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Haloperidol is extensively used in current psychiatric practice for the treatment of various psychotic disorders. However, this substance is known to be toxic and sometimes cause poisoning despite its generally positive therapeutic effect. Moreover, some of its metabolites also possess high toxic activity. It has been shown in the literature that haloperidol is metabolized to 4-(4-chlorophenyl)-4-hydroxypiperidine (CPHP) and 3-(4-fluorobenzoyl)-propionic acid (FBPA). We have developed the most efficacious method for isolation of both CPHP and FBPA from aqueous solutions ensuring the output of 99.6% and 99.8% of the respective product. Also, their spectral characteristics were studied by the UV spectrophotometric technique. Animal experiments demonstrated that only CPHP was excreted in the urea whereas the second metabolite was not detected in any sample, probably because it is further metabolized to 3-(4-fluorophenyl)-acetic acid. Methods for the isolation of CPHP from urine, its identification, and quantitative determination were developed based on the use of high-performance liquid chromatography (HPLC).

Haloperidol is widely used in psychiatric practice both in monotherapy and in combination with neuroleptics, phenothiazine derivatives (chlorpromasin, levomepromasin) and antidepressants (amitriptilin, imipramin). We have developed techniques of haloperidol isolation from blood in combined poisonings with phenothiazine derivatives (chlorpromazine, levomepromasine) and antidepressants (amitriptilin, imipramin), their identification and quantitation with high-performance liquid chromatography. The highest output of the substances studied was achieved in alkaline hydrolysis. The techniques are expressive, sensitive and well reproducible. This makes them convenient for practice of forensic-chemical and chemico-toxicological laboratories.