Cis(Z)‐clopenthixol and clopenthixol (Sordinol®) in chronic psychotic patients: A DOUBLE‐BLIND CLINICAL INVESTIGATION

Abstract

The clinical effect of cis(Z)-clopenthixol has been compared with that of clopenthixol, which is a mixture of the pharmacologically active cis(Z)-isomer and the inactive trans(E)-isomer. In the 2-month double-blind trial were included 57 psychotic patients, mainly schizophrenics. Ratings evaluating severity of illness, therapeutic effect, possible interference of side effects with the patient's functioning, as well as any individual side effects were done at months 0, 1, and 2. The antipsychotic effect of cis(Z)-clopenthixol was found equal to that of clopenthixol whereas the cis(Z)-isomer on a mg/mg basis was twice as active as clopenthixol. Apart from the finding that the unspecific sedative effect appeared to be less marked with cis(Z)-clopenthixol, the type, degree, and frequency of side effects were the same in the two groups of patients. More than half of the patients experienced no side effects.

Serum concentrations of cis(Z)‐ and trans(E)‐clopenthixol after administration of cis(Z)‐clopenthixol and clopenthixol to human volunteers

“…On the basis of the results obtained in this study, it should be expected that cis(Z)-clopenthixol tablets are thrice as active as clopenthixol tablets, as the serum concentration curves of cis(Z)-clopenthixol were on mg basis equal for the two preparations, and the trans(E)-isomer is found to be without neuroleptic activity (Petersen et al (1977)). However, in patients cis(Z)-clopenthixol tablets were found twice as active as clopenthixol tablets, (Gravem et al (1978), Gravem & Bugge (1981) and Heikkila (1981)). Likewise were relatively higher serum levels obtained in patients after administration of clopenthixol tablets (Aaes-Jdrgensen et al (1981)).…”

Enantioselective Allylation Using Allene, a Petroleum Cracking Byproduct

“…We further demonstrated the utility of the reaction in the synthesis of anti-psychotic drug Clopenthixol (Sordinol, 4d), first introduced by Lundbeck in 1961, and one of several structurally related thioxanthene antagonists of dopamine receptor D2, commercially available as either a mixture of E/Z-isomers or as the pure Z-isomer, obtained by selective crystallization 25 (Fig. 2C).…”

Zuclopenthixol acetate for acute schizophrenia and similar serious mental illnesses

“…not zuclopenthixol acetate Study 3:Allocation: randomised.Particpants: people with schizophrenia.Interventions: oral thiothixene, oral chlorprothixene and oral clopenthixol, not zuclopenthixol acetate Bobon 1989 Allocation: randomised, but unequal numbers in groups said to be because hospitals probably “did not use the 4 envelopes randomisation of each block” Category C.Participants: acute psychoses.Interventions: zuclopenthixol acetate versus haloperidol IM and oral Burke 2002 Allocation: not randomised. Chakravarti 1990 Allocation: not randomised, open clinical trial. Conca 2003 Allocation: not randomised.Participants: people with catatonia including schizophrenia, psychosis and schizoaffective disorder. Interventions: zuclopenthixol acetate Dehnel 1968 Allocation: randomised.Participants: people with schizophrenia.Interventions: oral clopenthixol, oral perphenazine, not zuclopenthixol acetate Fischer-Cornelssen Allocation: not clearly stated.Participants: people with moderate and severe schizophrenia.Interventions: oral clozapine, oral chlorpromazine, oral haloperidol, oral trifluperazine and oral clopenthixol, not zuclopenthixol acetate Glenthoj 2000 Allocation: randomised.Participants: people with drug-naive, first-episode schizophrenia.Interventions: risperidone, oral zuclopenthixol, not zuclopenthixol acetate Gravem 1978 Allocation: not clearly stated.Participants: people with “mainly schizophrenia”.Interventions: oral clopenthixol, oral cis (Z) -clopenthixol, not zuclopenthixol acetate Gravem 1981a Allocation: not stated.Participants: people with classical or paranoid schizophrenia.Interventions: oral clopenthixol, oral cis (Z) -clopenthixol, not zuclopenthixol acetate Gravem 1981b Allocation: not randomised, review article. Gravem 1990 Allocation: randomised.Participants: people with schizophrenia, manic-depressive illness, paranoid psychosis.Interventions: single combined injection of zuclopenthixol acetate and zuclopenthixol decanoate, separate injections of zuclopenthixol acetate and zuclopenthixol decanoate. No comparison of zuclopenthixol acetate with standard treatment…”