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PubMed1987

Plasma prolactin and fluphenazine concentrations in patients receiving fluphenazine decanoate: stability over injection intervals.

Plasma prolactin and fluphenazine concentrations were measured in a group of 17 patients (9 males, 8 females) with schizophrenia who were receiving chronic treatment with fluphenazine decanoate. Neither measure was significantly correlated with clinical effect, as measured by the Brief Psychiatric Rating Scale, at any of the 5 pre-injection times examined. None of the measures showed statistically significant (P greater than 0.05; MANOVA) variations with time. Neither measure showed a significant correlation with the dose (expressed as mg/kg) of fluphenazine. The implications of the study for monitoring chronic treatment of schizophrenia are discussed.

Adult↗
PubMed1994

Quantitative EEG and BPRS data following Haldol-Decanoate administration in schizophrenics.

Approximately one-third of schizophrenic patients receiving antipsychotic drugs obtain little or no benefit from them. In some reports, response has been linked with "prognostic" factors, including abnormal EEG and drug response (pharmaco-EEG). Measurements of topological EEG spectral power and Brief Psychiatric Rating Scale (BPRS) values were obtained in 15 schizophrenics over a period of 20 min immediately after the first application, and at weekly intervals after single intramuscular injection of 2 ml depot haloperidol (Haldol-Decanoate). A highly significant increase in the alpha-1 power density at almost all positions and an increase in theta power at parietotemporal regions can be described as electrophysiological parameters of the acute pharmaco-EEG. BPRS values decreased continuously within the first 2 weeks followed by an increase to the predrug level after the fourth week. Over the whole observation period there was a correlation between neurophysiological data (alpha-1 power) and clinical symptomatology (BPRS total score; r = -0.7). Therefore, it can be concluded that quantitative EEG recordings are able to serve as a tool for the optimization of the depot neuroleptic treatment in schizophrenics.

Adult↗
PubMed1995

Recurrent priapism as a side effect of zuclopenthixol decanoate.

Priapism has been described as a rare side effect of certain phenothiazine antipsychotics with high alpha1-adrenergic blocking potential. We describe a patient who in the course of clinical treatment with the thioxanthene antipsychotic zuclopenthixol (Clopixol) decanoate had several episodes of priapism. Although the alpha-blocking potential of zuclopenthixol is only moderate, it seems that in sufficient dose, or in combination with other antipsychotics, this drug is capable of inducing priapism.

Adult↗
PubMed1980

The diagnosis of rapid abnormal involuntary movements associated with fluphenazine decanoate.

Three patients with low grade tardive dyskinesia developed an acute episode of abnormal involuntary movements after a single injection of fluphenazine decanoate. All three patients had their symptoms relieved after treatment with antiparkinsonian medication. The differential diagnosis of these movements is discussed, and a possible animal model for this phenomenon is described.

Benztropine↗
PubMed1994

Fluctuation of serum zuclopenthixol concentrations in patients treated with zuclopenthixol decanoate in viscoleo.

Zuclopenthixol serum concentrations were measured in 58 psychiatric patients referred for routine therapeutic drug monitoring (TDM). Patients were treated for prolonged time with zuclopenthixol decanoate in viscoleo in doses of 50-500 mg, administered intramuscularly at 14-day intervals. The serum concentration was determined at days 7 (C7) and 14 (C14) following injection. The mean ratio C7/C14 was 2.0 and was independent of the dosage given. In 14 patients, additional blood samples were drawn at day 3 (C3) following injection. The mean ratio C3/C14 of this group was 3.2. An almost log-linear decline of the serum concentration from day 3 to 14 appeared, which corresponds to an apparent half-life of zuclopenthixol in this dosage form of 7.4 days. The marked fluctuations of serum concentrations of zuclopenthixol from peak to trough levels in patients given fortnightly injections of the depot preparation indicate that shorter intervals between injections should be considered in many cases in order to diminish side effects.

Clopenthixol↗
PubMed1979

Plasma fluphenazine levels by radioimmunoassay in schizophrenic patients treated with depot injections of fluphenazine decanoate.

1 Using a radioimmunoassay, plasma fluphenazine (FPZ) concentrations were examined in 33 schizophrenic patients during 38 intervals between injections of FPZ decanoate. Doses ranged from 12.5 to 150 mg and intervals from 1 to 5 weeks. At least three blood samples were taken between injections from each subject; also in 26 subjects additional samples were taken during the first 24 h post-injection. 2 FPZ was measurable in all plasma samples. 3 Each injection was followed by a rapid rise in plasma FPZ concentration to a maximum at 1-8 h. The height of this peak varied considerably. Within the next 12-36 h plasma FPZ fell to a level slightly above that found before injection and then remained stable until the next injection, thus confirming the steady release of FPZ from the depot over this period. 4 For the group, dose and mean plasma FPZ levels correlated strongly. 5 Despite this, there was a four-fold variation in plasma FPZ concentration among subjects receiving the same dose. 6 The FPZ level on the last day of an interval between injections was a satisfactory estimate of the mean FPZ level for the interval. 7 In one subject examined in this way, a positive correlation was found (r = 0.76) between plasma FPZ (by radioimmunoassay) and plasma prolactin levels.

Adult↗
PubMed1975

The percutaneous penetration of nandrolone decanoate.

A study has been carried out on the penetration of nandrolone decanoate through human cadaver skin in vitro using radioactive tracer material. The radiochemical purity of the material desorbed from the dermal skin surface is very much less than that of the material absorbed into the epidermal surface. These observations are a consequence of the low level of overall penetration of the skin by the steroid. There is also a possibility that a small percentage of the steroid is being metabolized by micro-organisms present in the skin samples.

Aged↗
PubMed1987

Effect of chronic administration of haloperidol (intermittently) and haloperidol-decanoate (continuously) on D2 dopamine and muscarinic cholinergic receptors and on carbachol-stimulated phosphoinositide hydrolysis in the rat striatum.

It has been reported that apomorphine-induced stereotypy is sensitized after a chronic intermittent administration of haloperidol (HPD), but not after a chronic continuous exposure to haloperidol-decanoate (HPD-D). The present study was undertaken to investigate changes in the D2 dopamine and muscarinic receptors in the rat striatum after the administration of HPD intermittently and HPD-D continuously. The number of striatal [3H]spiperone binding sites increased significantly after HPD-D, but did not change after HPD. Neither the number of [3H](-)QNB binding sites nor carbachol-stimulated phosphoinositide hydrolysis changed after either HPD or HPD-D. These results indicate that the increase in striatal D2 receptors in rats administered HPD-D represents behavioral and biochemical tolerance, and that neither the D2 dopamine receptor supersensitivity nor muscarinic receptor hyposensitivity underlies sensitization of apomorphine-induced stereotypy.

Animals↗
PubMed1991

Effect of haloperidol decanoate on the cardiovascular system.

Rapid speed electrocardiograms were recorded in 13 chronic schizophrenic patients before, and at regular intervals during a six-month trial of haloperidol decanoate. Measurements of conduction intervals in the EEG were carried out blind to patient and to assessment interval. No significant changes in heart rate; PR, QRS on QTc intervals; or T-wave height were found. Neither was there a significant change in the blood pressure. The findings confirm that haloperidol does not have clinically relevant cardiac effects when given in therapeutic doses to physically healthy individuals.

Adult↗
PubMed1996

Morphological changes in met(5)-enkephalin-immunoreactive synaptic boutons in the rat neostriatum after haloperidol decanoate treatment.

The morphological plasticity of an identified population of synaptic boutons in the rat neostriatum was investigated 24 h (short-term treatment) or 14 days (long-term treatment) after administration of the depot neuroleptic, haloperidol decanoate. Specific methionine(5)-enkephalin antiserum was used to label bouton profiles in the dorsal neostriatum. The size and shape of these boutons was subsequently analysed with quantitative methods at the ultrastructural level. Immunoreactive synaptic bouton profiles were found to have a larger cross-sectional area, to be less circular in shape and to have a longer maximum diameter after long-term neuroleptic treatment. These parameters were not significantly affected by short-term neuroleptic treatment. The morphological parameters indicate that methionine(5)-enkephalin-immunoreactive boutons become enlarged, probably by elongating. This suggests that boutons containing methionine(5)-enkephalin increase their potential synaptic efficacy in the long term after neuroleptic treatment.

Animals↗
PubMed1980

Long-term fluphenazine decanoate maintenance dosage requirements of chronic schizophrenic patients.

Forty-seven schizophrenic out-patients, who were satisfactorily maintained on a depot injection of fluphenazine decanoate, and who received the injection every 28 days, were progressively withdrawn from medication by increasing the time interval between injections while maintaining the amount of of drug per injection. The rate of reduction varied with each patient depending on various factors such as environmental stress considerations, and the patient's wishes. Finally three injections at 8-weekly intervals were given before complete withdrawal. The follow-up period was 23.7 months with a standard deviation of 1.9. A relapse rate of 80% was found, 25 patients relapsing during the withdrawal phase and 22 patients after the drug had been completely withdrawn.

Adult↗
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↗
PubMed2003

Overload-induced androgen receptor expression in the aged rat hindlimb receiving nandrolone decanoate.

This study's purpose was to examine whether functional overload with nandrolone decanoate (ND) administration increased muscle mass and steroid receptor concentration in aged rat soleus (Sol) and plantaris (Plan) muscle. ND (6 mg/kg body wt) was administered once a week for 4 wk, whereas control rats received sesame seed oil injections. Functional overload of the hindlimb Sol and Plan was induced by synergistic gastrocnemius muscle ablation at the beginning of the fourth week. Adult (5 mo of age) and aged rats (25 mo of age) were randomly assigned to four groups: control, overload, control-ND, and overload-ND. Seven days of functional overload increased adult Sol muscle mass 27%, whereas the aged Sol muscle mass did not change. The aged overloaded Sol muscle receiving ND significantly increased muscle weight by 35% and total muscle protein by 24%. Aged Plan muscle did not increase muscle weight with overload or ND treatment. Androgen receptor protein was induced by ND treatment and functional Ov, and combining the two treatments induced Sol androgen receptor protein concentration above either alone. Sol glucocorticoid receptor protein concentration increased in overload groups of both ages. ND administration can increase aged Sol muscle mass and protein content after 7 days of functional overload, and the cooperative induction of androgen receptor may be important for this response.

Anabolic Agents↗
PubMed1981

Follow-up study of 281 schizophrenic patients treated with high dosage fluphenazine decanoate.

281 newly admitted female schizophrenic patients were treated with high dosage fluphenazine decanoate intramuscularly, starting with 250 mg per injection together with antiparkinsonian and antidepressant drugs. On a set day the 3 groups 'with neuroleptics' (NL) (n = 54), 'without NL' (n = 152) and 'relapsed when without NL' (n = 42) were compared concerning age, diagnosis, hereditary disposition, first admission and readmissions, number of admissions and global judgement. From the differences no clear conclusion for practical clinical work could be obtained. The good tolerance is discussed using the list of side effects including tardive dyskinesia and laboratory data.

Age Factors↗
PubMed1982

A double-blind comparison of fluspirilene and fluphenazine decanoate in schizophrenia.

A double-blind comparison of fluspirilene and fluphenazine decanoate in 28 schizophrenic patients over six months showed equal improvement and the same incidence of side-effects in each group of patients. It would be expected from the literature that a better ratio of therapeutic to side-effects would appear with fluspirilene than with fluphenazine. The absence of such an effect in this study may be attributable to an initial lack of familiarity by the investigators with the use of fluspirilene, indicating an important potential variable in the comparison of a new drug with an established one.

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↗
PubMed1988

Haloperidol decanoate: a depot antipsychotic.

This article reviews the role of a new depot antipsychotic dosage form, haloperidol decanoate (HD), in relationship to other comparable pharmacotherapies (oral and injectable). The chemistry, indications, contraindications, and pharmacokinetics of HD are discussed. The available clinical research in humans is presented and evaluated with respect to efficacy, adverse effects, and dosing. HD is clearly an effective antipsychotic dosage form. Certainly, HD can improve compliance and possibly outcome for selected patients. HD should be reserved for chronic relapsing schizophrenic patients who have responded to oral haloperidol. Considering the pharmacokinetics, potential risks, and cost of HD, the clinician needs to be prepared with recommendations to effect optimal use of HD (guidelines are presented).

Antipsychotic Agents↗