Sudebno-meditsinskaia ekspertiza 2009-01-01

[Chemical toxicological analysis of haloperidol metabolite 4-(4-chlorophenyl)-4-hydroxypipiridine in urine by high-performance liquid chromatography].

A B Skorniakova, D S Lazarian

Index: Sud. Med. Ekspert. 52(1) , 45-8, (2009)

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Abstract

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).