The pharmacokinetics of intravenous and oral sulpiride in healthy human subjects

@article{Wiesel2004ThePO,
  title={The pharmacokinetics of intravenous and oral sulpiride in healthy human subjects},
  author={Frits-axel Wiesel and Gunnel Alfredsson and Mats Ehrnebo and G{\"o}ran Sedvall},
  journal={European Journal of Clinical Pharmacology},
  year={2004},
  volume={17},
  pages={385-391}
}
SummaryThe pharmacokinetics of sulpiride was studied in 6 healthy volunteers after intravenous and oral (tablets) administration of 100 mg. An open two- and in two subjects a three-compartment model was applied following intravenous administration. The average total distribution volume during the terminal slope was 2.72±0.66 l/kg and total systemic clearance was 415±84 ml/min. The serum half-life of the terminal slope following intravenous administration averaged 5.3 h (range 3.7–7.1 h… 

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The concentrations of prolactin remained at an elevated plateau for 9–36 h after drug treatment despite low drug concentrations, and may be due to high affinity and strong binding of the compound to the regulating receptors or the formation of an active sulpiride metabolite.

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It is concluded that therapeutic doses of sulpiride induce prolactin secretion that is dose-dependent in a first phase and stimulated independently of the sulPiride concentration in a second phase.

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