Clinical and Pharmacokinetic Evaluation of Zuclopenthixol Acetate in Viscoleo®

Abstract

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.

Long-Acting Antipsychotic Medication, Restraint and Treatment in the Management of Acute Psychosis

“…The levels gradually fall from this time and are at approximately one-third of the peak level at 72 h [1]. A number of open studies have demonstrated a reduction in Brief Psychiatric Rating Scale [6] scores during the 3-day period of action, including scores on psychotic items such as hallucinatory behaviour and unusual thought content [7,8]. This is consistent with the proportion of dopamine receptor blockade that is usually associated with antipsychotic efficacy in typical neuroleptics [3][4][5].…”

Consensus Guidelines for Therapeutic Drug Monitoring in Neuropsychopharmacology: Update 2017

“…Many neuropsychopharmacological drugs are used as racemic compounds, and their enantiomers differ markedly in their pharmacodynamic and pharmacokinetic properties [88,1104]. So far, however, methadone and methylphenidate are at present the only racemic psychotropic compounds for which TDM of the enantiomers has been introduced [68,322]. The active enantiomer of racemic methadone is (R)-methadone, and l-methylphenidate (i. e., levorotary methylphendiate) is primarily responsible for the therapeutic effect of racemic methylphenidate.…”

Joint BAP NAPICU evidence-based consensus guidelines for the clinical management of acute disturbance: De-escalation and rapid tranquillisation

“…Two independently conducted open studies produced similar results with a slow onset of effect peaking at 24 hours and still being evident at 72 hours (Balant et al, 1989;Lowert et al, 1989). Thereafter, the first UK study reported that a significant reduction in psychosis score was first evident at 8 hours and scores continued to fall until the last measurement at 72 hours; of 25 participants assessed only four showed signs of tranquillisation at 1 hour, 19 participants at 2 hours and 22 participants at 24 hours (Chakravarti et al, 1990).…”