Zuclopenthixol acetate in Viscoleo® ‐ a new drug formulation

Abstract

Eighty-three acutely disturbed, psychotic patients were included in an open multicentre study. The aim of the study was to evaluate the clinical effect of zuclopenthixol acetate in Viscoleo (CPT-A). Each patient received from one to four intramuscular injections of CPT-A during the 6-day study period. The duration of action after one injection was between 2 and 3 days and doses from 50 mg to 150 mg were sufficient for most patients. Treatment with CPT-A caused a pronounced and rapid reduction of the psychotic symptoms. At the end of the 6-day test period the mean total score on BPRS in acute non-manic and exacerbated chronic patients was reduced by more than 50 per cent. In acute manic patients the mean total score on BRMS was reduced by 57 per cent already 1 day after injection. Rapidly after the injection of CPT-A a useful short-acting sedation can be expected, but the risk for oversedation even after a second injection is low. The frequency of unwanted effects, including extrapyramidal reactions, was low and the severity of symptoms was most often mild. With a rapid onset of action, a duration of effect of 2 to 3 days, and few and mild side effects, CPT-A offers advantages over the neuroleptic preparations conventionally used in the initial treatment of acutely disturbed, psychotic patients.

Clinical and Pharmacokinetic Evaluation of Zuclopenthixol Acetate in Viscoleo®

“…Several studies show the efficacy of zuclopenthixol for the treatment of acute psychosis or exacerbated chronic psychosis (Gravem and Bugge, 1981;Sechter et al, 1981;Lang and Winteler, 1983;Mann et al, 1985;Bourdouxheet al, 1987), but little information is yet available about zuclopenthixol acetate (Amdisen et al, 1987;Kuefferle et al, 1987). Our results confirm that this prodrug is a useful antipsychotic medication for the treatment of acute psychotic episodes or acute deteriorations of a chronic psychotic state (Amdisen et al, 1986).…”

Evaluation of Zuclopenthixol Acetate to Decrease Handling Stress in Wapiti

“…Injectable neuroleptics were developed for the management of acute psychoses in people who refused to take oral neuroleptics in the initial stages of their treatment (Amdisen et al, 1987). These drugs are used to alleviate anxiety, have various durations of action depending on formulation, and have few side effects when used appropriately.…”

The Development of Clinical Guidelines for the Use of Zuclopenthixol Acetate

“…This is contrary to the recommendations from the manufacturer, and to the guidelines given in prescribing manuals, which suggest a course of injections is usually optimal. [8], [9], [10] Just under half ( n = 40) of the respondents routinely gave ZA with another psychoactive medication, most frequently a benzodiazepine (clonazepam being most frequently used). Sedation was cited as being the most frequent side effect of ZA, and although EPSE were recognised as a complication of treatment, respondents rated this as relatively uncommon (on a linear scale of 1-5, mean score was <3).…”

“…In sum, there was a reasonable consistency between trials on the following: Several studies suggested that, depending on the individual's diagnosis, a differential response to ZA can be expected. That is, those with an exacerbation of chronic psychotic illness or acute mania tended to show a more rapid response, evidenced by decline in clinical global impression (CGI) score ( P < 0.0001) 8 and Bech Rafaelsen Mania scale (BRMAS) scores ( P < 0.001). [8], [14] There was reasonable agreement that the time of onset of sedation was between 15-90 minutes and that this level of sedation increases to reach a maximum after 8 hours.…”

“…That is, those with an exacerbation of chronic psychotic illness or acute mania tended to show a more rapid response, evidenced by decline in clinical global impression (CGI) score ( P < 0.0001) 8 and Bech Rafaelsen Mania scale (BRMAS) scores ( P < 0.001). [8], [14] There was reasonable agreement that the time of onset of sedation was between 15-90 minutes and that this level of sedation increases to reach a maximum after 8 hours. The sedative effect decreases with subsequent injections of ZA unless the dose is increased. Those individuals with mania and first episode psychosis were found to have less of a sedative response and took longer to show a sedative response as compared to those with a relapse of chronic psychosis. …”