% of the patients from 40 to 80 mg) of penfluridol was used per week as was employed for flupenthixol decanoate per fortnight. Changes in the intensity of the symptoms (total Brief Psychiatric Rating Scale (BPRS) score) were moe pronounced in the preliminary period (during unchanged treatment) than on changed medication in the blind period. Both drugs induced approximately the same degree of akathisia, Parkinsonism and autonomic side effects. The practical consequences of equipotent therapeutical effect of a peroral and parenteral long-acting neuroleptic are briefly discussed.

Administration, Oral↗

PubMed1975

A double-blind comparison of fluphenazine decanoate and flupenthixol decanoate in the treatment of acute schizophrenia.

A double-blind comparison of fluphenazine decanoate and flupenthixol decanoate in 40 consecutive admissions showed no difference in anti-psychotic effect or extrapyramidal side effects after 56 days. However, the trial identified a different effect of the drugs on mood. Flupenthixol decanoate had an elating effect that was most marked during the week following injection. Fluphenazine decanoate tended to lower mood. The results would suggest that in acute schizophrenia, fluphenazine decanoate would be the more appropriate drug in elated or acutely disturbed patients, but that in patients with a lowered mood or a history of depression, flupenthixol decanoate would be the more appropriate drug. It was emphasised that these mood changes were observed in patients with acute schizophrenia and that extrapolation from these results to maintenance therapy of chronic relapsing schizophrenia should only be made with caution. The results suggest that 40 mg of flupenthixol decanoate is approximately equal to 25 mg of fluphenazine decanoate. Analyses of covariance showed a significant positive correlation between the incidence of extrapyramidal side effects and duration of illness.

Acute Disease↗

PubMed1976

Effect of flupenthixol on depression with special reference to combination use with tricyclic antidepressants. An uncontrolled pilot study with 45 patients.

In an open, uncontrolled trial flupenthixol was administered to 45 patients with endogenous depression. The drug was markedly effective in eight patients, effective in nine patients, fairly effective in 12 patients, and ineffective or aggravating in 16 patients. Four patients showed transient manic symptoms. Dosage was 1-3 mg daily. In 36 patients flupenthixol was used in combination with previously administered tricyclic antidepressants, and in nine patients it was used alone. Clinical effect was quickly apparent. It appeared within 1 week in 63% and within 2 weeks in 93% of subjects. Side-effects were observed in 13 patients: insomnia, five patients; slight extrapyramidal symptoms, nine patients. Sedative-hypnogenic effects were rarely seen. In 71% of 17 patients in whom the drug was found to be markedly effective or effective, flupenthixol's influence on psychomotor retardation was particularly striking. Other clear benefits were relief of depressive mood, psychic anxiety, and agitation. It is recommended that flupenthixol is given, as supplementary medication, to patients (1) whose depressive symptoms other than psychomotor retardation have already improved with current tricyclic antidepressants, and (2) in whom, before antidepressant medication, psychomotor retardation is a principal feature.

Adolescent↗

PubMed1979

Blood levels of flupenthixol in patients with acute and chronic schizophrenia.

Plasma levels of flupenthixol were estimated by three methods in 30 patients with acute schizophrenia and 29 patients with chronic schizophrenia. These levels were related to clinical response, anterior pituitary hormone secretion, platelet monoamine oxidase activity, the effects of the concurrent administration of anticholinergic drugs, and body weight. No clearcut relationships between plasma flupenthixol levels and any of these variables were demonstrated. The practical clinical value of the estimation of plasma flupenthixol is limited at the present time.

Acute Disease↗

PubMed1979

3-Methoxy-4-hydroxyphenylglycol excretion in acutely schizophrenic patients during a controlled clinical trial of the isomers of flupenthixol.

Urinary MHPG excretion in patients with acute schizophrenia was studied before and during a trial of the isomers of flupenthixol and placebo. Pretrial MHPG excretion was not related to severity of illness before the trial or to other pretrial clinical variables. In male subjects higher pretrial MHPG excretion was associated with a better outcome 1 year post-trial. However in females no relationship between MHPG excretion and outcome was established. During the trial there was a reduction in MHPG excretion in patients treated with beta-flupenthixol but no decrease in the group treated with alpha-flupenthixol or chlorpromazine. In patients on placebo there was a reduction in MHPG excretion in those who did well clinically, but not in those who did poorly. Thus low MHPG excretion may be a predictor of poor outcome in schizophrenia, but MHPG excretion also changes both as a function of clinical state and of neuroleptic drug administration.

Adult↗

PubMed1977

Effect of flupenthixol and butaclamol isomers on prolactin secretion in rats.

Cis (alpha)-flupenthixol and (+)-butaclamol are effective anti-psychotic agents but trans (beta)-flupenthixol and (-)-butaclamol are not. alpha-Flupenthixol was found to be 245 times more active in elevating rat plasma prolactin than the beta-isomer. The discrepancy between (+)-butaclamol and (-)-butaclamol was even greater. These results support the hypothesis that the dopamine receptors that mediate the effects of dopamine on prolactin secretion are similar to those that mediate the anti-psychotic effect of neuroleptic drugs.

Animals↗

PubMed1976

Alpha-flupenthixol-induced hyperactivity by chronic dosing in rats.

Socially reared and isolation-reared rats treated chronically since weaning with alpha-flupenthixol showed elevated levels of spontaneous locomotor activity compared with control treated rats. However, chronic apomorphine treatment had no effect on spontaneous locomotor activity. Chronic alpha-flupenthixol treatment enhanced stereotyped behaviour after 1.5 mg/kg d-amphetamine or 0.5 mg/kg apomorphine in the socially reared condition. 'Spontaneous stereotypies' were also observed in the chronic alpha-flupenthixol-treated animals. Chronic apomorphine treatment did not affect stereotyped responding. The results are discussed in terms of 'behavioural supersensitivity'.

Animals↗

PubMed1979

A double-blind comparison of flupenthixol, nortriptyline and diazepam in neurotic depression.

A double-blind trial of flupenthixol, nortriptyline and diazepam in neurotic depression using flexible dose schedules suggested that each drug is an efficient treatment for this category of depression although the patterns of response and prevalence of side-effects varied. No differences reaching a level of significance could be shown on rating scales of depression or anxiety, but trends favoured flupenthixol. However, clinical evaluation suggested flupenthixol to be more effective than diazepam on mental state examination (P less than 0.05) and to have a greater overall therapeutic effect than nortriptyline (P less than 0.05). It also had fewer side-effects than nortriptyline (P less than 0.05).

Adjustment Disorders↗

PubMed1976

A double-blind study of flupenthixol ('Fluanxol') in general practice.

A double-blind crossover trial was carried out in the general practice to compare the effectiveness of flupenthixol and placebo in 43 patients with mild to moderate anxiety/depression states. Patients received either 0.5 mg flupenthixol or identical placebo tablets 2 to 4-times daily for 2 weeks and were then crossed over to the alternative preparation for a further 2 weeks. A simple 5-point rating scale was used to assess patients' symptoms at first visit and at subsequent follow-up. Even though there was a high placebo response, the results showed flupenthixol to be significantly more effective than placebo in relieving symptoms. Few side-effects were reported and were mild in nature.

Adolescent↗

PubMed1975

A comparative trail of fluphenazine decanoate and flupenthixol decanoate.

A double-blind cross-over study is reported which compares the antipsychotic properties and the side effects of depot flupenthixol with fluphenazine decanoate in chronic schizophrenic inpatients. Special emphasis was laid on examining changes in the target symptoms of apathy/anergia and depression in which flupenthixol has been claimed to be particulary effective. No significant differences were found between treatments on schizophrenic symptoms, or as regards the extrapyramidal side effects produced by equipotent doses of the two drugs. Reasons for the essentially negative results are discussed against a background review of earlier optimistic studies of flupenthixol.

Adult↗

PubMed1979

A comparative trial of the decanoates of flupenthixol and fluphenazine.

A double-blind trial was carried out comparing the effects of decanoates of flupenthixol and fluphenazine on the symptoms, ward behaviour and functional capacity in occupational therapy in 51 chronic schizophrenic patients. The patients were carefully selected on the basis of rigid criteria for diagnoses. To exclude nonresponders to neuroleptics the patients were first taken off neuroleptic drugs and only those who appeared to show deterioration were included in the trial. The dosage of drugs was varied according to clinical indications. The length of the trial was initially 4 months and 31 patients were followed for an additional 4 months. To ensure reliability multiple assessments were made at the start and the end of the trial. Most of the statistical tests showed no differences between the treatments, but some of those relating to affective symptoms showed an advantage for flupenthixol as compared with fluphenazine. There were no differences in the incidence of extra-pyramidal side-effects which required treatment in only 32% of the patients on each drug.

Adult↗

PubMed1975

The actions of flupenthixol upon 5-hydroxytryptamine-induced aggregation and the uptake of 5-hydroxytryptamine and dopamine by human blood platelets.

The effects of the alpha- and beta-isomers of flupenthixol on 5-hydroxytryptamine (5-HT)-induced platelet aggregation and on 5-HT and dopamine uptake were investigated. Alpha-Flupenthixol was 185 times more potent than the beta-isomer as an inhibitor of platelet aggregation. In contrast both isomers were equipotent as inhibitors of uptake of 5-HT and dopamine. The data suggest that 5-HT-induced aggregation and uptake are separate processes.

Blood Platelets↗

PubMed1979

A double-blind comparison of flupenthixol decanoate and fluphenazine decanoate in the treatment of chronic schizophrenia.

Sixty-four chronic stabilised schizophrenics were studied for 18 months in order to assess the possible difference in therapeutic effects and side effects between flupenthixol decanoate and fluphenazine decanoate. Although certain differences in the BPRS sub-scores in favour of flupenthixol were present at various stages in the study, there was no significant difference between the two drugs in the overall antipsychotic scores at the end of the assessment period; however, more patients on fluphenating required additional therpay for depression or anxiety during the trial period.

Chronic Disease↗

PubMed1977

Clinical and social comparison of fluphenazine decanoate and flupenthixol decanoate in the community maintenance therapy of schizophrenia.

The clinical and social effects of flupenthixol decanoate and fluphenazine decanoate were compared in the maintenance treatment of a population of chronic schizophrenic out-patients over a period of 9 months. The results failed to show significant difference between the treatments, and in particular, reports suggesting specific advantages for flupenthixol decanoate in alleviating the negative symptoms of apathy, anergia and depression in chronic schizophrenics were not confirmed. It seems that chronic schizophrenic patients who are well established on one depot preparation are unlikely to be benefited by being changed to the alternative.

Adolescent↗