Zotepine Neuroleptics

Zotepine, like ziprasidone, is a potent 5-HT2 antagonist which also reduces the reuptake of noradrenaline. Its side effects, sedation and postural hypotension, are attributable to its antagonistic action on histaminel and alpha-1 receptors. Zotepine, which has not yet been marketed in Europe, may have a similar profile to ziprasidone and could be useful in the treatment of depression associated with schizophrenia. Because of the evident clinical superiority of the atypical antipsychotics over the traditional neuroleptics, the World Psychiatric Association Task Force has... 

The use of zotepine in short-term trials (4-8 weeks) has been reviewed (86). Comparisons have been carried out with haloperidol (three trials n = 212), chlorpromazine (two trials n = 328), perazine (two trials n = 81), and tiotixene (one trial n = 94). In these double-blind trials, zotepine 150-300 mg/day was as effective as typical neuroleptic drugs in controlling the symptoms of schizophrenia. The results suggested that zotepine may be effective in the management of patients with negative symptoms... 

Zotepine is a dibenzothiepine neuroleptic drug, an antagonist at Di dopamine receptors and at 5-HTi and 5-HT2 receptors (1). It rarely causes extrapyramidal disturbances, and when they do occur they are usually mild. 

Ackenheil M. Das biochemische Wirkprofil von Zotepin im Vergleich zu anderen Neuroleptika. [The biochemical effect profile of zotepine in comparison with other neuroleptics.] Fortschr Neurol Psychiatr 1991 59(Suppl. l) 2-9. 

A series of 6-aminoalkyltetrahydroindol-4-ones related to molindone (91) show potent affinities for D, and 5-HT receptors (610). Molindone exhibits many similarities to typical neuroleptics, including Dg antagonism, antipsychotic efficacy, and EPS (611). Zotepine (136) is a potent D, and 5-HT antagonist with high affinity for the 5-HT, receptor. 

Since damotepine (257) was found to show sedative activity <66NEP6514187>, a variety of modified dibenzo[ /]thiepines have been prepared and their physiological activities have been researched. Zotepine (258) has psychosedative and antipsychotic activity <78CPB3058>. Citatepine (259) was found to have neuroleptic, psychosedative activity, and to be a potential dopamine antagonist. <83EUP125484>. A lH-dibenzo[2,3 6,7]thieno[4,5-c]pyrrole derivative (260) (CGP-19865) was... 

Neuroleptic malignant syndrome is characterised by hyperthermia, severe muscle rigidity, autonomic dysfunction and altered mental state. A study of 24 patients who had received a variety of antipsychotics (chlorpromazine, zotepine, paliperidone, bromperidol, supliride, risperidone, thioridazine, olanzapine, fluphenazine, haloperidol, levoproma-zine) demonstrated a temporal relationship of muscle rigidity and elevated creatine kinase to fever [46 ]. 

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