A simple and rapid method for isolation of five butyrophenones with Sep-Pak C18 cartridges from human samples, and their wide-bore capillary gas chromatography (GC), are presented. The GC was made by both flame ionization and electron capture detections. The drugs contained in alkaline samples were directly applied to the cartridges and eluted with chloroform/isopropanol (9:1). The recoveries with use of the cartridges were excellent for most drugs in both urine and plasma samples. We can recommend the Sep-Pak C18 cartridges for isolation of butyrophenones because of simplicity and rapidity, and also wide-bore capillary GC because of high sensitivity and low decomposition of drugs during passage through the column.