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PubMed1985

In vitro modulation of human neutrophil chemotaxis by cis(Z)- and trans(E)-clopenthixol, and chlorpromazine.

Phenothiazines have been shown to depress several functions of neutrophils, including chemotaxis. A biphasic effect of chlorpromazine (CPZ) and other phenothiazines on human neutrophil chemotaxis has recently been described. We investigated the effect of the stereo-isomers of clopenthizol, a thioxanthene, and of CPZ on human neutrophil chemotaxis. CPZ, at a concentration of 157 microM, and cis(Z)- or trans(E)-clopenthixol, at 105 microM, decreased cell viability. Cis(Z)- and trans(E)-clopenthixol as well as CPZ exerted a biphasic effect on neutrophil chemotaxis with a maximal enhancement of 57%, 92%, and 119%, respectively, and inhibition at higher concentrations. Enhancement of human neutrophil chemotaxis and possibly of the antibacterial activity of these cells by CPZ and the stereo-isomeric compounds of clopenthixol may have clinical implications especially in immunocompromised hosts. The enhancing effect of trans(E)-clopenthixol is of particular importance as this stereo-isomer of clopenthixol exhibits both antimicrobial and antiplasmodial activity but has no antipsychotic or antihypersecretory effect.

Bacterial Infections↗
PubMed1988

Effect of trans(E)-clopenthixol on Plasmodium berghei in vivo.

Previous in vitro studies have shown suppression of the growth of Plasmodium falciparum by the neuroleptic agents chlorpromazine and zuclopenthixol (formerly known as cis(Z)-clopenthixol) as well as by the neuroleptic inactive steroisomer trans(E)-clopenthixol. These compounds are chemically related to riboflavin and may act as inhibitors of riboflavin metabolism. As trans(E)-clopenthixol has been found active against chloroquine-resistant strains of P. falciparum in vitro and has been approved for human use, though inactive as a neuroleptic, this drug was selected for the present in vivo study. The dosage of trans(E)-clopenthixol was optimized through a pharmacokinetic study, and the suppression of the growth of Plasmodium berghei in vivo was tested in mice, with chloroquine acting as the positive and saline as the negative control. Trans(E)-clopenthixol did not inhibit the growth of P. berghei, whereas chloroquine almost eradicated the infection. The use of in vitro screening for anti-malarial activity in drugs approved for human use for other indications is discussed in the light of the results. It is concluded that the selection of drugs for further studies in vivo cannot solely be based on positive results in vitro.

Animals↗
PubMed1981

Stereo-isomeric dissociation of the antibacterial and the neuroleptic effect of clopenthixol.

Measurement of the IC50 of cis(Z)-clopenthixol and trans(E)-clopenthixol on 188 bacterial strains from human clinical specimens shows that the antibacterial activity of clopenthixol is exerted by both isomerical components and trans(E)-clopenthixol is the most active antibiotic of the two drugs against the sensitive strains. It is known that the trans(E)-clopenthixol isomere is without neuroleptic effect. The possibility of creating new antibiotics by e.g. steric alteration of neuroleptical agents is stressed. These drugs have different antibiotic patterns from those of classical antibiotics. It seems particularly promising that Pseudomonas aeruginosa is sensitive to these drugs.

Anti-Bacterial Agents↗
PubMed1981

Cis(Z)-clopenthixol and haloperidol in chronic schizophrenic patients--a double-blind clinical multicentre investigation.

Sixty-three chronic schizophrenic in-patients were included in the double-blind, double-dummy clinical trial comparing antipsychotic activity and side effects of cis(Z)-clopenthixol and haloperidol. Test treatment was administered at least 8 and in most cases 12 weeks with clinical evaluations including BPRS, NOSIE-30, CGI and single side effects done at weeks 0, 2, 4, 8, and 12. The average end-of-trial doses were 40 mg cis(Z)-clopenthixol and 10 mg haloperidol. Statistically significant improvements of total BPRS-score and Thinking disturbance were registered with both drugs from week 2 onwards. At week 12 when 36 patients were receiving test treatment total BPRS-score was reduced by 31% in the cis(Z)-clopenthixol group and by 17% in the haloperidol group. At week 4 Thinking disturbance was reduced by 32% in the cis(Z)-clopenthixol group and by 16% in the haloperidol group--these findings constituted the only significant difference between test drugs. Compared to the BPRS-results less improvements and no differences between test drugs were registered with NOSIE-30 and CGI. Any trends towards different frequency and severity of side effects were in the favour of cis(Z)-clopenthixol.

Adult↗
PubMed1983

A double-blind comparative trial of the decanoates of clopenthixol and fluphenazine in the treatment of chronic schizophrenic out-patients.

Forty-five patients were entered into a 24-week double-blind trial of clopenthixol decanoate and fluphenazine decanoate. The 24-week double-blind period was preceded by a 12-week open period. Of the 45 patients entered, 6 failed to attend the second interview and 1 left the country before the final assessment. Doses administered were in the range 100 mg 4-weekly to 400 mg 2-weekly for clopenthixol decanoate and 12.5 mg 4-weekly to 37.5 mg 3-weekly for fluphenazine decanoate. Both depot neuroleptics appeared to have an equivalent duration of action, with 200 mg clopenthixol decanoate approximately equivalent to 25 mg fluphenazine decanoate. Patients' mental state was assessed on the Brief Psychiatric Rating Scale, Clinical Global Impression, Krawiecka, Goldberg and Vaughan Rating Scale, and unwanted effects were recorded on a checklist. No differences were detected between the two drugs with regard to therapeutic activity or side-effects. It is concluded that clopenthixol decanoate is as effective and as well-tolerated a depot neuroleptic as fluphenazine decanoate.

Antipsychotic Agents↗
PubMed1981

Neuroleptic treatment of oligophrenic patients. A double-blind clinical multicentre trial of cis(Z)-clopenthixol and haloperidol.

One hundred mentally retarded patients from five Finnish institutions took part in a double-blind, double-dummy 12-week trial assessing the therapeutic effect of cis(Z)-clopenthixol and haloperidol. Assessments including CGI by psychiatrists and ward personnel as well as a 4-item target symptom scale was done at weeks 0, 4, 8, and 12. Improvement was registered by the psychiatrists in 16, 21, and 24 cis(Z)-clopenthixol patients and in 11, 6, and 7 haloperidol patients at weeks 4, 8, and 12, respectively--the difference between the two drugs being significant at weeks 8 and 12. The ratings of CGI by the personnel and the 4-item scale by the psychiatrists showed less improvements and no significant differences between the two drugs. While the overall impression of interference of patients' functioning by side-effects were in the favour of haloperidol the number of single side effects increased more with haloperidol than with cis(Z)-clopenthixol during the 12 weeks. Average doses administered at week 12 were 34 mg cis(Z)-clopenthixol and 5 mg haloperidol.

Adult↗
PubMed1981

A double-blind comparison of the effects of haloperidol and cis(Z)-clopenthixol in senile dementia.

The therapeutic effects in senile dementia of haloperidol and cis(Z)-clopenthixol were compared in a double-blind, double-dummy clinical 8-week study in 47 demented patients after wash-out periods of 3 weeks or less. Forty patients, most of whom received 0.5 mg haloperidol or 5 mg cis(Z)-clopenthixol, completed the study in which assessments with the geriatric rating scales of Gottfries-Cronholm and Crichton in addition to CGI were done at weeks--3, 0, 1, 2, 4, and 8. With the Gottfries-Cronholm Scale few significant changes from week 0 were seen in the two groups of patients. Significant deteriorations at weeks 1 and 8 in the haloperidol group were, however, registered. The only significant difference between the two groups of patients regarded motor activity which was most positively influenced by cis(Z)-clopenthixol. Accordingly, most results suggesting a difference between the two test drugs were in the favour of cis(Z)-clopenthixol. With the Crichton and the CGi scales changes in the over-all impression of the patients were very few. Side effects were mild and transient.

Aged↗
PubMed1980

Clopenthixol decanoate and perphenazine enanthate in schizophrenic patients. A double-blind Nordic multicentre trial.

The clinical properties of clopenthixol decanoate has been investigated versus perphenazine enanthate in a double-blind clinical multicentre trial including 14 psychiatric hospitals in Finland, Sweden, Norway, and Denmark. Test treatment was initiated in 172 chronic schizophrenic patients and the planned 6 months test period was completed by 57 patients receiving clopenthixol decanoate and 48 receiving perphenazine enanthate. The therapeutic effect was assessed by means of CGI, BPRS, and NOSIE-30 and was found significant with both test drugs. Significant differences in the effect were seen only in "Hostile-suspiciousness" (BPRS) and "Social interest" (NOSIE-30). For these items clopenthixol decanoate was found superior to perphenazine enanthate. The influence of side effects on the patients' functioning was found to be slightly, but not significantly more troublesome in the perphenazine enanthate patients.

Adult↗
PubMed1984

A 5-year follow-up study of chronic schizophrenics treated with clopenthixol decanoate.

Twenty-three chronic schizophrenic patients were followed-up over periods up to 5 years (1978-1983) while receiving treatment with depot injections of clopenthixol decanoate in doses ranging from 100 to 600 mg every 2 to 4 weeks. The highest single dose given was 1600 mg. Improvement in psychotic symptoms occurred progressively over the 5 years, with reduction in mean overall symptom score for schizophrenia from 7.43 to 0.88. Mean side-effects scores decreased over the same period from 2.0 to 0.5. After 5 years, 10 patients were still maintained on clopenthixol decanoate. Although during the first 2 months there was little improvement in 'negative' or 'loss' symptoms, improvement was similar in 'positive' and 'negative' symptoms after 5 years. Clopenthixol decanoate appeared to have a better calming effect than that encountered with flupenthixol decanoate. At higher doses, it caused drowsiness and subdued hostility and aggression.

Adult↗
PubMed1984

[A new injectable delayed-action neuroleptic with sedative and antipsychotic action: cis-(Z)-clopenthixol decanoate. Clinical trials].

70 psychiatric patients were treated with a depot preparation of cis (Z) clopenthixol decanoate, a new sedative and anti-psychotic neuroleptic. The mean dosage interval was two weeks, an amount of drug from 50 to 1000 mg for each I.M. injection. Significant improvements were obtained on thinking disturbance, hostile-suspiciousness and anxious-depression symptoms groups. Thus, paranoid schizophrenia seems the best indication of cis (Z) clopenthixol decanoate. Side effects (parkinsonism, weight increase) were of low intensity, and no depression was observed. This new long-acting depot neuroleptic may be used not only in hospitalized chronic schizophrenic patients, but also in outpatients as maintenance treatment: excellent results were obtained in such patients with a very low (less than 200 mg) fortnightly dosage. Advantages and indications of cis (Z) clopenthixol decanoate are discussed.

Adult↗
PubMed1981

[Treatment of pharmacotoxic psychoses with clopenthixol in patients with Parkinson's disease (author's transl)].

Pharmacotoxic psychoses resulting from therapy of advanced Parkinson's disease can occur in up to 60% of the patients. Treatment must not be completely discontinued in such cases. Clopenthixol (Sordinol, Ciatyl) in small dosage has been shown to be much more effective than all other types of therapy in the management of those psychoses. In a group of 28 patients treated with clopenthixol the progression of Parkinson's disease was not quicker than a control group of 30 patients not treated with clopenthixol. Both groups were of similar age and at a similar stage of the disease.

Antiparkinson Agents↗
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↗
PubMed1991

Molecular structure and dynamics of cis(Z)-and trans(E)-flupenthixol and clopenthixol.

The three-dimensional structures and molecular electrostatic potentials of the cis(Z) and trans(E)-isomers of flupenthixol and clopenthixol were examined by computer graphics and molecular mechanical and quantum mechanical calculations, and their internal molecular motions were studied by molecular dynamics simulations in vacuo and in aqueous solution. The simulations demonstrated that both the side chains and the tricyclic ring systems of clopenthixol and flupenthixol are highly flexible. The angle between the two phenyl ring planes varied between 105 and 171 degrees during the simulations in solution. The electrostatic potentials around the 2-substituent were significantly more negative in the trans(E)-isomers than in the cis(Z)-isomers. The stronger negative potentials may weaken electrostatic receptor interactions and, thereby, cause the trans(E)-isomers to be less active than cis(Z)-isomers. Differences both in three-dimensional structure and in electronic structure may cause the difference in pharmacological activity between cis(Z)- and trans(E)-thioxanthenes.

Clopenthixol↗
PubMed1986

Findings with cis-Z-clopenthixol in the treatment of acute mania and schizophrenia.

The authors report the results of an open clinical trial with Cis(Z)-Clopenthixol (Cisordinol), the isolated Cis-isomer of the Clopenthixol racemate (Sordinol). The drug was applied to 18 patients with severe forms of manic or schizophrenic disease, diagnosed according to ICD 9. The compound was applied intravenously or orally, daily doses ranging from 10-160 mg. For the duration of the study (6 weeks) the patients were repeatedly rated with the CGI, BPRS or IMPS (abbreviated version), and several hematological and enzyme patterns, cardiac, renal function and electrolytes were monitored, as was the FFA. Due to the relatively small number of patients in relatively heterogeneous diagnostic composition, a number of items rated failed to reach statistical significance. The CGI showed a good therapeutic effect with a minimal incidence or severity of side effects. BPRS and IMPS documented an impressive decline in formal thought-disorders, agitation, logorrhea and tenseness. The sedative effects of the drug were slight and of short duration, anti-Parkinson medication was necessary in more than 50% of the patients studied. The results of the study show a good efficacy of the drug in manic and schizophrenic disorders, Cisordinol being well tolerated intravenously. The range of doses administered is approximately 50% of the dose-range of the parent-drug (Sordinol).

Adult↗
PubMedDate not supplied

LC/MS determination of bromazepam, clopenthixol, and reserpine in serum of a non-fatal case of intoxication.

Combined liquid chromatography and mass spectrometry (LC/MS) with a moving belt interface can be used as a rapid method for the determination of bromazepam, clopenthixol, and reserpine in serum samples obtained from cases of acute overdoses with combinations of these drugs. Low resolution detection limits are about 100 pg for the three drugs, while in high resolution mode the detection limit for bromazepam is shown to be at least 35 pg. Accurate masses were obtained in a serum sample within 5 ppm using high voltage scanning over a narrow mass range for about 10 ng of bromazepam and clopenthixol, respectively. Chemical deactivation of the belt was shown to effectively reduce memory effects and to improve the desorption characteristics of the belt leading to higher yields of evaporated intact molecules.

Anti-Anxiety Agents↗
PubMedDate not supplied

HPLC-DAD and HPLC-MS findings in fatality involving (Z)-cis-clopenthixol (zuclopenthixol).

A fatality that was due to massive ingestion of the thioxanthene neuroleptic (Z)-cis-clopenthixol (zuclopenthixol, Z-CPT) is described. The total toxicological screening and the quantitation of both the ingested drugs and its inactive isomer (E)-trans-clopenthixol (E-CPT, produced by in vivo isomerization) in postmortem fluids and viscerae were produced by high-performance liquid chromatography (HPLC)-diode array detection. Drug confirmation was carried out by HPLC-mass spectrometry with an ionspray interface. Although death occurred 40 h after the drug intake, postmortem blood concentrations were 391 and 275 mg/mL for Z-CPT and E-CPT, respectively (50 to 100 times the usual therapeutic values). The cause of death was suicide, and the manner was acute neuroleptic overdosage.

Adolescent↗
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↗
PubMed1982

Clopenthixol decanoate in the treatment of chronic schizophrenic in-patients.

Nineteen chronic schizophrenic in-patients were entered into a 12-week open study of intramuscular clopenthixol decanoate. Fourteen patients completed the full 12-week treatment period; 3 were withdrawn due to inadequate clinical response or untoward adverse effects, and 2 were discharged and lost to follow-up. Doses administered were in the range 200 to 400 mg, weekly or fortnightly. Patients were assessed weekly using the Brief Psychiatric Rating Scale (BPRS). Nurses' Observation Scale for In-patient Evaluation (NOSIE-30) and the Clinical Global Impression (CGI). Unwanted effects were recorded on a checklist. Statistically significant improvements in the overall mean scores were noted on the BPRS at every assessment and on the NOSIE-30 at every assessment except in Week 4. Unwanted effects were generally mild and they decreased during the study. The results suggest that clopenthixol decanoate is an effective, well-tolerated antipsychotic agent, suitable for the treatment of chronic, long-stay schizophrenic in-patients.

Adult↗