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PubMed1996

Contralateral turning caused by metabotropic glutamate receptor stimulation in the dorsal striatum is reversed by MCPG, TTX, and cis-flupenthixol.

Recent evidence suggests an involvement of metabotropic glutamate receptors in the physiology of the striatum. In this study, rotation was recorded in an automated rotometer for 20 min following dorsal striatal injections (0.5 microliter) in cannulated rats. The metabotropic agonist 1-aminocyclopentane-trans-1, 3-dicarboxylic acid (1S,3R-ACPD) caused dose-dependent contralateral rotation. Turning caused by 500 microM 1S,3R-ACPD was reversed by coinjections of the metabotropic antagonist (+)-alpha-methyl-4-carboxyphenylglycine (MCPG, 1 mM) and by tetrodotoxin (100 microM). Injections of MCPG alone (10 microM, 100 microM, 1 mM) failed to elicit turning. Increasing doses of the dopamine antagonist cis-flupenthixol also reversed 1S,3R-ACPD-induced rotation. Thus unilateral striatal metabotropic glutamate receptor stimulation can cause receptor-specific rotation that may result from an increase in neural activity, and is dependent on intact dopamine neurotransmission.

Animals↗
PubMed2003

Rapid assessment of choice between cocaine and food in rhesus monkeys: effects of environmental manipulations and treatment with d-amphetamine and flupenthixol.

The present study describes a procedure that permits rapid assessment of environmental and pharmacological factors that may influence the choice between cocaine and food in rhesus monkeys. Daily 2 h sessions were divided into five components. During each component, monkeys (N=4) chose between i.v. cocaine (0-0.1 mg/kg/injection) and food (0, 1, or 3 food pellets). Up to 10 reinforcers were available during each component, and different discriminative stimuli were associated with each magnitude of each reinforcer. Cocaine choice was directly related to cocaine dose, and a cocaine choice dose-effect curve could be determined in a single experimental session. The choice between cocaine and food was influenced by the schedules of cocaine and food reinforcement, the magnitude of the food reinforcer, and the amount of noncontingent food provided outside the experimental session. These results confirm and extend previous findings with other choice procedures and validate the sensitivity of the present procedure to environmental manipulations. The choice between cocaine and food could also be influenced by treatment with candidate pharmacotherapies for cocaine abuse and dependence. The "agonist" medication d-amphetamine produced rightward shifts in the cocaine choice dose-effect curve and decreased cocaine choice, whereas the "antagonist" medication flupenthixol had little effect on cocaine choice. Overall, these results suggest that this choice procedure may be useful for the evaluation of both environmental determinants of cocaine use and candidate pharmacotherapies for the treatment of cocaine abuse.

Animals↗
PubMed1978

[Studies on the long acting neuroleptic agent flupenthixol decanoate--a review (author's transl)].

The development of long acting neuroleptic agents is considered as important progress in the treatment of schizophrenic psychoses. An outline of pharmacological and clinical results with flupenthixol decanoate is given. Special attention is paid to pharmacokinetics, the methods for determining plasma concentration, to the profile of action and duration of action, to other dosage as well as to safety. Importance is also placed on the possible use for prophylaxis of affective psychoses.

Delayed-Action Preparations↗
PubMed2004

Olanzapine versus flupenthixol in the treatment of inpatients with schizophrenia: a randomized double-blind trial.

OBJECTIVE: The atypical antipsychotic olanzapine has extensively been compared with haloperidol, whereas studies vs. other (conventional) neuroleptics are scarce. This exploratory double-blind 4-week study was designed to compare the efficacy and the safety of olanzapine (OLA) and flupenthixol (FLU) which have recently been considered as a "partially atypical" antipsychotics. METHODS: Twenty-eight inpatients with schizophrenia (DSM-IV) were randomly assigned for treatment with OLA (N = 15, 5-20 mg/d) or FLU (N = 13, 5-20 mg/d). The Brief Psychiatric Rating Scale (BPRS) and the Negative Symptoms Rating Scale (NSRS), plus the Patient Global Impression (PGI) and Clinical Global Impression (CGI) scales, were used to assess the efficacy of both compounds; safety was determined by using the Simpson Angus Scale (SAS) and the Abnormal Involuntary Movement Scale (AIMS) and by assessing treatment-emergent adverse events. Non-parametric statistics were applied. RESULTS: BPRS and NSRS scores improved in both groups (exploratory tests; all p < or = 0.02). Similar results were observed for CGI-Severity, CGI- and PGI-Improvement. There were no significant group differences. Responder rates (at least 40 % decrease in BPRS total) were 9/13 OLA patients (69 %) and 9/12 FLU patients (75 %). EPS events were reported only in the FLU group (p < 0.01); FLU patients needed significantly more anticholinergic medication. Weight gain was higher in OLA patients (p < 0.01). Overall, fewer patients with adverse events were observed in the OLA group (p = 0.04). No significant changes were noted on SAS and AIMS scores. CONCLUSION: Findings from this study suggest that overall and negative symptomatology improved in both treatment groups, while the safety and tolerability profiles differed for both substances.

Adult↗
PubMed1978

The effect of baclofen on alpha-flupenthixol-induced catalepsy in the rat.

1 alpha-Flupenthixol (alpha-FPT; 0.2 mg/kg i.p.) when administered to rats produced catalepsy. 2 Baclofen (10 mg/kg i.p.) given 30 min after alpha-FPT had a biphasic effect on the catalepsy. Initially there was a potentiation of the effect, followed by a significant attenuation of the degree of catalepsy. 3 Possible mechanisms of action are discussed.

Aminobutyrates↗
PubMed1983

A role for 5-hydroxytryptamine in the GABA-mimetic potentiation of alpha-flupenthixol-induced catalepsy in the rat.

1 alpha-Flupenthixol (alpha-FPT)-induced catalepsy in the rat was potentiated by diaminobutyric acid (DABA), an inhibitor of the neuronal high affinity uptake of gamma-aminobutyric acid (GABA). 2 The depletion of 5-hydroxytryptamine (5-HT) with p-chlorophenylalanine (PCPA) abolished the DABA potentiation of alpha-FPT-induced catalepsy; this response was restored with 5-hydroxytryptophan. 3 Potentiation of alpha-FPT-induced catalepsy by clonazepam was significantly reduced by methysergide. Conversely, the potentiation of catalepsy by clomipramine was significantly reduced by picrotoxin. 4 These results are interpreted as evidence supporting a role for 5-HT in modifying the GABA-ergic inhibition of dopaminergic pathways, possibly by regulating the release of GABA.

Aminobutyrates↗
PubMed1980

Clopenthixol and flupenthixol depot preparations in outpatient schizophrenics. IV. Serum levels and clinical outcome.

Two pharmacolkinetic parameters viz. the minimum serum concentration in the dosage interval and the sera under the serum concentration curve have been correlated to 14 parameters for clinical outcome, viz. total points and factor points from the three rating scales, BPRS, CPRS, and side effects scale, in a double blind clinical trial of clopenthixol and flupenthixol depot preparations in outpatient schizophrenics. No statistically significant correlations were observed. It is of some interest, however, that the results suggest that the treatment of individual patients with neurleptics may be adjusted by means of repeated ratings, residual percentage, changes in psychopathology, and determinations of serum concentrations. Our results do not indicate any optimal concentration range for these depot neuroleptics in the maintenance phase of schizophrenia. The so-called therapeutic window as to neuroleptics obviously varies with regard to the phase of the disease as well as the patients' social situation.

Ambulatory Care↗
PubMed1997

Diagnosis of photosensitivity to flupenthixol by photoprick testing.

We report the case of a 38-year-old patient with an erythematous eruption, initially confined to photo-exposed areas and then becoming more generalized, which was attributable to flupenthixol, a thioxanthene derivative used for its neuroleptic properties. The compound has the same polycyclic aromatic hydrocarbons as phenothiazines, but without any cross-reaction in our patient. A photoallergic cause for the eruption was verified on clinical, histological and photobiologic grounds. Photopatch tests were negative, but photoprick testing was positive after UV irradiation of the test site. Photopatch test methods using better skin penetration have been already reported for testing drug photosensitivity. Photoprick testing combines better penetration with greater ease of use.

Adult↗
PubMed1975

The problem of post-psychotic schizophrenic depressions and their pharmacological induction. Long-term studies with fluspirilene and penfluridol and single-blind trial with fluphenazine-decanoate and flupenthixol-decanoate.

The authors discuss the historical aspects, as well as the various etiological and clinical factors which contribute to the so-called pharmacogenically induced depressions during treatment by means of neuroleptics generally, and long-term neuroleptics especially. An open study on 161 schizophrenic patients treated by means of fluspirilene and 123 patients treated by means of penfluridol is described. A single blind trial on 48 patients, by means of fluphenazine-decanoate and flupenthixol-decanoate, which compares the possible depression-inducing or antidepressant activity of the above drugs, is presented. The criteria for evaluating drug-induced depressions and their two clinical types are discussed.

Adult↗
PubMed1986

Imipramine-flupenthixol decanoate interaction.

The authors describe a case in which flupenthixol decanoate and imipramine were co-administered to a patient with schizophrenia, resulting in extremely high levels of imipramine and its metabolite, desipramine. The literature on the co-administration of neuroleptics and antidepressants is reviewed and guidelines for limiting possible iatrogenic effects of the combination are suggested.

Adult↗
PubMed1990

A double-blind comparison of oral amitriptyline and low-dose intramuscular flupenthixol decanoate in depressive illness.

Fifty-seven hospital out-patients with depressive symptoms were studied in a double-blind manner for up to 4 weeks, 30 whilst being treated with intramuscular flupenthixol decanoate (5 to 10 mg/fortnight) and 27 with oral amitriptyline (75 to 150 mg/day). The results of assessment using the Hamilton Rating Scale for Depression, the Leeds Self-Rating Scale for Depression and the Clinical Global Impressions severity scale showed that both therapies were effective in resolving depression in the patients studied. The two treatments were well tolerated and side-effect profiles were similar, dry mouth, faintness/dizziness and drowsiness being the most frequently reported adverse events. Extrapyramidal signs were seen in similar numbers of patients in each treatment group. One patient from each of the two groups was withdrawn from therapy before the end of the study because of adverse events.

Administration, Oral↗
PubMed1979

Depressive and extrapyramidal symptoms and clinical effects: a trial of fluphenazine versus flupenthixol in maintenance of schizophrenic out-patients.

Fifty-seven patients with a diagnosis of schizophrenia were started on either fluphenazine decanoate or flupenthixol decanoate injections in a double-blind trial just prior to discharge into the community. During the six month follow-up 30 per cent dropped out of the treatment. Of those observed for six months, 7 per cent relapsed, 54 per cent experienced depressive symptoms and 88 per cent extrapyramidial side-effects. Analysis of both clinical data and the ratings failed to discriminate between the two drugs.

Adolescent↗
PubMed1998

Flupenthixol treatment for cocaine abusers with schizophrenia: a pilot study.

Cocaine use is common among individuals with schizophrenia and schizoaffective illness, with a prevalence ranging from 15-60% of patient samples. It is hypothesized that some schizophrenic cocaine abusers may use cocaine as an attempt to improve anhedonic symptoms or combat neuroleptic side-effects. Flupenthixol (FLX) has the distinct advantage of being both a neuroleptic medication and a potential treatment for cocaine abuse. We evaluated the efficacy of FLX in this dually diagnosed population in an open pilot study consisting of a 4-week inpatient phase and a 6-week outpatient phase. Eight individuals were initially cross-tapered off their neuroleptic medication and were given FLX in a dose of 40 mg of the decanoate every 2 weeks. Psychiatric symptomatology was assessed weekly, using the Positive and Negative Symptom Scale (PANSS) and the Beck Depression Inventory (BDI). Medication side-effects were monitored weekly, using the Simpson Neurological Rating Scale and the Abnormal Involuntary Movement Scale (AIMS). Substantial improvement in psychiatric symptomatology was noted when preadmission scores were compared to scores obtained during the last week of study enrollment. On the PANSS, positive symptom scores and negative symptom scores decreased by 31% and 29%, respectively. Similarly, BDI scores decreased by 57%. Comparing preadmission urine results to those for the last 6 weeks of enrollment in the study showed that cocaine-positive urines decreased by 28%, although most of the patients had a reduction of >75%. Missed clinic visits decreased by 26%. Thus, FLX was well-tolerated by schizophrenic cocaine abusers, suggesting that FLX may be useful for the treatment of this dually diagnosed population.

Adult↗
PubMed1985

Flupenthixol and Melitracen in the management of trigeminal neuralgia.

Twelve patients with trigeminal neuralgia were treated with a daily dose of 2 mg Melitracen and 40 mg Flupenthixol. The majority of patients derived benefit from it. The former drug is a bipolar thymoeleptic and the latter a neuroleptic. There was no adverse side effects. The regime of treatment is recommended in cases that do not respond to conventional treatment.

Anthracenes↗
PubMed1983

[Clinical aspects and therapy of acute poisoning by the drug combination melitracen-flupenthixol (Deanxit)].

From 1975 to 1982, the Austrian Poison Information Centre gave medical advice in forty cases of acute melitracenee-flupenthixol poisoning. The case reports were reviewed and analysed in retrospect. 13 patients who either had ingested less than 20 pills (n = 5) or who underwent early gastric lavage (n = 8) showed no symptoms. In 19 patients who had swallowed 20 to 60 (n = 11), 60 to 100 (n = 3) pills respectively, or an unknown dose (n = 5) atropine like symptoms predominated. Five patients developed atropine like and extrapyramidal symptoms. The number of pills taken by these patients ranged from 20 to 60 (n = 4) and in one up to 100. Extrapyramidal reactions were encountered as predominant symptoms in three patients one of which had taken 20, the other 60 and the third an unknown number of pills. Additionally, five patients were unconscious. 21 patients developed ECG changes, 19 of which showing sinus tachycardia. The remaining two patients who had ingested 600 to 1000 mg melitracen atrial premature beats or T-wave inversions were observed. All 40 patients recovered.

Adolescent↗
PubMed1994

Treatment of depression with flupenthixol in terminally ill patients.

In recent years, there has been much interest in the psychological well-being of cancer patients (Buckberg et al., 1980; Plumb & Holland, 1977; Razavi et al., 1990; Grassi et al., 1989). It is recognized that if depression is detected and treated, the quality of life for the patient is improved (Holland, 1987; Valentine & Saunders, 1989). Many patients are treated with tricyclic anti-depressants which work well in some cases, but these drugs can have the disadvantage of taking 3 weeks before any improvement in the mood of the patient is observed. They can also cause unpleasant side-effects, e.g. dry mouth, urinary retention and constipation. These symptoms are often already present in the terminally ill and their exacerbation can make these drugs unacceptable to such patients. Two cases of depression which were detected on admission to a hospice and which were successfully treated with flupenthixol dihydrochloride are reported.

Aged↗
PubMedDate not supplied

Gastric responses to flupenthixol, a new thioxanthene derivative in rats.

Flupenthixol, a new thioxanthene derivative, was studied for its effects on gastric secretion and gastric ulcers in rats. The compound diminished the volume of gastric secretion, decreased total acid output and protected the glandular gastric mucosa. The observations may be of clinical significance.

Animals↗