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Haloperidol kinetics after oral and intravenous doses
Author(s) -
Holley Frederick O,
Magliozzi Joseph R,
Stanski Donald R,
Lombrozo Leon,
Hollister Leo E
Publication year - 1983
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1983.65
Subject(s) - volume of distribution , haloperidol , bioavailability , pharmacokinetics , distribution (mathematics) , pharmacology , absorption (acoustics) , chemistry , oral administration , medicine , mathematics , mathematical analysis , physics , acoustics , dopamine
Haloperidol kinetics were determined after oral and intravenous drug doses in 15 men. Mean elimination t½ for the subjects was 17.9 ± 6.4 (SD) hr. After 0.125 mg/kg IV, mean distribution t½s 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 t½ was 0.37 ± 0.18 hr and mean distribution t½ 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 t½ of haloperidol is explained by the drug's extensive tissue distribution. Clinical Pharmacology and Therapeutics (1983) 33, 477–484; doi: 10.1038/clpt.1983.65