On the pharmacokinetics of domperidone in animals and man IV. The pharmacokinetics of intravenous domperidone and its bioavailability in man following intramuscular, oral and rectal administration

  • J. Heykants
  • R. Hendriks
  • W. Meuldermans
  • M. Michiels
  • H. Scheygrond
  • H. Reyntjens
Original Papers


The pharmacokinetics and bioavailability of domperidone, a novel gastrokinetic, were studied in healthy male subjects by comparing plasma concentrations and urinary excretion following intravenous, intramuscular, oral and rectal administration. Two oral dosage forms were studied: 10-mg tablets and a 10-mg/ml oral solution. The influence of a meal on the oral bioavailability and the dose-proportionality were also investigated.

Plasma levels of intravenous domperidone could be described by a three-compartment model with a rapid distribution of 40% of the dose to as «shallow» peripheral compartment. The final elimination half-life was 7.5 hours. Peak plasma levels were reached within 30 minutes following intramuscular and oral administration and at 1–4 hours following rectal administration. Since domperidone showed an extensive first-pass elimination, AUC-values -a measure for the bioavailability- were consider-ably lower after oral than after parenteral administration. Equal oral and rectal doses gave a similar bioavailability. AUC-values increased proportionally with the dose over a 10–60 mg range. Cumulative urinary excretion of unchanged domperidone was proportional to corresponding AUC-values.

The bioavailability was discussed in the light of the therapeutic results.

Key words

domperidone gastrokinetic pharmacokinetics bioavailability man 


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Copyright information

© Springer-Verlag 1981

Authors and Affiliations

  • J. Heykants
    • 1
    • 2
  • R. Hendriks
    • 1
    • 2
  • W. Meuldermans
    • 1
    • 2
  • M. Michiels
    • 1
    • 2
  • H. Scheygrond
    • 1
    • 2
  • H. Reyntjens
    • 1
    • 2
  1. 1.Department of Drug Metabolism and PharmacokineticsJanssen PharmaceuticaBeerseBelgium
  2. 2.Medical DepartmentJanssen PharmaceuticaBeerseBelgium

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