Haloperidol kinetics after oral and intravenous doses

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Abstract
Haloperidol [an antipsychotic] kinetics were determined after oral and i.v. drug doses in 15 men. Mean elimination t1/2 [half-life] for the subjects was 17.9 .+-. 6.4 h. After 0.125 mg/kg i.v. mean distribution t1/2 in 6 subjects were 0.19 .+-. 0.07 and 2 .+-. 1 h, and in 12 subjects mean clearance was 11.8 .+-. 2.9 ml/kg per min and mean steady-state volume of distribution was 17.8 .+-. 6.5 l/kg. After 0.50-mg/kg oral doses in 8 subjects, mean lag time before drug absorption was 0.82 .+-. 0.25 h. Mean absorption t1/2 was 0.37 .+-. 0.18 h and mean distribution t1/2 was 0.96 .+-. 0.20 h. Bioavailability was 0.65 .+-. 0.14 after oral doses. In 14 kinetic studies in 9 subjects, data was analyzed by both model-dependent (open 2- and 3-compartment models using nonlinear regression) and model-independent (AUC [area under the plasma concentration time curve] and 1st moment curve) approaches. Results of the 2 were in close agreement. The long elimination t1/2 of haloperidol is explained by the drug''s extensive tissue distribution.