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PubMed1984

Can neuroleptics influence the function of the brain hemispheres asymmetrically?

A long-term intracarotid tube was implanted in 32 rats. Intracarotid injection of 4 different neuroleptics (haloperidol, cis- and trans-flupenthixol, clopenthixol and reserpine) elicited a typical posture with abduction of the limbs on one side and and adduction on the other. Only the neuroleptically-active cis-isomers of flupenthixol and clopenthixol provoked this dystonic reaction. The posture spontaneously vanished after 24 hr and could be antagonized with the anticholinergic biperiden. Sham injections of Ringer's solution and isotonic glucose proved to be behaviourally inert. These results indicate an asymmetric distribution of the drugs in this experimental procedure. Their implications concerning drug-induced and spontaneous dystonias as well as psythopathology are discussed.

Animals↗
PubMed1979

Increase in weight after treatment with depot neuroleptics.

A trial has been performed investigating changes in weight in 99 female patients who have been treated with clopenthixol decanoate or perpehnazine enanthate after prior treatment with different oral neuroleptics. We found a significantly higher mean weight after the oral treatment period and a slight, but not statistically significant, further weight increase after the following depot period. In addition the rate of increase in weight was significantly lower during the depot treatment period. These increases might be due to achievement of a steady-state in weight during the first treatment period with oral intake. We found no difference between clopenthixol decanoate and perphenazine enanthate as regards change in weight or rate of change in weight.

Administration, Oral↗
PubMed1985

Tests for local toxicity of intramuscular drug preparations: comparison of in vivo and in vitro methods.

Different concentrations of aqueous preparations of metoclopramide, gaboxadol, cis(Z)-clopenthixol, digoxin and chlorpromazine and of cis(Z)-clopenthixol acetate in Viscoleo have been tested for local toxicity after intramuscular injection in rabbits. The weight of macroscopically changed muscle tissue isolated 3 days after injection was determined. In addition, homogenized injection site muscle tissue was analysed for creatine kinase (CK) activity and by comparison with the CK activity of contralateral muscle tissue, the amount of injection site muscle tissue totally depleted for CK activity was calculated. The substances have also been tested for in vitro toxicity. The concentrations of the substances which caused 100% haemolysis of human erythrocytes or minimal cytotoxicity in cell culture assays using MRC-5 fibroblasts were estimated. Metoclopramide and gaboxadol caused no or only minimal local muscle damage in the rabbits. Metoclopramide caused local bleeding. The four other substances caused concentration-dependent muscle damage. Although there was some deviations, the two in vitro tests reflected reasonably well the in vivo findings. The results of this study suggest that the in vitro tests employed can be useful as screening tests for local toxic effect of intramuscular drug preparations. However, further studies are required before conclusion as to predictability can be drawn. The in vitro methods are inexpensive and quick, especially the haemolysis test.

Animals↗
PubMed2000

Depot perphenazine decanoate and enanthate for schizophrenia.

BACKGROUND: Anti-psychotic drugs are usually given orally but compliance with medication given by this route may be difficult to quantify. The development of depot injections in the 1960s gave rise to extensive use of depots as a means of long-term maintenance treatment. Perphenazine decanoate and enanthate are depot antipsychotics that belong to the phenothiazine family and have a piperazine ethanol side chain. OBJECTIVES: To assess the effects of depot perphenazine decanoate and enanthate versus placebo, oral anti-psychotics and other depot antipsychotic preparations for people with schizophrenia in terms of clinical, social and economic outcomes. SEARCH STRATEGY: Biological Abstracts (1982-1998), the Cochrane Library (Issue 2, 1998), the Cochrane Schizophrenia Group's Register (June 1998), EMBASE (1980-1998), MEDLINE (1966-1998), and PsycLIT (1974-1998) were searched. References of all identified trials were also inspected for more studies and industry contacted. SELECTION CRITERIA: Randomised clinical trials focusing on people with schizophrenia where depot perphenazine decanoate and enanthate, oral anti-psychotics or other depot preparations were compared. DATA COLLECTION AND ANALYSIS: Studies were reliably selected, quality rated and data extracted. For dichotomous data Peto odds ratios (OR) with the 95% confidence intervals (CI) were estimated. Where possible, the number needed to treat statistic (NNT) was calculated. Analysis was by intention-to-treat. MAIN RESULTS: One study of six months duration, compared perphenazine enanthate to clopenthixol decanoate. There was no differences between the two for outcomes of global improvement, relapse and leaving the study early. More people in the perphenazine enanthate group required anticholinergic drugs than those allocated to clopenthixol decanoate (OR 3.6 CI 1.2-10, NNT 10). A single study (n=64, duration six weeks) compared perphenazine enanthate and its longer acting decanoate ester. Data on relapse and leaving the study early failed to show convincing differences. The enanthate group, however, experienced more movement disorders (OR 0.2 CI 0.06-0.7) than those allocated the decanoate ester of the same drug (NNT 4.0) and required more anticholinergic drugs (OR 0.2 CI 0.08-0.7, NNT 3.7). REVIEWER'S CONCLUSIONS: Depot perphenazine is in clinical use in the Nordic countries, Belgium, Portugal and the Netherlands. At a conservative estimate a quarter of a million people suffer from schizophrenia in those countries and could be treated with depot perphenazine. The total number of participants in the two trials with useful data is 236. Neither study observes the effect of oral versus depot antipsychotic drugs. Until well conducted and reported randomised trials are undertaken clinicians will be in doubt as to the effects of perphenazine depots and people with schizophrenia should exercise their own judgement or ask to be randomised.

Antipsychotic Agents↗
PubMed2005

Depot perphenazine decanoate and enanthate for schizophrenia.

BACKGROUND: Antipsychotic drugs are usually given orally but compliance with medication given by this route may be difficult to quantify. The development of depot injections in the 1960s gave rise to extensive use of depots as a means of long-term maintenance treatment. Perphenazine decanoate and enanthate are depot antipsychotics that belong to the phenothiazine family and have a piperazine ethanol side chain. OBJECTIVES: To assess the effects of depot perphenazine decanoate and enanthate versus placebo, oral antipsychotics and other depot antipsychotic preparations for people with schizophrenia in terms of clinical, social and economic outcomes. SEARCH STRATEGY: We updated previous searches of the Cochrane Schizophrenia Group Register (June 1998), Biological Abstracts (1982-1998), the Cochrane Library (Issue 2, 1998), EMBASE (1980-1998), MEDLINE (1966-1998), and PsycLIT (1974-1998) by searching the Cochrane Schizophrenia Group Register (March 2004). References of all identified trials were also inspected for more studies and industry contacted. SELECTION CRITERIA: We compared randomised clinical trials focusing on people with schizophrenia where depot perphenazine decanoate and enanthate, oral antipsychotics or other depot preparations. DATA COLLECTION AND ANALYSIS: We reliably selected studies, quality rated them and extracted data. For dichotomous data we estimated the Relative Risk (RR) with the 95% confidence intervals (CI). Where possible, we calculated the number needed to treat statistic (NNT). Analysis was by intention-to-treat. MAIN RESULTS: Only four studies (Ahlfors 1980, Eufe 1979, Knudsen 1985c, Tegeler 1979), randomising a total 313 people could be included in this review and this combined with an overall lack of usable data limits any interpretation of results. Perphenazine enanthate was not significantly any better or worse than other depot antipsychotics in most of the main outcomes such as global state, relapse or leaving the study early. We found some differences favouring the control groups for adverse effects. One study (Ahlfors 1980) of six months' duration (n=172), compared perphenazine enanthate to clopenthixol decanoate. There were no differences between the two groups for outcomes of global improvement, relapse and leaving the study early. More people in the perphenazine enanthate group, however, required anticholinergic drugs than those allocated to clopenthixol decanoate (RR 1.12 CI 1.0 to 1.2, NNT 10).A single study (n=64, duration six weeks) compared perphenazine enanthate and its longer acting decanoate ester. Data on relapse and leaving the study early failed to show convincing differences. The enanthate group, however, experienced more movement disorders (RR 1.36, CI 1.1 to 1.8 NNT 5) than those allocated the decanoate ester of the same drug and required more anticholinergic drugs (RR 1.47 CI 1.1 to 2.0, NNT 4). AUTHORS' CONCLUSIONS: Depot perphenazine is in clinical use in the Nordic countries, Belgium, Portugal and the Netherlands. At a conservative estimate, a quarter of a million people suffer from schizophrenia in those countries and could be treated with depot perphenazine. The total number of participants in the four trials with useful data is 313. None of the studies observed the effects of oral versus depot antipsychotic drugs. Until well conducted and reported randomised trials are undertaken clinicians will be in doubt as to the effects of perphenazine depots and people with schizophrenia should exercise their own judgement or ask to be randomised.

Antipsychotic Agents↗
PubMed1989

The electrically-stimulated spinal reflex in pithed rats: a possible test model for evaluating blockade of central dopamine D1 and D2 receptors.

Intravenous injection of the dopamine (DA) D1 receptor agonist SK&F 38393 (4.3 mumol/kg = 1.25 mg/kg), or the DA D2 receptor agonist pergolide (3.2 mumol/kg = 1.25 mg/kg) increased the electrically-stimulated spinal reflex in pithed rats by more than 600 per cent. The specific DA D1 receptor antagonist SCH 23390 potently inhibited the SK&F 38393-induced spinal reflex but not the pergolide-induced reflex. The DA D2 receptor antagonists clebopride and YM 09151-2 inhibited the pergolide-induced reflex only. Two mixed DA D1/D2 antagonists (cis(Z)-flupentixol and zuclopenthixol) inhibited the effects of both SK&F 38393 and pergolide on the spinal reflex, while the neuroleptically inactive isomer of clopenthixol (trans(E)-clopenthixol) was also inactive in this context. Various antagonists (prazosin (alpha 1), idazoxan (alpha 2), 1- propranolol (beta), bicuculline (GABA] were inactive in the test model. The 5-HT2 receptor antagonists altanserin and ketanserin also showed antagonistic effect. It is concluded that the electrically-stimulated spinal reflex in pithed rats can be used as a test model to estimate the blockade of central DA D1 and DA D2 receptors without influence from alpha 1-adrenergic, alpha 2-adrenergic, beta-adrenergic and GABA-ergic receptors. However, a serotonergic receptor antagonism does influence the specificity of the test model.

Animals↗
PubMed1992

The antibacterial effect of some neuroleptics on strains isolated from patients with meningitis.

Eighty-two strains of bacteria (Neisseria meningitidis, Haemophilus influenzae, Enterobacteriaceae, Streptococcus pneumoniae, group B streptococci and Listeria monocytogenes) were examined for their in vitro susceptibility to eight drugs, seven neuroleptics (perphenazine, fluphenazine, cis(Z)-clopenthixol, haloperidol, clozapine, clebopride and SCH 23390), and the neuroleptically inactive trans(E)-clopenthixol. The phenothiazines and the thioxanthenes were, on the whole, the most active drugs when measured, the IC50(50) for each group of bacteria being 7.4 to 84 mg/l (with the exception of the activity against the enterobacteriaceae). The antibacterial potency of clozapine, which has an atypical neuroleptic profile, was between 50 and 140 mg/l. Haloperidol also showed an antibacterial activity in the concentration range 35-140 mg/l. The selective D1 antagonist, SCH 23390 and the selective D2 antagonist, clebopride, inhibited only few of the bacteria in the concentration range investigated.

Antipsychotic Agents↗
PubMed1986

The antibacterial effect of selected phenothiazines and thioxanthenes on slow-growing mycobacteria.

The aim of the present investigation was to illustrate the antibacterial effect of various phenothiazine and thioxanthene derivatives on mycobacteria in vitro. It was demonstrated that clopenthixol is about twice as potent as chlorpromazine (CPZ) and levomepromazine-maleate is about half as potent as CPZ, measured by the inhibitory effect on the growth of the mycobacterial strains. Measured in the same way the stereoisomeric compounds of flupenthixol are shown to be more potent than the stereo-isomeric compounds of clopenthixol and chlorprothixen. The two last-named compounds are equal in potency. The stereo-isomeric analogs of the thioxanthene derivatives are equal in antibacterial potency against the slow-growing mycobacteria. The mycobacterial strains investigated show no difference in sensitivity between the cis (Z)--and and trans (E)--compounds of the thioxanthenes. It seems particularly promising that also the more resistant mycobacteria other than Mycobacterium tuberculosis, e.g. M. avium and M. intracellulare, are sensitive in the concentration range investigated. Considered as a whole, these results might be a stimulus to investigate the antimicrobial effect of the thioxanthenes in vivo.

Anti-Bacterial Agents↗
PubMed1984

Intramuscular injections and muscle damage: effects of concentration, volume, injection speed and vehicle.

An intramuscular injection was given to rabbits with the needle inserted in the longissimus dorsi muscle. The muscle tissue at the injection site was examined post-mortem 3 days after the injection and areas of necrotic muscle tissue were dissected for weighing. With a fixed dose of the neuroleptic drug cis(Z)-clopenthixol it was shown that a small volume of a concentrated solution caused less muscle damage than a larger volume of a relatively less concentrated solution. Injection speed, on the other hand, was not an important factor. Aqueous solutions of neuroleptic drugs caused local muscle damage which was diminished or prevented by oily vehicles.

Animals↗
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↗
PubMed1984

Differential inhibition by dopamine D-1 and D-2 antagonists of circling behaviour induced by dopamine agonists in rats with unilateral 6-hydroxydopamine lesions.

The selective dopamine (DA) D-1 antagonist SCH 23390 antagonized the contralateral circling behaviour induced by the DA D-1 agonist SK & F 38393 in rats lesioned unilaterally with 6-hydroxy-DA but had a 600 times weaker effect against the preferential DA D-2 agonist pergolide. The D-2 antagonists clebopride and spiroperidol had the reverse selectivity. The mixed D-1/D-2 antagonists cis(Z)-flupentixol and cis(Z)-clopenthixol blocked the circling induced by either agonist. It is concluded that circling behaviour is mediated by closely related but independent DA D-1 and D-2 receptor sites.

2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-ben↗
PubMed2002

Separation of cis- and trans-isomers of thioxanthene and dibenz[b,e]oxepin derivatives on calixarene- and resorcinarene-bonded high-performance liquid chromatography stationary phases.

The chromatographic behavior of six calix[n]arene phases (n=4, 6, 8) and one calix[4]resorcinarene phase is described for the separation of cis- and trans-isomers of three thioxanthene (flupentixol, clopenthixol, chlorprothixene) and one benz[b,e]oxepin derivative (doxepin). The influences of two different organic modifiers (MeOH, MeCN) for the separation of the isomers on every column are described. Different selectivities of the stationary phases exist as a function of the ring size of the calixarenes and their substitution at the "upper rim" with p-tert.-butyl groups. Furthermore, the influence of free phenol groups on the resorcinarene phase is discussed. Relations between structural elements of the analytes and the retention behavior on the stationary phases are found. The selectivity of the calixarene and resorcinarene stationary phases is compared with a RP-C18 phase containing the same base silica. Advantages of the resorcinarene as well as of the calixarene columns exist for the separation of cis- and trans-isomers of three compounds dependent from the substitution in position 2 of the thioxanthenes, respectively the kind of the basic side chain of all substances.

Calixarenes↗
PubMed2003

Zuclopenthixol-acetate treatment in catatonic patients: the implication of iron metabolism.

There is some evidence of ferropenia correlating with neuroleptic malignant syndrome and catatonic symptoms. The aim of this prospective and naturalistic study was to investigate the implications of ferremia in patients undergoing an intramuscular injection treatment of Zuclopenthixol-acetate in Visceolo. We recruited 59 catatonic patients (33 females). Age, sex, psychiatric and somatic diagnoses, body mass index (BMI), dosage and duration of Zuclopenthixol-acetate medication and the timing of the changeover from intramuscular to oral prescription, the single dosage of Clopenthixol if initially coadministered, incidence, onset and duration of transient benign hyperthermia, iron, ferritin, transferrin and saturation values, and white and red blood cell counts as well as liver function and electrolytes were registered. A transient and benign hyperthermic reaction (mean degrees: 37.5 + 0.3 degrees C) lasting for an average of 3.0 + 1.9 d was shown by 72.9% patients (N = 43, 22 females), during a mean treatment period of 5.8 + 3.1 d. These patients were medicated with significant different mean doses of Zuclopenthixol-acetate and compared to the patients with normal body temperature (ANOVA P < 0.01). The duration of Zuclopenthixol-acetate application did not vary between these patients groups. Furthermore, significant differences of iron (59.5 + 30.6 micromol/dl vs. 87.8 + 40.8 micromol/dl; ANOVA P < 0.006) and transferrin saturation values (18.3 + 10.4% vs. 27.2 + 17.0%; ANOVA P < 0.02) were found. Ferritin and transferrin were not implicated in the episode of hyperthermia. Diagnoses, sex, white and red blood cell counts also did not vary between these groups. Our findings indicate a possible involvement of ferropenia in catatonic patients, regardless of the diagnoses, and in the development of benign transient hyperthermia, also known as drug fever.

Administration, Oral↗
PubMed1975

The interaction of neuroleptic and muscarinic agents with central dopaminergic systems.

1. The effect of muscarinic and neuroleptic agents on the turning behaviour induced by methamphetamine and apomorphine in rats with unilateral lesions of the substantia nigra induced by 6-hydroxydopamine has been examined. 2. Turning towards the side of the lesion induced by (+)-methamphetamine (5 mg/kg) was inhibited by alpha-flupenthixol (1 mg/kg) and alpha-clopenthixol (8 mg/kg) but not by high doses of their beta-isomers. 3. Turning was inhibited by chlorpromazine (4 mg/kg) and pimozide (0.2 mg/kg). Thioridazine and clozapine (16 mg/kg) were ineffective. Turning in the same direction produced by scopolamine (10 mg/kg) was also inhibited by alpha-flupenthixol (1 mg/kg) and pimozide (0.25 mg/kg). 4. Turning produced by methamphetamine (5 mg/kg) was inhibited by oxotremorine (0.75 mg/kg) even in the presence of methylatropine (5 mg/kg). 5. Turning away from the side of the lesion induced by apomorphine (0.1 mg/kg) was inhibited by oxotremorine (0.75 mg/kg) but not by thioridazine or clozapine (16 mg/kg). 6. These results are discussed with regard to the mode of action of neuroleptic drugs in producing anti-psychotic effects and drug-induced Parkinsonism.

Adenylyl Cyclase Inhibitors↗
PubMed1980

Do schizophrenics well adapted in the community need neuroleptics? A depot neuroleptic withdrawal study.

Two depot neuroleptics (flupenthixol plamitate and clopenthixol decanoate) used for at least 15 months were withdrawn in 32 schizophrenic outpatients belonging to the most symptom-free and social cohort of a total patient population. They all had only slight schizophrenic symptoms, were well adapted in the community, and had been free from relapse for at least 2 years before the study. They were assessed by means of rating scales every month during the first six months and then after 9 and 12 months. After the one-year trial 26 patients had relapsed. Moreover, after the control period further 4 out of 6 patients relapsed during the following drug-free year. These results indicate the necessity of a long follow-up period after withdrawal of depot neuroleptics. Moreover, the results suggest that periodical drug-free periods of about 3 months are appropriate in symptom-poor patients during long-term treatment with long-acting antipsychotic drugs.

Ambulatory Care↗
PubMed1988

Synergy between a non-neuroleptic thioxanthene stereo-isomer and penicillin in vivo.

Some neuroleptic drugs of the phenothiazine and thioxanthene groups have an antimicrobial effect in vitro. This is also true for neuroleptically inactive stereo-isomeric analogs of the thioxanthenes e.g. trans(E)-clopenthixol (t-CPT). In a murine pneumococcus peritonitis model t-CPT demonstrated a slight, but non-significant antibacterial effect in doses of 0.3-0.9 mg per mouse, while higher doses seemed to enhance the bacterial virulence. If combined with subtherapeutic doses of penicillin, a significantly higher survival rate was obtained compared with either drug given alone. In vitro studies demonstrated a similar synergistic effect. These results indicate that at least one non-neuroleptic thioxanthene stereo-isomer has an antibiotic potential also in vivo. The mechanism of action is not known.

Animals↗
PubMed1997

Phototoxic properties of neuroleptic drugs.

BACKGROUND: Photo-induced eruptions are well-known adverse effects of some neuroleptic drugs, particularly chlorpromazine. OBJECTIVE: By a photohemolysis test we assessed in vitro the phototoxic properties of 12 phenothiazines (chlorpromazine, dixyrazine, fluphenazine, levomepromazine, perazine, perphenazine, promazine, promethazine, prothipendyl, thioridazine, trifluoperazine, triflupromazine) and 5 thioxanthenes (chlorprothixene, clopenthixol, flupenthixol, thiothixene, zuclopenthixol). METHODS: Human erythrocytes from 3 donors were incubated with the compounds and irradiated with light sources rich in UVA or UVB, respectively. Doses were up to 100 J/cm2 UVA or up to 1,600 mJ/cm2 UVB. Photo-induced hemolysis was calculated as percentage of complete hemolysis. RESULTS: Photo-induced hemolysis >10% due to radiation rich in UVA was found with chlorpromazine (maximal median: 98%), dixyrazine (100%), fluphenazine (84%), perazine (100%), perphenazine (100%), promazine (16%), promethazine (25%), prothipendyl (96%), trifluoperazine (100%), triflupromazine (76%), chlorprothixene (100%) and thiothixene (31%). UVB-rich radiation induced hemolysis only with chlorpromazine (73%), dixyrazine (45%) and perazine (60%). CONCLUSION: Most neuroleptics are strongly phototoxic in vitro indicating a potential risk for photo-induced reactions also to occur in patients treated with these drugs.

Antipsychotic Agents↗