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PubMed1980

Prevention of relapse in schizophrenia. An evaluation of fluphenazine decanoate.

We tested the role of guaranteed delivery of medication in the prevention of relapse and the enhancement of adjustment in the community in patients with schizophrenia. Two hundred and ninety newly hospitalized patients at four hospitals were randomly assigned to groups receiving either long-acting injectable fluphenazine decanoate or short-acting oral fluphenazine hydrochloride. After discharge and stabilization, patients were treated in the community for up to one year. By the end of the year, 28% of all the patients had relapsed. Contrary to hypothesis, differences between the two treatment groups in relapse percentages were not significant. Furthermore, there were no differences between the treatment groups as to development of affective symptomatology or social adjustment. Patients who rated themselves as having more symptom distress at the start of the community-maintenance phase of the study relapsed much earlier while receiving fluphenazine decanoate rather than fluphenazine hydrochloride. The results suggest that compliance is not an important determinant of relapse among newly discharged schizophrenic patients.

Adult↗
PubMed1997

Delayed normalization of central D2 dopamine receptor availability after discontinuation of haloperidol decanoate. Preliminary findings.

BACKGROUND: Antipsychotic drugs in depot formulations may prevent psychotic relapses, even after complete withdrawal. To examine the duration of drug remaining in the brain, central D2 dopamine receptor occupancy was measured with positron emission tomography for a year after discontinuation of depot neuroleptic treatment. METHODS: Four schizophrenic patients were withdrawn from low-dose treatment with haloperidol decanoate (30-50 mg every 4 weeks). They were examined repeatedly with positron emission tomography and the radioligand carbon 11-labeled raclopride during the following year. At end point, a Scatchard analysis was performed to determine the density and affinity of D2 dopamine receptors. RESULTS: Occupancy of D2 dopamine receptors was highest 1 week after depot injection (66%, 77%, 82%, and 78% in 4 patients) and then decreased slowly. Six months after discontinuation of treatment, D2 dopamine receptor occupancy was 24%, 32%, and 34% in 3 patients. After 1 year, D2 dopamine receptor density and affinity in 2 patients were within the ranges of control subjects, suggesting no remaining haloperidol. CONCLUSIONS: Our preliminary finding of persistence of D2 dopamine receptor occupancy indicates that commonly used doses of haloperidol decanoate (200 mg every 4 weeks) maintain antipsychotic levels of receptor occupancy even 16 weeks after discontinuation of treatment. This may explain the lower relapse rates in patients withdrawn from depot neuroleptic treatment compared with those withdrawn from oral treatment. In addition, the remaining occupancy may confound the clinical evaluation of subsequent treatments. For controlled clinical trials of new antipsychotic drugs, we suggest a minimum washout of 6 months after the last depot injection.

Adult↗
PubMed1979

Comparison of serum levels after intramuscular injections of 2% and 10% cis(Z)-flupentixol decanoate in Viscoleo to schizophrenic patients.

The serum concentrations of cis(Z)-flupentixol after injection of 2% and 10% cis(Z)-flupentixol decanoate in Viscoleo (Depixol injection, Fluanxol Depot) have been investigated in a crossover study with eight schizophrenic patients. No statistically significant difference was found between the two preparations when the data from individual days or areas under the serum concentration curves were considered. For the individual patients a difference was found between the two treatments in six cases; one preparation gave the higher serum concentration in four cases and the other preparation in two cases. Thus, the difference found within individual patients reflects the intraindividual variation rather than a difference between preparations. The maximum serum concentration was seen at 4 or 7 days after injection. The maximum/minimum fluctuation ratio indicates that dosage intervals longer than 2 weeks seem reasonable for most of the patients. The similarity in the serum concentrations, no matter which concentration of flupentixol decanoate solution was given, indicates that a dispersal and possibly a metabolic breakdown of the oil depot takes place in the muscle.

Adult↗
PubMed1980

Tolerance to fluphenazine and supersensitivity to apomorphine in central dopaminergic systems after chronic fluphenazine decanoate treatment.

Fluphenazine decanoate was administered chronically to rats on a schedule for which marked tolerance developed to acute fluphenazine effects on several parameters of dopaminergic neuronal function. DOPAC and HVA levels, indicators of dopaminergic activity, were quantitated in terminal areas of the mesocortical, mesolimbic and nigrostriatal systems. With this fluphenazine regimen tolerance developed not only in the nigrostriatal and mesolimbic but also in the mesocortical dopamine system to the elevation of metabolite levels induced by acute fluphenazine administration. Evidence was obtained that tolerance was functional rather than metabolic and was characterized by a large reduction in the accumulation of metabolites which normally follows a challenge dose of fluphenazine. Other experiments suggested that the results were not due to the effects of chronic fluophenazine on the noradrenergic innervation of the cortex and were not explained by altered catabolism or clearance of the dopamine metabolites. During withdrawal from chronic fluphenazine decanoate treatment supersensitivity to apomorphine developed in the striatum. The time courses of the disappearance of apomorphine supersensitivity and of the reversal of tolerance to a fluphenazine challenge were different.

3,4-Dihydroxyphenylacetic Acid↗
PubMed1994

Comparative bioavailability study of two haloperidol decanoate containing products.

In our hospital pharmacy an injectable solution of haloperidol decanoate 141 mg/ml (equivalent to haloperidol 100 mg/ml) in sesame oil was prepared. The aim of this study was to prove bioequivalence of this formulation with the reference product, Haldol Decanoas. 15 schizophrenic patients, already stabilized with Haldol Decanoas, were enrolled. Intramuscular injections were given every three weeks in the following doses: 100 mg (1 x), 200 mg (7 x) and 300 mg (7 x). In this open, randomized, cross-over study all patients received four injections of the reference product, and four injections of the test product. Only after the fourth injection of each product (when steady-state levels were reached) a concentration-time profile of haloperidol was established during the dose interval of 21 days. The pharmacokinetic parameters AUC0-21 and Cmax were statistically evaluated. Based on these parameters the conclusion was drawn that both products were bioequivalent. The preparation of this injectable haloperidol decanoate solution in our hospital pharmacy amounts to an annual saving of approximately $39,000.

Adult↗
PubMed1990

Pharmacokinetics of haloperidol and fluphenazine decanoates in chronic schizophrenia.

In a double-blind comparison of haloperidol decanoate and fluphenazine decanoate given 4-weekly for 60 weeks as maintenance therapy in 38 chronic schizophrenic in-patients, plasma haloperidol, fluphenazine and prolactin levels were measured at regular intervals by radioimmunoassay. After the first injection, the mean plasma haloperidol level was highest at week 1 and fell gradually towards week 4. Mean pre-dose haloperidol levels changed little after week 8. Results suggested an absorption half-life of 4 weeks, although, in three cases steady state was only achieved after 11 monthly injections. Steady state levels of both haloperidol and fluphenazine correlated highly with dose. In two sub-groups observed at steady state, both drugs produced a biphasic pattern of plasma drug concentration between injections, a rapid rise on day 1 followed by stable elevated levels and a gradual return to pre-injection concentration by the end of week 4. In the fluphenazine sub-group there was a second peak on day 7 and a steeper decline, so that the mean area-under-curve in week 4 was 64% of that in week 1. Drug injections at steady state induced an increase in prolactin secretion in all of the fluphenazine sub-group and in half of those receiving haloperidol. Plasma prolactin changes resembled those for drug concentrations, but differences in times of peaks on day 1 resulted in weak correlations. Fluphenazine appeared more potent than haloperidol in provoking prolactin secretion.

Adult↗
PubMed1986

Serum levels and clinical response in long-term pharmacotherapy with zuclopenthixol decanoate.

Twenty-six patients diagnosed as chronic schizophrenics were given injections of zuclopenthixol decanoate (cis(Z)-clopenthixol decanoate) 200 mg every 3 weeks for at least 6 months. Before treatment and on each day of injection the patients' mental state was assessed by Brief Psychiatric Rating Scale (BPRS), 18 items. A registration of side effects and basal laboratory data was also performed. Blood samples were drawn on each day of injection before injection and 3-7 days after injection (time of maximum concentration). Neuroleptic activity, which was considered equivalent to the concentration of zuclopenthixol, was determined in serum by radio-receptor assay (RRA). Based on amelioration scores greater than or equal to 50% on the BPRS, 15 patients were characterized as responders and 11 as non-responders. The responder group showed a statistically significant reduction in BPRS score, whereas this was not the case for the non-responders. Apart from a few patients, the serum concentrations showed a low intra-individual variation, but a relatively high inter-individual variation. The responder group had a significantly higher mean pre-injection concentration than the non-responder group, whereas no significant difference was found in day 3-7 concentrations. The fluctuation of the serum concentration expressed as the ratio between maximum (days 3-7) and minimum (pre-inj.) was found to be significantly lower for responders than for non-responders. Thus although the present study did not demonstrate a clear relationship between serum level and clinical effect, it indicates that the best antipsychotic effect is obtained with a serum concentration which fluctuates only slightly (the ratio max/min concentration not exceeding 2.1).

Adult↗
PubMed2003

Gender-related differences in pharmacological relapse prevention with flupenthixol decanoate in detoxified alcoholics.

A study recently finished by our research group elucidated the effectiveness of flupenthixol decanoate (FLX) in maintaining abstinence in detoxified alcoholics. Flupenthixol decanoate is an established antipsychotic drug, which is well known for its mild antidepressant and anxiolytic activity as well as for its minimal sedation at low doses. It blocks dopamine binding at a number of receptor subtypes, primarily at D-1, D-2, D-3 and with less affinity at D4-receptors. It also affects serotonin binding at 5-HT2A and 5-HT2C receptors. In a double-blind placebo-controlled multicenter trial, 77 women and 204 men suffering from moderate or severe DSM-II-R alcohol dependence were randomly assigned to either 10 mg FLX or placebo both injected every second week over a period of 24 weeks (treatment phase) succeeded by a medication-free 24-weeks follow-up period. In the overall analysis the number of patients relapsed after 24 weeks of treatment (=main criterion of efficacy) was significantly higher in the FLX treated group (85.2%) than under placebo (65.5%). However, when differentiating this result according to sex the analysis revealed a gender-related discrepancy: while male patients had an almost 4-fold higher risk to relapse under FLX than under placebo (OR=3.95) this risk was barely elevated for female patients (OR=1.51). A significantly negative outcome due to FLX treatment was restricted to male alcoholics solely. In conclusion, gender-related differences to pharmacological relapse prevention with FLX have probably contributed to a better treatment outcome in women than in men.

Adult↗
PubMed1994

Comparative study of dopamine metabolism with local cerebral glucose utilization in rat brain following the administration of haloperidol decanoate.

The effects of haloperidol decanoate on dopamine (DA) metabolism in discrete regions of rat brain were investigated and compared with changes in local cerebral glucose utilization (LCGU). The concentration of DA and its metabolite, homovanillic acid, and the alpha-methyl-p-tyrosine (alpha-MT)-induced decline of DA were measured in 6 brain regions by a high-performance liquid chromatographic assay. LCGU in 26 brain regions were examined by [14C]2-deoxy-D-glucose autoradiography. At 24-hr after intramuscular injection of haloperidol decanoate (60 mg eq/kg to haloperidol), the concentration of homovanillic acid in the prefrontal cortex, caudate-putamen, accumbens nucleus, lateral amygdala, and medial thalamus showed significant increase compared with control values. On day 21, the increase in these regions was significantly attenuated with no significant difference from the controls. Furthermore, chronic haloperidol rats showed alpha-MT-induced decline of DA to a similar extent in the control rats. LCGU on day 21 showed significant decrease in the parietal cortex, and a tendency toward decrease in the prefrontal cortex, lateral amygdala and medial thalamus compared with the controls. There was no significant change in LCGU in the caudate-putamen or accumbens nucleus. Chronic haloperidol would thus appear to affect energy metabolism mainly in the cortico-thalamo-limbic circuits, and this may not correspond well to presynaptic DA metabolism.

Animals↗
PubMed1979

Low dose fluphenazine decanoate in maintenance treatment of schizophrenia.

To test the clinical efficacy of low dose fluphenazine decanoate (1.25 mg to 5.0 mg biweekly), we carried out two separate experiments: (1) an open trial in 57 schizophrenic outpatients, lasting 6 months; (2) a double-blind, placebo-controlled discontinuation study in a subgroup of patients who maintained good remission throughout the entire 6-month open trial. The results suggest that lower doses of fluphenazine decanoate than those usually used may be effective in preventing psychotic relapse while keeping total cumulative dosage to a minimum.

Aftercare↗
PubMed1994

Do enzyme inducers modify haloperidol decanoate rate of release?

1. Plasma levels were monitored for about 18 months during therapy with haloperidol decanoate. When steady-state was reached, patients treated without enzyme inducers showed in their plasma concentrations a stable plateau and a very low fluctuation. Furthermore, doses were correlated to plasma levels (r = 0.9). 2. Contrary, patients treated with both haloperidol decanoate and enzyme inducers seemed to present in their plasma concentration a very large fluctuation with C min (plasma concentrations measured just before the injection) significantly lower than those of the other group. Moreover their C min values were excluded from the linear regression curve calculated between plasma levels and doses in patients without enzyme inducers. 3. Our data suggest a shortening of the absorption half-time of haloperidol. In this case, it seems necessary to diminish the interval between injections than to give higher dosage in order to maintain plasma concentrations.

Antipsychotic Agents↗
PubMedDate not supplied

Fluphenazine decanoate. Its steady-state pharmacologic profile and relationship to tardive dyskinesia.

A sensitive radioimmunoassay was developed to determine the steady-state, fixed-dose pharmacokinetic profile of fluphenazine decanoate in nine outpatients. To see if neuroleptic blood levels measured by this assay correlated with a clinical event, we performed a cross-sectional study of fluphenazine blood levels in 11 patients with and 17 patients without tardive dyskinesia. The results do not support the hypothesis that fluphenazine decanoate serum levels correlate with TD occurrence.

Adult↗
PubMed2001

Lymphatic transport of fat in rats with normal- and malabsorption following intake of fats made from fish oil and decanoic acid. Effects of triacylglycerol structure.

Fish oils contain essential polyunsaturated fatty acids of the n-3 family. In fat malabsorption the n-3 fatty acids are poorly absorbed. Absorption may be improved by modifying the fatty acid profile of fish oil through interesterification with medium chain fatty acids. We examined the absorption of fish oil interesterified with decanoic acid in rats with normal- and malabsorption compared to a physical mixture and the fish oil itself. The interesterified fats were: 1) a regiospecific fat with decanoic acid located mainly in the sn1/3-positions and a long chain fatty acid from fish oil in the sn2-position, 2) a fat with a random distribution of fatty acids in all positions of the triacylglycerol. The main mesenteric lymph duct was cannulated for collection of lymph. In the malabsorbing rats the common bile duct was cannulated as well to divert both pancreatic juice and bile. The fatty acid composition in lymph samples collected for 24 hours was determined. Accumulated transport of n-3 fatty acids from fish oil was improved in malabsorbing rats and recoveries of fatty acids after 24 hours were improved in both rats with normal- and malabsorption administered the randomized fat compared to fish oil.

Journal Article↗
PubMed1998

[Positive and negative symptoms in chronic schizophrenic patients under maintenance therapy with flupenthixol decanoate for a twelve month perioid].

62 chronic schizophrenics, who after a psychotic exacerbation were stabilized again, were randomized on 3 different maintenance dosages of flupentixol-decanoate and observed for 12 months. 15 (24.2%) patients had a relapse independently of the dose. 34 of the 47 patients without relapse had complete documentations of the follow-up. After 3 to 6 months there was an obvious and constant clinical improvement as assessed by various test inventories. The BPRS-scores for psychopathology, negative and positive symptoms improved significantly between 14 to 18%. There was also significant reduction of negative symptoms assessed by SANS (22%) as well in the severity of illness (CGI) and an amelioration of psychosocial functioning (GAS, Strauss-Carpenter). At the end of trial 26.4% of the patients had mild involuntary movements (AIMS), 23.5% were on antiparkinson-medication. It is concluded that there could be an indication for flupentixol-decanoate in the long term maintenance therapy especially of chronic schizophrenics with negative symptoms and problems of compliance under oral medication.

Adult↗
PubMedDate not supplied

Flupenthixol decanoate and relapse prevention in alcoholics: results from a placebo-controlled study.

Flupenthixol, with its broad receptor profile, interacts with a variety of dopamine and serotonin binding sites which are important in the neurobiology of alcohol dependence. Its pharmacology, together with encouraging results from both animal studies and clinical trials with cocaine users, led us to postulate that flupenthixol would significantly prevent relapse in detoxified alcohol-dependent individuals. We conducted a prospective, randomized, double-blind, placebo-controlled, multi-centre trial with two parallel groups and appropriate statistical evaluation. Subjects met criteria for moderate to severe alcohol dependence (DSM-III-R), without any concomitant psychiatric disorder. After complete detoxification, 281 women and men received either 10 mg of flupenthixol decanoate or placebo as i.m. injection every second week for 6 months on an out-patient basis, followed by 6 months of follow-up. Efficacy was based on absolute abstinence, with relapse being defined as consumption of any alcohol after inclusion in the study. In contrast to the hypothesis, flupenthixol did not reduce, but was associated with more, relapses. Though well tolerated, relapse rates after 6 months of treatment were 85.2% (flupenthixol) versus 65.5% (placebo), a highly significant difference from the medication. Flupenthixol was also inferior to placebo with regard to other secondary criteria of efficacy (cumulative abstinence duration, relapse rate after 12 months). These results indicate that a 10 mg dose of flupenthixol decanoate does not have a beneficial effect on abstinence maintenance in alcohol-dependent individuals.

Adult↗
PubMed1990

Single-dose pharmacokinetics of fluphenazine after fluphenazine decanoate administration.

Fluphenazine decanoate is commonly used as part of maintenance treatment of schizophrenia, but its pharmacokinetics are poorly understood. We administered a single intramuscular dose of fluphenazine decanoate to nine patients and found that plasma fluphenazine level did not decline to 50% of the peak level by day 26 in any of the patients. This means that it has a long half-life measurable in months rather than weeks.

Adult↗
PubMed1987

The effects of a 50% reduction of cis(z)-flupenthixol decanoate in chronic schizophrenic patients maintained on a high dose regime.

Eighteen chronic schizophrenic patients who had shown improvement from increased maintenance dosages of cis(z)-flupenthixol decanoate were entered into a double-blind study in which half of the patients were randomly allocated to be maintained on 50% of their pre-trial dosage. During the 44 week study the reduced dosage group showed increased morbidity and one-third of these patients had a schizophrenic relapse. The greatest deterioration occurred in patients reduced from above to below 200 mg cis(z)-flupenthixol decanoate biweekly. A review of all the patients entered into the study showed a relationship between deterioration of schizophrenic and depressive features and cis(z)-flupenthixol plasma levels which reflected the administered dosage. Prolactin levels in general did not reflect control of schizophrenic symptoms. Side-effects were few, and there was no emergence of tardive dyskinesia. A multicentre trial is needed for further evaluation.

Adult↗
PubMed1978

Maintenance treatment of chronic schizophrenic patients. A study with the long-acting thioxanthene derivative, cis(Z)-clopenthixol decanoate-sordinol depot.

The clinical effect of clopenthixol decanoate has been assessed in a 5-month controlled including 21 hospitalized chronic schizophrenic patients. The ratings were done with BPRS, NOSIE 30, the two psychological tests of WAIS and Grübaum, and the rating scale of Simpson & Angus to assess extrapyramidal side effects. Clopenthixol decanoate was found an effective and long-acting antipsychotic compound with few autonomic and neurological side effects. Compared with previous maintenance treatment it also showed a positive influence on depression and facilitation of the social adaptation of the patients.

Adult↗