clopenthixol-acetate-ester and Psychotic-Disorders

Zuclopenthixol acetate (ZA) is the first parenteral antipsychotic medication introduced for clinical use in the treatment of aggression and agitation that has a relatively prolonged duration of action. The aim of this paper is to explore a number of important ethical and clinical issues that are raised by the use of this novel therapeutic formulation.. Relevant literature is explored and several issues are identified from which arguments for and against the use of medication of this type are raised. These issues are considered in general and with the use of a number of stylised clinical scenarios.. The use of long-acting antipsychotic medication is complicated by its impact upon patient autonomy, by considerations of informed consent and by the need to provide justice to all patients and staff in a psychiatric treatment setting. The use of ZA in the emergency treatment of psychotic patients may only be justified under specific clinical circumstances and its use is not appropriate as routine chemical restraint.. Zuclopenthixol acetate is a novel and potentially useful treatment alternative in the acutely disturbed patient. Institutions in which ZA is used in emergency settings should develop protocols to guide clinicians in its appropriate use and provide monitoring.

Topics: Acute Disease; Antipsychotic Agents; Clopenthixol; Ethics, Medical; Humans; Informed Consent; Psychotic Disorders; Restraint, Physical; Time Factors

Zuclopenthixol acetate--a new injectable formulation with a duration of action of 2-3 days--was compared with conventional intramuscular and oral formulations of haloperidol and zuclopenthixol in the initial treatment of acutely disturbed, psychotic patients. The patients were stratified into 3 diagnostic categories: acute psychoses (48 patients), mania (22 patients), and exacerbation of chronic psychoses (73 patients). The patients were rated on the Brief Psychiatric Rating Scale (BPRS), the Bech-Rafaelsen Mania Rating Scale (BRMAS) (only manic patients) and globally on the Clinical Global Impression (CGI). The study was an open, randomized multicentre trial with a 6-day treatment period. The zuclopenthixol acetate patients received 1-4 doses, the haloperidol patients 1-26 and the zuclopenthixol patients 1-22 doses. The assessments on the CGI showed that all 3 treatments caused a clear reduction of the severity of illness scores in all 3 diagnostic categories, with no differences between treatments. The ratings of the acute and chronic psychotic patients on the BPRS also showed significant reductions in scores with no differences between treatments. All 3 treatments caused a rapid remission of symptoms on the BRMAS. Haloperidol induced hypokinesia in significantly more patients than zuclopenthixol acetate after 24 h. Later there were no significant differences between treatments. Zuclopenthixol acetate fulfils many desires for an amended neuroleptic formulation for the initial treatment of acutely disturbed psychotic patients.

Topics: Acute Disease; Adult; Analysis of Variance; Antipsychotic Agents; Clopenthixol; Delayed-Action Preparations; Female; Haloperidol; Humans; Male; Middle Aged; Oils; Psychiatric Status Rating Scales; Psychotic Disorders

Fifteen patients (20-49 years of age) with mania or acute psychosis were treated with zuclopenthixol acetate (Clopixol, Acuphase). One injection of 75-100 mg produced significant amelioration of psychotic symptoms with minimal side effects. The duration of action of the drug was found to be about 72 hours.

Topics: Adult; Antipsychotic Agents; Clopenthixol; Dose-Response Relationship, Drug; Female; Humans; Male; Middle Aged; Psychiatric Status Rating Scales; Psychotic Disorders

Many psychotic patients are treated with antipsychotic medications during acute agitation and aggressive behavior episodes in an attempt to achieve a rapid calming effect. Those medications include olanzapine, zuclopenthixol acetate, and haloperidol intramuscular administration. This study compared the effectiveness of these injections in reducing the need for restraint during agitated-psychotic episodes that include aggression. Sociodemographical and clinical data were retrieved from the electronic medical records of 179 patients who needed rapid calming while hospitalized in a mental health center with acute psychosis. The treatments administered were olanzapine intramuscular, zuclopenthixol acetate intramuscular, and haloperidol intramuscular. The assessed outcomes were rate of restraint and violent behavior. Olanzapine was found significantly more effective in reducing the need for restraint compared to zuclopenthixol acetate. No significant differences were found between haloperidol and the other two with regard to restraint. Neither were other significant differences found between the groups with regard to violent or self-harming behaviors. No significant differences were found in the rate of violent behavior and antipsychotic dosage at discharge. In conclusion, in inpatients with acute agitated psychosis, olanzapine intramuscular shows better efficacy in reducing the need for restraint, at least as compared to zuclopenthixol acetate intramuscular.

Topics: Antipsychotic Agents; Benzodiazepines; Clopenthixol; Haloperidol; Humans; Injections, Intramuscular; Olanzapine; Psychomotor Agitation; Psychotic Disorders

Topics: Aged; Antipsychotic Agents; Clopenthixol; Dementia; Depressive Disorder; Dose-Response Relationship, Drug; Drug Administration Schedule; Female; Humans; Injections, Intramuscular; Psychomotor Agitation; Psychotic Disorders

Nineteen acutely disturbed psychotic Asian patients were treated with a single intramuscular injection of 50 mg of zuclopenthixol acetate in Viscoleo. Patients were assessed clinically before and after treatment using the Brief Psychiatric Rating Scale (BPRS). Serum zuclopenthixol and the inactive geometric isomer trans(E)-clopenthixol were determined by high-performance liquid chromatography after intramuscular injection. All patients improved, with the BPRS being significantly reduced (p < 0.001) at 72 h after injection. Adverse effects were generally few. The mean +/- SEM serum zuclopenthixol concentrations at 24, 48, and 72 h were 19.9 +/- 2.8, 31.5 +/- 4.5, and 17.8 +/- 2.9 micrograms/L, respectively. trans(E)-Clopenthixol concentrations ranged from negligible to 39.5 micrograms/L. This study confirms that a single intramuscular injection of 50 mg is adequate for managing severely disturbed psychotic patients for the first 3 days. The serum zuclopenthixol concentrations attained in the Asian patients were higher than those reported in Caucasian psychiatric patients. In some patients, a considerable amount of zuclopenthixol had been transformed to trans(E)-clopenthixol.

Topics: Adolescent; Adult; Aged; Antipsychotic Agents; Bipolar Disorder; China; Clopenthixol; Female; Humans; India; Injections, Intramuscular; Malaysia; Male; Middle Aged; Psychotic Disorders; Schizophrenia; Singapore

This report describes an open pilot study of ten acutely disturbed and agitated psychotic patients who received CPT-A zuclopenthixol injections. The dosage ranged from 50 mg to 100 mg. Sedative effects were noticed already after 2 hours, and the patients were all sleepy and sedated after 8 hours. There was a definite improvement in the CGI within 24 hours. The BPRS improved within 24 hours, having the greatest effect on activation, anxiety, depression, and hostile suspiciousness. These effects were sufficient to control these patients. The findings show a rapid onset of therapeutic effect, with no side effects, a duration of 2-3 days and a good local tolerability.

Topics: Acute Disease; Adult; Antipsychotic Agents; Clopenthixol; Dose-Response Relationship, Drug; Humans; Injections, Intramuscular; Middle Aged; Pilot Projects; Psychiatric Status Rating Scales; Psychotic Disorders

Twenty-five acutely disturbed psychotic patients were treated in an open study with a single injection of zuclopenthixol acetate 5% in 'Viscoleo, a thin vegetable oil. Patients were assessed post-injection for 3 days using the BPRS, CGI, and a specially designed behaviour/activity scale. Doses of 50 to 150 mg proved effective in 24 (96%) of 25 patients, with pronounced and rapid reduction in psychotic symptoms over the study period. The mean total BPRS score after 72 hours was reduced by over 57%. Tranquillization and sedation appeared within 15 to 90 minutes of injection. Unwanted symptoms were generally mild and of low incidence. The results showed that a single injection of zuclopenthixol acetate 5% in 'Viscoleo' provided rapid tranquillization and sedation coupled with an antipsychotic effect over 3 days. This profile offers a distinct advantage over neuroleptic preparations conventionally used for the initial treatment of acutely disturbed psychotic patients.

Topics: Adult; Antipsychotic Agents; Clopenthixol; Dyskinesia, Drug-Induced; Female; Humans; Injections, Intramuscular; Male; Middle Aged; Psychiatric Status Rating Scales; Psychotic Disorders; Thioxanthenes

1. The zuclopenthixol concentrations in serum has been investigated in man and dog after injection of three different zuclopenthixol preparations. These were zuclopenthixol dihydrochloride in aqueous solution, zuclopenthixol acetate in oil and zuclopenthixol decanoate in oil. 2. The pharmacokinetic profiles of the three injectable zuclopenthixol preparations are very different. Maximum serum levels are obtained after about 1 hour for zuclopenthixol dihydrochloride, after 36 hours for zuclopenthixol acetate and after one week for zuclopenthixol decanoate. 3. The different pharmacokinetics of the three injectable zuclopenthixol preparations are reflected in their clinical properties.

Topics: Adult; Aged; Animals; Antipsychotic Agents; Clopenthixol; Dogs; Female; Humans; Injections, Intramuscular; Male; Middle Aged; Psychotic Disorders; Reference Values; Schizophrenia; Thioxanthenes

The purpose of the present study was to evaluate zuclopenthixol acetate in Viscoleo, a new preparation to be administered once every 3 days, in the early treatment of acute psychotic episodes and acute deterioration of chronic psychosis. 21 cases were included in the study: patients received 1 to 3 injections. Clinical evaluation was made at 24, 48 and 72 hours after each injection, using the Clinical Global Impressions (CGI) and the Brief Psychiatric Rating Scale (BPRS). Results at end-point indicated a marked or moderate therapeutic effect in the 11 cases of acute psychosis. A statistically significant decrease was observed for the total BPRS score as well as for its subscales. Among 8 cases of exacerbation of chronic psychosis, 4 patients showed a moderate therapeutic effect, and minimal or no effect was found in the other 4 subjects. The total BPRS decreased significantly, but to a lesser extent than for acute psychosis. Two patients suffering from mania showed a moderate therapeutic effect according to CGI. 8 cases of acute psychosis and 5 cases of chronic psychosis did not suffer from any neurological side-effects. Plasma concentration measurements suggest that a dose of 50 mg per 3 days may be sufficient for early treatment of most acutely ill psychotic patients.

Topics: Adolescent; Adult; Antipsychotic Agents; Bipolar Disorder; Clopenthixol; Female; Humans; Male; Middle Aged; Parkinson Disease, Secondary; Psychiatric Status Rating Scales; Psychotic Disorders; Thioxanthenes