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

Eur J Drug Metab Pharmacokinet. 1981;6(1):61-70. doi: 10.1007/BF03189516.


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 a "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 considerably 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.

MeSH terms

  • Administration, Oral
  • Adult
  • Antiemetics / administration & dosage
  • Antiemetics / metabolism*
  • Benzimidazoles / administration & dosage
  • Benzimidazoles / metabolism*
  • Biological Availability
  • Blood Proteins / metabolism
  • Domperidone
  • Humans
  • Injections, Intramuscular
  • Injections, Intravenous
  • Kinetics
  • Male
  • Piperidines / administration & dosage
  • Piperidines / metabolism*
  • Protein Binding
  • Rectum
  • Suppositories


  • Antiemetics
  • Benzimidazoles
  • Blood Proteins
  • Piperidines
  • Suppositories
  • Domperidone