Haloperidol kinetics after oral and intravenous doses

Clin Pharmacol Ther. 1983 Apr;33(4):477-84. doi: 10.1038/clpt.1983.65.

Abstract

Haloperidol kinetics were determined after oral and intravenous drug doses in 15 men. Mean elimination t1/2 for the subjects was 17.9 +/- 6.4 (SD) hr. After 0.125 mg/kg IV, mean distribution t1/2s in six subjects were 0.19 +/- 0.07 and 2 +/- 1 hr, and in 12 subjects mean clearance was 11.8 +/- 2.9 ml/kg/min and mean steady-state volume of distribution was 17.8 +/- 6.5 l/kg. After 0.50-mg/kg oral doses in eight subjects, mean lag time before drug absorption was 0.82 +/- 0.25 hr. Mean absorption t1/2 was 0.37 +/- 0.18 hr and mean distribution t1/2 was 0.96 +/- 0.20 hr. Bioavailability was 0.65 +/- 0.14 after oral doses. In 14 kinetic studies in nine subjects, data was analyzed by both model-dependent (open two- and three-compartment models using nonlinear regression) and model-independent (AUC and first moment curve) approaches. Results of the two were found to be in close agreement. The long elimination t1/2 of haloperidol is explained by the drug's extensive tissue distribution.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Administration, Oral
  • Adult
  • Biological Availability
  • Chromatography, Gas
  • Haloperidol / administration & dosage
  • Haloperidol / blood
  • Haloperidol / metabolism*
  • Humans
  • Injections, Intravenous
  • Kinetics
  • Male
  • Models, Biological

Substances

  • Haloperidol