Introduction: Butyrophenone drugs including haloperidol are being widely used in the field of psychiatry. The acute butyrophenone poisoning incidents sometimes take place; in such cases, the analysis of a butyrophenone becomes necessary in forensic toxicology or clinical toxicology. Their analysis is being made by GC [1–4], GC/MS [5–6], HPLC [7–15] and LC/MS [16,17]. Six butyrophenones are now available as ethical drugs in Japan ( Fig. ); the most typical ones are haloperidol and bromperidol, which most frequently cause poisoning incidents among butyrophenones. These drugs are rapidly metabolized in human bodies into reduced haloperidol and reduced bromperidol, respectively. In this. | Butyrophenones by Kazuo Igarashi Introduction Butyrophenone drugs including haloperidol are being widely used in the field of psychiatry. The acute butyrophenone poisoning incidents sometimes take place in such cases the analysis of a butyrophenone becomes necessary in forensic toxicology or clinical toxicology. Their analysis is being made by GC 1-4 GC MS 5-6 HPLC 7-15 and LC MS 16 17 . Six butyrophenones are now available as ethical drugs in Japan Fig. the most typical ones are haloperidol and bromperidol which most frequently cause poisoning incidents among butyrophenones. These drugs are rapidly metabolized in human bodies into reduced haloperidol and reduced bromperidol respectively. In this chapter the methods of GC MS HPLC and LC MSa are presented for analysis of haloperidol bromperidol and their reduced forms. R - CH2 3 P O Figure floropipamide haloperidol bromperidol timiperone spiperone Structures of butyrophenones. Springer-Verlag Berlin Heidelberg 2005 264 Butyrophenones GC MS analysis Reagents and their preparation Haloperidol can be purchased from Sigma St. Louis MO USA and other manufacturers bromperidol reduced haloperidol and reduced bromperidol from Research Biochemical International Natick MA USA . A 4-g aliquot of NaOH and 6 g NaCl are dissolved in distilled water to prepare 100 mL solution 1 M NaOH solution b. n-Hexane isopropanol 95 5 v v mixture solution M Hydrochloric acid solution As internal standard IS c bromperidol 500 ng mL in M hydrochloric acid solution is used for analysis of haloperidol and vise versa. Preparation of standard solutions haloperidol or bromperidol solutions at 2-50 ng mL in M hydrochloric acid are prepared and each 2-mL aliquot is placed in a 15-mL volume glass centrifuge tube with a ground-in stopper. GC MS conditions Instrument an Agilent 5890 GC instrument Agilent Technologies Palo Alto CA USA connected with a JEOL Automass quadrupole mass spectrometer JEOL Tokyo Japan . GC .
