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PubMed1979

Fluphenazine and social therapy in the aftercare of schizophrenic patients. Relapse analyses of a two-year controlled study of fluphenazine decanoate and fluphenazine hydrochloride.

The ability of long-acting fluphenazine decanoate and oral fluphenazine hydrochloride to forestall relapse among newly discharge schizophrenic patients is examined in the context of high and low degrees of social therapy (ST). A total of 105 patients were randomly assigned to the various treatments and maintained under controlled conditions for two years or until relapse. Relapse rates for all treatments remained traditionally high. Relpase rates for long-acting fluphenazine decanoate and oral fluphenazine hydrochloride are nearly identical in the first year, indicating that drug noncompliance does not adequately explain early schizophrenic relapse. However, patients who received long-acting fluphenazine decanoate and ST have a reduced risk of relapse over time. Relapsers who received long-acting fluphenazine decanoate appeared more affectively disturbed than other relapsers, yet both groups were diagnostically and symptomatically equivalent prior to treatment. Personal discomfort and intrafamilial stress are important predictors.

Administration, Oral↗
PubMed1989

Outpatient treatment of 'crack' cocaine smoking with flupenthixol decanoate. A preliminary report.

"Crack" cocaine abuse often produces severe cocaine dependence that is refractory to available pharmacological and outpatient psychotherapeutic treatments. We conducted two preliminary investigations evaluating the efficacy of flupenthixol decanoate, a depot xanthene requiring infrequent intramuscular administration, in the treatment of cocaine withdrawal. Ten outpatient crack cocaine smokers with poor prognoses were administered flupenthixol decanoate in an open-label, open-ended trial. Flupenthixol decanoate was well tolerated and appeared to decrease cocaine craving and use markedly and rapidly, producing a 260% increase in the average time retained in treatment among these subjects. These promising but preliminary data, combined with the magnitude of problems presented by crack, warrant rapid, expanded double-blind assessment of flupenthixol decanoate in cocaine-abuse treatment.

Adult↗
PubMed1976

Fluphenazine enanthate and fluphenazine decanoate: intramuscular injection and esterification as requirements for slow - release characteristics in dogs.

14C-Fluphenazine base was administered intramuscularly in sesame oil to five male beagles (2 mg/kg). The concentration of radioactivity in plasma and the excretion of radioactivity in urine and feces were measured for 14 days. Maximum concentrations of radioactivity were found in plasma 2 hr after administration. These levels declined with elimination half-lives of 3.20 hr during the 2-12-hr interval after dosing and of 4.02 days during the 2-14-day interval. Most administered radioactivity was excreted during the first 2 days after dosing, predominantly in the feces. An average of 0.43% of the dose was present at the injection site 14 days after dosing; some residual radioactivity was found in the liver and in the ocular portion consisting of the combined retina, choroid, and sclera. 14C-Fluphenazine and its enanthate and decanoate esters were each administered intravenously to three different groups of intact dogs at doses of 1 mg/kg. Regardless of which compound was administered, concentrations of radioactivity in the plasma of these dogs were comparable. Thirty minutes after these dogs had been dosed with 14C-fluphenazine enanthate or 14C-fluphenazine decanoate, most radioactivity in the plasma was present as 14C-fluphenazine base and other unidentified metabolites; at this time, at least 79% of either of the two 14C-fluphenazine esters had been biotransformed. The excretion of radioactivity by these same three groups of dogs was very similar, regardless of which of the compounds was given. In 7 days, an average of only 3-4% of the dose was excreted in urine; the remainder was excreted in feces. 14C Fluphenazine and its enanthate and decanoate esters (1 mg/kg) were administered intravenously to dogs whose bile ducts had been cannulated. The amounts of radioactivity excreted in the urine and bile in 8 hr were very similar, as were the residual amounts of radioactivity present in selected tissues. Comparison of the data obtained from dogs given these three compounds intravenously (unformulated) or intramuscularly in sesame oil points to the following conclusions: (a) fluphenazine base per se does not provide slow-release characteristics unless it has been esterified, for example, with heptanoic or decanoic acid, and (b) intramuscular rather than intravenous administration of these two esters is responsible for producing their slow-release characteristics.

Animals↗
PubMed1984

Blood and plasma kinetics of cis(Z)-clopenthixol and fluphenazine in psychiatric patients after intramuscular injection of their decanoic esters.

Whole blood and plasma concentrations of active neuroleptic drugs were measured in eight schizophrenic outpatients who had received cis(Z)-clopenthixol decanoate in Viscoleo or fluphenazine decanoate in sesame oil by intramuscular injection. Whole blood and plasma concentrations were very similar, though there was a slight tendency for blood concentrations to be higher than plasma concentrations. Maximum concentrations appeared at 1 week after administration of cis(Z)-clopenthixol decanoate, whereas the highest concentrations after fluphenazine decanoate were seen at the end of the 3-week dosage interval. Some between-individual variation and a limited within-individual variation was seen.

Adult↗
PubMedDate not supplied

Hydrolysis of haloperidol decanoate in vitro by cultured cells.

[14C]Haloperidol decanoate was hydrolysed by partially purified carboxylesterase but not in plasma, blood, lymph and lymphatic liquid. These fluids inhibited the enzyme-mediated hydrolysis of the ester. Within the same incubation period as above, the ester was found hydrolysed to various extents in cell cultures of isolated rat liver cells, of human and rat lymphocytes and of established cell lines (BGM cells, WI-38 cells and L6 cells). Thus, the hydrolysis of the ester was demonstrated in vitro with use of viable cell cultures instead of enzyme preparation. From the time course study on the metabolism of haloperidol decanoate in cell cultures, it was concluded that haloperidol decanoate was first concentrated in the cells and hydrolysed to haloperidol. Based on these results, the metabolic sequences in vivo leading to the formation of active principle haloperidol after intramuscular administration of its decanoate were discussed.

Animals↗
PubMed2002

Maintenance therapy with zuclopenthixol decanoate: associations between plasma concentrations, neurological side effects and CYP2D6 genotype.

RATIONALE: Several antipsychotic drugs are metabolised by the polymorphic cytochrome P(450) CYP2D6. The impact of the polymorphism on the plasma levels and the occurrence of side effects have not been clearly established. OBJECTIVE: To investigate the impact of the CYP2D6 polymorphism on the steady-state plasma concentrations of zuclopenthixol and the occurrence of extrapyramidal side effects (EPS) and tardive dyskinesia (TD) during treatment with zuclopenthixol-decanoate. METHODS: Fifty-two clinically stable schizophrenic outpatients on monotherapy with zuclopenthixol-decanoate (100-400 mg/4 weeks) were genotyped for the CYP2D6 variants CYP2D6*3 and CYP2D6*4. Steady-state plasma levels of zuclopenthixol were analysed using high-performance liquid chromatography. Assessments of EPS, TD and psychopathology were performed twice with an 8-week interval using the extrapyramidal symptoms rating scale, the abnormal involuntary movement scale and the brief psychiatric rating scale. RESULTS: Thirty-five patients were homozygous extensive metabolisers (EMs), 13 were heterozygous EMs and 4 were poor metabolisers (PMs). While there were no significant genotype-related differences in the doses of zuclopenthixol decanoate, PMs as well as heterozygous EMs had significantly higher steady-state plasma levels of zuclopenthixol than homozygous EMs (median 9.5 nmol/l; 8.2 nmol/l and 5.9 nmol/l, respectively, P<0.05). The median dose-corrected plasma concentrations were 0.029, 0.038 and 0.048 nmol.l(-1).mg(-1) in homozygous EMs, heterozygous EMs and PMs, respectively, with statistically significant differences between homozygous EMs and heterozygous EMs ( P=0.014) and homozygous EMs and PMs ( P=0.03). Patients with neurological side effects were significantly older than patients without ( P=0.02 in case of parkinsonism and P=0.04 in case of TD). Mutant CYP2D6*3 and *4 alleles tended to occur more frequently in patients with neurological side effects. An odds ratio (OR) of 2.3 (95% confidence interval 0.7-6.9) for development of parkinsonism and an OR of 1.7 (95% confidence interval 0.5-4.9) for TD was calculated in an individual with at least one mutated allele. However, the ORs were not statistically significant. CONCLUSIONS: The higher zuclopenthixol steady-state plasma concentrations in heterozygous EM and PM schizophrenic patients receiving monotherapy with zuclopenthixol-decanoate than in homozygous EMs indicates a significant role of CYP2D6 in the systemic elimination of zuclopenthixol. The tendencies for patients carrying at least one mutated CYP2D6 gene to have an increased risk of parkinsonism and TD are in accordance with previous studies. Age was a significant risk factor for neurological side effects.

Adult↗
PubMed2004

[Incidence of rigor during treatment with flupentixol decanoate in comparison to risperidone].

STUDY OBJECTIVE: We investigated as to whether dosedependent extrapyramidal tolerance of Flupentixol decanoate is inferior to that of Risperidone. METHOD: 143 Risperidone and 177 Flupentixol decanoate treated patients were consecutively entered into this non - randomized open study and assessed with the Simpson-Angus-Scale regarding presence of rigor. Treatment comparisons of rigor frequency was done by Kaplan-Meier analysis. RESULTS: The risk of rigor increased with dose on both treatments. EPMS-risk was not increased under treatment with Flupentixol decanoate (mean dose 35.06 +/- 19.7 mg/2 weeks) compared to Risperidone (mean daily dose: 5.2 +/- 2.5 mg/kg) when comparable weight standardized Haloperidol equivalence doses (WHE) were used. CONCLUSION: This study offers limited evidence for methodological reasons. Yet, results do not support the view that EPS are more frequent on Flupentixol decanoate than on Risperidone when doses are comparable.

Adult↗
PubMed2005

A multicentre study investigating subcutaneous etonogestrel implants with injectable testosterone decanoate as a potential long-acting male contraceptive.

BACKGROUND: The combination of etonogestrel implants with injectable testosterone decanoate was investigated as a potential male contraceptive. METHODS: One hundred and thirty subjects were randomly assigned to three treatment groups, all receiving two etonogestrel rods (204 mg etonogestrel) and 400 mg testosterone decanoate either every 4 weeks (group I, n = 42), or every 6 weeks (group II, n = 51) or 600 mg testosterone decanoate every 6 weeks (group III, n = 37) for a treatment period of 48 weeks. RESULTS: One hundred and ten men completed 48 weeks of treatment. Sperm concentrations of <1 x 10(6)/ml were achieved in 90% (group I), 82% (group II) and 89% (group III) of subjects by week 24. Suppression was slower in group II, which also demonstrated more frequent escape from gonadotrophin suppression than groups I and III. Peak testosterone concentrations remained in the normal range throughout in all groups. Mean trough testosterone concentrations were initially subphysiological but increased into the normal range during treatment. Mean haemoglobin levels increased in group I, and a non-significant increase in weight and decline in high-density lipoprotein cholesterol was observed in all groups. Fourteen subjects discontinued treatment due to adverse events. CONCLUSIONS: Subcutaneous etonogestrel implants in combination with injectable testosterone decanoate resulted in profound suppression of spermatogenesis that could be maintained for up to 1 year. Efficacy of suppression was less in group II, probably due to inadequate testosterone dosage. This combination has potential as a long-acting male hormonal contraceptive.

Administration, Cutaneous↗
PubMed1997

Haloperidol serum concentrations and D2 dopamine receptor occupancy during low-dose treatment with haloperidol decanoate.

The aim of this study was to examine the relationship between serum concentrations of haloperidol and central D2 receptor occupancy in eight schizophrenic patients treated with low doses of haloperidol decanoate. The accompanying psychopathology was assessed. During a 4-week interval after administration of haloperidol decanoate (dose range 30-70 mg), serum concentrations of haloperidol were determined once a week by using a sensitive high-performance liquid chromatography method. The patients' D2 receptor occupancy was determined with single-photon emission computed tomography on two separate occasions. One week after depot administration the mean haloperidol serum concentration was 7.3 nmol/l (range 3.9-22.7 nmol/l) and the mean D2 receptor occupancy was 75% (range 52-100%). After 4 weeks the mean haloperidol serum concentration had decreased to 1.8 nmol/l (range 0-5.7 nmol/l) and the mean D2 receptor occupancy to 53% (range 12-89%). Differences were seen in two subgroups, defined by their history of neuroleptic exposure before inclusion into the study. Patients treated with depots of haloperidol decanoate for months showed higher D2 receptor occupancy and corresponding higher serum haloperidol concentrations at week 4 than did patients who had a history of oral haloperidol treatment. Because the difference in the dynamics of D2 receptor occupancy could be reflected by corresponding serum concentrations of haloperidol, it seems useful to involve haloperidol drug monitoring as a possible surrogate marker for D2 receptor occupancy in optimizing low-dose treatment with haloperidol decanoate.

Adult↗
PubMed1977

Effects of orally administered oestradiol decanoate on plasma oestradiol, oestrone and gonadotrophin levels, vaginal cytology, cervical mucus and endometrium in ovariectomized women.

Six ovariectomized women with the uterus left in situ were given a daily oral dose of 0.5 mg of oestradiol decaneoate in oil for 14 days. After a single dose of oestradiol decanoate mean plasma oestradiol rose from 26.8 pg/ml to 66.8 pg/ml within 30 min. There was a further rise to 100-110 pg/ml (P less than 0.001) remaining at the same level over a 24 h period. On repeated daily administration of oestradiol decanoate this rise continued reaching the mean value of 187.1 pg/ml (P less than 0.001) at 2 weeks, while plasma oestrone remained at the same level (147.1 pg/ml) as it was at 24 h. The ratio of plasma oestrone:oestradiol was less than 1 at 2 weeks. Plasma FSH and LH fell progressively during the medication. Changes of the Maturation Index, cervical mucus Ferning and Spinnbarkeit demonstrated the strong 'peripheral' activity of this dose of oestradiol decanoate. All endometrial specimens showed late proliferative changes at 2 weeks. It was concluded that the favourable properties of oestradiol decanoate offer new possibilities for a more physiological oestrogen supplementation therapy.

Adult↗
PubMed1978

Double-blind therapeutic evaluation of fluspirilene compared with fluphenazine decanoate in chronic schizophrenics.

Fifty chronic schizophrenics were randomly assigned to a 16-week treatment either with fluspirilene or with fluphenazine decanoate. The aim of the study was to compare the antipsychotic action and the side effects of the two neuroleptics. Fluphenazine decanoate caused more side effects and the difference between the two groups was statistically significant in the items tremor, severe extrapyramidal effects and parkinsonism. More patients in the fluspirilene group (nine patients) compared with only three in the fluphenazine decanoate group remained free of side effects during the whole trial. Judged from the BPRS fluspirilene proved an equally potent neuroleptic with fluphenazine decanoate although statistically significant improvement has been obtained in more items of the scale in the fluspirilene group. The improvement in the NOSIE-30 was much more clear in the fluspirilene group. Although Clinical Global Impressions of the investigators and the nursing personnel favored fluspirilene, the differences between the two groups were not statistically significant.

Adult↗
PubMed1991

Plasma levels of fluphenazine in patients receiving fluphenazine decanoate. Relationship to clinical response.

The levels of fluphenazine and fluphenazine sulphoxide in schizophrenic patients who were randomly assigned to receive either 5 mg or 25 mg of fluphenazine decanoate every two weeks were monitored. Patients treated with 25 mg of fluphenazine decanoate required three months to reach a steady-state plasma level, indicating that those patients who are being converted from oral to depot fluphenazine should continue to receive oral supplementation during the first three months of treatment with fluphenazine decanoate. Plasma levels of fluphenazine sulphoxide were lower than levels of fluphenazine. At six and nine months following randomisation, there was a statistically significant relationship between lower fluphenazine plasma levels and an increased risk of psychotic exacerbations. A relatively weak relationship was found between fluphenazine plasma levels and akinesia, but non-significant relationships between fluphenazine levels and other neurological side-effects including akathisia, retardation, and tardive dyskinesia. Monitoring the plasma levels may be helpful to clinicians who are attempting to treat stabilised patients with the lowest effective dose of fluphenazine decanoate.

Adult↗
PubMed2006

Adverse extrapyramidal effects in four horse given fluphenazine decanoate.

CASE DESCRIPTION: 4 racehorses were examined because of markedly abnormal behavior following administration of fluphenazine decanoate. CLINICAL FINDINGS: Clinical signs included restlessness, agitation, profuse sweating, hypermetria, aimless circling, intense pawing and striking with the thoracic limbs, and rhythmic swinging of the head and neck alternating with episodes of severe stupor. Fluphenazine was detected in serum or plasma from all 4 horses. The dose of fluphenazine decanoate administered to 3 of the 4 horses was within the range (25 to 50 mg) routinely administered to adult humans. TREATMENT AND OUTCOME: In 2 horses, there was no response to IV administration of diphenhydramine hydrochloride, but the abnormal behavior in these 2 horses appeared to resolve following administration of benztropine mesylate, and both horses returned to racing. The other 2 horses responded to diphenhydramine administration. One returned to racing. The other was euthanized because of severe neurologic signs, respiratory failure, and acute renal failure. CLINICAL RELEVANCE: Findings indicate that adverse extrapyramidal effects may occur in horses given fluphenazine decanoate. These effects appear to be unpredictable and may be severe and life threatening. Use of fluphenazine decanoate as an anxiolytic in performance horses is not permitted in many racing and horse show jurisdictions, and analytic procedures are now available to detect the presence of fluphenazine in serum or plasma.

Animals↗
PubMed1991

Duration of neuroleptic treatment and relapse rate: a 5-year follow-up study with haloperidol decanoate.

The role of neuroleptic drugs in controlling acute psychotic symptoms and reducing relapse is well established. It is the clinical management of chronically disabled patients that has major implications for health care planning. Drug discontinuation studies have indicated that patients with chronic schizophrenia should receive maintenance drug therapy for some years. This was a 5-year follow-up study to assess the long-term effects of depot haloperidol decanoate vs. other neuroleptics in 62 psychotic patients treated in the community. The study indicates that there were more relapses and hospitalization for patients maintained on other neuroleptics than for patients maintained on haloperidol decanoate. The study indicates that haloperidol decanoate even in low dosage is effective maintenance therapy is preventing relapse. Indeed, some of the good responders to haloperidol therapy may have benefitted from lowering the dosage of the drug. It is our experience that haloperidol decanoate is of good value in the management of psychotic illnesses that require long-term treatment. A more controlled longer-term study is needed to confirm our results.

Antipsychotic Agents↗
PubMed1990

Injection site reactions after intramuscular administration of haloperidol decanoate 100 mg/mL.

The authors report four cases of injection site reaction after intramuscular administration of haloperidol decanoate 100 mg/mL. In each case, the injection site became edematous, red, pruritic, and tender, and a palpable mass remained for up to 3 months. No systemic symptoms were reported. All four patients had previously received the 50 mg/mL haloperidol decanoate injection without incident. Two of these events followed the initial injection of haloperidol decanoate 100 mg/mL. Rechallenge with the 100 mg/mL product in one case and the 50 mg/mL product in two resulted in similar reactions. The incidence of this reaction at the authors' facility is estimated to be 7.7%. The authors speculate that the reaction is most likely to be related to the concentration of haloperidol decanoate in the injection.

Adult↗
PubMed1977

[Comparison of the effects of pipothiazine palmitate and fluphenazine decanoate. Results of a multicenter double-blind trial].

Fluphenazine decanoate and pipothiazine palmitate were compared concerning their effect and side-effects. 61 schizophrenic patients were treated up to 6 months in a multicenter double-blind trial. Assessments were made on day 0 and after 5, 10, 17 and 22 weeks of treatment using the AMP system. Pipothiazine palmitate was injected every 4th week and fluphenazine decanoate every 3rd week. The most often applied dosage was 100 mg pipothiazine palmitate and 25 or 37.5 mg fluphenazine decanoate. Data analysis of the AMP system at the symptom level showed the better antipsychotic effect of pipothiazine palmitate. A comparison between the two groups by means of analysis of covariance at the syndrome level showed no statistical significant differences between the effects of fluphenazine decanoate and pipothiazine palmitate.

Antipsychotic Agents↗
PubMed1988

Zuclopenthixol decanoate in the management of behavioural disorders in mentally handicapped patients.

One hundred and sixteen mentally handicapped patients with behavioural disorders were studied in a double-blind clinical comparison of zuclopenthixol decanoate injection (mean dosage 123 mg/week) and placebo. The study consisted of a 4-week open phase, in which all patients were treated with zuclopenthixol decanoate, followed by a 12-week double-blind phase where approximately half of the patients were changed to placebo. Patients were assessed every 2 weeks using the Clinical Global Impression, the Nurse's Observation Scale for In-patient Evaluation, a specific behaviour rating scale designed for this study and a side-effects check-list. Fourteen patients in the placebo group were withdrawn because of an increase in the frequency and severity of their behavioural disorders compared to only 4 in the zuclopenthixol decanoate group. Analyses of the rating scales of the patients remaining in the study also showed zuclopenthixol decanoate to be superior to placebo in the treatment of mentally handicapped patients with behavioural disorders. Side-effects in general were not a problem and did not affect treatment.

Adolescent↗
PubMed1986

Pharmacology, pharmacokinetics and clinical development of haloperidol decanoate.

The absorption mechanism of haloperidol decanoate from the intramuscular depot was studied in dogs. Haloperidol, a pharmacologically active molecule characterised by selective dopamine antagonism, was detectable in plasma within one hour after dosing. Peak plasma levels were obtained within three to seven days. After single and repeated doses of haloperidol decanoate, plasma levels were found to be dose related. Human pharmacokinetics in schizophrenic patients were studied by giving four-weekly deep intramuscular injections of haloperidol decanoate at doses equivalent to the patients' previous antipsychotic medication. Within each interval between doses, haloperidol plasma levels were maximal within the first week after each dose, decaying with an average half-life of three weeks. Steady-state was reached within three months giving therapeutic plasma levels in the same range as those found during oral treatment with haloperidol. Open and double-blind clinical trials have demonstrated the clinical efficacy of haloperidol decanoate given four-weekly by deep intramuscular injection over a dose range from 50 to 300 mg, principally in schizophrenic patients. Low incidences of extrapyramidal side effects were noted, often allowing a reduction of antiparkinsonian medication required through previous antipsychotic treatment.

Animals↗